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(+/-)-2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(1-adamantylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(1-adamantylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cycloheptylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cycloheptylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclohexylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclohexylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclooctylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-(1-norbornylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-(7-norbornylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-2-(1-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-2-(3-noradamantylamino)-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-2-(7-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-5-propyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(-)-catechin
about 98% activity at 0.2 mM
(-)-epicatechin
about 95% activity at 0.2 mM
(-)-epigallocatechin
less than 80% activity at 0.2 mM
(-)-epigallocatechin 3-gallate
potent inhibitor, less than 10% activity at 0.2 mM
(-)-gallocatechin
less than 30% activity at 0.2 mM
(1'-[(adamantan-2-yl)carbamoyl]-7-bromo-2,3-dihydrospiro[indene-1,4'-piperidin]-3-yl)acetic acid
selective isoform 11beta-HSD1 inhibitor
(1-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]cyclopentyl)acetic acid
11% inhibition at 0.001 mM
(1-[2-[(2,4-dichlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
27% inhibition at 0.001 mM
(1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
-
(1-[2-[(2-chlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
22% inhibition at 0.001 mM
(1-[2-[(4-methoxypyridin-3-yl)amino]-2-oxoethyl]cyclopentyl)acetic acid
7% inhibition at 0.001 mM
(1-[2-[(cyclohexylmethyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
7% inhibition at 0.001 mM
(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid
-
(1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one
derivative of curcumin, IC50 value in intact cells 93 nM. Not inhibitory to isoform 11beta-HSD2 in kidney at 100 microM
(1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
(1r,4s)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
-
(1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
(1S)-4-([1-[(4-bromophenyl)methyl]-1H-tetrazol-5-yl]methyl)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-ol
-
(1s,4r)-4-[3-[(2,3-dichlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(2,3-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(2,4-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(3,5-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(3-chloro-2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
-
(1s,4r)-4-[3-[(3-chlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(3-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1s,4r)-4-[3-[(4-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
-
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
-
(2R)-1,1,1-trifluoro-2-(3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine-1-sulfonyl]phenyl)propan-2-ol
HSD-016
(2R)-1-(2-chloro-4-(2-methoxyethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(2-chloro-4-(difluoromethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(2-chloro-4-ethoxyphenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxamide
-
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxylic acid
-
(2R)-1-(3-chloro-4-([4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazin-1-yl]sulfonyl)phenyl)piperidin-4-ol
-
(2R)-1-(4-bromo-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(4-bromophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazine
-
(2R)-1-(4-tert-butoxy-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-([2-chloro-4-[(3S)-3-methylpiperazin-1-yl]phenyl]sulfonyl)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[(2-chloro-4-piperidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[(2-chloro-4-pyrrolidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-N,N-dimethylpiperidin-4-amine
-
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
-
(2R)-1-[[2-chloro-4-(1H-1,2,4-triazol-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[[2-chloro-4-(4,4-difluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[[2-chloro-4-(4-fluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[[2-chloro-4-(4-methylpiperazin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-2-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenoxy)-N,N-dimethylethanamine
-
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)-N,N-dimethylaniline
-
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
-
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenol
-
(2R)-3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)benzamide
-
(2R)-4-(3-fluoro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)morpholine
-
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzamide
-
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
-
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-1-(4-methoxyphenylsulfonyl)-2-methylpiperazine
-
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methyl-1-(4-(trifluoromethoxy)-phenylsulfonyl)-piperazine
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]thiomorpholine-1,1-dioxide
-
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(4-piperidin-1-ylphenyl)sulfonyl]piperazine
-
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine
-
(2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-(tricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-[(1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide
-
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
-
(2R,4aS,6aS,12bR,14aS)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylate
-
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
(3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid
-
(3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
-
(3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
-
(3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid
-
(3beta)-3-hydroxy-11-oxoolean-12-en-30-amide
-
(3beta)-3-hydroxy-18,29-epoxyolean-12-ene-11,29-dione
IC50 value for isoform 11beta-HSD2 above 25 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-3-[(3-carboxypropanoyl)oxy]urs-12-en-28-oic acid
IC50 value for isoform 11beta-HSD2 above 3 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-30-[hydroxy(methyl)amino]-11,30-dioxoolean-12-en-3-yl acetate
IC50 value for isoform 11beta-HSD1 above 1 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
-
(3beta,18alpha)-3-hydroxy-11-oxoolean-12-en-30-oate
-
(3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
-
(3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
-
(3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
-
(3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
-
(3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
-
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
-
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
-
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
-
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
-
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
-
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
-
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
-
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
-
(3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
-
(3E)-3-[[(4-bromo-3-methylphenoxy)acetyl]hydrazono]-N-tricyclo[3.3.1.13,7]dec-1-ylbutanamide
-
(3R)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
-
(3S)-1-(3-chloro-2-methylbenzene-1-sulfonyl)-N-cyclohexylpiperidine-3-carboxamide
INCB-13739, selective inhibitor for isoform 11beta-HSD1
(3S)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
-
(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-4,4,6a,6b,8a,11,14b-heptamethyl-11-[(methylsulfonyl)amino]-14-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,14,14a,14b-icosahydropicen-3-yl acetate
IC50 value for isoform 11beta-HSD1 above 40 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
-
(6S)-6-(2-hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-one
BI-135585
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(2',4'-difluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
displays more than 1000fold selectivity for isoform 11beta-HSD1 over three related hydroxysteroid dehydrogenases, three CYP isozymes, hERG, and three nuclear receptors. When dosed orally at 30 mg/kg to mice, compound is distributed into adipose and liver
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
-
(R)-1-((S)-2-acetamido-3-(2-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-2-acetamido-3-(4-methoxyphenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-3-([1,1'-biphenyl]-3-yl)-2-aminopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(3-acetamidopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(acetyl-L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(acetylglycyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(L-tryptophyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
(R)-N-(adamantan-2-yl)-1-((S)-2-(2-aminoacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(R)-N-(adamantan-2-yl)-1-((S)-2-(2-hydroxyacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(3-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine]
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine]
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine]
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine]
-
1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydroxypropan-2-yl)phenylsulfonyl)-piperazin-1-yl)methyl)-cyclopropanecarboxamide
substrate competitive inhibitor, specific for 11beta-hydroxysteroid dehydrogenase type 1
1-(2,4-dichlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)-ethanone
-
1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
poor stability in liver microsomes
1-(4-chlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)ethanone
-
1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol
-
1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(2,4-dichloro-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(2-chloro-benzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfinyl)ethanone
-
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-ylamino)ethanone
-
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-yloxy)ethanone
-
1-adamantan-1-yl-2-(3,4-dimethoxy-benzyloxy)ethanone
-
1-adamantan-1-yl-2-(3,4-dimethoxy-phenoxy)ethanone
-
1-adamantan-1-yl-2-(3-methylbenzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(3-trifluoromethyl-phenoxy)ethanone
-
1-adamantan-1-yl-2-(3-trifluoromethylbenzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzenesulfinyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzenesulfonyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenoxy)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfinyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(4-methoxy-benzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-methylbenzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfinyl)ethanone
-
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(4-tert-butylbenzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(4-trifluoromethyl-phenoxy)ethanone
-
1-adamantan-1-yl-2-(4-trifluoromethylbenzyloxy)ethanone
-
1-adamantan-1-yl-2-(biphenyl-4-ylmethoxy)ethanone
-
1-adamantan-1-yl-2-(biphenyl-4-yloxy)ethanone
-
1-adamantan-1-yl-2-(toluene-4-sulfinyl)ethanone
-
1-adamantan-1-yl-2-(toluene-4-sulfonyl)ethanone
-
1-adamantan-1-yl-2-m-tolylmethanesulfonyl-ethanone
-
1-adamantan-1-yl-2-p-tolyloxy-ethanone
-
1-adamantan-1-yl-2-p-tolylsulfanyl-ethanone
-
1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
-
1-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
poor stability in liver microsomes
1-[(2-chlorobenzyl)oxy]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
compound with a superior metabolic stability profile, but sub-optimal with respect to aqueous solubility
1-[(2-chlorobenzyl)sulfanyl]-3-hydroxy-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile
good inhibitory activity. Compound undergoes oxidative metabolism at several sites
1-[(2-chlorobenzyl)sulfanyl]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
overall good inhibitory activity and metabolic stability
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
-
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
-
18alpha-glycyrrhetinic acid
selective inhibition of 11beta-HSD1, does not inhibit 11beta-HSD2 at concentrations up to 0.02 mM
18beta-glycyrrhetinic acid
inhibits both 11beta-HSD1 and 11beta-HSD2, but preferentially inhibits 11beta-HSD2
2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability
2,6,7-trimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
30.88% inhibition of isoform 11beta-HSD1 at 0.01 mM
2,6-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM
2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
17.65% inhibition of isoform 11beta-HSD1 at 0.01 mM
2,7-dimethyl-6-nitro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(1-adamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(1-adamantylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide
-
2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane
-
2-(3-noradamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one
38.03% inhibition of isoform 11beta-HSD1 at 0.01 mM, 22.6% inhibition of isoform 11beta-HSD2 at 0.01 mM
2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one
71.27% inhibition of isoform 11beta-HSD1 at 0.01 mM, 23.97% inhibition of isoform 11beta-HSD2 at 0.01 mM
2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one
13.46% inhibition of isoform 11beta-HSD1 at 0.01 mM, 1.34% inhibition of isoform 11beta-HSD2 at 0.01 mM
2-(bicyclo[2.2.1]hept-2-ylamino)-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
-
2-(bromomethyl)-6,7-dimethyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
33.82% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(bromomethyl)-7-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(bromomethyl)-7-methyl-6-nitro-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(cyclooctylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(iodomethyl)-2,3,6,7,8,9-hexahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one
27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(iodomethyl)-2,3,7,8,9,10-hexahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one
23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(iodomethyl)-6-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane
competitive. Also inhibitory to isoform 11beta-HSD2
2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
29.41% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-methyl-6,7,8,9-tetrahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one
13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-methyl-7,8,9,10-tetrahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one
14.71% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
-
2-[(2-chlorobenzyl)sulfanyl]-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
lead compound for development of inhibitors, the hydroxypyrimidine may act as a H-bonding pharmacophore. Compound has good cross species 11beta-HSD1 inhibitory activity for the mouse, cynomolgus monkey, and human enzymes
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
-
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
-
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
-
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane
-
2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane
-
2-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
the triazole methyl group fits in a pocket formed by I121, T124 and Y183. The carbonyl group is predicted to form hydrogen bonds to residues Y183 and S170. The adamantyl group is predicted to fit tightly in a hydrophobic pocket formed by L171, Y177 and L217. Half-life in liver microsomes 68 min
2-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfonyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
additionally inhibits cytochrome P450 enzyme 3A4-BFC with an IC50 value of 6.3 microM. Half-life in liver microsomes 34 min
2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide
-
2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine
-
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N,N-dimethyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-benzyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-ethyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-furan-2-ylmethyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-isopropyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-methyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-phenyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-tert-butyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
-
2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[4-(3-methylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzothiazole
89% residual activity at 0.02 mM
2-[4-(3-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzoxazole
18% residual activity at 0.02 mM
2-[4-(3-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
60% residual activity at 0.02 mM
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
-
2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole
-
2-[4-(4-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
90% residual activity at 0.02 mM
2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
-
2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
-
3,11-dioxoolean-12-en-30-oic acid
-
3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-[3-fluoro-5-(trifluoromethyl)thiophen-2-yl]propan-2-yl]-4H-1,2,4-triazole
potent and selective inhibitor for isoform 11beta-HSD1
3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole
-
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability
3-(1-(4-fluorophenyl)cyclopropyl)-4-isopropyl-5-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazole
mixed-type inhibitor, specific for 11beta-hydroxysteroid dehydrogenase type 1
3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid
-
3-(2-adamantan-1-yl-2-oxoethanesulfinyl)-N,N-dimethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethanesulfonyl)-N,N-dimethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)benzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
-
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
-
3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide
-
3-chloro-2-methyl-N-[4-[2-(3-oxomorpholin-4-yl)ethyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide
BVT-3498
3-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
-
3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
-
3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
-
3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-1-yl)butanamide
-
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
-
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cycloheptyl-3-methylbutanamide
-
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cyclohexyl-3-methylbutanamide
-
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-(methanesulfonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
-
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
-
3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one
moderate stability in liver microsomes
3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole
-
3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
MK-0916
3-[[(2-chlorophenyl)methyl]sulfanyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
-
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N,N-dimethyl benzamide
-
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N-methylbenzamide
-
4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-((S)-2-acetamido-3-((R)-2-(adamantan-2-ylcarbamoyl)piperidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-((S)-2-acetamido-3-((R)-2-(azepane-1-carbonyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-((S)-2-acetamido-3-((S)-2-(adamantan-2-ylcarbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-(1-benzofuran-2-ylcarbonyl)-5-(2-fluorophenyl)-3-hydroxy-1-[5-[(4-methylbenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-1,5-dihydro-2H-pyrrol-2-one
-
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N,N-diethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)benzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
-
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N,N-dimethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-benzylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-methylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid methyl ester
-
4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(4-butoxy-3-methylbenzyl)-3-hydroxy-5-(4-methylphenyl)-1-(pyridin-3-ylmethyl)-1,5-dihydro-2H-pyrrol-2-one
-
4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(cyclopentylsulfanyl)-3-[[1-(2,4-dichlorobenzamido)cyclopropyl]methoxy]-N-[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]-1,2-oxazole-5-carboxamide
-
4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol
-
4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole
-
4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
-
4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
-
4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
-
4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
4-[3-(4-methoxyphenoxy)-3-methyl-2-oxobutyl]adamantane-1-carboxamide
-
4-[4-(1-methyl-1H-benzimidazol-2-yl)piperazine-1-sulfonyl]benzoic acid
90% residual activity at 0.02 mM
4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
-
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
high metabolic lability
5,5-diethyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole
-
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine
potent and metabolically stable inhibitor with about 200fold selectivity for isoform 11beta-HSD-1 versus isoform 11beta-HSD-2
5-methyl-4-[(1E)-3-[(3-methylphenoxy)acetyl]triaz-1-en-1-yl]benzene-1,3-diol
-
5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole
-
5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile
-
5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
-
5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
-
5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
-
6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol
-
6-bromo-2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
6-bromo-2-(bromomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
25% inhibition of isoform 11beta-HSD1 at 0.01 mM
6-bromo-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM
6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one
-
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
-
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
-
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
-
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one
selective inhibitor for isoform 11beta-HSD1, 59.15% inhibition of isoform 11beta-HSD1 at 0.01 mM, 4.74% inhibition of isoform 11beta-HSD2 at 0.01 mM
7-(cyclohexylmethyl)-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
7-ethyl-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM
7-ethyl-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM
7-keto,25-hydroxycholesterol
inhibits the oxoreduction of cortisone to cortisol by the recombinant isoform 11beta-HSD1
7-keto,27-hydroxycholesterol
potent inhibitor of the isoform 11beta-HSD1-dependent oxoreduction of cortisone
7alpha,25-Dihydroxycholesterol
-
7beta,25-dihydroxycholesterol
-
7beta,27-dihydroxycholesterol
-
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
shows excellent stability against cytochrome P450 metabolism
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
methyl substitution at the 8-position achieves an approximately 15fold improvement in potency over the non-substituted compound
8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile
-
arylsulfoamidothiazoles
specific, tight-binding inhibitors, inhibition mode and profiles
-
AZD-4017
selective inhibitor for isoform 11beta-HSD1
BVT-528
competitive, tight-binding inhibition pattern
curcumin
inhibitory against isoform 11beta-HSD1 in intact cells with IC50 value of 2.29 microM
epigallocatechin gallate
-
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate
-
INCB-13739
selective inhibitor for isoform 11beta-HSD1
methoxychlor
competitive. Not inhibitory to isoform 11beta-HSD2
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
-
Momordica charantia extract
-
-
N'-[(1E)-(5-bromo-2-hydroxyphenyl)methylidene]-2-([5-[(phenylamino)methyl]-4-prop-2-en-1-yl-4H-1,2,4-triazol-3-yl]sulfanyl)propanehydrazide
-
N'-[(1Z)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide
-
N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide
-
N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-acetyl-beta-alanyl-N-adamantan-1-yl-D-prolinamide
-
N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
N-cyclohexyl-6-(piperidin-1-yl)picolinamide
-
N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
-
N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
-
N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
-
N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
-
N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
potent 11beta-HSD1 inhibitor
N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide
-
N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide
-
N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[3-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
-
N-[3-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
-
N-[3-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
-
N-[3-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-chloro-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-fluoro-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-methyl-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-chloro-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-methyl-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethylamino)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
-
N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
UE2343
selective inhibitor for isoform 11beta-HSD1
[(1R,3r,5S)-3-hydroxy-3-(pyrimidin-2-yl)-8-azabicyclo[3.2.1]octan-8-yl][5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone
selective inhibitor for isoform 11beta-HSD1
[1-[2-(cyclohexylamino)-2-oxoethyl]cyclopentyl]acetic acid
13% inhibition at 0.001 mM
[1-[2-(octahydroisoquinolin-2(1H)-yl)-2-oxoethyl]cyclopentyl]acetic acid
34% inhibition at 0.001 mM
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethyl]cyclopentyl]acetic acid
8% inhibition at 0.001 mM
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid
-
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
lead compound for high throughput screening of inhibitors. A hydrophobic group at C-2 position dramatically enhances potency
[4-(1H-benzimidazol-2-yl)piperazin-1-yl](4-methylphenyl)methanone
65% residual activity at 0.02 mM
[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid
-
[4-(2-Adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid methyl ester
-
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
potent inhibitor with a high permeability value, and low metabolic lability in mouse and human microsomes
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
good in vitro potency for the human enzyme while exhibiting enhanced metabolic stability in liver microsomes compared to lead compound [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
-
(11beta)-11-hydroxyallopregnanolone
-
-
(11beta)-11-hydroxyprogesterone
-
-
(1E,4E)-1,5-bis(3-methylthiophen-2-yl)penta-1,4-dien-3-one
-
-
(1E,4E)-1,5-bis(thiophen-2-yl)cyclohexanone
-
-
(1E,4E)-1,5-bis(thiophen-2-yl)penta-1,4-dien-3-one
-
-
(1S,2R,3S,5R,6R)-4-methylidene-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]heptane-2,3,5-triol
-
-
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aR,6S,8aR)-6-hydroxy-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
-
-
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
-
-
(1S,3R,4R,7S)-4-[[2-(4-methoxyphenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxamide
-
-
(1S,3R,4S,5S,7S)-4-(3-(2-fluorophenylsulfonamido)-3-methylbutanamido) adamantane-1-carboxamide
-
-
(2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
-
(20R,23E)-eupha-8,23-diene-3beta,25-diol
-
-
(24R)-eupha-8,25-diene-3beta,24-diol
-
-
(2E,4S)-4-hydroxy-5-[(1S,5S,6S)-6-(hydroxymethyl)-2-methylidenebicyclo[3.1.1]hept-6-yl]-2-methylpent-2-enoic acid
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine
-
-
(2R)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine
-
-
(2S)-5-(acetyloxy)-2-hydroxypentyl acetate
-
-
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
-
-
(3R,4R,7S)-4-[[(1-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]cyclopropyl)carbonyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxamide
-
-
(3R,4R,7S)-4-[[(1-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]cyclopropyl)carbonyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
-
-
(3R,4R,7S)-4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxamide
-
-
(4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
-
(4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
-
(4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decan-1-yl)acetic acid
-
-
(4aS,5R,8aR)-5,6-bis(hydroxymethyl)-1,1,4a-trimethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
-
-
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
-
-
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-3,4,4a,5,8,8a-hexahydronaphthalen-2(1H)-one
-
-
(5R)-2-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-5-methyl-5-(trifluoromethyl)-1,3-thiazol-4(5H)-one
-
-
(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)acetic acid
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
1-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)-2-methyl-1H-benzimidazole
-
-
1-(3-methoxyphenyl)-2-(phenylsulfonyl)ethanone
-
-
1-(5-oxo-2,5-dihydrofuran-3-yl)urea
-
specific for isozyme 11beta-HSD1
1-methyl-4-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
-
-
1-methyl-4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]-1H-indole
-
-
1-methyl-5-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
-
-
1-piperidinecarboxylic acid
-
-
1-[(1R,2R,7S)-5-[(aminooxy)methyl]tricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethyl-4-([[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]oxy]methyl)pyrrolidin-2-one
-
-
1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane
-
-
1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(3,4-dimethylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(3-amino-4-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(3-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol
-
-
1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
-
-
1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
-
-
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide
-
-
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide
-
-
1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
-
-
11-deoxycorticosterone
-
-
11-oxo-3alpha,5alpha-tetrahydrotestosterone
-
-
11-oxo-allopregnanolone
-
-
11-oxo-androstenedione
-
-
11alpha-hydroxyprogesterone
-
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione
-
i.e. cortisol
11beta-hydroxy-androstanediol
-
-
11beta-hydroxy-testosterone
-
-
18beta-glycyrrhetinic acid
2,2'-Dihydroxybiphenyl
-
-
2,4-dichloro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]naphthalen-1-yl]benzamide
-
-
2,4-dichloro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]phenyl]benzamide
-
-
2,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzenesulfonamide
-
-
2,6-dichloro-4-[(5,7,7-trimethyl-2-azabicyclo[3.2.1]oct-2-yl)carbonyl]aniline
-
-
2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide
-
-
2-(2-chloro-4-fluorophenoxy)-2-methyl-N-[(1R,2R,7S)-5-(methylsulfonyl)tricyclo[3.3.1.13,7]dec-2-yl]propanamide
-
-
2-(2-chloro-4-fluorophenoxy)-2-methyl-N-[(1R,2R,7S)-5-sulfamoyltricyclo[3.3.1.13,7]dec-2-yl]propanamide
-
-
2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
-
2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
-
2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide
-
-
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone
-
-
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone
-
-
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
-
-
2-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
-
-
2-(4-chlorophenoxy)-N-[(1R,2R,7S)-5-(hydroxycarbamimidoyl)tricyclo[3.3.1.13,7]dec-2-yl]-2-methylpropanamide
-
-
2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
-
2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
-
2-(4-methylphenyl)-2-oxoethyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoate
-
-
2-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine
-
-
2-(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)-N,N-diethylacetamide
-
-
2-(adamantan-1-yl)-N-methyl-N-(thiophen-3-ylmethyl)acetamide
-
-
2-(cycloheptylamino)-5-methyl-5-(1-methylethyl)-1,3-thiazol-4(5H)-one
-
-
2-adamantan-1-yl-N-methyl-N-thiophen-2-ylmethyl-acetamide
-
-
2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane
-
-
2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane
-
2-bromo-N-[2-([2-oxo-2-[(2-phenylethyl)amino]ethyl]sulfanyl)-2,3-dihydro-1,3-benzothiazol-6-yl]benzamide
-
-
2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
-
-
2-oxopentane-1,5-diyl diacetate
-
-
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
-
-
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
-
-
2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone
-
-
2-[4-(2,6-difluorobenzenesulfonyl)-[1,4]diazepan-1-yl]-1-(octahydroquinolin-1-yl)-ethanone
-
-
2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
-
-
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
-
-
2-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
-
-
2-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-5-methyl-5-(trifluoromethyl)-1,3-thiazol-4(5H)-one
-
-
2-[[(2,6-dichlorophenyl)thio]methyl]-6-[(4-methylpiperidin-1-yl)carbonyl]pyridine
-
-
3,5-bis(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3,5-bis(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide
-
-
3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(1-adamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
-
3-(1-fluoronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(1-methoxy-2-naphthyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(2,3-difluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-4-methyl-5-(2-nitrophenyl)-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-bromophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2-bromophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-bromophenyl)-5-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chloro-4-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2-chloro-4-fluorophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-4-methyl-5-(4-pentylphenyl)-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-5-(3,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-5-[2-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM
3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
-
-
3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM
3-(4-benzylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-butyl-2-methylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-butylphenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-(4-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-chloro-2-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-chloro-3-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-4-methyl-5-(1-[4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]cyclobutyl)-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-4-methyl-5-[1-[3'-(methylsulfonyl)biphenyl-4-yl]cyclobutyl]-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-(1-biphenyl-3-ylcyclobutyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(2,4-dichlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(3-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(4-fluorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-[2'-(ethylsulfonyl)biphenyl-4-yl]cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-[3'-(ethylsulfonyl)biphenyl-4-yl]cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-[4-(1H-imidazol-1-yl)phenyl]cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-fluorophenyl)-5-(4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]bicyclo[2.2.2]oct-1-yl)-1,2,4-oxadiazole
-
-
3-(4-pentylbicyclo[2.2.2]oct-1-yl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(4-tert-butylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine
-
-
3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol
-
isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(7-chloro-1-methoxy-2-naphthyl)-4-methyl-5-[2-(methylsulfonyl)phenyl]-4H-1,2,4-triazole
-
-
3-(7-chloro-1-methoxy-2-naphthyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
-
isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM
3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
-
-
3-benzyl-1-cyclohexylpyrrolidin-2-one
-
-
3-biphenyl-3-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-biphenyl-4-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
-
3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide
-
-
3-chloro-2-methyl-N-[4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1,3-thiazol-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-(2-morpholin-4-yl-2-oxoethyl)-pyridin-2-yl]-benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-4-fluorobenzenesulfonamide
-
-
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
-
-
3-chloro-N-[4-(morpholin-4-ylcarbonyl)benzyl]benzenesulfonamide
-
-
3-chloro-N-[4-(piperidin-1-ylcarbonyl)benzyl]benzenesulfonamide
-
-
3-chloro-N-[4-(pyrrolidin-1-ylcarbonyl)benzyl]benzenesulfonamide
-
-
3-chloro-N-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]benzenesulfonamide
-
-
3-monoglucuronyl-glycyrrhetinic acid
-
3-tricyclo[3.3.1.13,7]dec-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
potent and selective inhibitor of 11beta-HSD1
3-[(1R,3R,4R,7S)-4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]dec-1-yl]propanoic acid
-
-
3-[(1R,5S)-tricyclo[3.3.1.13,7]dec-2-yl]-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
-
3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
-
IC50 in the presence of NADP+: 0.12 mM, IC50 in the presence of NAD+: 5.6 mM; i.e. CHAPS
3-[(3R,5R)-tricyclo[3.3.1.13,7]dec-1-yl]-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
-
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(4-phenoxyphenyl)-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[3-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1,3-thiazol-2-yl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1H-pyrrol-1-yl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluoro-4-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4'-fluorobiphenyl-4-yl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-iodophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-[2-chloro-4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(cyclopropyloxy)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzothiazol-2(3H)-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzoxazol-2(3H)-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-indol-2-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-4-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenol
-
-
3-[2,3-bis(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[2-chloro-4-(1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[2-chloro-4-(2,4-dimethyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[2-chloro-4-(2-cyclopropyl-4-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[2-chloro-4-(2-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[2-chloro-4-[2-(methylsulfanyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[2-chloro-4-[2-(methylsulfonyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[2-chloro-4-[3-(ethylsulfonyl)propyl]phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[3-chloro-2'-(ethylsulfanyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[3-chloro-2'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[3-chloro-3'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[3-chloro-3'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[3-chloro-4'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[3-chloro-4'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)bicyclo[2.2.2]oct-1-yl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[4-chloro-2-(trifluoromethyl)phenyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[4-[2-(ethylsulfonyl)ethyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]bicyclo[2.2.2]oct-1-yl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[4-[3-(cyclopropylmethyl)-1,2,4-oxadiazol-5-yl]bicyclo[2.2.2]oct-1-yl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[4-[3-(ethylsulfonyl)propyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
-
-
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
-
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
-
3alpha,5alpha-tetrahydrocorticosterone
-
-
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
-
IC50 in the presence of NAD+: 0.000097 mM, IC50 in the presence of NADP+: 0.0003 mM; i.e. glycyrrhetinic acid
4'-chloro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-(6-cyclopropylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-(6-ethylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-[6-(ethylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
-
4'-cyano-N-[6-(methylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
-
4'-cyano-N-[6-(propan-2-yl)pyridin-2-yl]biphenyl-4-sulfonamide
-
-
4'-fluoro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-methyl-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4-(1-benzofuran-2-ylcarbonyl)-5-(2-fluorophenyl)-3-hydroxy-1-[5-[(4-methylbenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-1,5-dihydro-2H-pyrrol-2-one
-
-
4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide
-
-
4-(2-[1-[(2-fluorobenzene-1-sulfonyl)amino]cyclopropyl]-2-methylpropanamido)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
-
-
4-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine
-
-
4-([(3R)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline
-
-
4-([(3S)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N,N-diethylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)benzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-methylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-propylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclohexylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclopentylbenzamide
-
-
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
-
-
4-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
-
-
4-fluoro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]phenyl]benzamide
-
-
4-methoxy-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
-
4-methyl-3,5-bis[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(2-methylnaphthalen-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(4-pentylbicyclo[2.2.2]oct-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(4-pentylphenyl)-5-phenyl-4H-1,2,4-triazole
-
-
4-methyl-3-(4-pentylphenyl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(7-methylnaphthalen-2-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-naphthalen-2-yl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-tricyclo[3.3.1.13,7]dec-1-yl-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-[(3R,5R)-tricyclo[3.3.1.13,7]dec-1-yl]-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-[2-(trifluoromethoxy)phenyl]-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
potent and selective inhibitor of 11beta-HSD1
4-propyl-N-[2-(thiophen-2-yl)ethyl]benzenesulfonamide
-
-
4-tert-butyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
-
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid
-
-
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
-
-
4-[(E)-[(2Z)-2-[(2-chlorophenyl)imino]-4-oxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenyl benzoate
-
-
4-[(N-[4-[(dimethylamino)methoxy]benzene-1-sulfonyl]-2-methylalanyl)amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[([[(1S,3R,4R,7S)-4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]dec-1-yl]carbonyl]amino)methyl]benzoic acid
-
-
4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenol
-
-
4-[2-(1-[[(2-fluorobenzene-1-sulfonyl)amino]methyl]cyclopropyl)-2-methylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[4-methyl-5-(1-methyl-1H-indol-4-yl)-4H-1,2,4-triazol-3-yl]phenol
-
-
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2,3,3-tetramethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indole
-
-
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]-2-fluorophenol
-
-
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
-
-
4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]bicyclo[2.2.2]octane-1-carboxamide
-
-
4-[[2-methyl-N-(2,4,5-trifluorobenzene-1-sulfonyl)alanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(2,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(2,6-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(2-chloro-4-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
-
-
4-[[N-(3,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(3,5-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(3-chloro-2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(3-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(4-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(4-hydroxybenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(4-tert-butylbenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[[N-(benzenesulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
5,5-diethyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1,3-thiazol-4(5H)-one
-
-
5-(adamantan-1-ylcarbonyl)-4H,5H,6H,7H-thieno[3,2-c]pyridine
-
-
5-fluoro-1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
5-hydroxy-4-oxopentyl acetate
-
-
5-methyl-5-(1-methylethyl)-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1,3-thiazol-4(5H)-one
-
-
5alpha-dihydrocorticosterone
-
-
6-[(1-[(1R,2R,7S)-5-[(aminooxy)methyl]tricyclo[3.3.1.13,7]dec-2-yl]-4,4-dimethyl-5-oxopyrrolidin-3-yl)methoxy]pyridine-3-carbonitrile
-
-
6-[(1-[(3s,9s)-3-[(aminooxy)methyl]bicyclo[3.3.1]non-9-yl]-4,4-dimethyl-5-oxopyrrolidin-3-yl)methoxy]pyridine-3-carbonitrile
-
-
7-chloro-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-ol
-
-
7-hydroxy-2-(2-hydroxyethyl)-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
-
-
7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
-
-
7-keto,25-hydroxycholesterol
-
7-keto,27-hydroxycholesterol
-
7-oxo-5alpha-androstane-3beta,17beta-diol
-
mixed type inhibition of cortisone reduction
7-oxo-dehydroepiandrosterone
-
mixed type inhibition of cortisone reduction
7-oxo-epiandrosterone
-
competitive type inhibition of cortisone reduction
7alpha-hydroxy-dehydroepiandrosterone
-
competitive type inhibition of cortisol oxidation
7alpha-hydroxy-epiandrosterone
-
competitive type inhibition of cortisol oxidation
7beta,25-dihydroxycholesterol
-
7beta,27-dihydroxycholesterol
potent inhibitor of the isoform 11beta-HSD2-dependent oxidation of cortisol
7beta-hydroxy-dehydroepiandrosterone
-
competitive type inhibition of cortisol oxidation
7beta-hydroxy-epiandrosterone
-
mixed type inhibition of cortisol oxidation
8-benzyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1-thia-3,8-diazaspiro[4.5]dec-2-en-4-one
-
-
adamantyl triazoles
-
eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview
-
arylsulfonamidothiazole derivatives
-
specific for isozyme 11beta-HSD1
-
azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
-
-
BDE-100
-
inhibitor of isoform HSD11B2
BDE-153
-
inhibitor of isoform HSD11B2
benzothiazole derivatives
-
specific inhibition of isozyme 11beta-HSD1, inhibitory potency and IC50 values, overview, structure-activity relationship, introduction of a chlor atom at position 4 greatly enhances the inhibitory activity, inhibitory mechanism and enzyme/cofactor interaction analysis from molecular docking studies
-
butylated hydroxyanisole
highly selective inhibitor of isoform 11beta-HSD2
chenodeoxycholic acid
-
-
coffee
-
Coffea arabica fruit extract, corresponding to an italian espresso, inhibits recombinant and endogenous isozyme 11beta-HSD1 in HEK-293 cells up by 80% at 2% of extract, the inhibitory component is heat-stable with considerable polarity, extract blocks 11beta-HSD1-dependent cortisol formation in vivo preventing the subsequent nuclear translocation of the glucocorticoid receptor and abolishes glucocorticoid-induced expression of the key gluconeogenic enzyme phosphoenolpyruvate carboxykinase, at least part of the anti-diabetic effects of coffee consumption is due to inhibition of 11beta-HSD1-dependent glucocorticoid reactivation, overview, the inhibitory effect on isozyme 11beta-HSD1 is 7-10fold higher compared to isozyme 11beta-HSD2
-
danazol
competitive inhibition
dicyclohexyl benzene-1,2-dicarboxylate
-
-
diethyldithiocarbamate
uncompetitive inhibition of isoform 11beta-HSD2
epigallocatechine-3-gallate
-
-
ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
-
-
ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
-
-
ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate
-
-
euphane-3beta,20-dihydroxy-24-ene
-
-
fluoxymesterone
potent inhibitor of isoform 11beta-HSD2
interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2
-
-
-
methyl 2-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
-
-
methyl 2-[5-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
-
-
methyl 4-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)bicyclo[2.2.2]octane-1-carboxylate
-
-
methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate
-
-
methyl 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
-
-
methyl {(1S,2S)-3-oxo-2-[(2Z)-pent-2-en-1-yl]cyclopentyl}acetate
-
weak inhibition
mono(2-ethylhexyl)phthalate
-
-
N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide
-
-
N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide
-
-
N'-[(E)-(5-bromo-2-hydroxyphenyl)methylidene]-2-([5-[(phenylamino)methyl]-4-(prop-2-en-1-yl)-4H-1,2,4-triazol-3-yl]sulfanyl)propanehydrazide
-
-
N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide
-
-
N-(4-biphenyl-4-yl-1,3-oxazol-2-yl)benzenesulfonamide
-
-
N-(4-chloro-2-methyl-1,3-benzothiazol-5-yl)adamantane-1-carboxamide
-
-
N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-3-(trifluoromethyl)benzenesulfonamide
-
-
N-(5-cyanotricyclo[3.3.1.1~3,7~]decan-2-yl)-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide
-
-
N-(6-methylpyridin-2-yl)-2-(trifluoromethyl)benzenesulfonamide
-
-
N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide
-
-
N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
N-(6-methylpyridin-2-yl)naphthalene-1-sulfonamide
-
-
N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide
-
-
N-(furan-2-ylmethyl)-N-methyladamantane-1-carboxamide
-
-
N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
-
-
n-alkyl-substituted adamantyl triazoles
-
substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview
-
N-butyl-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
-
-
N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine
-
-
N-methyl-N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
-
-
N-methyl-N-(thiophen-3-ylmethyl)adamantane-1-carboxamide
-
-
N-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
-
-
N-methyl-N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
-
-
N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
-
-
N-[(1R,2R,7S)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]acetamide
-
-
N-[(1R,2R,7S)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamide
-
-
N-[(1S,2R,3R,5S,7R)-1,5-dihydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamide
-
-
N-[(1S,2R,3R,5S,7R)-1,5-dihydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamide
-
-
N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide
-
-
N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
-
-
N-[3-hydroxy-4-(piperidin-1-ylcarbonyl)phenyl]-3,4,5-trimethoxybenzamide
-
-
N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-[4-[(2,6-dimethylpyrimidin-4-yl)sulfamoyl]phenyl]-4-[oxo(phenyl)acetyl]benzamide
-
-
N-[5-(2-amino-2-oxoethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-[5-(3-amino-3-oxopropyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-[5-(cyanomethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-[6-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]-3-chloro-2-methylbenzenesulfonamide
-
-
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydrazinecarbonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
-
-
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydroxymethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
-
-
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-[(2-hydroxyhydrazinyl)methyl]tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
-
-
perfluorohexane sulfonate
-
perfluorohexanesulfonate
-
-
perfluorooctane sulfonate
-
perfluorooctyl sulfonate
-
-
PF-877423
-
specific 11beta-HSD1 inhibitor
pyrrolidine dithiocarbamate
resorcinol
-
weak inhibition
sterenin A
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin B
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin C
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin D
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
[1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol
-
-
[3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone
-
-
[4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone
-
-
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone
-
-
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
-
-
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
75% residual activity at 0.02 mM
carbenoxolone
-
carbenoxolone
unspecific inhibitor
carbenoxolone
specific for 11beta-hydroxysteroid dehydrogenase type 1
carbenoxolone
89.7% inhibition of isoform 11beta-HSD1 at 0.01 mM
T0504
-
T0504
inhibitor of 11beta-HSD1
18beta-glycyrrhetinic acid
-
18beta-glycyrrhetinic acid
-
11beta-HSD1 inhibitor with submicromolar potency
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
potent inhibitor of 11beta-HSD1
4-nonylphenol
-
-
4-nonylphenol
-
inhibition of liver isozyme 11beta-HSD1 and kidney isozyme 11beta-HSD2, 11beta-HSD1 IC50: 49.3 mM, isozyme 11beta-HSD2 IC50: 0.0203 mM
abietic acid
-
-
abietic acid
-
weak inhibition
bisphenol A
-
-
bisphenol A
weak inhibition of isoform 11beta-HSD2, 51.16% inhibition at 0.1 mM
BVT-14225
-
-
BVT-14225
-
isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2
dibutyltin
-
-
diethylhexyl adipate
-
-
diethylhexyl adipate
-
inhibition of liver isozyme 11beta-HSD1, IC50: 49.4 mM
diphenyltin
-
-
Disulfiram
-
-
Disulfiram
potent inhibitor of isoform 11beta-HSD2
glycyrrhetinic acid
-
-
glycyrrhetinic acid
-
inhibits both 11beta-hydroxysteroid dehydrogenase and carbonyl reductase activities of the enzyme potently
glycyrrhetinic acid
-
isozyme 11beta-HSD1 inhibitor, residue Tyr177 is important in binding, molecular modeling
glycyrrhetinic acid
-
11beta-HSD1 shows 21% residual activity at 0.01 mM, 11beta-HSD2 shows 16% residual activity at 0.01 mM
glycyrrhetinic acid
inhibitor of isoform 11beta-HSD2
maneb
-
-
Perfluorooctanoic acid
-
-
pyrrolidine dithiocarbamate
-
-
pyrrolidine dithiocarbamate
-
thiram
-
-
thiram
potent inhibitor of isoform 11beta-HSD2
tributyltin
-
-
Triphenyltin
-
-
zearalenone
-
-
zearalenone
selective inhibitor of isoform 11beta-HSD2
zineb
-
-
additional information
structure-activity analysis for inhibitor design
-
additional information
-
structure-activity analysis for inhibitor design
-
additional information
tea extracts inhibit isoform 11beta-HSD1 mediated cortisone reduction, where green tea exhibits the highest inhibitory potency with an IC50 value of 3.749 mg dried tea leaves per ml
-
additional information
7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD1 activity at concentrations up to 0.01 mM
-
additional information
7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD1 activity at concentrations up to 0.01 mM
-
additional information
not inhibited by (R)-1-(l-prolyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide trifluoroacetate, (R)-1-(l-histidyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide bis trifluoroacetate, (R)-1-(l-tyrosyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide trifluoroacetate, (R)-1-(l-lysyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide bis trifluoroacetate, (R)-1-(acetylglycyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, (R)-1-(acetyl-l-prolyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, (R)-1-(acetyl-l-tyrosyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, and (R)-1-(acetyl-l-prolyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
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additional information
not inhibited by 2-(allylamino)thiazol-4(5H)-one, 2-(allylamino)-5-methylthiazol-4(5H)-one, 2-(allylamino)-5-ethylthiazol-4(5H)-one, 2-(allylamino)-5-propylthiazol-4(5H)-one, 2-(allylamino)-5-isopropylthiazol-4(5H)-one, 2-(allylamino)-5,5-dimethylthiazol-4(5H)-one, and 2-(allylamino)-5-phenylthiazol-4(5H)-one
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additional information
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no inhibition by caffeic acid, chlorogenic acid or trigonelline
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additional information
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no inhibition by DETC, flavone, and bisphenol A, molecular docking and modeling of enzyme-inhibitor interactions the model can discriminate between known isozyme 11beta-HSD1 inhibitors or substrates and non-inhibitors, inhibitroy binding mode, overview
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additional information
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oxidation of the enzymes disulfides with K3Fe(CN)6 reduces the activity
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additional information
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leaf extracts of Eriobotrya japonica preferentially inhibit 11beta-HSD1 over 11beta-HSD2, extracts of roasted but not native coffee beans preferentially inhibit 11beta-HSD1 over 11beta-HSD2
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additional information
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isoform HSD11B1 is not inhibited by 4-bromobiphenyl, BDE-3, BDE-47, BDE-100, and BDE-153
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additional information
7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD2 activity at concentrations up to 0.01 mM
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additional information
7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD2 activity at concentrations up to 0.01 mM
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additional information
not inhibited by 7alpha,25-dihydroxycholesterol
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additional information
not inhibited by 7alpha,25-dihydroxycholesterol
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additional information
not inhibited by perfluorobutane sulfonic acid
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11beta-hydroxysteroid dehydrogenase deficiency
11beta-hydroxysteroid dehydrogenase in cultured human vascular cells. Possible role in the development of hypertension.
11beta-hydroxysteroid dehydrogenase deficiency
11beta-hydroxysteroid dehydrogenase type 1 deficiency ('apparent cortisone reductase deficiency') in a 6-year-old boy.
11beta-hydroxysteroid dehydrogenase deficiency
11Beta-hydroxysteroid dehydrogenase-1 deficiency or inhibition enhances hepatic myofibroblast activation in murine liver fibrosis.
11beta-hydroxysteroid dehydrogenase deficiency
A prospective study of the prevalence of clear-cut endocrine disorders and polycystic ovaries in 350 patients presenting with hirsutism or androgenic alopecia.
11beta-hydroxysteroid dehydrogenase deficiency
Cortisol metabolism in the postoperative period after cardiac surgery.
11beta-hydroxysteroid dehydrogenase deficiency
Defects in the HSD11 gene encoding 11 beta-hydroxysteroid dehydrogenase are not found in patients with apparent mineralocorticoid excess or 11-oxoreductase deficiency.
11beta-hydroxysteroid dehydrogenase deficiency
Endothelial cell dysfunction in mice after transgenic knockout of type 2, but not type 1, 11beta-hydroxysteroid dehydrogenase.
11beta-hydroxysteroid dehydrogenase deficiency
Enhanced hippocampal long-term potentiation and spatial learning in aged 11beta-hydroxysteroid dehydrogenase type 1 knock-out mice.
11beta-hydroxysteroid dehydrogenase deficiency
Epidemiologic study of adrenal gland disorders in Japan.
11beta-hydroxysteroid dehydrogenase deficiency
Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome.
11beta-hydroxysteroid dehydrogenase deficiency
Genetics of hypertensive syndrome.
11beta-hydroxysteroid dehydrogenase deficiency
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase in adipose tissue.
11beta-hydroxysteroid dehydrogenase deficiency
Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice.
11beta-hydroxysteroid dehydrogenase deficiency
Interactions between 11beta-hydroxysteroid dehydrogenase and COX-2 in kidney.
11beta-hydroxysteroid dehydrogenase deficiency
Low doses of liquorice can induce hypertension encephalopathy.
11beta-hydroxysteroid dehydrogenase deficiency
Pubertal presentation of congenital delta 5-3 beta-hydroxysteroid dehydrogenase deficiency.
11beta-hydroxysteroid dehydrogenase deficiency
Regulation of the genes for 11beta-hydroxysteroid dehydrogenase type 1 and type 2 in the kidney of the Dahl rat.
11beta-hydroxysteroid dehydrogenase deficiency
Renin-Independent hypermineralocorticoidism.
11beta-hydroxysteroid dehydrogenase deficiency
Steroid metabolism in metabolic syndrome X.
11beta-hydroxysteroid dehydrogenase deficiency
The type I and type II 11beta-hydroxysteroid dehydrogenase enzymes.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
11{beta}-Hydroxysteroid Dehydrogenase Type 1: A Tissue-Specific Regulator of Glucocorticoid Response.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
A study of the hexose-6-phosphate dehydrogenase gene R453Q and 11beta-hydroxysteroid dehydrogenase type 1 gene 83557insA polymorphisms in the polycystic ovary syndrome.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Alterations of Cortisol Metabolism in Human Disorders.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Apparent cortisone reductase deficiency: a functional defect in 11beta-hydroxysteroid dehydrogenase type 1.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Cortisol metabolism and the role of 11beta-hydroxysteroid dehydrogenase.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Genotypes at 11beta-hydroxysteroid dehydrogenase type 11B1 and hexose-6-phosphate dehydrogenase loci are not risk factors for apparent cortisone reductase deficiency in a large population-based sample.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Lack of Association of the 11beta-hydroxysteroid dehydrogenase type 1 gene 83,557insA and hexose-6-phosphate dehydrogenase gene R453Q polymorphisms with body composition, adrenal androgen production, blood pressure, glucose metabolism, and dementia.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Mutations in the genes encoding 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase interact to cause cortisone reductase deficiency.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Novel H6PDH mutations in two girls with premature adrenarche: 'apparent' and 'true' CRD can be differentiated by urinary steroid profiling.
3alpha(or 20beta)-hydroxysteroid dehydrogenase deficiency
Steroid biomarkers and genetic studies reveal inactivating mutations in hexose-6-phosphate dehydrogenase in patients with cortisone reductase deficiency.
Acidosis
Effects of changes in dietary intake of sodium and potassium and of metabolic acidosis on 11beta-hydroxysteroid dehydrogenase activities in rat kidney.
Acidosis
Effects of sustained hypoxaemia with 72 hours recovery on 11beta-hydroxysteroid dehydrogenase types 1 and 2 gene expression in near-term fetal sheep.
Acne Vulgaris
Molecular skin changes in Cushing syndrome and the effects of treatment.
Acromegaly
Immunohistochemical analysis of 11-beta-hydroxysteroid dehydrogenase type 2 and glucocorticoid receptor in subclinical Cushing's disease due to pituitary macroadenoma.
Acromegaly
Modulation of cortisol metabolism by the growth hormone receptor antagonist pegvisomant in patients with acromegaly.
Acromegaly
Modulation of cortisol metabolism during treatment of acromegaly is independent of body composition and insulin sensitivity.
Acromegaly
Urinary steroid excretion rates in acromegaly.
ACTH Syndrome, Ectopic
Apparent mineralocorticoid excess syndrome: an overview.
ACTH-Secreting Pituitary Adenoma
Effects of Carbenoxolone on the Canine Pituitary-Adrenal Axis.
ACTH-Secreting Pituitary Adenoma
Expression of genes related to corticotropin production and glucocorticoid feedback in corticotroph adenomas of dogs with Cushing's disease.
ACTH-Secreting Pituitary Adenoma
Inhibition of 11beta-hydroxysteroid dehydrogenase eliminates impaired glucocorticoid suppression and induces apoptosis in corticotroph tumor cells.
Acute Lung Injury
Inflammatory mediators down-regulate 11beta-hydroxysteroid dehydrogenase type 2 in a human lung epithelial cell line BEAS-2B and the rat lung.
Addison Disease
Epidemiologic study of adrenal gland disorders in Japan.
Addison Disease
Polymorphic variants of the HSD11B1 gene may be involved in adverse metabolic effects of glucocorticoid replacement therapy in Addison's disease.
Addison Disease
Polymorphisms of the GR and HSD11B1genes influence body mass index and weight gain during hormone replacement treatment in patients with Addison's disease.
Adenocarcinoma
Inflammation-associated gene expression is altered between normal human ovarian surface epithelial cells and cell lines derived from ovarian adenocarcinomas.
Adenocarcinoma
NNK reduction pathway gene polymorphisms and risk of lung cancer.
Adenocarcinoma
Regulation of 11beta-hydroxysteroid dehydrogenase type 2 by steroid hormones and epidermal growth factor in the Ishikawa human endometrial cell line.
Adenoma
11beta-Hydroxysteroid dehydrogenase types 1 and 2 are up- and downregulated in cortisol-secreting adrenal adenomas.
Adenoma
A case of cortisol producing adrenal adenoma without phenotype of Cushing's syndrome due to impaired 11beta-hydroxysteroid dehydrogenase 1 activity.
Adenoma
Cortisol-secreting adrenal adenomas express 11beta-hydroxysteroid dehydrogenase type-2 gene yet possess low 11beta-HSD2 activity.
Adenoma
Expression of 11beta-hydroxysteroid dehydrogenase type 2 (11betaHSD-2) in the developing human adrenal gland and human adrenal cortical carcinoma and adenoma.
Adenoma
Human adrenal cortex and aldosterone secreting adenomas express both 11beta-hydroxysteroid dehydrogenase type 1 and type 2 genes.
Adenoma
Inhibition of 11beta-hydroxysteroid dehydrogenase type II selectively blocks the tumor COX-2 pathway and suppresses colon carcinogenesis in mice and humans.
Adenoma
Role of local 11 beta-hydroxysteroid dehydrogenase type 2 expression in determining the phenotype of adrenal adenomas.
Adenoma
Role of local 11beta-hydroxysteroid dehydrogenase type 2 (HSD11B2) expression in determining the phenotype of adrenal adenomas.
Adrenal Hyperplasia, Congenital
11Beta-Hydroxylase Deficiency and Other Syndromes of Mineralocorticoid Excess as a Rare Cause of Endocrine Hypertension.
Adrenal Hyperplasia, Congenital
Effect of carbenoxolone on the plasma renin activity and hypothalamic-pituitary-adrenal axis in congenital adrenal hyperplasia due to 21-hydroxylase deficiency.
Adrenal Hyperplasia, Congenital
Failure of cortisone acetate treatment in congenital adrenal hyperplasia because of defective 11beta-hydroxysteroid dehydrogenase reductase activity.
Adrenal Hyperplasia, Congenital
Genetics of hypertensive syndrome.
Adrenal Insufficiency
Effect of growth hormone deficiency and recombinant hGH (rhGH) replacement on the hypothalamic-pituitary-adrenal axis in children with idiopathic isolated GH deficiency.
Adrenal Insufficiency
Mechanism of adrenal insufficiency following trauma and severe hemorrhage: role of hepatic 11beta-hydroxysteroid dehydrogenase.
Adrenal Insufficiency
Placental 11beta-HSD2 activity, early postnatal clinical course, and adrenal function in extremely low birth weight infants.
Adrenal Insufficiency
The role of progesterone metabolism and androgen synthesis in renal blood pressure regulation.
Adrenocortical Adenoma
Cortisol-secreting adrenal adenomas express 11beta-hydroxysteroid dehydrogenase type-2 gene yet possess low 11beta-HSD2 activity.
Adrenocortical Carcinoma
Expression of 11beta-hydroxysteroid dehydrogenase type 2 (11betaHSD-2) in the developing human adrenal gland and human adrenal cortical carcinoma and adenoma.
Adrenocortical Carcinoma
Uneventful delivery following series of successive treatments for virilized Cushing syndrome due to adrenocortical carcinoma.
Adrenogenital Syndrome
[Unusual adrenogenital syndrome. Probable blockade of 3 beta-hydroxysteroid dehydrogenase in a 4-year-old boy]
Albuminuria
Expression of renal 11beta-hydroxysteroid dehydrogenase type 2 is decreased in patients with impaired renal function.
Alkalosis
Association of hypertension and hypokalemia with Cushing's syndrome caused by ectopic ACTH secretion: a series of 58 cases.
Alkalosis
Impaired protein stability of 11beta-hydroxysteroid dehydrogenase type 2: a novel mechanism of apparent mineralocorticoid excess.
Alkalosis
Late-onset apparent mineralocorticoid excess caused by novel compound heterozygous mutations in the HSD11B2 gene.
Alopecia
delta 5-3 beta-hydroxysteroid dehydrogenase activity in sebaceous glands of scalp in male-pattern baldness.
Alzheimer Disease
Quantitative measurements of corticosteroids in ex vivo samples using on-line SPE-LC/MS/MS.
Anti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis
Clinical outcome in anti-neutrophil cytoplasmic antibody-associated vasculitis and gene variants of 11?-hydroxysteroid dehydrogenase type 1 and the glucocorticoid receptor.
Arthritis
11 Beta-hydroxysteroid dehydrogenase type 1 regulates synovitis, joint destruction, and systemic bone loss in chronic polyarthritis.
Arthritis
Arthritis and endogenous glucocorticoids: the emerging role of the 11beta-HSD enzymes.
Arthritis
Local metabolism of glucocorticoids and its role in rat adjuvant arthritis.
Arthritis, Experimental
Local metabolism of glucocorticoids and its role in rat adjuvant arthritis.
Arthritis, Rheumatoid
11 Beta-hydroxysteroid dehydrogenase type 1 regulates synovitis, joint destruction, and systemic bone loss in chronic polyarthritis.
Arthritis, Rheumatoid
Differential expression, function and response to inflammatory stimuli of 11beta-hydroxysteroid dehydrogenase type 1 in human fibroblasts: a mechanism for tissue-specific regulation of inflammation.
Asthma
Clinical relevance of airway 11beta-hydroxysteroid dehydrogenase type II enzyme in asthma.
Asthma
Cortisol resistance in conditions such as asthma and the involvement of 11beta-HSD-2: a hypothesis.
Asthma
Effect of inhaled glucocorticoid treatment on placental 11beta-hydroxysteroid dehydrogenase type 2 activity and neonatal birthweight in pregnancies complicated by asthma.
Asthma
Metabolism of synthetic steroids by the human placenta.
Asthma
Postmenopausal asthma: the estradiol 11beta-hydroxysteroid dehydrogenase connection.
Asthma
Reduced 11beta-hydroxysteroid dehydrogenase type 2 activity is associated with decreased birth weight centile in pregnancies complicated by asthma.
Atherosclerosis
11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice.
Atherosclerosis
11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes.
Atherosclerosis
7-oxysterols modulate glucocorticoid activity in adipocytes through competition for 11beta-hydroxysteroid dehydrogenase type.
Atherosclerosis
Antidiabetic effects of 11beta-HSD1 inhibition in a mouse model of combined diabetes, dyslipidaemia and atherosclerosis.
Atherosclerosis
Human and rodent type 1 11beta-hydroxysteroid dehydrogenases are 7beta-hydroxycholesterol dehydrogenases involved in oxysterol metabolism.
Atherosclerosis
Inhibition of 11beta-hydroxysteroid dehydrogenase type II selectively blocks the tumor COX-2 pathway and suppresses colon carcinogenesis in mice and humans.
Atherosclerosis
Rapid hepatic metabolism of 7-ketocholesterol by 11beta-hydroxysteroid dehydrogenase type 1: species-specific differences between the rat, human, and hamster enzyme.
Atherosclerosis
The role of the Stress-Related Anti-Inflammatory Hormones ACTH and Cortisol in Atherosclerosis.
Atherosclerosis
Therapeutic manipulation of glucocorticoid metabolism in cardiovascular disease.
Atrial Fibrillation
Increased expression of mineralocorticoid receptor and 11beta-hydroxysteroid dehydrogenase type 2 in human atria during atrial fibrillation.
Atrial Fibrillation
[Atrial 11beta-hydroxysteroid dehydrogenase type 2 expression in rheumatic heart disease patients with or without atrial fibrillation]
Atrial Fibrillation
[Expression of mineralocorticoid receptor and 11-beta-hydroxysteroid dehydrogenase type 2 in human atria during chronic atrial fibrillation: study of 25 cases]
Brain Diseases
Low doses of liquorice can induce hypertension encephalopathy.
Brain Ischemia
11beta-hydroxysteroid dehydrogenase type II inhibition causes cerebrovascular remodeling and increases infarct size after cerebral ischemia.
Breast Neoplasms
Contribution of protein kinase A and protein kinase C signalling pathways to the regulation of HSD11B2 expression and proliferation of MCF-7 cells.
Breast Neoplasms
Expression of the 11beta-hydroxysteroid dehydrogenase type II enzyme in breast tumors and modulation of activity and cell growth in PMC42 cells.
Breast Neoplasms
Genetic variation in candidate obesity genes ADRB2, ADRB3, GHRL, HSD11B1, IRS1, IRS2, and SHC1 and risk for breast cancer in the Cancer Prevention Study II.
Breast Neoplasms
Impaired 11?-Hydroxysteroid Dehydrogenase Type 2 in Glucocorticoid Resistant Patients.
Breast Neoplasms
Impairment of the antiproliferative effect of glucocorticosteroids by 11beta-hydroxysteroid dehydrogenase type 2 overexpression in MCF-7 breast-cancer cells.
Breast Neoplasms
Inhibition of 11 beta-hydroxysteroid dehydrogenase activity enhances the antiproliferative effect of glucocorticosteroids on MCF-7 and ZR-75-1 breast cancer cells.
Breast Neoplasms
Progesterone induction of the 11beta-hydroxysteroid dehydrogenase type 2 promoter in breast cancer cells involves coordinated recruitment of STAT5A and progesterone receptor to a distal enhancer and polymerase tracking.
Breast Neoplasms
Progestin regulation of 11beta-hydroxysteroid dehydrogenase expression in T-47D human breast cancer cells.
Breast Neoplasms
The 11beta-hydroxysteroid dehydrogenases: functions and physiological effects.
Breast Neoplasms
The 5,6-epoxycholesterol metabolic pathway in breast cancer: Emergence of new pharmacological targets.
Breast Neoplasms
The type I and type II 11beta-hydroxysteroid dehydrogenase enzymes.
Breast Neoplasms
[Diseases caused by adrenal dyshormonogenesis. The concept of minor enzymopathy. The 3 beta-hydroxysteroid dehydrogenase block; its possible importance in the pathogenesis of breast cancer]
Carcinogenesis
Immunohistochemical analysis of 11-beta-hydroxysteroid dehydrogenase type 2 and glucocorticoid receptor in subclinical Cushing's disease due to pituitary macroadenoma.
Carcinogenesis
Inhibition of 11beta-hydroxysteroid dehydrogenase type II selectively blocks the tumor COX-2 pathway and suppresses colon carcinogenesis in mice and humans.
Carcinogenesis
Prereceptor regulation of glucocorticoid action by 11beta-hydroxysteroid dehydrogenase: a novel determinant of cell proliferation.
Carcinoma
11Beta-hydroxysteroid dehydrogenase 1 expression in squamous cell carcinomas of the head and neck.
Carcinoma
Expression of 11beta-hydroxysteroid dehydrogenase type 2 (11betaHSD-2) in the developing human adrenal gland and human adrenal cortical carcinoma and adenoma.
Carcinoma, Hepatocellular
11 beta-hydroxysteroid dehydrogenase type 1 expression in 2S FAZA hepatoma cells is hormonally regulated: a model system for the study of hepatic glucocorticoid metabolism.
Carcinoma, Hepatocellular
C/EBP regulates hepatic transcription of 11beta -hydroxysteroid dehydrogenase type 1. A novel mechanism for cross-talk between the C/EBP and glucocorticoid signaling pathways.
Carcinoma, Hepatocellular
Expression of 11beta-hydroxysteroid dehydrogenase type 2 in an ACTH-producing small cell lung cancer.
Carcinoma, Ovarian Epithelial
Type 2 11beta-hydroxysteroid dehydrogenase activity in human ovarian cancer.
Carcinoma, Squamous Cell
11Beta-hydroxysteroid dehydrogenase 1 expression in squamous cell carcinomas of the head and neck.
Carcinosarcoma
NAD dependent 11beta-hydroxysteroid dehydrogenase activity in human endometrium and endometrial tumors.
Cardiomegaly
11beta-Hydroxysteroid dehydrogenase in the heart of normotensive and hypertensive rats.
Cardiomegaly
Chronic intermittent hypoxia induces 11beta-hydroxysteroid dehydrogenase in rat heart.
Cardiovascular Diseases
11Beta-HSD type 1 expression in human adipose tissue: impact of gender, obesity, and fat localization.
Cardiovascular Diseases
A gene variant of 11?-hydroxysteroid dehydrogenase type 1 is associated with obesity in children.
Cardiovascular Diseases
Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors.
Cardiovascular Diseases
Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Cardiovascular Diseases
Endothelin 1 type a receptor antagonism prevents vascular dysfunction and hypertension induced by 11beta-hydroxysteroid dehydrogenase inhibition: role of nitric oxide.
Cardiovascular Diseases
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic sindrome.
Cardiovascular Diseases
Influence of aldosterone vs. endothelin receptor antagonism on renovascular function in liquorice-induced hypertension.
Cardiovascular Diseases
Reduced placental 11beta-hydroxysteroid dehydrogenase type 2 mRNA levels in human pregnancies complicated by intrauterine growth restriction: an analysis of possible mechanisms.
Cardiovascular Diseases
Therapeutic manipulation of glucocorticoid metabolism in cardiovascular disease.
Cardiovascular Diseases
Tissue-specific adaptive levels of glucocorticoid receptor alpha mRNA and their relationship with insulin resistance.
Cardiovascular Diseases
Type 1 11beta-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases?
Cerebrovascular Disorders
11beta-hydroxysteroid dehydrogenase type II inhibition causes cerebrovascular remodeling and increases infarct size after cerebral ischemia.
Choriocarcinoma
Angiotensin II regulates 11beta-hydroxysteroid dehydrogenase type 2 via AT2 receptors.
Choriocarcinoma
Effect of cadmium on cortisol production and 11beta-hydroxysteroid dehydrogenase 2 expression by cultured human choriocarcinoma cells (JEG-3).
Choriocarcinoma
Effect of pro-inflammatory cytokines on expression and activity of 11beta-hydroxysteroid dehydrogenase type 2 in cultured human term placental trophoblast and human choriocarcinoma JEG-3 cells.
Choriocarcinoma
Prostaglandins and leukotriene B4 are potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 2 activity in human choriocarcinoma JEG-3 cells.
Choriocarcinoma
Regulation of cytochrome P450 cholesterol side-chain cleavage, 3 beta-hydroxysteroid dehydrogenase/delta 5-delta 4 isomerase type 1 and estradiol-17 beta-hydroxysteroid dehydrogenase mRNA levels by calcium in human choriocarcinoma JEG-3 cells.
Choriocarcinoma
Retinoic acid stimulates the expression of 11beta-hydroxysteroid dehydrogenase type 2 in human choriocarcinoma JEG-3 cells.
Choriocarcinoma
Structure of the VPATPD gene encoding subunit D of the human vacuolar proton ATPase.
Colitis
11beta-hydroxysteroid dehydrogenase 1 and 2 expression in colon from patients with ulcerative colitis.
Colitis
Glucocorticoid availability in colonic inflammation of rat.
Colitis
Inflammation regulates 11?-hydroxysteroid dehydrogenase type 1 differentially in specific compartments of the gut mucosal immune system.
Colitis
Intestinal inflammation modulates expression of 11beta-hydroxysteroid dehydrogenase in murine gut.
Colitis
Upregulation of 11?-hydroxysteroid dehydrogenase 1 in lymphoid organs during inflammation in the rat.
Colitis, Ulcerative
11beta-hydroxysteroid dehydrogenase 1 and 2 expression in colon from patients with ulcerative colitis.
Colonic Neoplasms
Can licorice lick colon cancer?
Colorectal Neoplasms
A variant (rs932335) in the HSD11B1 gene is associated with colorectal cancer in a Chinese population.
Colorectal Neoplasms
Chinese herbal medicine promote tissue differentiation in colorectal cancer by activating HSD11B2.
Colorectal Neoplasms
Expression of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in colorectal cancer.
Colorectal Neoplasms
Type-2 11?-hydroxysteroid dehydrogenase promotes the metastasis of colorectal cancer via the Fgfbp1-AKT pathway.
Congenital Abnormalities
The type I and type II 11beta-hydroxysteroid dehydrogenase enzymes.
Cushing Syndrome
11Beta-Hydroxylase Deficiency and Other Syndromes of Mineralocorticoid Excess as a Rare Cause of Endocrine Hypertension.
Cushing Syndrome
A case of cortisol producing adrenal adenoma without phenotype of Cushing's syndrome due to impaired 11beta-hydroxysteroid dehydrogenase 1 activity.
Cushing Syndrome
Adipose tissue 11{beta}-hydroxysteroid dehydrogenase type 1 expression in obesity and Cushing's syndrome.
Cushing Syndrome
Adipose tissue expression of 11beta-hydroxysteroid dehydrogenase type 1 in Cushing's syndrome and in obesity.
Cushing Syndrome
Apparent mineralocorticoid excess syndrome: an overview.
Cushing Syndrome
Association of hypertension and hypokalemia with Cushing's syndrome caused by ectopic ACTH secretion: a series of 58 cases.
Cushing Syndrome
Cortisol metabolism in the postoperative period after cardiac surgery.
Cushing Syndrome
Mechanism of hypertension in Cushing's syndrome: possible role of 11beta-hydroxysteroid dehydrogenase type 2 in kidneys and vascular cells.
Cushing Syndrome
Obesity and cortisol status.
Cushing Syndrome
Persistent hypokalemia after successful adrenalectomy in a patient with Cushing's syndrome due to ectopic ACTH secretion: possible role of 11beta-hydroxysteroid dehydrogenase inhibition.
Cushing Syndrome
Quantitative real-time PCR for the measurement of 11beta-HSD1 and 11beta-HSD2 mRNA levels in tissues of healthy dogs.
Cushing Syndrome
Reduced 11beta-hydroxysteroid dehydrogenase type 1 activity in obese boys.
Cushing Syndrome
Role of ketoconazole treatment in urinary-free cortisol-to-cortisone and tetrahydrocortisol-to-tetrahydrocortisone ratios in nonectopic Cushing's syndrome.
Cushing Syndrome
Role of local 11 beta-hydroxysteroid dehydrogenase type 2 expression in determining the phenotype of adrenal adenomas.
Cushing Syndrome
The 83,557insA variant of the gene coding 11?-hydroxysteroid dehydrogenase type 1 enzyme associates with serum osteocalcin in patients with endogenous Cushing's syndrome.
Cushing Syndrome
The activity of 11?-hydroxysteroid dehydrogenase type 2 enzyme and cortisol secretion in patients with adrenal incidentalomas.
Cushing Syndrome
Uneventful delivery following series of successive treatments for virilized Cushing syndrome due to adrenocortical carcinoma.
Cystic Fibrosis
Mimicry and well known genetic friends: molecular diagnosis in an Iranian cohort of suspected Bartter syndrome and proposition of an algorithm for clinical differential diagnosis.
Cysts
Implication of cortisol and 11beta-hydroxysteroid dehydrogenase enzymes in the development of porcine (Sus scrofa domestica) ovarian follicles and cysts.
Dementia
11Beta-hydroxysteroid dehydrogenase-1 deficiency or inhibition enhances hepatic myofibroblast activation in murine liver fibrosis.
Dementia
Lack of Association of the 11beta-hydroxysteroid dehydrogenase type 1 gene 83,557insA and hexose-6-phosphate dehydrogenase gene R453Q polymorphisms with body composition, adrenal androgen production, blood pressure, glucose metabolism, and dementia.
Depression, Postpartum
Associations between a polymorphism in the hydroxysteroid (11-beta) dehydrogenase 1 gene, neuroticism and postpartum depression.
Depression, Postpartum
Maternal Prenatal Mental Health and Placental 11?-HSD2 Gene Expression: Initial Findings from the Mercy Pregnancy and Emotional Wellbeing Study.
Dermatitis, Contact
Inhibition of skin 11beta-hydroxysteroid dehydrogenase activity in vivo potentiates the anti-inflammatory actions of glucocorticoids.
Diabetes Mellitus
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus.
Diabetes Mellitus
11beta-Hydroxysteroid dehydrogenase Type 1: genetic polymorphisms are associated with Type 2 diabetes in Pima Indians independently of obesity and expression in adipocyte and muscle.
Diabetes Mellitus
Assessing systemic 11beta-hydroxysteroid dehydrogenase with serum cortisone/cortisol ratios in healthy subjects and patients with diabetes mellitus and chronic renal failure.
Diabetes Mellitus
Association of HSD11B1 polymorphic variants and adipose tissue gene expression with metabolic syndrome, obesity and type 2 diabetes mellitus: a systematic review.
Diabetes Mellitus
Association studies between the HSD11B2 gene (encoding human 11beta-hydroxysteroid dehydrogenase type 2), type 1 diabetes mellitus and diabetic nephropathy.
Diabetes Mellitus
Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Diabetes Mellitus
INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes.
Diabetes Mellitus
Inhibition of human and rat 11beta-hydroxysteroid dehydrogenase type 1 by 18beta-glycyrrhetinic acid derivatives.
Diabetes Mellitus
Lack of relationship between 11beta-hydroxysteroid dehydrogenase setpoint and insulin sensitivity in the basal state and after 24h of insulin infusion in healthy subjects and type 2 diabetic patients.
Diabetes Mellitus
Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor.
Diabetes Mellitus
Regulatory effect of common promoter polymorphisms on the expression of the 11beta-hydroxysteroid dehydrogenase type 1 gene.
Diabetes Mellitus, Experimental
[Adrenocortical and renin-angiotensin systems in dynamics of experimental diabetes].
Diabetes Mellitus, Type 1
?-Cell-Specific Glucocorticoid Reactivation Attenuates Inflammatory ?-Cell Destruction.
Diabetes Mellitus, Type 1
Association studies between the HSD11B2 gene (encoding human 11beta-hydroxysteroid dehydrogenase type 2), type 1 diabetes mellitus and diabetic nephropathy.
Diabetes Mellitus, Type 1
Variants in HSD11B1 gene modulate susceptibility to diabetes kidney disease and to insulin resistance in type 1 diabetes.
Diabetes Mellitus, Type 2
11 beta-hydroxysteroid dehydrogenase type 1 promotes differentiation of 3T3-L1 preadipocyte.
Diabetes Mellitus, Type 2
11? Hydroxysteroid dehydrogenase - 1 activity in type 2 diabetes mellitus: a comparative study.
Diabetes Mellitus, Type 2
11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice.
Diabetes Mellitus, Type 2
11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches.
Diabetes Mellitus, Type 2
11Beta-hydroxysteroid dehydrogenase inhibition improves cognitive function in healthy elderly men and type 2 diabetics.
Diabetes Mellitus, Type 2
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus.
Diabetes Mellitus, Type 2
11beta-Hydroxysteroid dehydrogenase Type 1 in obesity and Type 2 diabetes.
Diabetes Mellitus, Type 2
11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development.
Diabetes Mellitus, Type 2
11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes.
Diabetes Mellitus, Type 2
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors with oleanan and ursan scaffolds.
Diabetes Mellitus, Type 2
11beta-Hydroxysteroid dehydrogenase Type 1: genetic polymorphisms are associated with Type 2 diabetes in Pima Indians independently of obesity and expression in adipocyte and muscle.
Diabetes Mellitus, Type 2
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.
Diabetes Mellitus, Type 2
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Diabetes Mellitus, Type 2
A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome.
Diabetes Mellitus, Type 2
Adipose tissue 11-beta-Hydroxysteroid Dehydrogenase Type 1 and Hexose-6-Phosphate Dehydrogenase gene expressions are increased in patients with type 2 diabetes mellitus.
Diabetes Mellitus, Type 2
Alteration of 11beta-hydroxysteroid dehydrogenase type 1 in skeletal muscle in a rat model of type 2 diabetes.
Diabetes Mellitus, Type 2
Altered activity of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in skeletal muscle confers metabolic protection in subjects with type 2 diabetes.
Diabetes Mellitus, Type 2
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
Diabetes Mellitus, Type 2
Association of HSD11B1 gene polymorphisms with type 2 diabetes and metabolic syndrome in South Indian population.
Diabetes Mellitus, Type 2
Association of HSD11B1 polymorphic variants and adipose tissue gene expression with metabolic syndrome, obesity and type 2 diabetes mellitus: a systematic review.
Diabetes Mellitus, Type 2
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
Diabetes Mellitus, Type 2
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.
Diabetes Mellitus, Type 2
Cortisol release from adipose tissue by 11beta-hydroxysteroid dehydrogenase type 1 in humans.
Diabetes Mellitus, Type 2
Development of 11beta-HSD1 inhibitors for the treatment of type 2 diabetes.
Diabetes Mellitus, Type 2
Different expression and distribution of 11beta-hydroxysteroid dehydrogenase type 1 in obese and lean animal models of type 2 diabetes.
Diabetes Mellitus, Type 2
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
Diabetes Mellitus, Type 2
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Diabetes Mellitus, Type 2
Effect of licorice on patients with HSD11B1 gene polymorphisms- a pilot study.
Diabetes Mellitus, Type 2
Effects of peroxisome proliferator-activated receptor-alpha and -gamma agonists on 11beta-hydroxysteroid dehydrogenase type 1 in subcutaneous adipose tissue in men.
Diabetes Mellitus, Type 2
Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice.
Diabetes Mellitus, Type 2
Extra-adrenal regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: physiological regulator and pharmacological target for energy partitioning.
Diabetes Mellitus, Type 2
Functional effects of polymorphisms in the human gene encoding 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1): a sequence variant at the translation start of 11 beta-HSD1 alters enzyme levels.
Diabetes Mellitus, Type 2
Glucocorticoids and the insulin resistance syndrome.
Diabetes Mellitus, Type 2
H6PDH interacts directly with 11beta-HSD1: implications for determining the directionality of glucocorticoid catalysis.
Diabetes Mellitus, Type 2
INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes.
Diabetes Mellitus, Type 2
Increased expression and activity of 11beta-HSD-1 in diabetic islets and prevention with troglitazone.
Diabetes Mellitus, Type 2
Increased glucocorticoid receptor and 11{beta}-hydroxysteroid dehydrogenase type 1 expression in hepatocytes may contribute to the phenotype of type 2 diabetes in db/db mice.
Diabetes Mellitus, Type 2
Increased in vivo regeneration of cortisol in adipose tissue in human obesity and effects of the 11beta-hydroxysteroid dehydrogenase type 1 inhibitor carbenoxolone.
Diabetes Mellitus, Type 2
Increased whole-body and sustained liver cortisol regeneration by 11beta-hydroxysteroid dehydrogenase type 1 in obese men with type 2 diabetes provides a target for enzyme inhibition.
Diabetes Mellitus, Type 2
Interaction of HSD11B1 and H6PD polymorphisms in subjects with type 2 diabetes are protective factors against obesity: a cross-sectional study.
Diabetes Mellitus, Type 2
Lack of relationship between 11beta-hydroxysteroid dehydrogenase setpoint and insulin sensitivity in the basal state and after 24h of insulin infusion in healthy subjects and type 2 diabetic patients.
Diabetes Mellitus, Type 2
Liver X receptors downregulate 11beta-hydroxysteroid dehydrogenase type 1 expression and activity.
Diabetes Mellitus, Type 2
Longer HSD11B2 CA-repeat in impaired glucose tolerance and type 2 diabetes.
Diabetes Mellitus, Type 2
Minireview: 11beta-hydroxysteroid dehydrogenase type 1- a tissue-specific amplifier of glucocorticoid action.
Diabetes Mellitus, Type 2
Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor.
Diabetes Mellitus, Type 2
Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Diabetes Mellitus, Type 2
Optimization of high-resolution melting analysis for simultaneous genotyping of two 11?-hydroxysteroid dehydrogenase type 1 gene polymorphisms.
Diabetes Mellitus, Type 2
Physiological roles of 11 beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase.
Diabetes Mellitus, Type 2
Readjusting the glucocorticoid balance: an opportunity for modulators of 11beta-hydroxysteroid dehydrogenase type 1 activity?
Diabetes Mellitus, Type 2
Regulatory effect of common promoter polymorphisms on the expression of the 11beta-hydroxysteroid dehydrogenase type 1 gene.
Diabetes Mellitus, Type 2
Relationship of 11?-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase gene polymorphisms with metabolic syndrome and type 2 diabetes.
Diabetes Mellitus, Type 2
Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains.
Diabetes Mellitus, Type 2
Structural characterization and pharmacodynamic effects of an orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor.
Diabetes Mellitus, Type 2
Sub-chronic administration of the 11beta-HSD1 inhibitor, carbenoxolone, improves glucose tolerance and insulin sensitivity in mice with diet-induced obesity.
Diabetes Mellitus, Type 2
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Diabetes Mellitus, Type 2
Targeting the pre-receptor metabolism of cortisol as a novel therapy in obesity and diabetes.
Diabetes Mellitus, Type 2
The 11-Beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitor INCB13739 Improves Hyperglycemia in Patients with Type 2 Diabetes Inadequately Controlled By Metformin Monotherapy.
Diabetes Mellitus, Type 2
The activity of 11?-hydroxysteroid dehydrogenase type 2 enzyme and cortisol secretion in patients with adrenal incidentalomas.
Diabetes Mellitus, Type 2
The contribution of visceral adipose tissue to splanchnic cortisol production in healthy humans.
Diabetes Mellitus, Type 2
The glucocorticoid-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 has broad substrate specificity: Physiological and toxicological considerations.
Diabetes Mellitus, Type 2
The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors.
Diabetes Mellitus, Type 2
Type 2 diabetes and metabolic syndrome are associated with increased expression of 11beta-hydroxysteroid dehydrogenase 1 in obese subjects.
Diabetes Mellitus, Type 2
[Reduction of obesity-related metabolic risk by modulating tissue exposition to cortisol].
Diabetes, Gestational
Dysregulation of 11beta-hydroxysteroid dehydrogenases: implications during pregnancy and beyond.
Diabetic Nephropathies
Association studies between the HSD11B2 gene (encoding human 11beta-hydroxysteroid dehydrogenase type 2), type 1 diabetes mellitus and diabetic nephropathy.
Dyslipidemias
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus.
Dyslipidemias
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors for metabolic syndrome.
Dyslipidemias
Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors.
Dyslipidemias
Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Dyslipidemias
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Dyslipidemias
Overexpression of 11beta-Hydroxysteroid Dehydrogenase Type 1 in Hepatic and Visceral Adipose Tissue is Associated with Metabolic Disorders in Morbidly Obese Patients.
Dyslipidemias
Reduced levels of circulating 7alpha-hydroxy-dehydroepiandrosterone in treated adolescent obese patients.
Dyslipidemias
Tissue-specific glucocorticoid reactivating enzyme, 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)--a promising drug target for the treatment of metabolic syndrome.
Dyslipidemias
Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice.
Endometrial Neoplasms
NAD dependent 11beta-hydroxysteroid dehydrogenase activity in human endometrium and endometrial tumors.
Essential Hypertension
11beta-Hydroxysteroid dehydrogenase type 2 activity is associated with left ventricular mass in essential hypertension.
Essential Hypertension
A genetic defect resulting in mild low-renin hypertension.
Essential Hypertension
A new polymorphic restriction site in the human 11 beta-hydroxysteroid dehydrogenase type 2 gene.
Essential Hypertension
Analysis of the 11beta-hydroxysteroid dehydrogenase type 2 gene (HSD11B2) in human essential hypertension.
Essential Hypertension
Association between ins4436A in 11?-hydroxysteroid dehydrogenase type 1 gene and essential hypertension in Polish population.
Essential Hypertension
Detection of Urinary Exosomal HSD11B2 mRNA Expression: A Useful Novel Tool for the Diagnostic Approach of Dysfunctional 11?-HSD2-Related Hypertension.
Essential Hypertension
Endothelin 1 type a receptor antagonism prevents vascular dysfunction and hypertension induced by 11beta-hydroxysteroid dehydrogenase inhibition: role of nitric oxide.
Essential Hypertension
Genetic variations of HSD11B2 in hypertensive patients and in the general population, six rare missense/frameshift mutations.
Essential Hypertension
Genotype-phenotype correlations of mutations and polymorphisms in HSD11B2, the gene encoding the kidney isozyme of 11beta-hydroxysteroid dehydrogenase.
Essential Hypertension
HSD11B2 CA-repeat and sodium balance.
Essential Hypertension
Identification of polymorphisms in the human 11beta-hydroxysteroid dehydrogenase type 2 gene promoter: functional characterization and relevance for salt sensitivity.
Essential Hypertension
Insulin, CCAAT/enhancer-binding proteins and lactate regulate the human 11?-hydroxysteroid dehydrogenase type 2 gene expression in colon cancer cell lines.
Essential Hypertension
Possible association but no linkage of the HSD11B2 gene encoding the kidney isozyme of 11beta-hydroxysteroid dehydrogenase to hypertension in Black people.
Essential Hypertension
Role of HSD11B2 polymorphisms in essential hypertension and the diuretic response to thiazides.
Essential Hypertension
Role of the 11beta-hydroxysteroid dehydrogenase type 2 in blood pressure regulation.
Essential Hypertension
Steroid metabolism in metabolic syndrome X.
Essential Hypertension
Structural analysis and evaluation of the 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) gene in human essential hypertension.
Essential Hypertension
The role of 11beta-hydroxysteroid dehydrogenase type 2 in human hypertension.
Fatty Liver
Additive action of 11beta-HSD1 inhibition and PPAR-gamma agonism on hepatic steatosis and triglyceridemia in diet-induced obese rats.
Fatty Liver
Hepatic 11beta-HSD1 mRNA expression in fatty liver and non-alcoholic steatohepatitis.
Fatty Liver
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Fetal Growth Retardation
11Beta-hydroxysteroid dehydrogenase type 2 in human pregnancy and reduced expression in intrauterine growth restriction.
Fetal Growth Retardation
Changes in 11beta-hydroxysteroid dehydrogenase type 2 expression in a low-protein rat model of intrauterine growth restriction.
Fetal Growth Retardation
Diethylstilbestrol inhibits human and rat 11?-hydroxysteroid dehydrogenase 2.
Fetal Growth Retardation
Differences in expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 and 2 in human placentas of term pregnancies according to birth weight and gender.
Fetal Growth Retardation
Differential expression and activity of 11beta-hydroxysteroid dehydrogenase in human placenta and fetal membranes from pregnancies with intrauterine growth restriction.
Fetal Growth Retardation
Dysregulation of 11beta-hydroxysteroid dehydrogenases: implications during pregnancy and beyond.
Fetal Growth Retardation
Glucocorticoid programming.
Fetal Growth Retardation
Glucocorticoids, 11beta-hydroxysteroid dehydrogenase, and fetal programming.
Fetal Growth Retardation
Hypoxia blocks 11beta-hydroxysteroid dehydrogenase type 2 induction in human trophoblast cells during differentiation by a time-dependent mechanism that involves both translation and transcription.
Fetal Growth Retardation
Impact of restriction of placental and fetal growth on expression of 11beta-hydroxysteroid dehydrogenase type 1 and type 2 messenger ribonucleic acid in the liver, kidney, and adrenal of the sheep fetus.
Fetal Growth Retardation
Peroxisome proliferator-activated receptor delta suppresses 11beta-hydroxysteroid dehydrogenase type 2 gene expression in human placental trophoblast cells.
Fetal Growth Retardation
Placental 11beta-hydroxysteroid dehydrogenase type 2 is reduced in pregnancies complicated with idiopathic intrauterine growth Restriction: evidence that this is associated with an attenuated ratio of cortisone to cortisol in the umbilical artery.
Fetal Growth Retardation
Reduced placental 11beta-hydroxysteroid dehydrogenase type 2 mRNA levels in human pregnancies complicated by intrauterine growth restriction: an analysis of possible mechanisms.
Fetal Growth Retardation
Renal and extrarenal mechanisms of perinatal programming after intrauterine growth restriction.
Fetal Growth Retardation
Site-specific methylation of placental HSD11B2 gene promoter is related to intrauterine growth restriction.
Fetal Growth Retardation
The 11beta-hydroxysteroid dehydrogenases: functions and physiological effects.
Fetal Growth Retardation
The cortisol-cortisone shuttle in children born with intrauterine growth retardation.
Fibrosarcoma
Characterization of 11beta-hydroxysteroid dehydrogenase activity and corticosteroid receptor expression in human osteosarcoma cell lines.
Gallstones
Estimation of ursodeoxycholic acid in human and bear biles using Clostridium absonum 7 beta-hydroxysteroid dehydrogenase.
Genetic Diseases, Inborn
A novel mutation in HSD11B2 causes apparent mineralocorticoid excess in an Omani kindred.
Genetic Diseases, Inborn
Apparent mineralocorticoid excess syndrome: an overview.
Gestational Trophoblastic Disease
11beta-Hydroxysteroid dehydrogenase activity in pregnancies complicated by hydatidiform mole.
Glaucoma
11Beta-hydroxysteroid dehydrogenase type 1 in human disease: a novel therapeutic target.
Glaucoma
11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.
Glaucoma
11{beta}-Hydroxysteroid Dehydrogenase Type 1: A Tissue-Specific Regulator of Glucocorticoid Response.
Glaucoma
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 lowers intraocular pressure in patients with ocular hypertension.
Glaucoma
Type 1 11beta-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases?
Glioblastoma
CTL recognition of a novel HLA-A*0201-binding peptide derived from glioblastoma multiforme tumor cells.
Glomerulonephritis
Reduced 11beta-hydroxysteroid dehydrogenase activity in patients with the nephrotic syndrome.
Glucose Intolerance
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus.
Glucose Intolerance
Cell-type specific regulation of the human 11beta-hydroxysteroid dehydrogenase type 1 promoter.
Glucose Intolerance
Diabetic pregnancy in rats leads to impaired glucose metabolism in offspring involving tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 expression.
Glucose Intolerance
Impaired glucose tolerance and insulin resistance are associated with increased adipose 11beta-hydroxysteroid dehydrogenase type 1 expression and elevated hepatic 5alpha-reductase activity.
Glucose Intolerance
Influence of placental 11beta-hydroxysteroid dehydrogenase (11beta-HSD) inhibition on glucose metabolism and 11beta-HSD regulation in adult offspring of rats.
Glucose Intolerance
Longer HSD11B2 CA-repeat in impaired glucose tolerance and type 2 diabetes.
Glucose Intolerance
Tissue-specific changes in peripheral cortisol metabolism in obese women: increased adipose 11beta-hydroxysteroid dehydrogenase type 1 activity.
Glucose Intolerance
[Correlations between the hypothalamo-pituitary-adrenal axis and the metabolic syndrome]
Granuloma
11beta-hydroxysteroid dehydrogenases are regulated during the pulmonary granulomatous response to the mycobacterial glycolipid trehalose-6,6'-dimycolate.
Graves Ophthalmopathy
The role of 11beta-hydroxysteroid dehydrogenase 1 in adipogenesis in thyroid-associated ophthalmopathy.
HELLP Syndrome
The transplacental passage of prednisolone in pregnancies complicated by early-onset HELLP syndrome.
Herpes Zoster
Comparative enzymology of 11 beta -hydroxysteroid dehydrogenase type 1 from glucocorticoid resistant (Guinea pig) versus sensitive (human) species.
Herpes Zoster
Histochemical observations on the adrenal gland of bat Vesperugo pipistrellus (Dobson).
Herpes Zoster
Immunohistochemical localization of type 1 11beta-hydroxysteroid dehydrogenase in human tissues.
Herpes Zoster
Juvenile hypertension, the role of genetically altered steroid metabolism.
Hirsutism
Steroid metabolism in metabolic syndrome X.
Hydatidiform Mole
11beta-Hydroxysteroid dehydrogenase activity in pregnancies complicated by hydatidiform mole.
Hyperaldosteronism
11Beta-Hydroxylase Deficiency and Other Syndromes of Mineralocorticoid Excess as a Rare Cause of Endocrine Hypertension.
Hyperaldosteronism
Genetic determination of human essential hypertension.
Hyperaldosteronism
Genetics of hypertensive syndrome.
Hyperaldosteronism
Hyperaldosteronism in pregnancy.
Hyperaldosteronism
Induction of 11beta-hydroxysteroid dehydrogenase type 2 and hyperaldosteronism are essential for enhanced sodium absorption after total colectomy in rats.
Hyperaldosteronism
Primary aldosteronism treated by trilostane (3 beta-hydroxysteroid dehydrogenase inhibitor).
Hyperandrogenism
11beta-hydroxysteroid dehydrogenase type 1 deficiency ('apparent cortisone reductase deficiency') in a 6-year-old boy.
Hyperandrogenism
11{beta}-Hydroxysteroid Dehydrogenase Type 1 and Its Role in the Hypothalamus-Pituitary-Adrenal Axis, Metabolic Syndrome, and Inflammation.
Hyperandrogenism
A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome.
Hyperandrogenism
Alterations of Cortisol Metabolism in Human Disorders.
Hyperandrogenism
Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome.
Hyperandrogenism
Hyperandrogenism in polycystic ovary syndrome. Evidence of dysregulation of 11 beta-hydroxysteroid dehydrogenase.
Hyperglycemia
11beta-hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress.
Hyperglycemia
Abnormal cortisol metabolism and tissue sensitivity to cortisol in patients with glucose intolerance.
Hyperglycemia
Glucocorticoid exposure in late gestation permanently programs rat hepatic phosphoenolpyruvate carboxykinase and glucocorticoid receptor expression and causes glucose intolerance in adult offspring.
Hyperglycemia
Glucocorticoid programming.
Hyperglycemia
Glucocorticoids, prenatal stress and the programming of disease.
Hyperglycemia
Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice.
Hyperglycemia
Increased expression and activity of 11beta-HSD-1 in diabetic islets and prevention with troglitazone.
Hyperglycemia
Leptin activation of corticosterone production in hepatocytes may contribute to the reversal of obesity and hyperglycemia in leptin-deficient ob/ob mice.
Hyperglycemia
PPARalpha agonists reduce 11beta-hydroxysteroid dehydrogenase type 1 in the liver.
Hyperglycemia
Role of glucocorticoids in the physiopathology of excessive fat deposition and insulin resistance.
Hyperglycemia
Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice.
Hyperglycemia
The mother or the fetus? 11beta-hydroxysteroid dehydrogenase type 2 null mice provide evidence for direct fetal programming of behavior by endogenous glucocorticoids.
Hyperglycemia
Tissue-specific glucocorticoid reactivating enzyme, 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)--a promising drug target for the treatment of metabolic syndrome.
Hyperinsulinism
Acute in vivo regulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by insulin and intralipid infusions in humans.
Hyperinsulinism
MRNA and enzyme activity of hepatic 11beta-hydroxysteroid dehydrogenase type 1 are elevated in C57BL/KsJ-db/db mice.
Hyperinsulinism
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
Hyperkalemia
Licorice: a sweet alternative to prevent hyperkalemia in dialysis patients?
Hyperlipidemias
Carbenoxolone treatment attenuates symptoms of metabolic syndrome and atherogenesis in obese, hyperlipidemic mice.
Hyperlipidemias
Depot-specific modulation of rat intraabdominal adipose tissue lipid metabolism by pharmacological inhibition of 11beta-hydroxysteroid dehydrogenase type 1.
Hyperlipidemias
High-throughput screening of 11beta-hydroxysteroid dehydrogenase type 1 in scintillation proximity assay format.
Hyperlipidemias
Increased expression and activity of 11beta-HSD-1 in diabetic islets and prevention with troglitazone.
Hyperlipidemias
Pathophysiology of metabolic syndrome X and its links to the perinatal period.
Hypertension
11 beta-Hydroxysteroid dehydrogenase.
Hypertension
11?-Hydroxysteroid Dehydrogenase Type 2 Polymorphisms and Activity in a Chilean Essential Hypertensive and Normotensive Cohort.
Hypertension
11beta-hydroxysteroid dehydrogenase activity in human aortic smooth muscle cells.
Hypertension
11Beta-hydroxysteroid dehydrogenase activity in spontaneously hypertensive and Dahl rats.
Hypertension
11beta-hydroxysteroid dehydrogenase and its role in the syndrome of apparent mineralocorticoid excess.
Hypertension
11beta-hydroxysteroid dehydrogenase and the pre-receptor regulation of corticosteroid hormone action.
Hypertension
11beta-hydroxysteroid dehydrogenase in cultured human vascular cells. Possible role in the development of hypertension.
Hypertension
11Beta-hydroxysteroid dehydrogenase in the Dahl rat.
Hypertension
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors for metabolic syndrome.
Hypertension
A case of pseudoaldosteronism, accompanied with hypocalcemia and exaggerated ACTH response.
Hypertension
A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome.
Hypertension
A genetic defect resulting in mild low-renin hypertension.
Hypertension
A mutation in the cofactor-binding domain of 11beta-hydroxysteroid dehydrogenase type 2 associated with mineralocorticoid hypertension.
Hypertension
A new polymorphic restriction site in the human 11 beta-hydroxysteroid dehydrogenase type 2 gene.
Hypertension
A novel mutation in HSD11B2 causes apparent mineralocorticoid excess in an Omani kindred.
Hypertension
A rapid screening assay for inhibitors of 11beta-hydroxysteroid dehydrogenases (11beta-HSD): flavanone selectively inhibits 11beta-HSD1 reductase activity.
Hypertension
A urine-concentrating defect in 11?-hydroxysteroid dehydrogenase type 2 null mice.
Hypertension
Acute intrarenal administration of cortisol has no effect on renal blood flow in hypertensive individuals.
Hypertension
Age-dependent decrease in 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) activity in hypertensive patients.
Hypertension
Alterations of Cortisol Metabolism in Human Disorders.
Hypertension
Analbuminemic Nagase rats: blood pressure response to dietary salt challenge.
Hypertension
Analysis of the 11beta-hydroxysteroid dehydrogenase type 2 gene (HSD11B2) in human essential hypertension.
Hypertension
Angiotensin II regulates 11beta-hydroxysteroid dehydrogenase type 2 via AT2 receptors.
Hypertension
Apparent Mineralocorticoid Excess by a Novel Mutation and Epigenetic Modulation by HSD11B2 Promoter Methylation.
Hypertension
Apparent mineralocorticoid excess caused by novel compound heterozygous mutations in HSD11B2 and characterized by early-onset hypertension and hypokalemia.
Hypertension
Apparent mineralocorticoid excess in a Brazilian kindred: hypertension in the heterozygote state.
Hypertension
Apparent mineralocorticoid excess syndrome: an overview.
Hypertension
Apparent mineralocorticoid excess: report of six new cases and extensive personal experience.
Hypertension
Arginine vasopressin stimulates 11beta-hydroxysteroid dehydrogenase type 2 expression in the mineralocorticosteroid target cells.
Hypertension
Assessing systemic 11beta-hydroxysteroid dehydrogenase with serum cortisone/cortisol ratios in healthy subjects and patients with diabetes mellitus and chronic renal failure.
Hypertension
Association of HSD11B1 gene polymorphisms with type 2 diabetes and metabolic syndrome in South Indian population.
Hypertension
Biochemical and genetic characterization of 11 beta-hydroxysteroid dehydrogenase type 2 in low-renin essential hypertensives.
Hypertension
CA-Repeat polymorphism in intron 1 of HSD11B2 : effects on gene expression and salt sensitivity.
Hypertension
Carbenoxolone damages endothelium and enhances vasoconstrictor action in aortic rings.
Hypertension
Chronic hypoxemia selectively down-regulates 11beta-hydroxysteroid dehydrogenase type 2 gene expression in the fetal sheep kidney.
Hypertension
Cloning and expression of rat cDNA encoding corticosteroid 11 beta-dehydrogenase.
Hypertension
Common Variation at the 11-Beta Hydroxysteroid Dehydrogenase Type 1 (HSD11B1) Gene Is Associated with Left Ventricular Mass.
Hypertension
Conditional Deletion of Hsd11b2 in the Brain Causes Salt Appetite and Hypertension.
Hypertension
Cortisol as a mineralocorticoid in human disease.
Hypertension
Cortisol metabolism and the role of 11beta-hydroxysteroid dehydrogenase.
Hypertension
Cortisol metabolism in hypertension.
Hypertension
Cortisol, 11beta-hydroxysteroid dehydrogenases, and hypertension.
Hypertension
Detection of Urinary Exosomal HSD11B2 mRNA Expression: A Useful Novel Tool for the Diagnostic Approach of Dysfunctional 11?-HSD2-Related Hypertension.
Hypertension
Developmental programming of renal glucocorticoid sensitivity and the renin-angiotensin system.
Hypertension
Dopamine and the kidney: a role in hypertension?
Hypertension
Effect of immunosuppressive and other drugs on the cortisol-cortisone shuttle in human kidney and liver.
Hypertension
Effect of licorice on PTH levels in healthy women.
Hypertension
Effects of alcohol on blood pressure and production of vascular aldosterone and corticosterone.
Hypertension
Effects of cholic acid on blood pressure and production of vascular aldosterone and corticosterone.
Hypertension
Effects of glucose on blood pressure and production of vascular aldosterone and corticosterone.
Hypertension
Effects of glycyrrhizin on production of vascular aldosterone and corticosterone.
Hypertension
Effects of spironolactone on systolic blood pressure in experimental diabetic rats.
Hypertension
Endothelial cell dysfunction in mice after transgenic knockout of type 2, but not type 1, 11beta-hydroxysteroid dehydrogenase.
Hypertension
Endothelin 1 type a receptor antagonism prevents vascular dysfunction and hypertension induced by 11beta-hydroxysteroid dehydrogenase inhibition: role of nitric oxide.
Hypertension
Enhanced 11beta-hydroxysteroid dehydrogenase activity, the metabolic syndrome, and systemic hypertension.
Hypertension
Epigenetic control of 11 beta-hydroxysteroid dehydrogenase 2 gene promoter is related to human hypertension.
Hypertension
Epigenetic regulation of 11 beta-hydroxysteroid dehydrogenase type 2 expression.
Hypertension
Epigenetics and arterial hypertension: the challenge of emerging evidence.
Hypertension
Evidence of altered cortisol metabolism in critically ill patients: a prospective study.
Hypertension
Expression of renal 11beta-hydroxysteroid dehydrogenase type 2 is decreased in patients with impaired renal function.
Hypertension
Extra-adrenal regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: physiological regulator and pharmacological target for energy partitioning.
Hypertension
Extracellular ATP determines 11beta-hydroxysteroid dehydrogenase type 2 activity via purinergic receptors.
Hypertension
Functional adrenocorticotropic hormone receptor in cultured human vascular endothelial cells : possible role in control of blood pressure.
Hypertension
Functional effects of polymorphisms in the human gene encoding 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1): a sequence variant at the translation start of 11 beta-HSD1 alters enzyme levels.
Hypertension
Gene expression of 11beta-hydroxysteroid dehydrogenase type 1 and type 2 in the kidneys of insulin-dependent diabetic rats.
Hypertension
Genetic association of 11 beta-hydroxysteroid dehydrogenase type 2 (HSD11B2) flanking microsatellites with essential hypertension in blacks.
Hypertension
Genetic determination of human essential hypertension.
Hypertension
Genetic variations of HSD11B2 in hypertensive patients and in the general population, six rare missense/frameshift mutations.
Hypertension
Genotype-phenotype correlations of mutations and polymorphisms in HSD11B2, the gene encoding the kidney isozyme of 11beta-hydroxysteroid dehydrogenase.
Hypertension
Glucocorticoid programming.
Hypertension
Glucocorticoid-mediated mineralocorticoid receptor activation and hypertension.
Hypertension
Glucocorticoids and vascular reactivity.
Hypertension
Glucocorticoids, prenatal stress and the programming of disease.
Hypertension
Glycyrrhetinic acid attenuates vascular smooth muscle vasodilatory function in healthy humans.
Hypertension
Glycyrrhetinic acid decreases plasma potassium concentrations in patients with anuria.
Hypertension
Herbal Medicine Containing Licorice May Be Contraindicated for a Patient With an HSD11B2 Mutation.
Hypertension
HSD11B2 CA-repeat and sodium balance.
Hypertension
HSD11B2, RUNX3, and LINE-1 Methylation in Placental DNA of Hypertensive Disorders of Pregnancy Patients.
Hypertension
Hypertension and circulating mRNA for 11beta-hydroxysteroid dehydrogenase type II.
Hypertension
Hypertension and the cortisol-cortisone shuttle.
Hypertension
Hypertension in mice lacking 11beta-hydroxysteroid dehydrogenase type 2.
Hypertension
Impaired protein stability of 11beta-hydroxysteroid dehydrogenase type 2: a novel mechanism of apparent mineralocorticoid excess.
Hypertension
In vivo 11beta-HSD-2 activity: variability, salt-sensitivity, and effect of licorice.
Hypertension
Influence of aldosterone vs. endothelin receptor antagonism on renovascular function in liquorice-induced hypertension.
Hypertension
Inhibition of 11-beta-hydroxysteroid dehydrogenase in pregnant rats and the programming of blood pressure in the offspring.
Hypertension
Interaction between an 11betaHSD1 gene variant and birth era modifies the risk of hypertension in Pima Indians.
Hypertension
Interactions between 11beta-hydroxysteroid dehydrogenase and COX-2 in kidney.
Hypertension
Late-onset apparent mineralocorticoid excess caused by novel compound heterozygous mutations in the HSD11B2 gene.
Hypertension
Licorice reduces serum testosterone in healthy women.
Hypertension
Licorice-induced hypertension and common variants of genes regulating renal sodium reabsorption.
Hypertension
Maintenance of maternal diet-induced hypertension in the rat is dependent on glucocorticoids.
Hypertension
Maternal hypertension and progeny blood pressure: role of aldosterone and 11beta-HSD.
Hypertension
Mechanism of hypertension in Cushing's syndrome: possible role of 11beta-hydroxysteroid dehydrogenase type 2 in kidneys and vascular cells.
Hypertension
Medical and physiological aspects of the 11beta-hydroxysteroid dehydrogenase system.
Hypertension
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Hypertension
Molecular basis for hypertension in the "type II variant" of apparent mineralocorticoid excess.
Hypertension
Molecular basis for the apparent mineralocorticoid excess syndrome in the Oman population.
Hypertension
Molecular determinants of the adrenal gland functioning related to stress-sensitive hypertension in ISIAH rats.
Hypertension
Mutations in the 11 beta-hydroxysteroid dehydrogenase type II enzyme associated with hypertension and possibly stillbirth.
Hypertension
Phenotypic analysis of mice bearing targeted deletions of 11beta-hydroxysteroid dehydrogenases 1 and 2 genes.
Hypertension
Possible association but no linkage of the HSD11B2 gene encoding the kidney isozyme of 11beta-hydroxysteroid dehydrogenase to hypertension in Black people.
Hypertension
Prevalence of mild apparent mineralocorticoid excess in Mennonites.
Hypertension
Quantitative real-time PCR for the measurement of 11beta-HSD1 and 11beta-HSD2 mRNA levels in tissues of healthy dogs.
Hypertension
Reduced levels of circulating 7alpha-hydroxy-dehydroepiandrosterone in treated adolescent obese patients.
Hypertension
Regulation of 11beta-hydroxysteroid dehydrogenase type 2 by diuretics and the renin-angiotensin-aldosterone axis.
Hypertension
Renal Dysfunction Induced by Kidney-Specific Gene Deletion of Hsd11b2 as a Primary Cause of Salt-Dependent Hypertension.
Hypertension
Renal interstitial corticosterone and 11-dehydrocorticosterone in conscious rats.
Hypertension
Renal medullary 11 beta-hydroxysteroid dehydrogenase type 1 in Dahl salt-sensitive hypertension.
Hypertension
Role of cardiovascular aldosterone in hypertension.
Hypertension
Role of HSD11B2 polymorphisms in essential hypertension and the diuretic response to thiazides.
Hypertension
Role of the 11beta-hydroxysteroid dehydrogenase type 2 in blood pressure regulation.
Hypertension
Role of the placenta in fetal programming: underlying mechanisms and potential interventional approaches.
Hypertension
Salt-sensitive men show reduced heart rate variability, lower norepinephrine and enhanced cortisol during mental stress.
Hypertension
Spironolactone effective hypertension in the elderly due to 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) impairment: contributory role of determining serum cortisol/cortisone ratio as a marker of 11beta-HSD2 activity.
Hypertension
Structural analysis and evaluation of the 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) gene in human essential hypertension.
Hypertension
Structural analysis of the 11beta-hydroxysteroid dehydrogenase type 2 gene in end-stage renal disease.
Hypertension
Structure of the VPATPD gene encoding subunit D of the human vacuolar proton ATPase.
Hypertension
The (+)- and (-)-gossypols potently inhibit human and rat 11beta-hydroxysteroid dehydrogenase type 2.
Hypertension
The 11beta-hydroxysteroid dehydrogenases: functions and physiological effects.
Hypertension
The cortisol-cortisone shuttle in children born with intrauterine growth retardation.
Hypertension
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
Hypertension
The hypertensiogenetic steroid 19-nor-progesterone does not influence cortisol inactivation by 11beta-hydroxysteroid dehydrogenase type 2.
Hypertension
The maternal diet during pregnancy programs altered expression of the glucocorticoid receptor and type 2 11beta-hydroxysteroid dehydrogenase: potential molecular mechanisms underlying the programming of hypertension in utero.
Hypertension
The mother or the fetus? 11beta-hydroxysteroid dehydrogenase type 2 null mice provide evidence for direct fetal programming of behavior by endogenous glucocorticoids.
Hypertension
The role of 11beta-hydroxysteroid dehydrogenase type 2 in human hypertension.
Hypertension
The role of the 11beta-hydroxysteroid dehydrogenase type 2 in human hypertension.
Hypertension
The type I and type II 11beta-hydroxysteroid dehydrogenase enzymes.
Hypertension
Tissue-specific Cushing's syndrome, 11beta-hydroxysteroid dehydrogenases and the redefinition of corticosteroid hormone action.
Hypertension
Tissue-specific glucocorticoid reactivating enzyme, 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)--a promising drug target for the treatment of metabolic syndrome.
Hypertension
Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice.
Hypertension
Urinary cortisol to cortisone metabolites in hypertensive obese children.
Hypertension
Urinary cortisol/cortisone ratios in hypertensive and normotensive cats.
Hypertension
Variation in placental type 2 11beta-hydroxysteroid dehydrogenase activity is not related to birth weight or placental weight.
Hypertension
[Possible pathogenetic role of 11 beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) gene polymorphisms in arterial hypertension]
Hypertension
[The activity of 11beta-hydroxysteroid dehydrogenase of rat kidney and liver at inherited stress-induced arterial hypertension]
Hypertension, Pregnancy-Induced
Alteration of the activity of the 11beta-hydroxysteroid dehydrogenase in pregnancy: relevance for the development of pregnancy-induced hypertension?
Hypertension, Pregnancy-Induced
HSD11B2, RUNX3, and LINE-1 Methylation in Placental DNA of Hypertensive Disorders of Pregnancy Patients.
Hyperthyroidism
Comprehensive study of urinary cortisol metabolites in hyperthyroid and hypothyroid patients.
Hypertriglyceridemia
11beta-HSD1 inhibition improves triglyceridemia through reduced liver VLDL secretion and partitions lipids toward oxidative tissues.
Hypertrophy, Left Ventricular
Sexually dimorphic effects of maternal alcohol intake and adrenalectomy on left ventricular hypertrophy in rat offspring.
Hypoglycemia
Deletion of Hexose-6-phosphate Dehydrogenase Activates the Unfolded Protein Response Pathway and Induces Skeletal Myopathy.
Hypokalemia
Apparent mineralocorticoid excess caused by novel compound heterozygous mutations in HSD11B2 and characterized by early-onset hypertension and hypokalemia.
Hypokalemia
Correlation between decrease of 11beta-hydroxysteroid dehydrogenase activity and hypokalemia induced by furosemide in rats.
Hypokalemia
Cortisol metabolism in hypertension.
Hypokalemia
Genetic variations of HSD11B2 in hypertensive patients and in the general population, six rare missense/frameshift mutations.
Hypokalemia
Hypertension in mice lacking 11beta-hydroxysteroid dehydrogenase type 2.
Hypokalemia
Impaired protein stability of 11beta-hydroxysteroid dehydrogenase type 2: a novel mechanism of apparent mineralocorticoid excess.
Hypokalemia
Persistent hypokalemia after successful adrenalectomy in a patient with Cushing's syndrome due to ectopic ACTH secretion: possible role of 11beta-hydroxysteroid dehydrogenase inhibition.
Hypokalemia
Phenotypic analysis of mice bearing targeted deletions of 11beta-hydroxysteroid dehydrogenases 1 and 2 genes.
Hypokalemia
Role of the 11beta-hydroxysteroid dehydrogenase type 2 in blood pressure regulation.
Hypokalemia
Severe muscle weakness due to hypokalemia as a manifestation of small-cell carcinoma.
Hypokalemia
The (+)- and (-)-gossypols potently inhibit human and rat 11beta-hydroxysteroid dehydrogenase type 2.
Hypophosphatemia, Familial
Transcriptional and physiological responses to chronic ACTH treatment by the mouse kidney.
Hypopituitarism
Growth hormone, insulin-like growth factor-I and the cortisol-cortisone shuttle.
Hypopituitarism
Lack of contribution of 11betaHSD1 and glucocorticoid action to reduced muscle mass associated with reduced growth hormone action.
Hypopituitarism
Lack of regulation of 11beta-hydroxysteroid dehydrogenase type 1 during short-term manipulation of GH in patients with hypopituitarism.
Hypotension
Placental 11beta-HSD2 activity, early postnatal clinical course, and adrenal function in extremely low birth weight infants.
Hypothyroidism
Effects of thyroid hormone (thyroxine) and testosterone on hepatic 11beta-hydroxysteroid dehydrogenase mRNA and activity in pubertal hypothyroid male rats.
Hypothyroidism
Sex-specific effects of growth hormone on hepatic 11beta-hydroxysteroid dehydrogenase activity and gene expression in hypothyroid rats.
Infections
Aeromonas hydrophila infection in silver catfish causes hyperlocomotion related to stress.
Infections
Clinical outcome in anti-neutrophil cytoplasmic antibody-associated vasculitis and gene variants of 11?-hydroxysteroid dehydrogenase type 1 and the glucocorticoid receptor.
Infections
Effect of pro-inflammatory cytokines on expression and activity of 11beta-hydroxysteroid dehydrogenase type 2 in cultured human term placental trophoblast and human choriocarcinoma JEG-3 cells.
Infections
Enhancement of cortisol-induced 11beta-hydroxysteroid dehydrogenase type 1 expression by interleukin 1beta in cultured human chorionic trophoblast cells.
Infections
Stimulation of 11beta-HSD1 expression by IL-1beta via a C/EBP binding site in human fetal lung fibroblasts.
Infertility, Male
Transcriptional alterations of genes related to fertility decline in male rats induced by chronic sleep restriction.
Inflammatory Bowel Diseases
11beta-hydroxysteroid dehydrogenase 1 and 2 expression in colon from patients with ulcerative colitis.
Inflammatory Bowel Diseases
Expression profiles of human 11beta-hydroxysteroid dehydrogenases type 1 and type 2 in inflammatory bowel diseases.
Inflammatory Bowel Diseases
Type II 11beta-hydroxysteroid dehydrogenase expression in human colonic epithelial cells of inflammatory bowel disease.
Inflammatory Bowel Diseases
Upregulation of 11?-hydroxysteroid dehydrogenase 1 in lymphoid organs during inflammation in the rat.
Insulin Resistance
11 beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndrome.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase 2 activity is elevated in severe obesity and negatively associated with insulin sensitivity.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase activity in acromegalic patients with normal or impaired carbohydrate metabolism.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase and the pre-receptor regulation of corticosteroid hormone action.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue and prospective changes in body weight and insulin resistance.
Insulin Resistance
11Beta-hydroxysteroid dehydrogenase type 1 in human disease: a novel therapeutic target.
Insulin Resistance
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors for metabolic syndrome.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents.
Insulin Resistance
11beta-hydroxysteroid dehydrogenase type 1 mRNA is increased in both visceral and subcutaneous adipose tissue of obese patients.
Insulin Resistance
11{beta}-hydroxysteroid dehydrogenase type 1 regulates glucocorticoid-induced insulin resistance in skeletal muscle.
Insulin Resistance
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Insulin Resistance
Adipose tissue expression of 11beta-hydroxysteroid dehydrogenase type 1 in Cushing's syndrome and in obesity.
Insulin Resistance
Altered cortisol metabolism in polycystic ovary syndrome: insulin enhances 5alpha-reduction but not the elevated adrenal steroid production rates.
Insulin Resistance
Antidiabetic effects of 11beta-HSD1 inhibition in a mouse model of combined diabetes, dyslipidaemia and atherosclerosis.
Insulin Resistance
Association between 11beta-hydroxysteroid dehydrogenase type 1 gene polymorphisms and metabolic syndrome in Bosnian population.
Insulin Resistance
Association of HSD11B1 gene polymorphisms with type 2 diabetes and metabolic syndrome in South Indian population.
Insulin Resistance
Cortisol metabolism and the role of 11beta-hydroxysteroid dehydrogenase.
Insulin Resistance
Cortisol metabolism in healthy young adults: sexual dimorphism in activities of A-ring reductases, but not 11beta-hydroxysteroid dehydrogenases.
Insulin Resistance
Cortisol metabolism in human obesity: impaired cortisone-->cortisol conversion in subjects with central adiposity.
Insulin Resistance
Cortisone induces insulin resistance in C2C12 myotubes through activation of 11beta-hydroxysteroid dehydrogenase 1 and autocrinal regulation.
Insulin Resistance
Deep subcutaneous adipose tissue: a distinct abdominal adipose depot.
Insulin Resistance
Deletion of Hexose-6-phosphate Dehydrogenase Activates the Unfolded Protein Response Pathway and Induces Skeletal Myopathy.
Insulin Resistance
Diabetic pregnancy in rats leads to impaired glucose metabolism in offspring involving tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 expression.
Insulin Resistance
Diet-induced weight loss alters hepatic glucocorticoid metabolism in type 2 diabetes mellitus.
Insulin Resistance
Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors.
Insulin Resistance
Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Insulin Resistance
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Insulin Resistance
Ectopic lipid deposition mediates insulin resistance in adipose specific 11?-Hydroxysteroid dehydrogenase type 1 transgenic mice.
Insulin Resistance
Effect of voluntary exercise on peripheral tissue glucocorticoid receptor content and the expression and activity of 11beta-HSD1 in the Syrian hamster.
Insulin Resistance
Effects of a high-salt diet on adipocyte glucocorticoid receptor and 11-beta hydroxysteroid dehydrogenase 1 in salt-sensitive hypertensive rats.
Insulin Resistance
Effects of peroxisome proliferator-activated receptor-alpha and -gamma agonists on 11beta-hydroxysteroid dehydrogenase type 1 in subcutaneous adipose tissue in men.
Insulin Resistance
Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice.
Insulin Resistance
Enhanced cortisol production rates, free cortisol, and 11beta-HSD-1 expression correlate with visceral fat and insulin resistance in men: effect of weight loss.
Insulin Resistance
Expression of 11beta-hydroxysteroid dehydrogenase 1 and 2 in subcutaneous adipose tissue of lean and obese women with and without polycystic ovary syndrome.
Insulin Resistance
Gender-specific links between hepatic 11beta reduction of cortisone and adipokines.
Insulin Resistance
Glucocorticoid metabolism within superficial subcutaneous rather than visceral adipose tissue is associated with features of the metabolic syndrome in South African women.
Insulin Resistance
Glucocorticoid receptor gene expression in adipose tissue and associated metabolic risk in black and white South African women.
Insulin Resistance
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic sindrome.
Insulin Resistance
Growth hormone, insulin-like growth factor-I and the cortisol-cortisone shuttle.
Insulin Resistance
H6PDH interacts directly with 11beta-HSD1: implications for determining the directionality of glucocorticoid catalysis.
Insulin Resistance
Hepatic glucose regulation and metabolism in adult sheep: effects of prenatal betamethasone.
Insulin Resistance
Hexose-6-phosphate dehydrogenase in the endoplasmic reticulum.
Insulin Resistance
Immortalization of Porcine 11?-Hydroxysteroid Dehydrogenase Type 1-Transgenic Liver Cells Using SV40 Large T Antigen.
Insulin Resistance
Impaired glucose tolerance and insulin resistance are associated with increased adipose 11beta-hydroxysteroid dehydrogenase type 1 expression and elevated hepatic 5alpha-reductase activity.
Insulin Resistance
Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice.
Insulin Resistance
In the lipodystrophy associated with highly active antiretroviral therapy, pseudo-Cushing's syndrome is associated with increased regeneration of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue.
Insulin Resistance
In vivo activity of 11beta-hydroxysteroid dehydrogenase type 1 and free fatty acid-induced insulin resistance.
Insulin Resistance
Increased glucocorticoid receptor and 11{beta}-hydroxysteroid dehydrogenase type 1 expression in hepatocytes may contribute to the phenotype of type 2 diabetes in db/db mice.
Insulin Resistance
Increased glucocorticoid receptor expression in human skeletal muscle cells may contribute to the pathogenesis of the metabolic syndrome.
Insulin Resistance
Increased in vivo regeneration of cortisol in adipose tissue in human obesity and effects of the 11beta-hydroxysteroid dehydrogenase type 1 inhibitor carbenoxolone.
Insulin Resistance
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 in obesity.
Insulin Resistance
Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 for the treatment of metabolic syndrome.
Insulin Resistance
Insulin sensitisation in the treatment of Type 2 diabetes.
Insulin Resistance
Interactions between oestradiol and glucocorticoid regulatory effects on liver-specific glucocorticoid-inducible genes: possible evidence for a role of hepatic 11beta-hydroxysteroid dehydrogenase type 1.
Insulin Resistance
Is 11beta-hydroxysteroid dehydrogenase type 1 a therapeutic target? Effects of carbenoxolone in lean and obese Zucker rats.
Insulin Resistance
Lack of relationship between 11beta-hydroxysteroid dehydrogenase setpoint and insulin sensitivity in the basal state and after 24h of insulin infusion in healthy subjects and type 2 diabetic patients.
Insulin Resistance
Leptin activation of corticosterone production in hepatocytes may contribute to the reversal of obesity and hyperglycemia in leptin-deficient ob/ob mice.
Insulin Resistance
Local and systemic impact of transcriptional up-regulation of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue in human obesity.
Insulin Resistance
Mechanisms of disease: Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a novel treatment for the metabolic syndrome.
Insulin Resistance
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Insulin Resistance
Minireview: hexose-6-phosphate dehydrogenase and redox control of 11{beta}-hydroxysteroid dehydrogenase type 1 activity.
Insulin Resistance
Modulation of susceptibility to weight gain and insulin resistance in low birthweight rats by treatment of their mothers with leptin during pregnancy and lactation.
Insulin Resistance
Molecular determinants of the adrenal gland functioning related to stress-sensitive hypertension in ISIAH rats.
Insulin Resistance
MRNA and enzyme activity of hepatic 11beta-hydroxysteroid dehydrogenase type 1 are elevated in C57BL/KsJ-db/db mice.
Insulin Resistance
Overexpression of 11beta-Hydroxysteroid Dehydrogenase Type 1 in Hepatic and Visceral Adipose Tissue is Associated with Metabolic Disorders in Morbidly Obese Patients.
Insulin Resistance
Overexpression of 11beta-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of insulin resistance: studies in young adult monozygotic twins.
Insulin Resistance
Pathophysiology of metabolic syndrome X and its links to the perinatal period.
Insulin Resistance
Physiological roles of 11 beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase.
Insulin Resistance
Population Pharmacokinetic/Pharmacodynamic Model of Subcutaneous Adipose 11{beta}-Hydroxysteroid Dehydrogenase Type 1 (11{beta}-HSD1) Activity After Oral Administration of AMG 221, a Selective 11{beta}-HSD1 Inhibitor.
Insulin Resistance
Readjusting the glucocorticoid balance: an opportunity for modulators of 11beta-hydroxysteroid dehydrogenase type 1 activity?
Insulin Resistance
Reduced 11beta-hydroxysteroid dehydrogenase type 1 activity in obese boys.
Insulin Resistance
Reduced glucocorticoid production rate, decreased 5alpha-reductase activity, and adipose tissue insulin sensitization after weight loss.
Insulin Resistance
Reduced levels of circulating 7alpha-hydroxy-dehydroepiandrosterone in treated adolescent obese patients.
Insulin Resistance
Regulation of 11beta-HSD genes in human adipose tissue: influence of central obesity and weight loss.
Insulin Resistance
Regulation of glucocorticoid receptor alpha and beta isoforms and type I 11beta-hydroxysteroid dehydrogenase expression in human skeletal muscle cells: a key role in the pathogenesis of insulin resistance?
Insulin Resistance
Rosiglitazone decreases 11beta-hydroxysteroid dehydrogenase type 1 in subcutaneous adipose tissue.
Insulin Resistance
Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains.
Insulin Resistance
Several obesity- and nutrient-related gene polymorphisms but not FTO and UCP variants modulate postabsorptive resting energy expenditure and fat-induced thermogenesis in obese individuals: the NUGENOB Study.
Insulin Resistance
Skeletal muscle 11beta-HSD1 controls glucocorticoid-induced proteolysis and expression of E3 ubiquitin ligases atrogin-1 and MuRF-1.
Insulin Resistance
Sub-chronic administration of the 11beta-HSD1 inhibitor, carbenoxolone, improves glucose tolerance and insulin sensitivity in mice with diet-induced obesity.
Insulin Resistance
Subcutaneous Abdominal Adipose Tissue Subcompartments: Potential Role in Rosiglitazone Effects.
Insulin Resistance
The contribution of visceral adipose tissue to splanchnic cortisol production in healthy humans.
Insulin Resistance
The critical role of the N-terminus of 11beta-hydroxysteroid dehydrogenase type 1, as being encoded by exon 1, for enzyme stabilization and activity.
Insulin Resistance
The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors.
Insulin Resistance
Tissue-specific changes in peripheral cortisol metabolism in obese women: increased adipose 11beta-hydroxysteroid dehydrogenase type 1 activity.
Insulin Resistance
Tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 and pathogenesis of the metabolic syndrome.
Insulin Resistance
Tissue-specific glucocorticoid reactivating enzyme, 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)--a promising drug target for the treatment of metabolic syndrome.
Insulin Resistance
Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice.
Insulin Resistance
Variants in HSD11B1 gene modulate susceptibility to diabetes kidney disease and to insulin resistance in type 1 diabetes.
Insulin Resistance
Weight loss increases 11beta-hydroxysteroid dehydrogenase type 1 expression in human adipose tissue.
Kidney Diseases
Variants in HSD11B1 gene modulate susceptibility to diabetes kidney disease and to insulin resistance in type 1 diabetes.
Kidney Failure, Chronic
A new polymorphic restriction site in the human 11 beta-hydroxysteroid dehydrogenase type 2 gene.
Kidney Failure, Chronic
Assessing systemic 11beta-hydroxysteroid dehydrogenase with serum cortisone/cortisol ratios in healthy subjects and patients with diabetes mellitus and chronic renal failure.
Kidney Failure, Chronic
Genetic association of 11 beta-hydroxysteroid dehydrogenase type 2 (HSD11B2) flanking microsatellites with essential hypertension in blacks.
Kidney Failure, Chronic
Pediatric renal allograft transplantation does not normalize the increased cortisol/cortisone ratios of chronic renal failure.
Kidney Failure, Chronic
Role of 11beta-hydroxysteroid dehydrogenase 2 renal activity in potassium homeostasis in rats with chronic renal failure.
Kidney Failure, Chronic
Role of the 11beta-hydroxysteroid dehydrogenase type 2 in blood pressure regulation.
Kidney Failure, Chronic
Structural analysis of the 11beta-hydroxysteroid dehydrogenase type 2 gene in end-stage renal disease.
Kidney Failure, Chronic
The role of 11beta-hydroxysteroid dehydrogenase type 2 in human hypertension.
Leprosy
Alteration of the cortisol-cortisone shuttle in leprosy type 1 reactions in leprosy patients in Hyderabad, India.
Leukemia
Differential regulation of 11beta-hydroxysteroid dehydrogenase-1 by dexamethasone in glucocorticoid-sensitive and -resistant childhood lymphoblastic leukemia.
Leukemia
Meeting Report:The 7th ESPE Growth Plate Working Group Symposium - EUROGROP June 27th 2007, Helsinki, Finland.
Liddle Syndrome
Down-regulation of a hepatic transporter multidrug resistance-associated protein 2 is involved in alteration of pharmacokinetics of glycyrrhizin and its metabolites in a rat model of chronic liver injury.
Liddle Syndrome
Renal tubular transport and the genetic basis of hypertensive disease.
Lipodystrophy
In the lipodystrophy associated with highly active antiretroviral therapy, pseudo-Cushing's syndrome is associated with increased regeneration of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue.
Liver Cirrhosis
11Beta-hydroxysteroid dehydrogenase-1 deficiency or inhibition enhances hepatic myofibroblast activation in murine liver fibrosis.
Liver Cirrhosis
Apparent mineralocorticoid excess syndrome: an overview.
Liver Cirrhosis
Biphasic changes of epithelial sodium channel abundance and trafficking in common bile duct ligation-induced liver cirrhosis.
Liver Cirrhosis
Down-regulation of a hepatic transporter multidrug resistance-associated protein 2 is involved in alteration of pharmacokinetics of glycyrrhizin and its metabolites in a rat model of chronic liver injury.
Liver Cirrhosis
Glucocorticoid-mediated mineralocorticoid receptor activation and hypertension.
Liver Cirrhosis
Increased apical targeting of renal epithelial sodium channel subunits and decreased expression of type 2 11beta-hydroxysteroid dehydrogenase in rats with CCl4-induced decompensated liver cirrhosis.
Liver Cirrhosis
Renal sodium retention in cirrhotic rats depends on glucocorticoid-mediated activation of mineralocorticoid receptor due to decreased renal 11beta-HSD-2 activity.
Liver Diseases
Induction of hepatic 11beta-hydroxysteroid dehydrogenase type 1 in patients with alcoholic liver disease.
Liver Diseases, Alcoholic
Induction of hepatic 11beta-hydroxysteroid dehydrogenase type 1 in patients with alcoholic liver disease.
Lung Neoplasms
11Beta-hydroxysteroid dehydrogenase 1 expression in squamous cell carcinomas of the head and neck.
Lung Neoplasms
Expression of 11beta-hydroxysteroid dehydrogenase type 2 in an ACTH-producing small cell lung cancer.
Lung Neoplasms
Interindividual variability in the expression and NNK carbonyl reductase activity of 11beta-hydroxysteroid dehydrogenase 1 in human lung.
Lung Neoplasms
NNK reduction pathway gene polymorphisms and risk of lung cancer.
Lung Neoplasms
Purification, characterization and NNK carbonyl reductase activities of 11beta-hydroxysteroid dehydrogenase type 1 from human liver: enzyme cooperativity and significance in the detoxification of a tobacco-derived carcinogen.
Malnutrition
Fetal exposure to excess glucocorticoid is unlikely to explain the effects of periconceptional undernutrition in sheep.
Malnutrition
Maternal undernutrition during early to midgestation programs tissue-specific alterations in the expression of the glucocorticoid receptor, 11beta-hydroxysteroid dehydrogenase isoforms, and type 1 angiotensin ii receptor in neonatal sheep.
Malnutrition
Perinatal maternal undernutrition programs the offspring hypothalamo-pituitary-adrenal (HPA) axis.
Menorrhagia
Cortisol inactivation by 11beta-hydroxysteroid dehydrogenase-2 may enhance endometrial angiogenesis via reduced thrombospondin-1 in heavy menstruation.
Metabolic Diseases
11beta-HSD1, inflammation, metabolic disease and age-related cognitive (dys)function.
Metabolic Diseases
11beta-Hydroxysteroid dehydrogenase type 1 is an important regulator at the interface of obesity and inflammation.
Metabolic Diseases
A Polygenic Model of the Metabolic Syndrome With Reduced Circulating and Intra-Adipose Glucocorticoid Action.
Metabolic Diseases
Alteration in methylation level at 11?-hydroxysteroid dehydrogenase type 2 gene promoter in infants born to preeclamptic women.
Metabolic Diseases
Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Metabolic Diseases
Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11 -hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys.
Metabolic Diseases
Development of a high-throughput cell-based assay for 11beta-hydroxysteroid dehydrogenase type 1 using BacMam technology.
Metabolic Diseases
Diabetic pregnancy in rats leads to impaired glucose metabolism in offspring involving tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 expression.
Metabolic Diseases
Docking-based 3D-QSAR study for 11beta-HSD1 inhibitors.
Metabolic Diseases
Down-regulation of adipose 11beta-hydroxysteroid dehydrogenase type 1 by high-fat feeding in mice: a potential adaptive mechanism counteracting metabolic disease.
Metabolic Diseases
Fructose consumption enhances glucocorticoid action in rat visceral adipose tissue.
Metabolic Diseases
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic sindrome.
Metabolic Diseases
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 by plant extracts used as traditional antidiabetic medicines.
Metabolic Diseases
Inhibition of human and rat 11beta-hydroxysteroid dehydrogenase type 1 by 18beta-glycyrrhetinic acid derivatives.
Metabolic Diseases
Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
Metabolic Diseases
Obesity and Corticosteroids: 11beta-Hydroxysteroid Type 1 as a Cause and Therapeutic Target in Metabolic Disease.
Metabolic Diseases
Role of the placenta in fetal programming: underlying mechanisms and potential interventional approaches.
Metabolic Diseases
Selection and optimization of MCF-7 cell line for screening selective inhibitors of 11beta-hydroxysteroid dehydrogenase 2.
Metabolic Diseases
Selective inhibition of 11beta-hydroxysteroid dehydrogenase 1 by 18alpha-glycyrrhetinic acid but not 18beta-glycyrrhetinic acid.
Metabolic Diseases
The role and regulation of 11beta-hydroxysteroid dehydrogenase type 1 in the inflammatory response.
Metabolic Diseases
The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors.
Metabolic Diseases
Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease.
Metabolic Diseases
Type 1 11beta-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases?
Metabolic Syndrome
11 beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndrome.
Metabolic Syndrome
11-Beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors in type 2 diabetes mellitus and obesity.
Metabolic Syndrome
11?-Hydroxysteroid dehydrogenase type 1: relevance of its modulation in the pathophysiology of obesity, the metabolic syndrome and type 2 diabetes mellitus.
Metabolic Syndrome
11Beta-HSD type 1 expression in human adipose tissue: impact of gender, obesity, and fat localization.
Metabolic Syndrome
11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice.
Metabolic Syndrome
11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 as a modulator of glucocorticoid action: from metabolism to memory.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 as a novel therapeutic target in metabolic and neurodegenerative disease.
Metabolic Syndrome
11Beta-hydroxysteroid dehydrogenase type 1 in human disease: a novel therapeutic target.
Metabolic Syndrome
11beta-Hydroxysteroid dehydrogenase Type 1 in obesity and Type 2 diabetes.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development.
Metabolic Syndrome
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors for metabolic syndrome.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents.
Metabolic Syndrome
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors: novel agents for the treatment of metabolic syndrome and obesity-related disorders?
Metabolic Syndrome
11beta-Hydroxysteroid Dehydrogenase Type 1 is Overexpressed in Subcutaneous Adipose Tissue of Morbidly Obese Patients.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 mRNA is increased in both visceral and subcutaneous adipose tissue of obese patients.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1 of the subcutaneous adipose tissue is dysregulated but not associated with metabolic disorders in adults born small for gestational age.
Metabolic Syndrome
11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.
Metabolic Syndrome
11Beta-hydroxysteroid dehydrogenase-1 deficiency or inhibition enhances hepatic myofibroblast activation in murine liver fibrosis.
Metabolic Syndrome
11{beta}-Hydroxysteroid Dehydrogenase Type 1 and Its Role in the Hypothalamus-Pituitary-Adrenal Axis, Metabolic Syndrome, and Inflammation.
Metabolic Syndrome
11{beta}-Hydroxysteroid Dehydrogenase Type 1: A Tissue-Specific Regulator of Glucocorticoid Response.
Metabolic Syndrome
2-(S)-phenethylaminothiazolones as potent, orally efficacious inhibitors of 11beta-hydroxysteriod dehydrogenase type 1.
Metabolic Syndrome
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
Metabolic Syndrome
7-oxysterols modulate glucocorticoid activity in adipocytes through competition for 11beta-hydroxysteroid dehydrogenase type.
Metabolic Syndrome
A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome.
Metabolic Syndrome
A novel promoter for the 11beta-hydroxysteroid dehydrogenase type 1 gene is active in lung and is C/EBPalpha independent.
Metabolic Syndrome
A Polygenic Model of the Metabolic Syndrome With Reduced Circulating and Intra-Adipose Glucocorticoid Action.
Metabolic Syndrome
Adipocyte-specific glucocorticoid inactivation protects against diet-induced obesity.
Metabolic Syndrome
Adrenal Steroids and the Metabolic Syndrome.
Metabolic Syndrome
Analysis of alternative promoter usage in expression of HSD11B1 including the development of a transcript-specific quantitative real-time PCR method.
Metabolic Syndrome
Antidiabetic effects of 11beta-HSD1 inhibition in a mouse model of combined diabetes, dyslipidaemia and atherosclerosis.
Metabolic Syndrome
Association between 11beta-hydroxysteroid dehydrogenase type 1 gene polymorphisms and metabolic syndrome in Bosnian population.
Metabolic Syndrome
Association Between a 11?-Hydroxysteroid Dehydrogenase Type 1 Gene Polymorphism and Metabolic Syndrome in a South Indian Population.
Metabolic Syndrome
Association of HSD11B1 gene polymorphisms with type 2 diabetes and metabolic syndrome in South Indian population.
Metabolic Syndrome
Association of HSD11B1 polymorphic variants and adipose tissue gene expression with metabolic syndrome, obesity and type 2 diabetes mellitus: a systematic review.
Metabolic Syndrome
Association study of 11beta-hydroxysteroid dehydrogenase type 1 gene polymorphisms and metabolic syndrome in urban Japanese cohort.
Metabolic Syndrome
Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors.
Metabolic Syndrome
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
Metabolic Syndrome
Carbenoxolone treatment attenuates symptoms of metabolic syndrome and atherogenesis in obese, hyperlipidemic mice.
Metabolic Syndrome
Cell-based assay for screening 11beta-hydroxysteroid dehydrogenase 1 inhibitors.
Metabolic Syndrome
Cell-type specific regulation of the human 11beta-hydroxysteroid dehydrogenase type 1 promoter.
Metabolic Syndrome
Characterisation of 11beta-hydroxysteroid dehydrogenase 1 in human orbital adipose tissue: a comparison with subcutaneous and omental fat.
Metabolic Syndrome
Charting biologically relevant chemical space: a structural classification of natural products (SCONP).
Metabolic Syndrome
Circulating 11beta-hydroxysteroid dehydrogenase type 1 mRNA and cardiovascular risk factors.
Metabolic Syndrome
Comparative enzymology of 11beta-hydroxysteroid dehydrogenase type 1 from six species.
Metabolic Syndrome
Comparison of a homology model and the crystallographic structure of human 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) in a structure-based identification of inhibitors.
Metabolic Syndrome
Cooperativity between 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase is based on a common pyridine nucleotide pool in the lumen of the endoplasmic reticulum.
Metabolic Syndrome
Cortisol--cause and cure for metabolic syndrome?
Metabolic Syndrome
Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11 -hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys.
Metabolic Syndrome
Development and application of a scintillation proximity assay (SPA) for identification of selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Metabolic Syndrome
Diabetic pregnancy in rats leads to impaired glucose metabolism in offspring involving tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 expression.
Metabolic Syndrome
Diazepane-acetamide derivatives as selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
Metabolic Syndrome
Different expression and distribution of 11beta-hydroxysteroid dehydrogenase type 1 in obese and lean animal models of type 2 diabetes.
Metabolic Syndrome
Different responsiveness in body weight and hepatic 11beta-hydroxysteroid dehydrogenase (11beta-HSD) type 1 mrna to 11beta-HSD inhibition by glycyrrhetinic acid treatment in obese and lean zucker rats.
Metabolic Syndrome
Differential modulation of 3T3-L1 adipogenesis mediated by 11beta-hydroxysteroid dehydrogenase-1 levels.
Metabolic Syndrome
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Metabolic Syndrome
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.
Metabolic Syndrome
Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
Metabolic Syndrome
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Metabolic Syndrome
Down-regulation of adipose 11beta-hydroxysteroid dehydrogenase type 1 by high-fat feeding in mice: a potential adaptive mechanism counteracting metabolic disease.
Metabolic Syndrome
Dysregulation of 11beta-hydroxysteroid dehydrogenases: implications during pregnancy and beyond.
Metabolic Syndrome
Effect of voluntary exercise on peripheral tissue glucocorticoid receptor content and the expression and activity of 11beta-HSD1 in the Syrian hamster.
Metabolic Syndrome
Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice.
Metabolic Syndrome
Enhanced 11beta-hydroxysteroid dehydrogenase activity, the metabolic syndrome, and systemic hypertension.
Metabolic Syndrome
Enzymology and molecular biology of glucocorticoid metabolism in humans.
Metabolic Syndrome
Evidence of altered cortisol metabolism in critically ill patients: a prospective study.
Metabolic Syndrome
Fetal origins of insulin resistance and obesity.
Metabolic Syndrome
Functional effects of polymorphisms in the human gene encoding 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1): a sequence variant at the translation start of 11 beta-HSD1 alters enzyme levels.
Metabolic Syndrome
Gender-dependent association of HSD11B1 single nucleotide polymorphisms with glucose and HDL-C levels.
Metabolic Syndrome
Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome.
Metabolic Syndrome
Global 11 Beta-Hydroxysteroid Dehydrogenase Activity Assessed by the Circulating Cortisol to Cortisone Ratio is Associated with Features of Metabolic Syndrome.
Metabolic Syndrome
Glucocorticoid metabolism within superficial subcutaneous rather than visceral adipose tissue is associated with features of the metabolic syndrome in South African women.
Metabolic Syndrome
Glucocorticoid regulation of the promoter of 11beta-hydroxysteroid dehydrogenase type 1 is indirect and requires CCAAT/enhancer-binding protein-beta.
Metabolic Syndrome
Glucocorticoid-mediated mineralocorticoid receptor activation and hypertension.
Metabolic Syndrome
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase in adipose tissue.
Metabolic Syndrome
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic sindrome.
Metabolic Syndrome
Hexose-6-phosphate dehydrogenase in the endoplasmic reticulum.
Metabolic Syndrome
Hexose-6-phosphate dehydrogenase knock-out mice lack 11 beta-hydroxysteroid dehydrogenase type 1-mediated glucocorticoid generation.
Metabolic Syndrome
High capacity homogeneous non-radioactive cortisol detection assays for human 11beta-hydroxysteroid dehydrogenase type 1.
Metabolic Syndrome
Immortalization of Porcine 11?-Hydroxysteroid Dehydrogenase Type 1-Transgenic Liver Cells Using SV40 Large T Antigen.
Metabolic Syndrome
Impact of HSD11B1 polymorphisms on BMI and components of the metabolic syndrome in patients receiving psychotropic treatments.
Metabolic Syndrome
Inhibition of 11beta-HSD1 as a novel treatment for the metabolic syndrome: do glucocorticoids play a role?
Metabolic Syndrome
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 in obesity.
Metabolic Syndrome
Inhibition of human and rat 11beta-hydroxysteroid dehydrogenase type 1 by 18beta-glycyrrhetinic acid derivatives.
Metabolic Syndrome
Inhibitors of 11beta-HSD1: a potential treatment for the metabolic syndrome.
Metabolic Syndrome
Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 for the treatment of metabolic syndrome.
Metabolic Syndrome
Insulin and dexamethasone dynamically regulate adipocyte 11beta-hydroxysteroid dehydrogenase type 1.
Metabolic Syndrome
Is the metabolic syndrome an intracellular Cushing state? Effects of multiple humoral factors on the transcriptional activity of the hepatic glucocorticoid-activating enzyme (11beta-hydroxysteroid dehydrogenase type 1) gene.
Metabolic Syndrome
Lack of association of the 11 beta-hydroxysteroid dehydrogenase type 1 gene 25669dupA polymorphism with obesity and metabolic syndrome.
Metabolic Syndrome
Lessons in obesity from transgenic animals.
Metabolic Syndrome
Liver X receptors downregulate 11beta-hydroxysteroid dehydrogenase type 1 expression and activity.
Metabolic Syndrome
Local metabolism of glucocorticoids in Prague hereditary hypertriglyceridemic rats - Effect of hypertriglyceridemia and gender.
Metabolic Syndrome
Mechanisms of disease: Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a novel treatment for the metabolic syndrome.
Metabolic Syndrome
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Metabolic Syndrome
Minireview: hexose-6-phosphate dehydrogenase and redox control of 11{beta}-hydroxysteroid dehydrogenase type 1 activity.
Metabolic Syndrome
Molecular screening of the 11beta-HSD1 gene in men characterized by the metabolic syndrome.
Metabolic Syndrome
Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Metabolic Syndrome
Omental 11beta-hydroxysteroid dehydrogenase 1 correlates with fat cell size independently of obesity.
Metabolic Syndrome
Optimization of high-resolution melting analysis for simultaneous genotyping of two 11?-hydroxysteroid dehydrogenase type 1 gene polymorphisms.
Metabolic Syndrome
Pathophysiology of metabolic syndrome X and its links to the perinatal period.
Metabolic Syndrome
Physiological roles of 11 beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase.
Metabolic Syndrome
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
Metabolic Syndrome
Postnatal programming of glucocorticoid metabolism in rats modulates high-fat diet-induced regulation of visceral adipose tissue glucocorticoid exposure and sensitivity and adiponectin and proinflammatory adipokines gene expression in adulthood.
Metabolic Syndrome
Prenatal programming of metabolic syndrome in the common marmoset is associated with increased expression of 11ss-hydroxysteroid dehydrogenase type 1.
Metabolic Syndrome
Preventing local regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1 enhances angiogenesis.
Metabolic Syndrome
Readjusting the glucocorticoid balance: an opportunity for modulators of 11beta-hydroxysteroid dehydrogenase type 1 activity?
Metabolic Syndrome
Regulation of 11beta-HSD genes in human adipose tissue: influence of central obesity and weight loss.
Metabolic Syndrome
Relationship of 11?-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase gene polymorphisms with metabolic syndrome and type 2 diabetes.
Metabolic Syndrome
Selection and optimization of MCF-7 cell line for screening selective inhibitors of 11beta-hydroxysteroid dehydrogenase 2.
Metabolic Syndrome
Selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 for patients with metabolic syndrome: is the target liver, fat, or both?
Metabolic Syndrome
Structural characterization and pharmacodynamic effects of an orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor.
Metabolic Syndrome
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Metabolic Syndrome
Targeting the pre-receptor metabolism of cortisol as a novel therapy in obesity and diabetes.
Metabolic Syndrome
The role of 11beta-hydroxysteroid dehydrogenase activity in the metabolic syndrome: lessons learned from the animal model.
Metabolic Syndrome
The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors.
Metabolic Syndrome
The role of glucocorticoid action in the pathophysiology of the Metabolic Syndrome.
Metabolic Syndrome
Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease.
Metabolic Syndrome
Tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 and pathogenesis of the metabolic syndrome.
Metabolic Syndrome
Tissue-specific glucocorticoid reactivating enzyme, 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)--a promising drug target for the treatment of metabolic syndrome.
Metabolic Syndrome
Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice.
Metabolic Syndrome
Type 1 11beta-hydroxysteroid dehydrogenase as universal drug target in metabolic diseases?
Metabolic Syndrome
Type 2 diabetes and metabolic syndrome are associated with increased expression of 11beta-hydroxysteroid dehydrogenase 1 in obese subjects.
Metabolic Syndrome
[Intracellular glucocorticoid reactivating enzyme, 11beta-HSD1 as a promising drug target against metabolic syndrome]
Metabolic Syndrome
[Reduction of obesity-related metabolic risk by modulating tissue exposition to cortisol].
Mineralocorticoid Excess Syndrome, Apparent
Apparent mineralocorticoid excess syndrome in a Brazilian boy caused by the homozygous missense mutation p.R186C in the HSD11B2 gene.
Mineralocorticoid Excess Syndrome, Apparent
Mimicry and well known genetic friends: molecular diagnosis in an Iranian cohort of suspected Bartter syndrome and proposition of an algorithm for clinical differential diagnosis.
Mineralocorticoid Excess Syndrome, Apparent
Serum Cortisol and Cortisone as potential biomarkers of Partial 11?-hydroxysteroid dehydrogenase type-2 Deficiency.
Mineralocorticoid Excess Syndrome, Apparent
[Measurement of free urinary cortisol and cortisone using liquid chromatography associated with tandem mass spectrometry method]
Muscular Atrophy
Lack of contribution of 11betaHSD1 and glucocorticoid action to reduced muscle mass associated with reduced growth hormone action.
Muscular Atrophy
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
Myotonic Dystrophy
Glucocorticoid metabolism and adrenocortical reactivity to ACTH in myotonic dystrophy.
Myotonic Dystrophy
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Neoplasm Metastasis
Can licorice lick colon cancer?
Neoplasm Metastasis
Inhibition of 11beta-hydroxysteroid dehydrogenase type II selectively blocks the tumor COX-2 pathway and suppresses colon carcinogenesis in mice and humans.
Neoplasm Metastasis
Type-2 11?-hydroxysteroid dehydrogenase promotes the metastasis of colorectal cancer via the Fgfbp1-AKT pathway.
Neoplasms
11Beta-hydroxysteroid dehydrogenase 1 expression in squamous cell carcinomas of the head and neck.
Neoplasms
11beta-Hydroxysteroid dehydrogenase types 1 and 2 are up- and downregulated in cortisol-secreting adrenal adenomas.
Neoplasms
11beta-hydroxysteroid dehydrogenases, cell proliferation and malignancy.
Neoplasms
A variant (rs932335) in the HSD11B1 gene is associated with colorectal cancer in a Chinese population.
Neoplasms
Analysis of alternative promoter usage in expression of HSD11B1 including the development of a transcript-specific quantitative real-time PCR method.
Neoplasms
Augmentation of 11beta-hydroxysteroid dehydrogenase type 1 in LPS-activated J774.1 macrophages--role of 11beta-HSD1 in pro-inflammatory properties in macrophages.
Neoplasms
Can licorice lick colon cancer?
Neoplasms
Cortisol is a suppressor of apoptosis in bovine corpus luteum.
Neoplasms
CTL recognition of a novel HLA-A*0201-binding peptide derived from glioblastoma multiforme tumor cells.
Neoplasms
Cushing's syndrome associated with a nested stromal epithelial tumor of the liver: hormonal, immunohistochemical, and molecular studies.
Neoplasms
Deep subcutaneous adipose tissue: a distinct abdominal adipose depot.
Neoplasms
Dexamethasone enhances basal and TNF-{alpha}-stimulated production of PAI-1 via the glucocorticoid receptor regardless of 11{beta}-hydroxysteroid dehydrogenase 2 status in human proximal renal tubular cells.
Neoplasms
Effect of pro-inflammatory cytokines on expression and activity of 11beta-hydroxysteroid dehydrogenase type 2 in cultured human term placental trophoblast and human choriocarcinoma JEG-3 cells.
Neoplasms
Effects of a high-salt diet on adipocyte glucocorticoid receptor and 11-beta hydroxysteroid dehydrogenase 1 in salt-sensitive hypertensive rats.
Neoplasms
Effects of Carbenoxolone on the Canine Pituitary-Adrenal Axis.
Neoplasms
Expression of 11beta-hydroxysteroid dehydrogenase type 2 in an ACTH-producing small cell lung cancer.
Neoplasms
Expression of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in colorectal cancer.
Neoplasms
Expression of glucocorticoid receptor and 11beta hydroxysteroid dehydrogenase in a case of pulmonary epithelioid haemangioendothelioma.
Neoplasms
Gender-specific links between hepatic 11beta reduction of cortisone and adipokines.
Neoplasms
Genetic variation in candidate obesity genes ADRB2, ADRB3, GHRL, HSD11B1, IRS1, IRS2, and SHC1 and risk for breast cancer in the Cancer Prevention Study II.
Neoplasms
Glucocorticoid availability in colonic inflammation of rat.
Neoplasms
Glucocorticoid-mediated mineralocorticoid receptor activation and hypertension.
Neoplasms
HSD11B2, RUNX3, and LINE-1 Methylation in Placental DNA of Hypertensive Disorders of Pregnancy Patients.
Neoplasms
Hypothalamic regulation of adiposity: the role of 11beta-hydroxysteroid dehydrogenase type 1.
Neoplasms
Immunohistochemical analysis of 11-beta-hydroxysteroid dehydrogenase type 2 and glucocorticoid receptor in subclinical Cushing's disease due to pituitary macroadenoma.
Neoplasms
Inflammatory mediators down-regulate 11beta-hydroxysteroid dehydrogenase type 2 in a human lung epithelial cell line BEAS-2B and the rat lung.
Neoplasms
Inhibition of 11beta-hydroxysteroid dehydrogenase eliminates impaired glucocorticoid suppression and induces apoptosis in corticotroph tumor cells.
Neoplasms
Inhibition of 11beta-hydroxysteroid dehydrogenase type II selectively blocks the tumor COX-2 pathway and suppresses colon carcinogenesis in mice and humans.
Neoplasms
Insulin attenuates the stimulatory effects of tumor necrosis factor alpha on 11beta-hydroxysteroid dehydrogenase 1 in human adipose stromal cells.
Neoplasms
Insulin, CCAAT/enhancer-binding proteins and lactate regulate the human 11?-hydroxysteroid dehydrogenase type 2 gene expression in colon cancer cell lines.
Neoplasms
Local metabolism of glucocorticoids and its role in rat adjuvant arthritis.
Neoplasms
Luteinizing hormone induces expression of 11beta-hydroxysteroid dehydrogenase type 2 in rat Leydig cells.
Neoplasms
Mineralocorticoid receptor and 11beta-hydroxysteroid dehydrogenase type II expression in renal cell neoplasms: a tissue microarray and quantitative RT-PCR study.
Neoplasms
Modulation of 11beta-hydroxysteroid dehydrogenase isozymes by proinflammatory cytokines in osteoblasts: an autocrine switch from glucocorticoid inactivation to activation.
Neoplasms
Morphological and immunological characteristics of a rat choriocarcinoma.
Neoplasms
NAD dependent 11beta-hydroxysteroid dehydrogenase activity in human endometrium and endometrial tumors.
Neoplasms
Pathophysiology of metabolic syndrome X and its links to the perinatal period.
Neoplasms
Regulation of expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue: tissue-specific induction by cytokines.
Neoplasms
Role of local 11 beta-hydroxysteroid dehydrogenase type 2 expression in determining the phenotype of adrenal adenomas.
Neoplasms
T cell-mediated inflammation in adipose tissue does not cause insulin resistance in hyperlipidemic mice.
Neoplasms
The 11-ketosteroid 11-ketodexamethasone is a glucocorticoid receptor agonist.
Neoplasms
The inflammatory response seen when human omental adipose tissue explants are incubated in primary culture is not dependent upon albumin and is primarily in the nonfat cells.
Neoplasms
TNF-alpha enhances intracellular glucocorticoid availability.
Neoplasms
Transcriptional alterations of genes related to fertility decline in male rats induced by chronic sleep restriction.
Neoplasms
Tumor necrosis factor alpha and phorbol 12-myristate-13-acetate down-regulate human 11beta-hydroxysteroid dehydrogenase type 2 through p50/p50 NF-kappaB homodimers and Egr-1.
Neoplasms
Tumor necrosis factor-alpha upregulates 11beta-hydroxysteroid dehydrogenase type 1 expression by CCAAT/enhancer binding protein-beta in HepG2 cells.
Neoplasms
Type 2 11beta-hydroxysteroid dehydrogenase activity in human ovarian cancer.
Neoplasms
Type 2 diabetes and metabolic syndrome are associated with increased expression of 11beta-hydroxysteroid dehydrogenase 1 in obese subjects.
Neoplasms
Type-2 11?-hydroxysteroid dehydrogenase promotes the metastasis of colorectal cancer via the Fgfbp1-AKT pathway.
Neoplasms
Upregulation of 11?-hydroxysteroid dehydrogenase 1 in lymphoid organs during inflammation in the rat.
Neoplasms
[Diseases caused by adrenal dyshormonogenesis. The concept of minor enzymopathy. The 3 beta-hydroxysteroid dehydrogenase block; its possible importance in the pathogenesis of breast cancer]
Nephrosis
Reduced 11beta-hydroxysteroid dehydrogenase activity in experimental nephrotic syndrome.
Nephrotic Syndrome
Glucocorticoid-mediated mineralocorticoid receptor activation and hypertension.
Nephrotic Syndrome
Increased apical targeting of renal ENaC subunits and decreased expression of 11betaHSD2 in HgCl2-induced nephrotic syndrome in rats.
Nephrotic Syndrome
Reduced 11beta-hydroxysteroid dehydrogenase activity in experimental nephrotic syndrome.
Nephrotic Syndrome
Reduced 11beta-hydroxysteroid dehydrogenase activity in patients with the nephrotic syndrome.
Nephrotic Syndrome
Reduced activity of 11beta-hydroxysteroid dehydrogenase type 2 is not responsible for sodium retention in nephrotic rats.
Neurodegenerative Diseases
11beta-hydroxysteroid dehydrogenase type 1 as a novel therapeutic target in metabolic and neurodegenerative disease.
Non-alcoholic Fatty Liver Disease
Association of 11?-hydroxysteroid dehydrogenase type 1 gene polymorphisms with serum alanine aminotransferase activity.
Obesity
1,25-dihydroxyvitamin D3 modulation of adipocyte glucocorticoid function.
Obesity
11 beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic syndrome.
Obesity
11 beta-hydroxysteroid dehydrogenase type 1 promotes differentiation of 3T3-L1 preadipocyte.
Obesity
11-Beta hydroxysteroid dehydrogenase type 2 expression in white adipose tissue is strongly correlated with adiposity.
Obesity
11?-Hydroxysteroid dehydrogenase type 1: relevance of its modulation in the pathophysiology of obesity, the metabolic syndrome and type 2 diabetes mellitus.
Obesity
11Beta-HSD type 1 expression in human adipose tissue: impact of gender, obesity, and fat localization.
Obesity
11beta-HSD1 inhibition improves triglyceridemia through reduced liver VLDL secretion and partitions lipids toward oxidative tissues.
Obesity
11beta-Hydroxysteroid dehydrogenase 1 inhibiting constituents from Eriobotrya japonica revealed by bioactivity-guided isolation and computational approaches.
Obesity
11beta-hydroxysteroid dehydrogenase 2 activity is elevated in severe obesity and negatively associated with insulin sensitivity.
Obesity
11beta-hydroxysteroid dehydrogenase and the pre-receptor regulation of corticosteroid hormone action.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 and obesity.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 as a modulator of glucocorticoid action: from metabolism to memory.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 as a novel therapeutic target in metabolic and neurodegenerative disease.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue and prospective changes in body weight and insulin resistance.
Obesity
11Beta-hydroxysteroid dehydrogenase type 1 in human disease: a novel therapeutic target.
Obesity
11beta-Hydroxysteroid dehydrogenase Type 1 in obesity and Type 2 diabetes.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 in obesity.
Obesity
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors for metabolic syndrome.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes.
Obesity
11beta-Hydroxysteroid dehydrogenase type 1 is an important regulator at the interface of obesity and inflammation.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 knockout mice show attenuated glucocorticoid-inducible responses and resist hyperglycemia on obesity or stress.
Obesity
11beta-hydroxysteroid dehydrogenase type 1 mRNA is increased in both visceral and subcutaneous adipose tissue of obese patients.
Obesity
11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.
Obesity
11beta-Hydroxysteroid dehydrogenase Type 1: genetic polymorphisms are associated with Type 2 diabetes in Pima Indians independently of obesity and expression in adipocyte and muscle.
Obesity
11{beta}-Hydroxysteroid Dehydrogenase Type 1: A Tissue-Specific Regulator of Glucocorticoid Response.
Obesity
7-oxysterols modulate glucocorticoid activity in adipocytes through competition for 11beta-hydroxysteroid dehydrogenase type.
Obesity
A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome.
Obesity
A gene variant of 11?-hydroxysteroid dehydrogenase type 1 is associated with obesity in children.
Obesity
A novel promoter for the 11beta-hydroxysteroid dehydrogenase type 1 gene is active in lung and is C/EBPalpha independent.
Obesity
A novel selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitor prevents human adipogenesis.
Obesity
A Polygenic Model of the Metabolic Syndrome With Reduced Circulating and Intra-Adipose Glucocorticoid Action.
Obesity
Abnormal cortisol metabolism and tissue sensitivity to cortisol in patients with glucose intolerance.
Obesity
Activation of the hypothalamic-pituitary-adrenal axis in obesity: cause or consequence?
Obesity
Adipose tissue 11{beta}-hydroxysteroid dehydrogenase type 1 expression in obesity and Cushing's syndrome.
Obesity
Adipose tissue expression of 11beta-hydroxysteroid dehydrogenase type 1 in Cushing's syndrome and in obesity.
Obesity
Alteration of 11beta-hydroxysteroid dehydrogenase type 1 in skeletal muscle in a rat model of type 2 diabetes.
Obesity
Association between 11beta-hydroxysteroid dehydrogenase type 1 gene polymorphisms and metabolic syndrome in Bosnian population.
Obesity
Association of HSD11B1 polymorphic variants and adipose tissue gene expression with metabolic syndrome, obesity and type 2 diabetes mellitus: a systematic review.
Obesity
Association studies between microsatellite markers within the gene encoding human 11beta-hydroxysteroid dehydrogenase type 1 and body mass index, waist to hip ratio, and glucocorticoid metabolism.
Obesity
Association study of candidate gene polymorphisms and obesity in a young Mexican-American population from South Texas.
Obesity
Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Obesity
Body fat distribution and cortisol metabolism in healthy men: enhanced 5beta-reductase and lower cortisol/cortisone metabolite ratios in men with fatty liver.
Obesity
Cell-type specific regulation of the human 11beta-hydroxysteroid dehydrogenase type 1 promoter.
Obesity
Charting biologically relevant chemical space: a structural classification of natural products (SCONP).
Obesity
Comparison of a homology model and the crystallographic structure of human 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) in a structure-based identification of inhibitors.
Obesity
Conformational flexibility in crystal structures of human 11beta-hydroxysteroid dehydrogenase type I provide insights into glucocorticoid interconversion and enzyme regulation.
Obesity
Cortisol metabolism and visceral obesity: role of 11beta-hydroxysteroid dehydrogenase type I enzyme and reduced co-factor NADPH.
Obesity
Cortisol metabolism in human obesity: impaired cortisone-->cortisol conversion in subjects with central adiposity.
Obesity
Cortisol release from adipose tissue by 11beta-hydroxysteroid dehydrogenase type 1 in humans.
Obesity
Cortisol--cause and cure for metabolic syndrome?
Obesity
Dehydroepiandrosterone inhibits the amplification of glucocorticoid action in adipose tissue.
Obesity
Depot-specific messenger RNA expression of 11 beta-hydroxysteroid dehydrogenase type 1 and leptin in adipose tissue of children and adults.
Obesity
Depot-specific modulation of rat intraabdominal adipose tissue lipid metabolism by pharmacological inhibition of 11beta-hydroxysteroid dehydrogenase type 1.
Obesity
Development of 11beta-HSD1 inhibitors for the treatment of type 2 diabetes.
Obesity
Diabetic pregnancy in rats leads to impaired glucose metabolism in offspring involving tissue-specific dysregulation of 11beta-hydroxysteroid dehydrogenase type 1 expression.
Obesity
Diet and the role of 11beta-hydroxysteroid dehydrogenase-1 on obesity.
Obesity
Differences in associations between HSD11B1 gene expression and metabolic parameters in subjects with and without impaired glucose homeostasis.
Obesity
Different responsiveness in body weight and hepatic 11beta-hydroxysteroid dehydrogenase (11beta-HSD) type 1 mrna to 11beta-HSD inhibition by glycyrrhetinic acid treatment in obese and lean zucker rats.
Obesity
Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors.
Obesity
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
Obesity
Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Obesity
Docking-based 3D-QSAR study for 11beta-HSD1 inhibitors.
Obesity
Effects of gonadectomy on glucocorticoid metabolism in obese Zucker rats.
Obesity
Effects of proportions of dietary macronutrients on glucocorticoid metabolism in diet-induced obesity in rats.
Obesity
Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model.
Obesity
Evidence of altered cortisol metabolism in critically ill patients: a prospective study.
Obesity
Exploring the pathogenesis of IIH: An inflammatory perspective.
Obesity
Expression of 11beta-hydroxysteroid dehydrogenase 1 and 2 in subcutaneous adipose tissue of lean and obese women with and without polycystic ovary syndrome.
Obesity
Expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue is not increased in human obesity.
Obesity
Expression of the mRNA coding for 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue from obese patients: an in situ hybridization study.
Obesity
Extra-adrenal regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: physiological regulator and pharmacological target for energy partitioning.
Obesity
Functional characterization of the human 11 beta-hydroxysteroid dehydrogenase 1B (11 beta-HSD 1B) variant.
Obesity
Functional effects of polymorphisms in the human gene encoding 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1): a sequence variant at the translation start of 11 beta-HSD1 alters enzyme levels.
Obesity
Gender-dependent association of HSD11B1 single nucleotide polymorphisms with glucose and HDL-C levels.
Obesity
Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome.
Obesity
Genetic variation in candidate obesity genes ADRB2, ADRB3, GHRL, HSD11B1, IRS1, IRS2, and SHC1 and risk for breast cancer in the Cancer Prevention Study II.
Obesity
Glucocorticoid metabolism and adrenocortical reactivity to ACTH in myotonic dystrophy.
Obesity
Glucocorticoid receptor gene expression in adipose tissue and associated metabolic risk in black and white South African women.
Obesity
Glucocorticoids and 11beta-hydroxysteroid dehydrogenase type 1 in obesity and the metabolic sindrome.
Obesity
High-throughput screening of 11beta-hydroxysteroid dehydrogenase type 1 in scintillation proximity assay format.
Obesity
Hippocampal 11beta-hydroxysteroid dehydrogenase type 1 messenger ribonucleic acid expression has a diurnal variability that is lost in the obese Zucker rat.
Obesity
Human adipose tissue under in vitro inhibition of 11beta-hydroxysteroid dehydrogenase type 1: differentiation and metabolism changes.
Obesity
Hypothalamic regulation of adiposity: the role of 11beta-hydroxysteroid dehydrogenase type 1.
Obesity
Immortalization of Porcine 11?-Hydroxysteroid Dehydrogenase Type 1-Transgenic Liver Cells Using SV40 Large T Antigen.
Obesity
Impact of MR on mature adipocytes in high-fat/high-sucrose diet-induced obesity
Obesity
Impact of MR on mature adipocytes in high-fat/high-sucrose diet-induced obesity.
Obesity
Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice.
Obesity
INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes.
Obesity
Increased expression and activity of 11beta-HSD-1 in diabetic islets and prevention with troglitazone.
Obesity
Increased expression of the macrophage markers and of 11beta-HSD-1 in subcutaneous adipose tissue, but not in cultured monocyte-derived macrophages, is associated with liver fat in human obesity.
Obesity
Increased in vivo regeneration of cortisol in adipose tissue in human obesity and effects of the 11beta-hydroxysteroid dehydrogenase type 1 inhibitor carbenoxolone.
Obesity
Influence of short-term dietary weight loss on cortisol secretion and metabolism in obese men.
Obesity
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 in obesity.
Obesity
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 reduces food intake and weight gain but maintains energy expenditure in diet-induced obese mice.
Obesity
Inhibition of human and rat 11beta-hydroxysteroid dehydrogenase type 1 by 18beta-glycyrrhetinic acid derivatives.
Obesity
Interaction between an 11betaHSD1 gene variant and birth era modifies the risk of hypertension in Pima Indians.
Obesity
Interaction of HSD11B1 and H6PD polymorphisms in subjects with type 2 diabetes are protective factors against obesity: a cross-sectional study.
Obesity
Is 11beta-hydroxysteroid dehydrogenase type 1 a therapeutic target? Effects of carbenoxolone in lean and obese Zucker rats.
Obesity
Lack of association of the 11 beta-hydroxysteroid dehydrogenase type 1 gene 25669dupA polymorphism with obesity and metabolic syndrome.
Obesity
Lack of mutations of type 1 11beta-hydroxysteroid dehydrogenase gene in patients with abdominal obesity.
Obesity
Leptin activation of corticosterone production in hepatocytes may contribute to the reversal of obesity and hyperglycemia in leptin-deficient ob/ob mice.
Obesity
Lessons in obesity from transgenic animals.
Obesity
Local and systemic impact of transcriptional up-regulation of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue in human obesity.
Obesity
Low-dose growth hormone inhibits 11 beta-hydroxysteroid dehydrogenase type 1 but has no effect upon fat mass in patients with simple obesity.
Obesity
Mechanisms of disease: Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a novel treatment for the metabolic syndrome.
Obesity
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Obesity
Minireview: 11beta-hydroxysteroid dehydrogenase type 1- a tissue-specific amplifier of glucocorticoid action.
Obesity
Modification of microsomal 11beta-HSD1 activity by cytosolic compounds: glutathione and hexose phosphoesters.
Obesity
Novel adipose tissue-mediated resistance to diet-induced visceral obesity in 11 beta-hydroxysteroid dehydrogenase type 1-deficient mice.
Obesity
Obese Zucker rats have reduced mineralocorticoid receptor and 11beta-hydroxysteroid dehydrogenase type 1 expression in hippocampus-implications for dysregulation of the hypothalamic-pituitary-adrenal axis in obesity.
Obesity
Omental 11beta-hydroxysteroid dehydrogenase 1 correlates with fat cell size independently of obesity.
Obesity
Optimization of high-resolution melting analysis for simultaneous genotyping of two 11?-hydroxysteroid dehydrogenase type 1 gene polymorphisms.
Obesity
Overexpression of 11beta-Hydroxysteroid Dehydrogenase Type 1 in Hepatic and Visceral Adipose Tissue is Associated with Metabolic Disorders in Morbidly Obese Patients.
Obesity
Overexpression of 11beta-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of insulin resistance: studies in young adult monozygotic twins.
Obesity
Physiological roles of 11 beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase.
Obesity
Preadipocyte 11{beta}-Hydroxysteroid Dehydrogenase Type 1 Is a Keto-Reductase and Contributes to Diet-Induced Visceral Obesity in Vivo.
Obesity
Prenatal programming of metabolic syndrome in the common marmoset is associated with increased expression of 11ss-hydroxysteroid dehydrogenase type 1.
Obesity
Quantitative real-time PCR for the measurement of 11beta-HSD1 and 11beta-HSD2 mRNA levels in tissues of healthy dogs.
Obesity
Readjusting the glucocorticoid balance: an opportunity for modulators of 11beta-hydroxysteroid dehydrogenase type 1 activity?
Obesity
Reduced adipose glucocorticoid reactivation and increased hepatic glucocorticoid clearance as an early adaptation to high-fat feeding in Wistar rats.
Obesity
Reduced levels of circulating 7alpha-hydroxy-dehydroepiandrosterone in treated adolescent obese patients.
Obesity
Reduction of hepatic glucocorticoid receptor and hexose-6-phosphate dehydrogenase expression ameliorates diet-induced obesity and insulin resistance in mice.
Obesity
Regulation of 11beta-HSD genes in human adipose tissue: influence of central obesity and weight loss.
Obesity
Regulation of expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue: tissue-specific induction by cytokines.
Obesity
Regulatory effect of common promoter polymorphisms on the expression of the 11beta-hydroxysteroid dehydrogenase type 1 gene.
Obesity
Role of 11-beta-hydroxysteroid dehydrogenase type 1 in differentiation of 3T3-L1 cells and in rats with diet-induced obesity.
Obesity
Role of calcitriol and cortisol on human adipocyte proliferation and oxidative and inflammatory stress: a microarray study.
Obesity
Role of glucocorticoids in the physiopathology of excessive fat deposition and insulin resistance.
Obesity
Safety, tolerability, pharmacokinetics and pharmacodynamics of single oral doses of BI 187004, an inhibitor of 11beta-hydroxysteroid dehydrogenase-1, in healthy male volunteers with overweight or obesity.
Obesity
Steroid hormones related to 11beta-hydroxysteroid dehydrogenase type 1 in treated obesity.
Obesity
Steroid metabolism in metabolic syndrome X.
Obesity
Sub-chronic administration of the 11beta-HSD1 inhibitor, carbenoxolone, improves glucose tolerance and insulin sensitivity in mice with diet-induced obesity.
Obesity
Sucrose access differentially modifies 11beta-hydroxysteroid dehydrogenase-1 and hexose-6-phosphate dehydrogenase message in liver and adipose tissue in rats.
Obesity
Suppression of 11{beta}-hydroxysteroid dehydrogenase type 1 with RNA interference substantially attenuates 3T3-L1 adipogenesis.
Obesity
Targeting the pre-receptor metabolism of cortisol as a novel therapy in obesity and diabetes.
Obesity
The contribution of visceral adipose tissue to splanchnic cortisol production in healthy humans.
Obesity
The critical role of the N-terminus of 11beta-hydroxysteroid dehydrogenase type 1, as being encoded by exon 1, for enzyme stabilization and activity.
Obesity
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening.
Obesity
The glucocorticoid-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 has broad substrate specificity: Physiological and toxicological considerations.
Obesity
The Role of 11Beta-Hydroxysteroid Dehydrogenase in Metabolic Disease and Therapeutic Potential of 11Beta-HSD1 Inhibitors.
Obesity
Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease.
Obesity
Tissue-specific changes in peripheral cortisol metabolism in obese women: increased adipose 11beta-hydroxysteroid dehydrogenase type 1 activity.
Obesity
Tissue-specific dysregulation of cortisol metabolism in human obesity.
Obesity
Tissue-specific dysregulation of cortisol regeneration by 11?HSD1 in obesity: has it promised too much?
Obesity
Tissue-specific increases in 11beta-hydroxysteroid dehydrogenase type 1 in normal weight postmenopausal women.
Obesity
Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice.
Obesity
Tumor necrosis factor-alpha upregulates 11beta-hydroxysteroid dehydrogenase type 1 expression by CCAAT/enhancer binding protein-beta in HepG2 cells.
Obesity
Understanding the role of glucocorticoids in obesity: tissue-specific alterations of corticosterone metabolism in obese Zucker rats.
Obesity
Urinary free cortisone, but not cortisol, is associated with urine volume in severe obesity.
Obesity
Vitamin A decreases pre-receptor amplification of glucocorticoids in obesity: study on the effect of vitamin A on 11beta-hydroxysteroid dehydrogenase type 1 activity in liver and visceral fat of WNIN/Ob obese rats.
Obesity
Weight Loss after Gastric Bypass Surgery in Women Is Followed by a Metabolically Favorable Decrease in 11{beta}-Hydroxysteroid Dehydrogenase 1 Expression in Subcutaneous Adipose Tissue.
Obesity
Weight loss increases 11beta-hydroxysteroid dehydrogenase type 1 expression in human adipose tissue.
Obesity
[Reduction of obesity-related metabolic risk by modulating tissue exposition to cortisol].
Obesity, Abdominal
11Beta-hydroxysteroid dehydrogenase type 1 in differentiating omental human preadipocytes: from de-activation to generation of cortisol.
Obesity, Abdominal
11beta-Hydroxysteroid dehydrogenase Type 1 in obesity and Type 2 diabetes.
Obesity, Abdominal
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors with oleanan and ursan scaffolds.
Obesity, Abdominal
Adipocyte-specific glucocorticoid inactivation protects against diet-induced obesity.
Obesity, Abdominal
Association studies between microsatellite markers within the gene encoding human 11beta-hydroxysteroid dehydrogenase type 1 and body mass index, waist to hip ratio, and glucocorticoid metabolism.
Obesity, Abdominal
Body fat distribution and cortisol metabolism in healthy men: enhanced 5beta-reductase and lower cortisol/cortisone metabolite ratios in men with fatty liver.
Obesity, Abdominal
Circulating 11beta-hydroxysteroid dehydrogenase type 1 mRNA and cardiovascular risk factors.
Obesity, Abdominal
Cortisol metabolism and visceral obesity: role of 11beta-hydroxysteroid dehydrogenase type I enzyme and reduced co-factor NADPH.
Obesity, Abdominal
Cortisol metabolism in human obesity: impaired cortisone-->cortisol conversion in subjects with central adiposity.
Obesity, Abdominal
Cortisol, 11 beta-hydroxysteroid dehydrogenase type 1 and central obesity.
Obesity, Abdominal
Depot-specific modulation of rat intraabdominal adipose tissue lipid metabolism by pharmacological inhibition of 11beta-hydroxysteroid dehydrogenase type 1.
Obesity, Abdominal
Differentiation of adipose stromal cells: the roles of glucocorticoids and 11beta-hydroxysteroid dehydrogenase.
Obesity, Abdominal
Down-regulation of adipose 11beta-hydroxysteroid dehydrogenase type 1 by high-fat feeding in mice: a potential adaptive mechanism counteracting metabolic disease.
Obesity, Abdominal
Enzymology and molecular biology of glucocorticoid metabolism in humans.
Obesity, Abdominal
Expression of genes related to glucocorticoid action in human subcutaneous and omental adipose tissue.
Obesity, Abdominal
Glucocorticoid-mediated mineralocorticoid receptor activation and hypertension.
Obesity, Abdominal
Growth hormone, insulin-like growth factor-I and the cortisol-cortisone shuttle.
Obesity, Abdominal
H6PDH interacts directly with 11beta-HSD1: implications for determining the directionality of glucocorticoid catalysis.
Obesity, Abdominal
Human adipose tissue under in vitro inhibition of 11beta-hydroxysteroid dehydrogenase type 1: differentiation and metabolism changes.
Obesity, Abdominal
Insulin and dexamethasone dynamically regulate adipocyte 11beta-hydroxysteroid dehydrogenase type 1.
Obesity, Abdominal
Lack of mutations of type 1 11beta-hydroxysteroid dehydrogenase gene in patients with abdominal obesity.
Obesity, Abdominal
Metabolic syndrome without obesity: Hepatic overexpression of 11beta-hydroxysteroid dehydrogenase type 1 in transgenic mice.
Obesity, Abdominal
Overexpression of 11beta-hydroxysteroid dehydrogenase-1 in adipose tissue is associated with acquired obesity and features of insulin resistance: studies in young adult monozygotic twins.
Obesity, Abdominal
Pathophysiology of metabolic syndrome X and its links to the perinatal period.
Obesity, Abdominal
Quantitative measurements of corticosteroids in ex vivo samples using on-line SPE-LC/MS/MS.
Obesity, Abdominal
Reduced 11beta-hydroxysteroid dehydrogenase type 1 activity in obese boys.
Obesity, Abdominal
Regulation of 11beta-HSD genes in human adipose tissue: influence of central obesity and weight loss.
Obesity, Abdominal
Regulation of expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue: tissue-specific induction by cytokines.
Obesity, Abdominal
Testosterone Stimulates Adipose Tissue 11{beta}-Hydroxysteroid Dehydrogenase Type 1 Expression in a Depot-Specific Manner in Children.
Obesity, Abdominal
The functional consequences of 11beta-hydroxysteroid dehydrogenase expression in adipose tissue.
Obesity, Abdominal
Tissue-specific changes in peripheral cortisol metabolism in obese women: increased adipose 11beta-hydroxysteroid dehydrogenase type 1 activity.
Obesity, Abdominal
Tissue-specific Cushing's syndrome, 11beta-hydroxysteroid dehydrogenases and the redefinition of corticosteroid hormone action.
Obesity, Abdominal
Tissue-specific glucocorticoid reactivating enzyme, 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)--a promising drug target for the treatment of metabolic syndrome.
Obesity, Abdominal
Tissue-specific increases in 11beta-hydroxysteroid dehydrogenase type 1 in normal weight postmenopausal women.
Obesity, Abdominal
Transgenic amplification of glucocorticoid action in adipose tissue causes high blood pressure in mice.
Obesity, Abdominal
[Correlations between the hypothalamo-pituitary-adrenal axis and the metabolic syndrome]
Obesity, Abdominal
[Glucocorticoids, 11 beta-hydroxysteroid dehydrogenase type 1, and visceral obesity]
Obesity, Morbid
11beta-hydroxysteroid dehydrogenase 2 activity is elevated in severe obesity and negatively associated with insulin sensitivity.
Obesity, Morbid
Carbenoxolone treatment attenuates symptoms of metabolic syndrome and atherogenesis in obese, hyperlipidemic mice.
Obstetric Labor, Premature
Effect of pro-inflammatory cytokines on expression and activity of 11beta-hydroxysteroid dehydrogenase type 2 in cultured human term placental trophoblast and human choriocarcinoma JEG-3 cells.
Obstetric Labor, Premature
Role of fetal membranes in signaling of fetal maturation and parturition.
Ocular Hypertension
In vivo evaluation of 11beta-hydroxysteroid dehydrogenase activity in the rabbit eye.
Ocular Hypertension
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 lowers intraocular pressure in patients with ocular hypertension.
Oropharyngeal Neoplasms
11Beta-hydroxysteroid dehydrogenase 1 expression in squamous cell carcinomas of the head and neck.
Osteoarthritis
Differential expression, function and response to inflammatory stimuli of 11beta-hydroxysteroid dehydrogenase type 1 in human fibroblasts: a mechanism for tissue-specific regulation of inflammation.
Osteolysis
11beta-hydroxysteroid dehydrogenase type 1 expression in periprosthetic osteolysis.
Osteonecrosis
[Genetic expression differences of 11 beta-hydroxysteroid dehydrogenase in the bone microvascular endothelial cells derived from different regions of the human femoral head].
Osteoporosis
11beta-hydroxysteroid dehydrogenase type 1 activity predicts the effects of glucocorticoids on bone.
Osteoporosis
11Beta-hydroxysteroid dehydrogenase type 1 in human disease: a novel therapeutic target.
Osteoporosis
11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.
Osteoporosis
11beta-Hydroxysteroid dehydrogenase: a regulator of glucocorticoid response in osteoporosis.
Osteoporosis
11{beta}-Hydroxysteroid Dehydrogenase Type 1: A Tissue-Specific Regulator of Glucocorticoid Response.
Osteoporosis
Characterization of 11beta-hydroxysteroid dehydrogenase activity and corticosteroid receptor expression in human osteosarcoma cell lines.
Osteoporosis
Circulating cortisone levels are associated with biochemical markers of bone formation and lumbar spine BMD: the Hertfordshire Cohort Study.
Osteoporosis
Expression and functional consequences of 11beta-hydroxysteroid dehydrogenase activity in human bone.
Osteoporosis
HSD11B1 polymorphisms predicted bone mineral density and fracture risk in postmenopausal women without a clinically apparent hypercortisolemia.
Osteosarcoma
Characterization of 11beta-hydroxysteroid dehydrogenase activity and corticosteroid receptor expression in human osteosarcoma cell lines.
Osteosarcoma
Expression and functional consequences of 11beta-hydroxysteroid dehydrogenase activity in human bone.
Osteosarcoma
Modulation of 11beta-hydroxysteroid dehydrogenase isozymes by proinflammatory cytokines in osteoblasts: an autocrine switch from glucocorticoid inactivation to activation.
Osteosarcoma
Prereceptor regulation of glucocorticoid action by 11beta-hydroxysteroid dehydrogenase: a novel determinant of cell proliferation.
Osteosarcoma
Synergistic induction of local glucocorticoid generation by inflammatory cytokines and glucocorticoids: implications for inflammation associated bone loss.
Ovarian Cysts
Implication of cortisol and 11beta-hydroxysteroid dehydrogenase enzymes in the development of porcine (Sus scrofa domestica) ovarian follicles and cysts.
Ovarian Cysts
Inactivation of glucocorticoids by 11beta-hydroxysteroid dehydrogenase enzymes increases during the meiotic maturation of porcine oocytes.
Ovarian Cysts
Ovarian modulators of 11beta-hydroxysteroid dehydrogenase (11beta HSD) activity in follicular fluid from bovine and porcine large antral follicles and spontaneous ovarian cysts.
Ovarian Diseases
Experimental micropolycystic ovarian disease. I. Measurement of body weight, ovarian weight and histochemical activity of 17 beta-hydroxysteroid dehydrogenase.
Overweight
Depot-specific messenger RNA expression of 11 beta-hydroxysteroid dehydrogenase type 1 and leptin in adipose tissue of children and adults.
Overweight
Endurance exercise training increases adipose tissue glucocorticoid exposure: adaptations that facilitate lipolysis.
Overweight
Safety, tolerability, pharmacokinetics and pharmacodynamics of single oral doses of BI 187004, an inhibitor of 11beta-hydroxysteroid dehydrogenase-1, in healthy male volunteers with overweight or obesity.
Pituitary ACTH Hypersecretion
Absence of Cushingoid phenotype in a patient with Cushing's disease due to defective cortisone to cortisol conversion.
Pituitary ACTH Hypersecretion
Immunohistochemical analysis of 11-beta-hydroxysteroid dehydrogenase type 2 and glucocorticoid receptor in subclinical Cushing's disease due to pituitary macroadenoma.
Pituitary ACTH Hypersecretion
Inhibition of 11beta-hydroxysteroid dehydrogenase eliminates impaired glucocorticoid suppression and induces apoptosis in corticotroph tumor cells.
Pituitary ACTH Hypersecretion
Modulatory effect of BclI GR gene polymorphisms on the obesity phenotype in Brazilian patients with Cushing's disease.
Pituitary Neoplasms
Hormonal Regulation of Glucocorticoid Inactivation and Reactivation in ?T3-1 and L?T2 Gonadotroph Cells.
Pneumonia
Inflammatory mediators down-regulate 11beta-hydroxysteroid dehydrogenase type 2 in a human lung epithelial cell line BEAS-2B and the rat lung.
Polycystic Ovary Syndrome
11Beta-hydroxysteroid dehydrogenase type 1 in human disease: a novel therapeutic target.
Polycystic Ovary Syndrome
A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome.
Polycystic Ovary Syndrome
A study of the hexose-6-phosphate dehydrogenase gene R453Q and 11beta-hydroxysteroid dehydrogenase type 1 gene 83557insA polymorphisms in the polycystic ovary syndrome.
Polycystic Ovary Syndrome
Association Analysis between the Polymorphisms of HSD11B1 and H6PD and Risk of Polycystic Ovary Syndrome in Chinese Population.
Polycystic Ovary Syndrome
Association Study of CYP17 and HSD11B1 in Polycystic Ovary Syndrome Utilizing Comprehensive Gene Coverage.
Polycystic Ovary Syndrome
Endogenous inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 do not explain abnormal cortisol metabolism in polycystic ovary syndrome.
Polycystic Ovary Syndrome
Expression of 11beta-hydroxysteroid dehydrogenase 1 and 2 in subcutaneous adipose tissue of lean and obese women with and without polycystic ovary syndrome.
Polycystic Ovary Syndrome
Genetic variants of the HSD11B1 gene promoter may be protective against polycystic ovary syndrome.
Polycystic Ovary Syndrome
Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome.
Polycystic Ovary Syndrome
Hyperandrogenism in polycystic ovary syndrome. Evidence of dysregulation of 11 beta-hydroxysteroid dehydrogenase.
Polycystic Ovary Syndrome
Increased 5alpha-reductase and normal 11beta-hydroxysteroid dehydrogenase metabolism of C19 and C21 steroids in a young population with polycystic ovarian syndrome.
Polyuria
Phenotypic analysis of mice bearing targeted deletions of 11beta-hydroxysteroid dehydrogenases 1 and 2 genes.
Pre-Eclampsia
11beta-Hydroxysteroid dehydrogenase activity in pregnancies complicated by hydatidiform mole.
Pre-Eclampsia
11beta-Hydroxysteroid dehydrogenase type 2 in pregnancy and preeclampsia.
Pre-Eclampsia
Alteration in methylation level at 11?-hydroxysteroid dehydrogenase type 2 gene promoter in infants born to preeclamptic women.
Pre-Eclampsia
Angiotensin II regulates 11beta-hydroxysteroid dehydrogenase type 2 via AT2 receptors.
Pre-Eclampsia
Apparent mineralocorticoid excess syndrome: an overview.
Pre-Eclampsia
Decreased gene expression of 11beta-hydroxysteroid dehydrogenase type 2 and 15-hydroxyprostaglandin dehydrogenase in human placenta of patients with preeclampsia.
Pre-Eclampsia
Ontogeny of placental structural development and expression of the renin-angiotensin system and 11beta-HSD2 genes in the rabbit.
Pre-Eclampsia
Prematurity is related to high placental cortisol in preeclampsia.
Pre-Eclampsia
The transplacental passage of prednisolone in pregnancies complicated by early-onset HELLP syndrome.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Differential regulation of 11beta-hydroxysteroid dehydrogenase-1 by dexamethasone in glucocorticoid-sensitive and -resistant childhood lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Expression of 11beta-hydroxysteroid dehydrogenase 2 contributes to glucocorticoid resistance in lymphoblastic leukemia cells.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Reciprocal Regulation of HSD11B1 and HSD11B2 Predicts Glucocorticoid Sensitivity in Childhood Acute Lymphoblastic Leukemia.
Pregnancy Complications
Maternal depressive symptoms during pregnancy, placental expression of genes regulating glucocorticoid and serotonin function and infant regulatory behaviors.
Pregnancy Complications
Ontogeny of placental structural development and expression of the renin-angiotensin system and 11beta-HSD2 genes in the rabbit.
Premature Birth
[Influence of dexamethasone on expression of 11beta-HSD2 in primary cultured cytotrophoblasts from human preterm placenta]
Prostatic Neoplasms
Differential expression of determinants of glucocorticoid sensitivity in androgen-dependent and androgen-independent human prostate cancer cell lines.
Prostatic Neoplasms
Modulation of 11beta-hydroxysteroid dehydrogenase expression by bombesin: a possible mechanism for glucocorticoid resistance in androgen independent prostate cancer.
Prostatic Neoplasms
Molecular epidemiologic studies within the Selenium and Vitamin E Cancer Prevention Trial (SELECT).
Proteinuria
Expression of renal 11beta-hydroxysteroid dehydrogenase type 2 is decreased in patients with impaired renal function.
Proteinuria
Reduced 11beta-hydroxysteroid dehydrogenase activity in experimental nephrotic syndrome.
Pseudohypoaldosteronism
Epidemiologic study of adrenal gland disorders in Japan.
Rheumatic Heart Disease
[Atrial 11beta-hydroxysteroid dehydrogenase type 2 expression in rheumatic heart disease patients with or without atrial fibrillation]
Rosacea
TLR3 augments glucocorticoid-synthetic enzymes expression in epidermal keratinocytes; Implications of glucocorticoid metabolism in rosacea epidermis.
Sarcopenia
Increased skeletal muscle 11?HSD1 mRNA is associated with lower muscle strength in ageing.
Sleep Deprivation
Sleep duration and fragmentation in relation to leukocyte DNA methylation in adolescents.
Sleep Deprivation
Transcriptional alterations of genes related to fertility decline in male rats induced by chronic sleep restriction.
Small Cell Lung Carcinoma
Expression of 11beta-hydroxysteroid dehydrogenase type 2 in an ACTH-producing small cell lung cancer.
steroid 21-monooxygenase deficiency
A prospective study of the prevalence of clear-cut endocrine disorders and polycystic ovaries in 350 patients presenting with hirsutism or androgenic alopecia.
Synovitis
11 Beta-hydroxysteroid dehydrogenase type 1 regulates synovitis, joint destruction, and systemic bone loss in chronic polyarthritis.
unspecific monooxygenase deficiency
Evidence for a role of sterol 27-hydroxylase in glucocorticoid metabolism in vivo.
Virus Diseases
Regulation of expression of 11beta-hydroxysteroid dehydrogenase type 1 in adipose tissue: tissue-specific induction by cytokines.
Vitamin D Deficiency
Maternal vitamin D deficiency during rat gestation elicits a milder phenotype compared to the mouse model: Implications for the placental glucocorticoid barrier.
Xanthomatosis, Cerebrotendinous
Evidence for a role of sterol 27-hydroxylase in glucocorticoid metabolism in vivo.
Xanthomatosis, Cerebrotendinous
Studies of the mechanism of the increased biosynthesis of cholestanol in cerebrotendinous xanthomatosis. The activity of delta 5-3 beta-hydroxysteroid dehydrogenase.
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0.05799 - 0.1312
(-)-epigallocatechin 3-gallate
0.0012
(1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
Homo sapiens
-
0.000018
(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid
Homo sapiens
at 37°C, pH not specified in the publication
0.0000037
(1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.001
(1r,4s)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
(1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
Homo sapiens
IC50 above 0.001 mM, in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000015
(1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(2,3-dichlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(2,3-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(2,4-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001 - 0.000002
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
0.000002
(1s,4r)-4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000007
(1s,4r)-4-[3-[(3,5-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(3-chloro-2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000057
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(3-chlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
(1s,4r)-4-[3-[(3-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(4-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.003 - 0.112
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
0.005 - 0.2
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
0.000031
(2R)-1-(2-chloro-4-(2-methoxyethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000018
(2R)-1-(2-chloro-4-(difluoromethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000063
(2R)-1-(2-chloro-4-ethoxyphenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000017
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxamide
Homo sapiens
at 37°C
0.00001
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxylic acid
Homo sapiens
at 37°C
0.00001
(2R)-1-(3-chloro-4-([4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazin-1-yl]sulfonyl)phenyl)piperidin-4-ol
Homo sapiens
at 37°C
0.00001
(2R)-1-(4-bromo-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000028
(2R)-1-(4-bromophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.00004
(2R)-1-(4-tert-butoxy-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000639
(2R)-1-([2-chloro-4-[(3S)-3-methylpiperazin-1-yl]phenyl]sulfonyl)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000097
(2R)-1-[(2-chloro-4-piperidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000011
(2R)-1-[(2-chloro-4-pyrrolidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000015
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-N,N-dimethylpiperidin-4-amine
Homo sapiens
at 37°C
0.000018
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
Homo sapiens
at 37°C
0.00001
(2R)-1-[[2-chloro-4-(1H-1,2,4-triazol-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000074
(2R)-1-[[2-chloro-4-(4,4-difluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.00005
(2R)-1-[[2-chloro-4-(4-fluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000136
(2R)-1-[[2-chloro-4-(4-methylpiperazin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000092
(2R)-2-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenoxy)-N,N-dimethylethanamine
Homo sapiens
at 37°C
0.000015
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)-N,N-dimethylaniline
Homo sapiens
at 37°C
0.000016
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
Homo sapiens
at 37°C
0.00005
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenol
Homo sapiens
at 37°C
0.00001
(2R)-3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)benzamide
Homo sapiens
at 37°C
0.000011
(2R)-4-(3-fluoro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)morpholine
Homo sapiens
at 37°C
0.000063
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzamide
Homo sapiens
at 37°C
0.00001
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
Homo sapiens
at 37°C
0.00002
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-1-(4-methoxyphenylsulfonyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000023
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methyl-1-(4-(trifluoromethoxy)-phenylsulfonyl)-piperazine
Homo sapiens
at 37°C
0.000185
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine
Homo sapiens
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
Homo sapiens
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
Homo sapiens
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]thiomorpholine-1,1-dioxide
Homo sapiens
at 37°C
0.000019
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(4-piperidin-1-ylphenyl)sulfonyl]piperazine
Homo sapiens
at 37°C
0.000674
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine
Homo sapiens
at 37°C
0.0000012
(2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000015
(2R)-N-(tricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000037
(2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000031
(2R)-N-[(1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000115
(2R)-N-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide
Homo sapiens
at 37°C
0.000056 - 0.012
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
0.0000619
(3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.007138
(3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000049
(3beta)-3-hydroxy-18,29-epoxyolean-12-ene-11,29-dione
Homo sapiens
pH 7.4, 37°C
0.000025
(3beta)-3-[(3-carboxypropanoyl)oxy]urs-12-en-28-oic acid
Homo sapiens
pH 7.4, 37°C
0.001157
(3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
Homo sapiens
pH not specified in the publication, 37°C
0.000825
(3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000626
(3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
Homo sapiens
pH not specified in the publication, 37°C
0.001012
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
Homo sapiens
pH not specified in the publication, 37°C
0.000929
(3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
Homo sapiens
pH not specified in the publication, 37°C
0.0000427
(3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.002 - 0.2
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
0.002 - 0.2
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
0.000049 - 0.016
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
0.011 - 0.074
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
0.009 - 0.2
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
0.000122 - 0.025
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
0.000008 - 0.000012
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.001 - 0.068
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
0.2
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
0.001508
(3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000053
(3R)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.000089
(3S)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.000074 - 0.016
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
0.0000008
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(2',4'-difluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
Homo sapiens
pH 7.4, 22°C, microsomal assay
0.0000005
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
Homo sapiens
pH 7.4, 22°C, microsomal assay
0.000197
(R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.000266
(R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.000902
(R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.000062
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.001505
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000568
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000885
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000373
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.0000286
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000931
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000101
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000153
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000094
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000025
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000022
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0021
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000012
1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydroxypropan-2-yl)phenylsulfonyl)-piperazin-1-yl)methyl)-cyclopropanecarboxamide
Homo sapiens
in PBS buffer, at 37°C
0.0058
1-(2,4-dichlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)-ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000116
1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
Homo sapiens
pH 7.0, 22°C, cellular assay
0.0064
1-(4-chlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000008
1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol
Homo sapiens
pH and temperature not specified in the publication
0.002975
1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000171
1-adamantan-1-yl-2-(2,4-dichloro-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000122
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000128
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000302
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-ylamino)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.004755
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-yloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000339
1-adamantan-1-yl-2-(3,4-dimethoxy-benzyloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.009379
1-adamantan-1-yl-2-(3,4-dimethoxy-phenoxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.001438
1-adamantan-1-yl-2-(4-chloro-benzenesulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.001
1-adamantan-1-yl-2-(4-chloro-phenoxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000231
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00135
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00081
1-adamantan-1-yl-2-(4-chloro-phenylsulfanyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000296
1-adamantan-1-yl-2-(4-methoxy-benzyloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.002069
1-adamantan-1-yl-2-(4-methylbenzyloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.002017
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.005236
1-adamantan-1-yl-2-(4-trifluoromethyl-phenoxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.0049
1-adamantan-1-yl-2-(biphenyl-4-yloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000443
1-adamantan-1-yl-2-(toluene-4-sulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000668
1-adamantan-1-yl-2-(toluene-4-sulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00251
1-adamantan-1-yl-2-p-tolyloxy-ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00672
1-adamantan-1-yl-2-p-tolylsulfanyl-ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.0007
1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.000257
1-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
Homo sapiens
pH 7.0, 22°C, cellular assay
0.000008
1-[(2-chlorobenzyl)oxy]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000005
1-[(2-chlorobenzyl)sulfanyl]-3-hydroxy-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000002
1-[(2-chlorobenzyl)sulfanyl]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.00000003
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0000004
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.002214
18alpha-glycyrrhetinic acid
Homo sapiens
37°C, pH not specified in the publication
0.000779
18beta-glycyrrhetinic acid
Homo sapiens
37°C, pH not specified in the publication
0.000027
2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000016
2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000009
2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000009
2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000018
2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000017
2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000048
2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000015
2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.036
2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one
Homo sapiens
isoform 11beta-HSD1, at pH 7.4 and 37°C
0.0025
2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one
Homo sapiens
isoform 11beta-HSD1, at pH 7.4 and 37°C
0.05
2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one
Homo sapiens
IC50 above 0.05 mM, isoform 11beta-HSD1, at pH 7.4 and 37°C
0.00888
2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane
Homo sapiens
37°C, pH not specified in the publication, microsomal assay
0.0000005
2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000092
2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000252
2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000126
2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000027
2-[(2-chlorobenzyl)sulfanyl]-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000006
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000078
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000222
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00045
2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00141
2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000019
2-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
Homo sapiens
37°C, pH not specified in the publication, cellular assay
0.000031
2-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfonyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
Homo sapiens
37°C, pH not specified in the publication, cellular assay
0.000048
2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000012
2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00016
2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000019
2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00034
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00006
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.003
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine
Homo sapiens
IC50 above 0.003 mM, isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000591
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000058
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N,N-dimethyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000472
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-benzyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000912
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-ethyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000094
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-methyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.002194
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-phenyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000204
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.0185
2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0272
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0042
2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.02
2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0048
2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0064
2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.000006
2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000003
2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000619
3,11-dioxoolean-12-en-30-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000057
3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000008
3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000134
3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000013
3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000012
3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000011
3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000019
3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000023
3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000024
3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000007
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000016
3-(1-(4-fluorophenyl)cyclopropyl)-4-isopropyl-5-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazole
Homo sapiens
in PBS buffer, at 37°C
0.0000087
3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid
Homo sapiens
at 37°C, pH not specified in the publication
0.000057
3-(2-adamantan-1-yl-2-oxoethanesulfinyl)-N,N-dimethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000069
3-(2-adamantan-1-yl-2-oxoethanesulfonyl)-N,N-dimethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000527
3-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000343
3-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000229
3-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.001222
3-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000068
3-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000876
3-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.001047
3-(2-adamantan-1-yl-2-oxoethoxy)benzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000153
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000078
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
Homo sapiens
pH not specified in the publication, 37°C
0.000013
3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00001
3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000014
3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00354
3-methylchrysazin
Homo sapiens
pH 7.4, 37°C
0.000016
3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00008
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-1-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.000004
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.00019
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cycloheptyl-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.00039
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cyclohexyl-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.000054
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-(methanesulfonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.000004
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.000114
3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one
Homo sapiens
pH 7.0, 22°C, cellular assay
0.000014
3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000012
3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000079
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000043
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000012
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000014
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000096
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000048
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000086
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000087
3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000015
3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000146
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N,N-dimethyl benzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000124
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N-methylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000496
4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
Homo sapiens
at pH 7.4 and 37°C
0.000002 - 0.0000026
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000798
4-(2-adamantan-1-yl-2-oxoethoxy)-N,N-diethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.001959
4-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000382
4-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000594
4-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000283
4-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.00114
4-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000117
4-(2-adamantan-1-yl-2-oxoethoxy)benzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000074
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000056
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N,N-dimethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.00025
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-methylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000359
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000006
4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000012
4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00001
4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000008
4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000026
4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000107
4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.00064
4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000152
4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol
Homo sapiens
pH and temperature not specified in the publication
0.000022
4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00408
4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000051
4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000051
4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.003
4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
IC50 above 0.003 mM, isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00019
4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000008
4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.0000023
4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000282
4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000343
4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0002
4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000102
4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000014
4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.00001
4-[4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
Homo sapiens
at 37°C
0.000037
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000449
5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.000012
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000085
5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.000095
5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000052
5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.0000048
5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.000002
5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.0000068
6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000039
6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000032
6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000032
6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.001929
6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol
Homo sapiens
pH and temperature not specified in the publication
0.0025
6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000057
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
Homo sapiens
pH 7.4, 37°C
0.000375
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
Homo sapiens
pH 7.4, 37°C
0.0000066
6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000041
6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000028
6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000031
6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000019
6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0069
7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one
Homo sapiens
isoform 11beta-HSD1, at pH 7.4 and 37°C
0.000405
7-keto,25-hydroxycholesterol
Homo sapiens
recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C
0.000357
7-keto,27-hydroxycholesterol
Homo sapiens
isoform 11beta-HSD1, at pH 7.4, temperature not specified in the publication
0.003
7beta,25-dihydroxycholesterol
Homo sapiens
IC50 of more than 0.003 mM, recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C
0.003
7beta,27-dihydroxycholesterol
Homo sapiens
isoform 11beta-HSD1, at pH 7.4, temperature not specified in the publication
0.000003
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000089
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000012
8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000879
Aloe-emodin
Homo sapiens
pH 7.4, 37°C
0.000007
AMG-221
Homo sapiens
pH and temperature not specified in the publication
0.000186
emodin
Homo sapiens
pH 7.4, 37°C
0.000068 - 0.2
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000778
glycyrrhetinic acid
Homo sapiens
pH not specified in the publication, 37°C
0.00191
methoxychlor
Homo sapiens
37°C, pH not specified in the publication, microsomal assay
0.000061 - 0.2
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000005 - 0.00002
methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
0.0000038 - 0.0000072
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
0.0000017
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000037
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000027
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000095
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000027
N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000084
N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000143
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
Homo sapiens
pH 7.4, 37°C
0.000058
N-cyclohexyl-6-(piperidin-1-yl)picolinamide
Homo sapiens
at 37°C, pH not specified in the publication
0.00015
N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.001
N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
Homo sapiens
IC50 above 0.001 mM, in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00055
N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000008
N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000046
N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000018
N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000064
N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000021
N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000014
N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000013
N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000037
N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000008
N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000014
N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000011
N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000105
N-[3-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000167
N-[3-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000285
N-[3-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.002037
N-[3-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000151
N-[4-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000058
N-[4-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000894
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-fluoro-phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000897
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-methyl-phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000211
N-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.00009
N-[4-(2-adamantan-1-yl-2-oxoethylamino)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000313
N-[4-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000036
N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000002
N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000028
N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000011
N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000076
N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000006
N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.00000088
N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000038
N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000007
N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000024
N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000055
N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000017
N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000542
rheochrysidin
Homo sapiens
pH 7.4, 37°C
0.0018
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000012
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0004
[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid
Homo sapiens
pH not specified in the publication, 37°C
0.00258
[4-(2-Adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid methyl ester
Homo sapiens
pH not specified in the publication, 37°C
0.000043
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000013
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000003
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.003
(11beta)-11-hydroxyallopregnanolone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.0056
(11beta)-11-hydroxyprogesterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.000002
(1S,3R,4S,5S,7S)-4-(3-(2-fluorophenylsulfonamido)-3-methylbutanamido) adamantane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000254
(2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000003
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000113
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000034
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000053
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000001
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000094
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00003
(2R)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000016
(2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000036
(2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000004
(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0007 - 0.008
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
0.0148
(4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000388
(4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001
(4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decan-1-yl)acetic acid
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000005
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000006
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000005
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000006
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000008
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000004
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00001
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000013
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000022
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000012
1-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)-2-methyl-1H-benzimidazole
Homo sapiens
-
-
0.000012
1-methyl-4-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
Homo sapiens
-
-
0.00000098
1-methyl-4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]-1H-indole
Homo sapiens
-
-
0.000963
1-methyl-5-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
Homo sapiens
-
-
0.000007
1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
1-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.00001
1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000004
1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000004
1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00011
1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0001
1-[1-[(3,4-dimethylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
1-[1-[(3-amino-4-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0003
1-[1-[(3-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000079
1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000007
1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000003
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000017
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000002
1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
Homo sapiens
-
pH and temperature not specified in the publication
0.00065 - 0.05
11-oxo-3alpha,5alpha-tetrahydrotestosterone
0.0008
11-oxo-allopregnanolone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.021
11-oxo-androstenedione
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.0095
11-oxo-progesterone
Homo sapiens
-
pH 8.4, 37°C
0.018
11-oxo-testosterone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.005 - 0.0115
11beta-hydroxy-androstanediol
0.009
11beta-hydroxy-testosterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.0032
2,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzenesulfonamide
Homo sapiens
-
at 37°C
0.0000029
2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.01
2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000052
2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00003
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000028
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000031
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000001
2-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Homo sapiens
-
-
0.0000011
2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.034
2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00026
2-(4-methylphenyl)-2-oxoethyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00035
2-(adamantan-1-yl)-N-methyl-N-(thiophen-3-ylmethyl)acetamide
Homo sapiens
-
-
0.000308
2-adamantan-1-yl-N-methyl-N-thiophen-2-ylmethyl-acetamide
Homo sapiens
-
-
0.05557
2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane
Homo sapiens
pH and temperature not specified in the publication
0.00357
2-bromo-N-[2-([2-oxo-2-[(2-phenylethyl)amino]ethyl]sulfanyl)-2,3-dihydro-1,3-benzothiazol-6-yl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00113
2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000001
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000011
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000547
2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000017
2-[4-(2,6-difluorobenzenesulfonyl)-[1,4]diazepan-1-yl]-1-(octahydroquinolin-1-yl)-ethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000005
2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000011
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000009
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000018
2-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000021
3,5-bis(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000029
3,5-bis(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0032
3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide
Homo sapiens
-
at 37°C
0.0000043
3-(1-fluoronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
IC50 below 0.000001 mM
0.000001 - 0.000008
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000013 - 0.0001
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000012
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000008 - 0.000172
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000032
3-(2,3-difluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000013
3-(2,4-dichlorophenyl)-4-methyl-5-(2-nitrophenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.00009
3-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00002
3-(2,4-dichlorophenyl)-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000002
3-(2-bromophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(2-bromophenyl)-5-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000026
3-(2-chloro-4-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000058
3-(2-chloro-4-fluorophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000077
3-(2-chlorophenyl)-4-methyl-5-(4-pentylphenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.000043
3-(2-chlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000031
3-(2-chlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0002
3-(2-chlorophenyl)-5-(3,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000028
3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000088
3-(2-chlorophenyl)-5-[2-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000089
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Homo sapiens
-
-
0.000001
3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000029
3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000068
3-(4-benzylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(4-butyl-2-methylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
IC50 below 0.000001 mM
0.00026
3-(4-butylphenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000023
3-(4-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000015
3-(4-chloro-2-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000027
3-(4-chloro-3-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.00063
3-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000027
3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000014
3-(4-tert-butylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
IC50 below 0.000001 mM
0.00074
3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000043
3-biphenyl-3-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000011
3-biphenyl-4-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.002631
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-4-fluorobenzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001672
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.01449
3-chloro-N-[4-(morpholin-4-ylcarbonyl)benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000647
3-chloro-N-[4-(piperidin-1-ylcarbonyl)benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001733
3-chloro-N-[4-(pyrrolidin-1-ylcarbonyl)benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0159
3-chloro-N-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000078
3-tricyclo[3.3.1.13,7]dec-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Homo sapiens
-
-
0.12
3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
Homo sapiens
-
pH and temperature not specified in the publication
0.000002 - 0.000199
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000016
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000027
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000078
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000019
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000052
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.00001 - 0.000057
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000035 - 0.000107
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
0.000005
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.000026
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(4-phenoxyphenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000017
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000023
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000002
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[3-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000044
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1,3-thiazol-2-yl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000003
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1H-pyrrol-1-yl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000013
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000093
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001 - 0.000014
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000002
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000027
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000003
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluoro-4-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000011
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4'-fluorobiphenyl-4-yl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000015
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000038
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-iodophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[1-(4-chlorophenyl)cyclobutyl]-5-[2-chloro-4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000035
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(cyclopropyloxy)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000032 - 0.000454
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000041
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.00023
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000003 - 0.000037
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000027 - 0.000494
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000008 - 0.000018
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000019
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000015 - 0.000374
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000025
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000332
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000043 - 0.000061
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
0.00017
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzothiazol-2(3H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00027
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzoxazol-2(3H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00024
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00014
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-4-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000005 - 0.000355
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000115
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.0000036
3-[2,3-bis(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-[2-chloro-4-(1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000069
3-[2-chloro-4-(2,4-dimethyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000098
3-[2-chloro-4-(2-cyclopropyl-4-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000026
3-[2-chloro-4-(2-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000039
3-[2-chloro-4-[2-(methylsulfanyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000014
3-[2-chloro-4-[2-(methylsulfonyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000028
3-[2-chloro-4-[3-(ethylsulfonyl)propyl]phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000011
3-[3-chloro-2'-(ethylsulfanyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[3-chloro-2'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[3-chloro-3'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[3-chloro-3'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000021
3-[3-chloro-4'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000017
3-[3-chloro-4'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000013
3-[4-chloro-2-(trifluoromethyl)phenyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000028
3-[4-[2-(ethylsulfonyl)ethyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000034
3-[4-[3-(ethylsulfonyl)propyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000005 - 0.000016
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
0.000022 - 0.000038
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
0.0013 - 0.05
3alpha,5alpha-tetrahydrocorticosterone
0.0003
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
Homo sapiens
-
pH and temperature not specified in the publication
0.0000012
4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000025
4-(2-[1-[(2-fluorobenzene-1-sulfonyl)amino]cyclopropyl]-2-methylpropanamido)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
4-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Homo sapiens
-
-
0.001
4-([(3R)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000073
4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001
4-([(3S)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000008
4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.002106
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N,N-diethylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000014
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)benzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000638
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-methylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000002
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-propylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000049
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000411
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclohexylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.008512
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclopentylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.002698
4-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000046
4-methyl-3-(2-methylnaphthalen-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.00025
4-methyl-3-(4-pentylphenyl)-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000052
4-methyl-3-(4-pentylphenyl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000009
4-methyl-3-(7-methylnaphthalen-2-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000026
4-methyl-3-naphthalen-2-yl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000078
4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000037
4-methyl-3-phenyl-5-tricyclo[3.3.1.13,7]dec-1-yl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000027
4-methyl-3-phenyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000013
4-methyl-3-[2-(trifluoromethoxy)phenyl]-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
49.3
4-nonylphenol
Homo sapiens
-
inhibition of liver isozyme 11beta-HSD1, pH 7.4, 37°C
0.00072
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00004
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00195
4-[(E)-[(2Z)-2-[(2-chlorophenyl)imino]-4-oxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenyl benzoate
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[(N-[4-[(dimethylamino)methoxy]benzene-1-sulfonyl]-2-methylalanyl)amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000006
4-[2-(1-[[(2-fluorobenzene-1-sulfonyl)amino]methyl]cyclopropyl)-2-methylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000039
4-[4-methyl-5-(1-methyl-1H-indol-4-yl)-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000009
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2,3,3-tetramethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.00000098
4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indole
Homo sapiens
-
-
0.000002
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]-2-fluorophenol
Homo sapiens
-
-
0.00000034
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000014
4-[[2-methyl-N-(2,4,5-trifluorobenzene-1-sulfonyl)alanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
4-[[N-(2,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
4-[[N-(2,6-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000001
4-[[N-(2-chloro-4-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000006
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000002
4-[[N-(3,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[[N-(3,5-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[[N-(3-chloro-2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000001
4-[[N-(3-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
4-[[N-(4-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000044
4-[[N-(4-hydroxybenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
4-[[N-(4-tert-butylbenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
4-[[N-(benzenesulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000435
5-(adamantan-1-ylcarbonyl)-4H,5H,6H,7H-thieno[3,2-c]pyridine
Homo sapiens
-
-
0.0002
5-fluoro-1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0021 - 0.0063
5alpha-dihydrocorticosterone
0.000089
7-chloro-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-ol
Homo sapiens
-
-
0.00024
7-hydroxy-2-(2-hydroxyethyl)-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00023
7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000049
7-keto,25-hydroxycholesterol
Homo sapiens
recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C
0.000015
7-keto,27-hydroxycholesterol
Homo sapiens
isoform 11beta-HSD2, at pH 7.4, temperature not specified in the publication
0.000091
7beta,25-dihydroxycholesterol
Homo sapiens
recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C
0.000011
7beta,27-dihydroxycholesterol
Homo sapiens
isoform 11beta-HSD2, at pH 7.4, temperature not specified in the publication
0.0000025
azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.01197
BDE-100
Homo sapiens
-
pH and temperature not specified in the publication
0.00441
BDE-153
Homo sapiens
-
pH and temperature not specified in the publication
0.01481
bisphenol A
Homo sapiens
pH and temperature not specified in the publication
0.01399
butylated hydroxyanisole
Homo sapiens
pH and temperature not specified in the publication
0.000052
BVT-14225
Homo sapiens
-
isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2, pH and temperature not specified in the publication
0.0005
carbenoxolone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00074
danazol
Homo sapiens
pH and temperature not specified in the publication
0.00195
dibutyltin
Homo sapiens
pH and temperature not specified in the publication
0.0017
diethyldithiocarbamate
Homo sapiens
pH and temperature not specified in the publication
49.4
diethylhexyl adipate
Homo sapiens
-
inhibition of liver isozyme 11beta-HSD1, pH 7.4, 37°C
0.00142
diphenyltin
Homo sapiens
pH and temperature not specified in the publication
0.000128
Disulfiram
Homo sapiens
pH and temperature not specified in the publication
0.003
ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0045
ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00006
fluoxymesterone
Homo sapiens
pH and temperature not specified in the publication
0.000256
glycyrrhetinic acid
Homo sapiens
pH and temperature not specified in the publication
0.00001
glycyrrhizic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000186
glycyrrhizinic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000186
glycyrrhizininc acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000187
hydroxyitraconazole
Homo sapiens
at pH 7.4 and 37°C
0.000122
itraconazole
Homo sapiens
at pH 7.4 and 37°C
0.000753
maneb
Homo sapiens
pH and temperature not specified in the publication
0.000038
methyl 2-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Homo sapiens
-
-
0.0000019
methyl 2-[5-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Homo sapiens
-
-
0.000031
methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00005
methyl 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Homo sapiens
-
-
0.00528
N-(4-chloro-2-methyl-1,3-benzothiazol-5-yl)adamantane-1-carboxamide
Homo sapiens
-
-
0.001208
N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-3-(trifluoromethyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001
N-(5-cyanotricyclo[3.3.1.1~3,7~]decan-2-yl)-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000249
N-(furan-2-ylmethyl)-N-methyladamantane-1-carboxamide
Homo sapiens
-
-
0.000403
N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
Homo sapiens
-
-
0.000047
N-butyl-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000008
N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000017
N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000014
N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine
Homo sapiens
-
-
0.000229
N-methyl-N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
Homo sapiens
-
-
0.000125
N-methyl-N-(thiophen-3-ylmethyl)adamantane-1-carboxamide
Homo sapiens
-
-
0.000113
N-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.000448
N-methyl-N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.0017
N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.000679
N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.0000007
N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000007
N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000014
N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00069
N-[4-[(2,6-dimethylpyrimidin-4-yl)sulfamoyl]phenyl]-4-[oxo(phenyl)acetyl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
N-[5-(2-amino-2-oxoethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
N-[5-(3-amino-3-oxopropyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
N-[5-(cyanomethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydrazinecarbonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000002
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydroxymethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000055
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-[(2-hydroxyhydrazinyl)methyl]tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00096
oxymesterone
Homo sapiens
pH and temperature not specified in the publication
0.00071
oxymetholone
Homo sapiens
pH and temperature not specified in the publication
0.00001897
perfluorohexane sulfonate
Homo sapiens
pH and temperature not specified in the publication
0.000000048
perfluorooctane sulfonate
Homo sapiens
pH and temperature not specified in the publication
0.00002441
Perfluorooctanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000512
posaconazole
Homo sapiens
at pH 7.4 and 37°C
0.0063
pyrrolidine dithiocarbamate
Homo sapiens
pH and temperature not specified in the publication
0.00023
sterenin A
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.0066
sterenin B
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.00024
sterenin C
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.0026
sterenin D
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.00137
testosterone
Homo sapiens
pH and temperature not specified in the publication
0.000132
thiram
Homo sapiens
pH and temperature not specified in the publication
0.0019
tributyltin
Homo sapiens
pH and temperature not specified in the publication
0.00319
Triphenyltin
Homo sapiens
pH and temperature not specified in the publication
0.031
zineb
Homo sapiens
pH and temperature not specified in the publication
0.000004
[1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00077 - 0.00185
[3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone
0.000234
[4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000017
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
Homo sapiens
-
pH and temperature not specified in the publication
additional information
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
0.05799
(-)-epigallocatechin 3-gallate
Homo sapiens
for cortisone reduction, at pH 7.4 and 37°C
0.1312
(-)-epigallocatechin 3-gallate
Homo sapiens
for cortisol oxidation, at pH 7.4 and 37°C
0.000001
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.003
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.112
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisone reduction
0.005
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.2
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisone reduction, IC50 above 0.2 mM
0.000056
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
Homo sapiens
11beta-HSD1, cortisol oxidation
0.000244
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
Homo sapiens
11beta-HSD1, cortisone reduction
0.012
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
Homo sapiens
11beta-HSD2, cortisol oxidation
0.002
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
Homo sapiens
11beta-HSD1, cortisol oxidation
0.039
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
Homo sapiens
11beta-HSD1, cortisone reduction
0.2
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
Homo sapiens
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM
0.002
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
Homo sapiens
11beta-HSD1, cortisol oxidation
0.037
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
Homo sapiens
11beta-HSD1, cortisone reduction
0.2
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
Homo sapiens
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM
0.000049
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
Homo sapiens
11beta-HSD1, cortisol oxidation
0.000149
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
Homo sapiens
11beta-HSD1, cortisone reduction
0.016
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
Homo sapiens
11beta-HSD2, cortisol oxidation
0.011
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.074
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
Homo sapiens
11beta-HSD1, cortisone reduction
0.009
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.2
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
Homo sapiens
11beta-HSD1, cortisone reduction, IC50 above 0.2 mM
0.000122
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
Homo sapiens
11beta-HSD1, cortisone reduction
0.000177
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
Homo sapiens
11beta-HSD1, cortisol oxidation
0.025
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
Homo sapiens
11beta-HSD2, cortisol oxidation
0.000008
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD2, cortisol oxidation
0.000012
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.000012
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD1, cortisone reduction
0.001
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.068
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisone reduction
0.2
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisol oxidation , IC50 above 0.2 mM
0.2
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
Homo sapiens
11beta-HSD1, cortisone reduction, IC50 above 0.2 mM
0.000074
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
Homo sapiens
11beta-HSD1, cortisol oxidation
0.000124
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
Homo sapiens
11beta-HSD1, cortisone reduction
0.016
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
Homo sapiens
11beta-HSD2, cortisol oxidation
0.000002
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.0000026
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000068
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.000141
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD1, cortisone reduction
0.2
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM
0.000061
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD1, cortisol oxidation
0.000119
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD1, cortisone reduction
0.2
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
Homo sapiens
11beta-HSD2, cortisol oxidation, IC50 above 0.2 mM
0.000005
methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
Homo sapiens
pH and temperature not specified in the publication
0.00002
methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
Homo sapiens
pH and temperature not specified in the publication
0.0000038
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000072
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0007
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.008
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.000016
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00065
11-oxo-3alpha,5alpha-tetrahydrotestosterone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.05
11-oxo-3alpha,5alpha-tetrahydrotestosterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.005
11beta-hydroxy-androstanediol
Homo sapiens
-
dehydrogenase reaction, dehydrogenase reaction, pH 8.4, 37°C
0.0115
11beta-hydroxy-androstanediol
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.000001
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000013
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.0001
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000012
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000008
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000172
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000199
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH and temperature not specified in the publication
0.000078
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000019
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000052
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.00001
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000057
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000035
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000107
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000013
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.0000013
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000014
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000032
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000454
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000041
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.00023
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000003
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000037
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000027
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000494
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000008
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000018
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000019
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000015
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000374
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000025
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000001
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
pH and temperature not specified in the publication
0.000332
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000043
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
Homo sapiens
-
-
0.000061
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
Homo sapiens
-
-
0.000005
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000355
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000002
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000115
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Homo sapiens
-
-
0.000005
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000016
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000022
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000038
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0013
3alpha,5alpha-tetrahydrocorticosterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.05
3alpha,5alpha-tetrahydrocorticosterone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.0021
5alpha-dihydrocorticosterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.0063
5alpha-dihydrocorticosterone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.00077
[3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.00185
[3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone
Homo sapiens
-
pH and temperature not specified in the publication
additional information
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
Homo sapiens
99% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid
Homo sapiens
4% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
32% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta)-3-hydroxy-11-oxoolean-12-en-30-amide
Homo sapiens
9% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid
Homo sapiens
6% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
Homo sapiens
87% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide
Homo sapiens
71% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
Homo sapiens
5% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
Homo sapiens
1% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide
Homo sapiens
38% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
Homo sapiens
72% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
Homo sapiens
15% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
58% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
Homo sapiens
71% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
(3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
Homo sapiens
93% residual activity at 0,0002 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone
Homo sapiens
68% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone
Homo sapiens
-
68% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(2-chloro-benzylsulfanyl)ethanone
Homo sapiens
24% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(2-chloro-benzylsulfanyl)ethanone
Homo sapiens
-
24% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(3-methylbenzylsulfanyl)ethanone
Homo sapiens
26% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(3-methylbenzylsulfanyl)ethanone
Homo sapiens
-
26% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(3-trifluoromethyl-phenoxy)ethanone
Homo sapiens
46% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(3-trifluoromethyl-phenoxy)ethanone
Homo sapiens
-
46% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(3-trifluoromethylbenzyloxy)ethanone
Homo sapiens
31% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(3-trifluoromethylbenzyloxy)ethanone
Homo sapiens
-
31% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-chloro-benzenesulfonyl)ethanone
Homo sapiens
56% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-chloro-benzenesulfonyl)ethanone
Homo sapiens
-
56% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-chloro-benzyloxy)ethanone
Homo sapiens
53% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-chloro-benzyloxy)ethanone
Homo sapiens
-
53% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-chloro-benzylsulfanyl)ethanone
Homo sapiens
74% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-chloro-benzylsulfanyl)ethanone
Homo sapiens
-
74% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfinyl)ethanone
Homo sapiens
60% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfinyl)ethanone
Homo sapiens
-
60% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-tert-butylbenzylsulfanyl)ethanone
Homo sapiens
68% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-tert-butylbenzylsulfanyl)ethanone
Homo sapiens
-
68% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-trifluoromethylbenzyloxy)ethanone
Homo sapiens
35% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(4-trifluoromethylbenzyloxy)ethanone
Homo sapiens
-
35% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(biphenyl-4-ylmethoxy)ethanone
Homo sapiens
38% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-(biphenyl-4-ylmethoxy)ethanone
Homo sapiens
-
38% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-m-tolylmethanesulfonyl-ethanone
Homo sapiens
45% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
1-adamantan-1-yl-2-m-tolylmethanesulfonyl-ethanone
Homo sapiens
-
45% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
Homo sapiens
30.88% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
Homo sapiens
-
30.88% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-furan-2-ylmethyl-acetamide
Homo sapiens
4% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-furan-2-ylmethyl-acetamide
Homo sapiens
-
4% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-isopropyl-acetamide
Homo sapiens
63% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-isopropyl-acetamide
Homo sapiens
-
63% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-tert-butyl-acetamide
Homo sapiens
45% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-tert-butyl-acetamide
Homo sapiens
-
45% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
3-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
Homo sapiens
59% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
3-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
Homo sapiens
-
59% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Homo sapiens
35.31% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Homo sapiens
-
35.31% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Homo sapiens
32.05% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Homo sapiens
-
32.05% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Homo sapiens
27.21% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Homo sapiens
-
27.21% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Homo sapiens
22.82% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Homo sapiens
-
22.82% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Homo sapiens
18.95% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Homo sapiens
-
18.95% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Homo sapiens
28.08% inhibition at 0.001 mM
additional information
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Homo sapiens
-
28.08% inhibition at 0.001 mM
additional information
4-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
Homo sapiens
69% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
Homo sapiens
-
69% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
Homo sapiens
63% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
Homo sapiens
-
63% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
Homo sapiens
25% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
Homo sapiens
-
25% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-benzylbenzamide
Homo sapiens
69% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-benzylbenzamide
Homo sapiens
-
69% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzamide
Homo sapiens
63% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzamide
Homo sapiens
-
63% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid methyl ester
Homo sapiens
55% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid methyl ester
Homo sapiens
-
55% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
Homo sapiens
18.94% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
Homo sapiens
-
18.94% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
Homo sapiens
36.61% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
Homo sapiens
-
36.61% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
carbenoxolone
Homo sapiens
12% residual activity at 0,001 mM, pH not specified in the publication, 37°C
additional information
flavone
Homo sapiens
16% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, 37°C
additional information
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-chloro-phenyl]acetamide
Homo sapiens
49% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-chloro-phenyl]acetamide
Homo sapiens
-
49% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-methyl-phenyl]acetamide
Homo sapiens
68% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-methyl-phenyl]acetamide
Homo sapiens
-
68% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-chloro-phenyl]acetamide
Homo sapiens
61% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-chloro-phenyl]acetamide
Homo sapiens
-
61% inhibition at 0.001 mM, pH not specified in the publication, 37°C
additional information
quercetin
Homo sapiens
27% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, 37°C
additional information
(1S,2R,3S,5R,6R)-4-methylidene-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]heptane-2,3,5-triol
Homo sapiens
-
IC50 = 0.0148 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aR,6S,8aR)-6-hydroxy-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
Homo sapiens
-
IC50 = 0.0035 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,5R,6R)-4-(hydroxymethyl)-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]hept-3-ene-2,5-diol
Homo sapiens
-
IC50 = 0.0091 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(2E,4S)-4-hydroxy-5-[(1S,5S,6S)-6-(hydroxymethyl)-2-methylidenebicyclo[3.1.1]hept-6-yl]-2-methylpent-2-enoic acid
Homo sapiens
-
IC50 = 0.0031 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(2S)-5-(acetyloxy)-2-hydroxypentyl acetate
Homo sapiens
-
IC50 = 0.0623 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(4aS,5R,8aR)-5,6-bis(hydroxymethyl)-1,1,4a-trimethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
Homo sapiens
-
IC50 = 0.0032 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
Homo sapiens
-
IC50 = 0.008 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-3,4,4a,5,8,8a-hexahydronaphthalen-2(1H)-one
Homo sapiens
-
IC50 = 0.0017 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)acetic acid
Homo sapiens
-
25% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
2-oxopentane-1,5-diyl diacetate
Homo sapiens
-
IC50 = 0.0287 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide
Homo sapiens
-
IC50 value between 0.0023 to 0.0032 mM, pH not specified in the publication, temperature not specified in the publication
additional information
3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide
Homo sapiens
-
IC50 value between 0.0023 to 0.0032 mM, pH not specified in the publication, temperature not specified in the publication
additional information
3-chloro-2-methyl-N-[6-(2-morpholin-4-yl-2-oxoethyl)-pyridin-2-yl]-benzenesulfonamide
Homo sapiens
-
6% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide
Homo sapiens
-
8% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
Homo sapiens
-
11% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide
Homo sapiens
-
39% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
4-(1-benzofuran-2-ylcarbonyl)-5-(2-fluorophenyl)-3-hydroxy-1-[5-[(4-methylbenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-1,5-dihydro-2H-pyrrol-2-one
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
4-methoxy-N-(6-methylpyridin-2-yl)benzenesulfonamide
Homo sapiens
-
23% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
4-propyl-N-[2-(thiophen-2-yl)ethyl]benzenesulfonamide
Homo sapiens
-
IC50 value between 0.0023 to 0.0032 mM, pH not specified in the publication, temperature not specified in the publication
additional information
4-tert-butyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
Homo sapiens
-
32% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
5-hydroxy-4-oxopentyl acetate
Homo sapiens
-
IC50 = 0.0474 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N'-[(E)-(5-bromo-2-hydroxyphenyl)methylidene]-2-([5-[(phenylamino)methyl]-4-(prop-2-en-1-yl)-4H-1,2,4-triazol-3-yl]sulfanyl)propanehydrazide
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N-(6-methylpyridin-2-yl)-2-(trifluoromethyl)benzenesulfonamide
Homo sapiens
-
1% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N-(6-methylpyridin-2-yl)naphthalene-1-sulfonamide
Homo sapiens
-
10% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide
Homo sapiens
-
IC50 value between 0.00085 to 0.00798 mM, pH not specified in the publication, temperature not specified in the publication
additional information
N-[6-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]-3-chloro-2-methylbenzenesulfonamide
Homo sapiens
-
22% inhibition at 0.0001 mM, pH not specified in the publication, temperature not specified in the publication
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Hult, M.; Nobel, C.S.I.; Abrahmsen, L.; Nicoll-Griffith, D.A.; Jrnvall, H.; Oppermann, U.C.T.
Novel enzymological profiles of human 11beta-hydroxysteroid dehydrogenase type 1
Chem. Biol. Interact.
130-132
805-8014
2001
Homo sapiens
brenda
Walker, E.A.; Clarks, A.M.; Hewison, M.; Ride, J.P.; Steward, P.M.
Functional expression, characterization, and purification of the catalytic domain of human 11-beta-hydroxysteroid dehydrogenase type 1
J. Biol. Chem.
276
21343-21350
2001
Homo sapiens
brenda
Oppermann, U.C.T.; Persson, B.; Jornvall, H.
The 11beta-hydroxysteroid dehydrogenase system, a determinant of glucocorticoid and mineralocorticoid action
Eur. J. Biochem.
249
355-360
1997
Comamonas testosteroni, Oryctolagus cuniculus, Homo sapiens, Mus musculus
-
brenda
Ferrari, P.; Smith, R.E.; Funder, J.W.; Krozowski, Z.S.
Substrate and inhibitor specificity of the clones human 11beta-hydroxysteroid dehydrogenase type 2 isoform
Am. J. Physiol.
270
E900-904
1996
Homo sapiens
brenda
Blum , S.; Buhler, H.
Characterization of human placental 11beta-hydroxysteroid dehydrogenase, a key enzyme of cortocosteroid metabolism
Cell. Physiol. Biochem.
5
167-175
1995
Homo sapiens
-
brenda
Lakshim, V.; Nath, N.; Muneyyirci-Delale, O.
Characterization of 11beta-hydroxysteroid dehydrogenase of human placenta: Evidence for the existence of two species of 11beta-hydroxysteroid dehydrogenases
J. Steroid Biochem. Mol. Biol.
45
391-397
1993
Homo sapiens
brenda
Pearson Murphy, B.E.
Specificity of human 11beta-hydroxysteroid dehydrogenase
J. Steroid Biochem.
14
807-809
1981
Homo sapiens
brenda
Maser, E.; Volker, B.; Friebertshauser, J.
11 beta-Hydroxysteroid dehydrogenase type 1 from human liver: dimerization and enzyme cooperativity support its postulated role as glucocorticoid reductase
Biochemistry
41
2459-2465
2002
Homo sapiens
brenda
Blum, A.; Raum, A.; Maser, E.
Functional characterization of the human 11 beta-hydroxysteroid dehydrogenase 1B (11 beta-HSD 1B) variant
Biochemistry
42
4108-4117
2003
Homo sapiens
brenda
Zbankova, S.; Bryndova, J.; Kment, M.; Pacha, J.
Expression of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in colorectal cancer
Cancer Lett.
210
95-100
2004
Homo sapiens
brenda
Maser, E.; Friebertshauser, J.; Volker, B.
Purification, characterization and NNK carbonyl reductase activities of 11beta-hydroxysteroid dehydrogenase type 1 from human liver: enzyme cooperativity and significance in the detoxification of a tobacco-derived carcinogen
Chem. Biol. Interact.
143-144
435-448
2003
Homo sapiens
brenda
Blum, A.; Maser, E.
The critical role of the N-terminus of 11beta-hydroxysteroid dehydrogenase type 1, as being encoded by exon 1, for enzyme stabilization and activity
Chem. Biol. Interact.
143-144
469-480
2003
Homo sapiens
brenda
Shafqat, N.; Elleby, B.; Svensson, S.; Shafqat, J.; Jornvall, H.; Abrahmsen, L.; Oppermann, U.
Comparative enzymology of 11beta -hydroxysteroid dehydrogenase type 1 from glucocorticoid resistant (guinea pig) versus sensitive (human) species
J. Biol. Chem.
278
2030-2035
2003
Cavia porcellus, Homo sapiens
brenda
Schweizer, R.A.; Zurcher, M.; Balazs, Z.; Dick, B.; Odermatt, A.
Rapid hepatic metabolism of 7-ketocholesterol by 11beta-hydroxysteroid dehydrogenase type 1: species-specific differences between the rat, human, and hamster enzyme
J. Biol. Chem.
279
18415-18424
2004
Homo sapiens, Rattus norvegicus, Mesocricetus auratus (Q6R0J2)
brenda
Frick, C.; Atanasov, A.G.; Arnold, P.; Ozols, J.; Odermatt, A.
Appropriate function of 11beta-hydroxysteroid dehydrogenase type 1 in the endoplasmic reticulum lumen is dependent on its N-terminal region sharing similar topological determinants with 50-kDa esterase
J. Biol. Chem.
279
31131-31138
2004
Homo sapiens
brenda
Roobol-Boza, M.; Dolby, V.; Doverskog, M.; Barrefelt, A.; Lindqvist, F.; Oppermann, U.C.; Kohler Van Alstine, K.; Tjerneld, F.
Membrane protein isolation by in situ solubilization, partitioning and affinity adsorption in aqueous two-phase systems. Purification of the human type 1 11beta-hydroxysteroid dehydrogenase
J. Chromatogr. A
1043
217-223
2004
Homo sapiens
brenda
Nobel, C.S.I.; Dunas, F.; Abrahmsen, L.B.
Purification of full-length recombinant human and rat type 1 11beta-hydroxysteroid dehydrogenases with retained oxidoreductase activities
Protein Expr. Purif.
26
349-356
2002
Homo sapiens, Rattus norvegicus
brenda
Wsol, V.; Szotakova, B.; Skalova, L.; Maser, E.
The novel anticancer drug oracin: different stereospecificity and cooperativity for carbonyl reduction by purified human liver 11beta-hydroxysteroid dehydrogenase type 1
Toxicology
197
253-261
2004
Homo sapiens
brenda
Garbrecht, M.R.; Schmidt, T.J.; Krozowski, Z.S.; Snyder, J.M.
11beta-Hydroxysteroid dehydrogenase type 2 and the regulation of surfactant protein A by dexamethasone metabolites
Am. J. Physiol. Endocrinol. Metab.
290
E653-E660
2006
Homo sapiens
brenda
Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.
The role of tyrosine 177 in human 11beta-hydroxysteroid dehydrogenase type 1 in substrate and inhibitor binding: an unlikely hydrogen bond donor for the substrate
Biochim. Biophys. Acta
1764
824-830
2006
Homo sapiens
brenda
Xiang, J.; Ipek, M.; Suri, V.; Massefski, W.; Pan, N.; Ge, Y.; Tam, M.; Xing, Y.; Tobin, J.F.; Xu, X.; Tam, S.
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
15
2865-2869
2005
Homo sapiens
brenda
Olson, S.; Aster, S.D.; Brown, K.; Carbin, L.; Graham, D.W.; Hermanowski-Vosatka, A.; LeGrand, C.B.; Mundt, S.S.; Robbins, M.A.; Schaeffer, J.M.; Slossberg, L.H.; Szymonifka, M.J.; Thieringer, R.; Wright, S.D.; Balkovec, J.M.
Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem. Lett.
15
4359-4362
2005
Homo sapiens, Mus musculus (P50172), Mus musculus (P51661)
brenda
Mai, K.; Kullmann, V.; Bobbert, T.; Maser-Gluth, C.; Moehlig, M.; Baehr, V.; Pfeiffer, A.F.; Spranger, J.; Diederich, S.
In vivo activity of 11beta-hydroxysteroid dehydrogenase type 1 and free fatty acid-induced insulin resistance
Clin. Endocrinol. (Oxf.)
63
442-449
2005
Homo sapiens
brenda
Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Alford, F.P.; Inder, W.J.
11beta Hydroxysteroid dehydrogenase type 1 is expressed and is biologically active in human skeletal muscle
Clin. Endocrinol. (Oxf.)
65
800-805
2006
Homo sapiens
brenda
Li, W.; Gao, L.; Wang, Y.; Duan, T.; Myatt, L.; Sun, K.
Enhancement of cortisol-induced 11beta-hydroxysteroid dehydrogenase type 1 expression by interleukin 1beta in cultured human chorionic trophoblast cells
Endocrinology
147
2490-2495
2006
Homo sapiens
brenda
Ohshima, M.; Ohno, S.; Nakajin, S.
Inhibitory effects of some possible endocrine-disrupting chemicals on the isozymes of human 11beta-hydroxysteroid dehydrogenase and expression of their mRNA in gonads and adrenal glands
Environ. Sci.
12
219-230
2005
Homo sapiens
brenda
Atanasov, A.G.; Dzyakanchuk, A.A.; Schweizer, R.A.; Nashev, L.G.; Maurer, E.M.; Odermatt, A.
Coffee inhibits the reactivation of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: a glucocorticoid connection in the anti-diabetic action of coffee?
FEBS Lett.
580
4081-4085
2006
Homo sapiens
brenda
Hosfield, D.J.; Wu, Y.; Skene, R.J.; Hilgers, M.; Jennings, A.; Snell, G.P.; Aertgeerts, K.
Conformational flexibility in crystal structures of human 11beta-hydroxysteroid dehydrogenase type I provide insights into glucocorticoid interconversion and enzyme regulation
J. Biol. Chem.
280
4639-4648
2005
Homo sapiens
brenda
Miguet, L.; Zhang, Z.; Barbier, M.; Grigorov, M.G.
Comparison of a homology model and the crystallographic structure of human 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) in a structure-based identification of inhibitors
J. Comput. Aided Mol. Des.
20
67-81
2006
Homo sapiens
brenda
Gilmour, J.S.; Coutinho, A.E.; Cailhier, J.F.; Man, T.Y.; Clay, M.; Thomas, G.; Harris, H.J.; Mullins, J.J.; Seckl, J.R.; Savill, J.S.; Chapman, K.E.
Local amplification of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1 promotes macrophage phagocytosis of apoptotic leukocytes
J. Immunol.
176
7605-7611
2006
Homo sapiens, Mus musculus
brenda
Ayachi, S.E.; Paulmyer-Lacroix, O.; Verdier, M.; Alessi, M.C.; Dutour, A.; Grino, M.
11beta-Hydroxysteroid dehydrogenase type 1-driven cortisone reactivation regulates plasminogen activator inhibitor type 1 in adipose tissue of obese women
J. Thromb. Haemost.
4
621-627
2006
Homo sapiens
brenda
Latif, S.A.; Pardo, H.A.; Hardy, M.P.; Morris, D.J.
Endogenous selective inhibitors of 11beta-hydroxysteroid dehydrogenase isoforms 1 and 2 of adrenal origin
Mol. Cell. Endocrinol.
243
43-50
2005
Ovis aries, Homo sapiens
brenda
Odermatt, A.; Atanasov, A.G.; Balazs, Z.; Schweizer, R.A.; Nashev, L.G.; Schuster, D.; Langer, T.
Why is 11beta-hydroxysteroid dehydrogenase type 1 facing the endoplasmic reticulum lumen? Physiological relevance of the membrane topology of 11beta-HSD1
Mol. Cell. Endocrinol.
248
15-23
2006
Homo sapiens (P28845)
brenda
Su, X.; Vicker, N.; Ganeshapillai, D.; Smith, A.; Purohit, A.; Reed, M.J.; Potter, B.V.
Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
248
214-217
2006
Homo sapiens
brenda
Hult, M.; Shafqat, N.; Elleby, B.; Mitschke, D.; Svensson, S.; Forsgren, M.; Barf, T.; Vallgarda, J.; Abrahmsen, L.; Oppermann, U.
Active site variability of type 1 11beta-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons
Mol. Cell. Endocrinol.
248
26-33
2006
Cavia porcellus, Mus musculus, Rattus norvegicus, Homo sapiens (P28845), Homo sapiens
brenda
Maser, E.; Wsol, V.; Martin, H.J.
11beta-Hydroxysteroid dehydrogenase type 1: purification from human liver and characterization as carbonyl reductase of xenobiotics
Mol. Cell. Endocrinol.
248
34-37
2006
Homo sapiens
brenda
Ito-Kobayashi, M.; Aoyagi, A.; Tanaka, I.; Muramatsu, Y.; Umetani, M.; Takatsu, T.
Sterenin A, B, C and D, novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors from Stereum sp. SANK 21205
J. Antibiot.
61
128-135
2008
Homo sapiens
brenda
Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Krozowski, Z.; Inder, W.J.; Alford, F.P.
Altered activity of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in skeletal muscle confers metabolic protection in subjects with type 2 diabetes
J. Clin. Endocrinol. Metab.
92
3314-3320
2007
Homo sapiens
brenda
Gong, R.; Morris, D.J.; Brem, A.S.
Human renal 11beta-hydroxysteroid dehydrogenase 1 functions and co-localizes with COX-2
Life Sci.
82
631-637
2008
Homo sapiens
brenda
Sun, L.; Stenken, J.A.; Yang, A.Y.; Zhao, J.J.; Musson, D.G.
An in vitro microdialysis methodology to study 11beta-hydroxysteroid dehydrogenase type 1 enzyme activity in liver microsomes
Anal. Biochem.
370
26-37
2007
Canis lupus, Homo sapiens
brenda
Flyren, K.; Bergquist, L.O.; Castro, V.M.; Fotsch, C.; Johansson, L.; St Jean, D.J.; Sutin, L.; Williams, M.
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
Bioorg. Med. Chem. Lett.
17
3421-3425
2007
Homo sapiens
brenda
Yang, H.; Dou, W.; Lou, J.; Leng, Y.; Shen, J.
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling
Bioorg. Med. Chem. Lett.
18
1340-1345
2008
Homo sapiens, Mus musculus
brenda
Aster, S.D.; Graham, D.W.; Kharbanda, D.; Patel, G.; Ponpipom, M.; Santorelli, G.M.; Szymonifka, M.J.; Mundt, S.S.; Shah, K.; Springer, M.S.; Thieringer, R.; Hermanowski-Vosatka, A.; Wright, S.D.; Xiao, J.; Zokian, H.; Balkovec, J.M.
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem. Lett.
18
2799-2804
2008
Homo sapiens, Mus musculus
brenda
Wang, H.; Ruan, Z.; Li, J.J.; Simpkins, L.M.; Smirk, R.A.; Wu, S.C.; Hutchins, R.D.; Nirschl, D.S.; Van Kirk, K.; Cooper, C.B.; Sutton, J.C.; Ma, Z.; Golla, R.; Seethala, R.; Salyan, M.E.; Nayeem, A.; Krystek, S.R.; Sheriff, S.; Camac, D.M.; Morin, P.E.; Carpenter, B.; Robl, J.A.; Zahler, R.; Gordon, D.A.; Hamann, L.G.
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem. Lett.
18
3168-3172
2008
Homo sapiens
brenda
Zhu, Y.; Olson, S.H.; Hermanowski-Vosatka, A.; Mundt, S.; Shah, K.; Springer, M.; Thieringer, R.; Wright, S.; Xiao, J.; Zokian, H.; Balkovec, J.M.
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
18
3405-3411
2008
Homo sapiens, Mus musculus
brenda
Zhu, Y.; Olson, S.H.; Graham, D.; Patel, G.; Hermanowski-Vosatka, A.; Mundt, S.; Shah, K.; Springer, M.; Thieringer, R.; Wright, S.; Xiao, J.; Zokian, H.; Dragovic, J.; Balkovec, J.M.
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
18
3412-3416
2008
Homo sapiens, Mus musculus
brenda
Sun, D.; Wang, Z.; Di, Y.; Jaen, J.C.; Labelle, M.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tomooka, C.S.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
Bioorg. Med. Chem. Lett.
18
3513-3516
2008
Homo sapiens, Mus musculus
brenda
Ahmed, A.; Saksena, S.; Sherlock, M.; Olliff, S.P.; Elias, E.; Stewart, P.M.
Induction of hepatic 11beta-hydroxysteroid dehydrogenase type 1 in patients with alcoholic liver disease
Clin. Endocrinol. (Oxf.)
68
898-903
2008
Homo sapiens
brenda
Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.
The selectivity of tyrosine 280 of human 11beta-hydroxysteroid dehydrogenase type 1 in inhibitor binding
FEBS Lett.
581
995-999
2007
Homo sapiens (P28845), Homo sapiens
brenda
Walker, E.A.; Ahmed, A.; Lavery, G.G.; Tomlinson, J.W.; Kim, S.Y.; Cooper, M.S.; Ride, J.P.; Hughes, B.A.; Shackleton, C.H.; McKiernan, P.; Elias, E.; Chou, J.Y.; Stewart, P.M.
11beta-Hydroxysteroid dehydrogenase type 1 regulation by intracellular glucose 6-phosphate provides evidence for a novel link between glucose metabolism and hypothalamo-pituitary-adrenal axis function
J. Biol. Chem.
282
27030-27036
2007
Homo sapiens, Mus musculus
brenda
Bujalska, I.J.; Durrani, O.M.; Abbott, J.; Onyimba, C.U.; Khosla, P.; Moosavi, A.H.; Reuser, T.T.; Stewart, P.M.; Tomlinson, J.W.; Walker, E.A.; Rauz, S.
Characterisation of 11beta-hydroxysteroid dehydrogenase 1 in human orbital adipose tissue: a comparison with subcutaneous and omental fat
J. Endocrinol.
192
279-288
2007
Homo sapiens
brenda
Johansson, L.; Fotsch, C.; Bartberger, M.D.; Castro, V.M.; Chen, M.; Emery, M.; Gustafsson, S.; Hale, C.; Hickman, D.; Homan, E.; Jordan, S.R.; Komorowski, R.; Li, A.; McRae, K.; Moniz, G.; Matsumoto, G.; Orihuela, C.; Palm, G.; Veniant, M.; Wang, M.; Williams, M.; Zhang, J.
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice
J. Med. Chem.
51
2933-2943
2008
Homo sapiens (P28845), Homo sapiens
brenda
Julian, L.D.; Wang, Z.; Bostick, T.; Caille, S.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Hungate, R.W.; Jaen, J.C.; Liu, J.; Monshouwer, M.; McMinn, D.; Rew, Y.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model
J. Med. Chem.
51
3953-3960
2008
Macaca fascicularis, Homo sapiens, Homo sapiens (P28845)
brenda
Munoz, R.; Carvajal, C.; Escalona, A.; Boza, C.; Perez, G.; Ibanez, L.; Fardella, C.
11beta-Hydroxysteroid dehydrogenase type 1 is overexpressed in subcutaneous adipose tissue of morbidly obese patients
Obes. Surg.
19
764-770
2008
Homo sapiens
brenda
Nashev, L.G.; Chandsawangbhuwana, C.; Balazs, Z.; Atanasov, A.G.; Dick, B.; Frey, F.J.; Baker, M.E.; Odermatt, A.
Hexose-6-phosphate dehydrogenase modulates 11beta-hydroxysteroid dehydrogenase type 1-dependent metabolism of 7-keto- and 7beta-hydroxy-neurosteroids
PLoS ONE
2
e561
2007
Homo sapiens
brenda
Hennebert, O.; Le Mee, S.; Pernelle, C.; Morfin, R.
5Alpha-androstane-3beta,7alpha,17beta-triol and 5alpha-androstane-3beta,7beta,17beta-triol as substrates for the human 11beta-hydroxysteroid dehydrogenase type 1
Steroids
72
855-864
2007
Homo sapiens
brenda
Rew, Y.; McMinn, D.L.; Wang, Z.; He, X.; Hungate, R.W.; Jaen, J.C.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Villemure, E.; Walker, N.P.; Yan, X.; Ye, Q.; Powers, J.P.
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors
Bioorg. Med. Chem. Lett.
19
1797-1801
2009
Homo sapiens (P28845)
brenda
Roche, D.; Carniato, D.; Leriche, C.; Lepifre, F.; Christmann-Franck, S.; Graedler, U.; Charon, C.; Bozec, S.; Doare, L.; Schmidlin, F.; Lecomte, M.; Valeur, E.
Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
19
2674-2678
2009
Homo sapiens (P28845), Homo sapiens
brenda
Lepifre, F.; Christmann-Franck, S.; Roche, D.; Leriche, C.; Carniato, D.; Charon, C.; Bozec, S.; Doare, L.; Schmidlin, F.; Lecomte, M.; Valeur, E.
Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold
Bioorg. Med. Chem. Lett.
19
3682-3685
2009
Homo sapiens (P28845), Homo sapiens
brenda
Tu, H.; Powers, J.P.; Liu, J.; Ursu, S.; Sudom, A.; Yan, X.; Xu, H.; Meininger, D.; Degraffenreid, M.; He, X.; Jaen, J.C.; Sun, D.; Labelle, M.; Yamamoto, H.; Shan, B.; Walker, N.P.; Wang, Z.
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem.
16
8922-8931
2008
Homo sapiens (P28845), Homo sapiens
brenda
Saiah, E.
The role of 11beta-hydroxysteroid dehydrogenase in metabolic disease and therapeutic potential of 11beta-HSD1 inhibitors
Curr. Med. Chem.
15
642-649
2008
Homo sapiens, Mus musculus
brenda
Swali, A.; Walker, E.A.; Lavery, G.G.; Tomlinson, J.W.; Stewart, P.M.
11beta-Hydroxysteroid dehydrogenase type 1 regulates insulin and glucagon secretion in pancreatic islets
Diabetologia
51
2003-2011
2008
Homo sapiens, Mus musculus
brenda
Mericq, V.; Medina, P.; Kakarieka, E.; Marquez, L.; Johnson, M.C.; Iniguez, G.
Differences in expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 and 2 in human placentas of term pregnancies according to birth weight and gender
Eur. J. Endocrinol.
161
419-425
2009
Homo sapiens
brenda
Yang, H.; Shen, Y.; Chen, J.; Jiang, Q.; Leng, Y.; Shen, J.
Structure-based virtual screening for identification of novel 11beta-HSD1 inhibitors
Eur. J. Med. Chem.
44
1167-1171
2009
Mus musculus, Homo sapiens (P28845)
brenda
Gumy, C.; Thurnbichler, C.; Aubry, E.M.; Balazs, Z.; Pfisterer, P.; Baumgartner, L.; Stuppner, H.; Odermatt, A.; Rollinger, J.M.
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 by plant extracts used as traditional antidiabetic medicines
Fitoterapia
80
200-205
2009
Homo sapiens
brenda
Mericq, V.; Medina, P.; Bouwman, C.; Johnson, M.C.; Godoy, J.; Lopez, T.; Iniguez, G.
Expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 enzyme in subcutaneous and visceral adipose tissue of prepubertal children
Horm. Res.
71
89-93
2009
Homo sapiens
brenda
Cooper, M.S.
11beta-Hydroxysteroid dehydrogenase: a regulator of glucocorticoid response in osteoporosis
J. Endocrinol. Invest.
31 (7 Suppl)
16-21
2008
Homo sapiens
brenda
Wan, Z.K.; Chenail, E.; Xiang, J.; Li, H.Q.; Ipek, M.; Bard, J.; Svenson, K.; Mansour, T.S.; Xu, X.; Tian, X.; Suri, V.; Hahm, S.; Xing, Y.; Johnson, C.E.; Li, X.; Qadri, A.; Panza, D.; Perreault, M.; Tobin, J.F.; Saiah, E.
Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model
J. Med. Chem.
52
5449-5461
2009
Mus musculus, Homo sapiens (P28845), Homo sapiens
brenda
Chen, B.B.; Lin, H.; Hu, G.X.; Su, Y.; Zhou, H.Y.; Lian, Q.Q.; Cai, H.; Hardy, D.O.; Gu, D.Y.; Ge, R.S.
The (+)- and (-)-gossypols potently inhibit human and rat 11beta-hydroxysteroid dehydrogenase type 2
J. Steroid Biochem. Mol. Biol.
113
177-181
2009
Homo sapiens, Rattus norvegicus
brenda
Classen-Houben, D.; Schuster, D.; Da Cunha, T.; Odermatt, A.; Wolber, G.; Jordis, U.; Kueenburg, B.
Selective inhibition of 11beta-hydroxysteroid dehydrogenase 1 by 18alpha-glycyrrhetinic acid but not 18beta-glycyrrhetinic acid
J. Steroid Biochem. Mol. Biol.
113
248-252
2009
Homo sapiens (P28845), Homo sapiens
brenda
Wang, D.Y.; Lu, Q.; Walsh, S.L.; Payne, L.; Modha, S.S.; Scott, M.J.; Sweitzer, T.D.; Ames, R.S.; Krosky, D.J.; Li, H.
Development of a high-throughput cell-based assay for 11beta-hydroxysteroid dehydrogenase type 1 using BacMam technology
Mol. Biotechnol.
39
127-134
2008
Homo sapiens, Mus musculus
brenda
Chapman, K.E.; Coutinho, A.E.; Gray, M.; Gilmour, J.S.; Savill, J.S.; Seckl, J.R.
The role and regulation of 11beta-hydroxysteroid dehydrogenase type 1 in the inflammatory response
Mol. Cell. Endocrinol.
301
123-131
2009
Homo sapiens, Mus musculus
brenda
Blum, A.; Favia, A.D.; Maser, E.
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors with oleanan and ursan scaffolds
Mol. Cell. Endocrinol.
301
132-136
2009
Homo sapiens (P28845), Homo sapiens
brenda
Dzyakanchuk, A.A.; Balazs, Z.; Nashev, L.G.; Amrein, K.E.; Odermatt, A.
11beta-Hydroxysteroid dehydrogenase 1 reductase activity is dependent on a high ratio of NADPH/NADP(+) and is stimulated by extracellular glucose
Mol. Cell. Endocrinol.
301
137-141
2009
Homo sapiens, Mus musculus
brenda
Su, X.; Vicker, N.; Trusselle, M.; Halem, H.; Culler, M.D.; Potter, B.V.
Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
301
169-173
2009
Homo sapiens
brenda
Gong, R.; Morris, D.J.; Brem, A.S.
Variable expression of 11beta Hydroxysteroid dehydrogenase (11beta-HSD) isoforms in vascular endothelial cells
Steroids
73
1187-1196
2008
Homo sapiens, Homo sapiens (P80365), Rattus norvegicus
brenda
Mondok, A.; Varga, I.; Glaz, E.; Szucs, N.; Toth, M.; Patocs, A.; Beko, G.; Racz, K.
11beta-hydroxysteroid dehydrogenase activity in acromegalic patients with normal or impaired carbohydrate metabolism
Steroids
74
725-729
2009
Homo sapiens
brenda
Skarydova, L.; Skarka, A.; Novotna, R.; Zivna, L.; Martin, H.J.; Wsol, V.; Maser, E.
Partial purification and characterization of a new human membrane-bound carbonyl reductase playing a role in the deactivation of the anticancer drug oracin
Toxicology
264
52-60
2009
Homo sapiens
brenda
Zhang, X.; Zhou, Y.; Shen, Y.; Du, L.L.; Chen, J.H.; Leng, Y.; Shen, J.H.
Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro
Acta Pharmacol. Sin.
30
1344-1350
2009
Homo sapiens (P28845), Homo sapiens, Mus musculus (P50172), Mus musculus
brenda
Sun, D.; Wang, Z.; Cardozo, M.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Jaen, J.C.; Labelle, M.; Liu, J.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)
Bioorg. Med. Chem. Lett.
19
1522-1527
2009
Homo sapiens
brenda
Siu, M.; Johnson, T.O.; Wang, Y.; Nair, S.K.; Taylor, W.D.; Cripps, S.J.; Matthews, J.J.; Edwards, M.P.; Pauly, T.A.; Ermolieff, J.; Castro, A.; Hosea, N.A.; LaPaglia, A.; Fanjul, A.N.; Vogel, J.E.
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275
Bioorg. Med. Chem. Lett.
19
3493-3497
2009
Homo sapiens
brenda
Zhang, X.; Zhou, Z.; Yang, H.; Chen, J.; Feng, Y.; Du, L.; Leng, Y.; Shen, J.
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice
Bioorg. Med. Chem. Lett.
19
4455-4458
2009
Homo sapiens, Mus musculus
brenda
Kim, S.H.; Ramu, R.; Kwon, S.W.; Lee, S.H.; Kim, C.H.; Kang, S.K.; Rhee, S.D.; Bae, M.A.; Ahn, S.H.; Ha, D.C.; Cheon, H.G.; Kim, K.Y.; Ahn, J.H.
Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors
Bioorg. Med. Chem. Lett.
20
1065-1069
2010
Homo sapiens, Mus musculus
brenda
Stanetty, C.; Czollner, L.; Koller, I.; Shah, P.; Gaware, R.; Cunha, T.D.; Odermatt, A.; Jordis, U.; Kosma, P.; Classen-Houben, D.
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11beta-hydroxysteroid dehydrogenase 2 inhibitors
Bioorg. Med. Chem.
18
7522-7541
2010
Homo sapiens (P28845)
brenda
Feng, Y.; Huang, S.L.; Dou, W.; Zhang, S.; Chen, J.H.; Shen, Y.; Shen, J.H.; Leng, Y.
Emodin, a natural product, selectively inhibits 11beta-hydroxysteroid dehydrogenase type 1 and ameliorates metabolic disorder in diet-induced obese mice
Br. J. Pharmacol.
161
113-126
2010
Mus musculus, Homo sapiens (P28845), Homo sapiens
brenda
Xu, D.; Sheng, Y.; Zhou, Z.Y.; Liu, R.; Leng, Y.; Liu, J.K.
Sesquiterpenes from cultures of the basidiomycete Clitocybe conglobata and their 11 beta-hydroxysteroid dehydrogenase inhibitory activity
Chem. Pharm. Bull.
57
433-435
2009
Homo sapiens, Mus musculus
brenda
Su, X.; Pradaux-Caggiano, F.; Thomas, M.P.; Szeto, M.W.; Halem, H.A.; Culler, M.D.; Vicker, N.; Potter, B.V.
Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors
ChemMedChem
5
1026-1044
2010
Homo sapiens (P28845), Homo sapiens
brenda
Ge, R.; Huang, Y.; Liang, G.; Li, X.
11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development
Curr. Med. Chem.
17
412-422
2010
Homo sapiens, Mus musculus
brenda
Torres-Piedra, M.; Ortiz-Andrade, R.; Villalobos-Molina, R.; Singh, N.; Medina-Franco, J.L.; Webster, S.P.; Binnie, M.; Navarrete-Vazquez, G.; Estrada-Soto, S.
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition
Eur. J. Med. Chem.
45
2606-2612
2010
Homo sapiens (P28845)
brenda
Odermatt, A.
Diazepane-acetamide derivatives as selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
Expert Opin. Ther. Pat.
19
1477-1483
2009
Homo sapiens
brenda
Zhang, L.; Shen, Y.; Zhu, H.J.; Wang, F.; Leng, Y.; Liu, J.K.
Pentanol derivatives from basidiomycete Catathelasma imperiale and their 11beta-hydroxysteroid dehydrogenases inhibitory activity
J. Antibiot.
62
239-242
2009
Homo sapiens, Mus musculus
brenda
Veniant, M.M.; Hale, C.; Hungate, R.W.; Gahm, K.; Emery, M.G.; Jona, J.; Joseph, S.; Adams, J.; Hague, A.; Moniz, G.; Zhang, J.; Bartberger, M.D.; Li, V.; Syed, R.; Jordan, S.; Komorowski, R.; Chen, M.M.; Cupples, R.; Kim, K.W.; St Jean, D.J.; Johansson, L.; Henriksson, M.A.; Williams, M.; Vallgarda, J.; Fots, F.o.t.s.c.
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221)
J. Med. Chem.
53
4481-4487
2010
Homo sapiens (P28845)
brenda
Zhang, L.; Shen, Y.; Wang, F.; Leng, Y.; Liu, J.K.
Rare merosesquiterpenoids from basidiomycete Craterellus odoratus and their inhibition of 11beta-hydroxysteroid dehydrogenases
Phytochemistry
71
100-103
2010
Homo sapiens, Mus musculus
brenda
Webster, S.P.; Binnie, M.; McConnell, K.M.; Sooy, K.; Ward, P.; Greaney, M.F.; Vinter, A.; Pallin, T.D.; Dyke, H.J.; Gill, M.I.; Warner, I.; Seckl, J.R.; Walker, B.R.
Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles
Bioorg. Med. Chem. Lett.
20
3265-3271
2010
Homo sapiens (P28845), Homo sapiens, Mus musculus (P50172), Mus musculus
brenda
Venier, O.; Pascal, C.; Braun, A.; Namane, C.; Mougenot, P.; Crespin, O.; Pacquet, F.; Mougenot, C.; Monseau, C.; Onofri, B.; Dadji-Faihun, R.; Leger, C.; Ben-Hassine, M.; Van-Pham, T.; Ragot, J.L.; Philippo, C.; Guessregen, S.; Engel, C.; Farjot, G.; Noah, L.; Maniani, K.; Nicolai, E.
Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1
Bioorg. Med. Chem. Lett.
21
2244-2251
2011
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Wang, H.; Robl, J.A.; Hamann, L.G.; Simpkins, L.; Golla, R.; Li, Y.X.; Seethala, R.; Zvyaga, T.; Gordon, D.A.; Li, J.J.
Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1)
Bioorg. Med. Chem. Lett.
21
4146-4149
2011
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Wu, S.C.; Yoon, D.; Chin, J.; van Kirk, K.; Seethala, R.; Golla, R.; He, B.; Harrity, T.; Kunselman, L.K.; Morgan, N.N.; Ponticiello, R.P.; Taylor, J.R.; Zebo, R.; Harper, T.W.; Li, W.; Wang, M.; Zhang, L.; Sleczka, B.G.; Nayeem, A.; Sheriff, S.; Camac, D.M.; Morin, P.E.; Everlof, J.G.; Li, Y.X.; Ferraro, C.A.; et al.
Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11beta-hydroxydehydrogenase 1 (11beta-HSD1)
Bioorg. Med. Chem. Lett.
21
6693-6698
2011
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Ye, X.Y.; Chen, S.Y.; Nayeem, A.; Golla, R.; Seethala, R.; Wang, M.; Harper, T.; Sleczka, B.G.; Li, Y.X.; He, B.; Kirby, M.; Gordon, D.A.; Robl, J.A.
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1)
Bioorg. Med. Chem. Lett.
21
6699-6704
2011
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Udagawa, S.; Sakami, S.; Takemura, T.; Sato, M.; Arai, T.; Nitta, A.; Aoki, T.; Kawai, K.; Iwamura, T.; Okazaki, S.; Takahashi, T.; Kaino, M.
Discovery of novel 7-membered cyclic amide derivatives that inhibit 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem. Lett.
23
1617-1621
2013
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Su, X.; Vicker, N.; Thomas, M.P.; Pradaux-Caggiano, F.; Halem, H.; Culler, M.D.; Potter, B.V.
Discovery of adamantyl heterocyclic ketones as potent 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
ChemMedChem
6
1439-1451
2011
Homo sapiens (P28845)
brenda
Xia, G.; Liu, L.; Liu, H.; Yu, J.; Xu, Z.; Chen, Q.; Ma, C.; Li, P.; Xiong, B.; Liu, X.; Shen, J.
Design and synthesis of (R)-1-arylsulfonylpiperidine-2-carboxamides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
ChemMedChem
8
577-581
2013
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Xu, Z.; Tice, C.M.; Zhao, W.; Cacatian, S.; Ye, Y.J.; Singh, S.B.; Lindblom, P.; McKeever, B.M.; Krosky, P.M.; Kruk, B.A.; Berbaum, J.; Harrison, R.K.; Johnson, J.A.; Bukhtiyarov, Y.; Panemangalore, R.; Scott, B.B.; Zhao, Y.; Bruno, J.G.; Togias, J.; Guo, J.; Guo, R.; Carroll, P.J.; McGeehan, G.M.; Zhuang, L. et al.
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
J. Med. Chem.
54
6050-6062
2011
Homo sapiens (P28845)
brenda
Kratschmar, D.V.; Vuorinen, A.; Da Cunha, T.; Wolber, G.; Classen-Houben, D.; Doblhoff, O.; Schuster, D.; Odermatt, A.
Characterization of activity and binding mode of glycyrrhetinic acid derivatives inhibiting 11beta-hydroxysteroid dehydrogenase type 2
J. Steroid Biochem. Mol. Biol.
125
129-142
2011
Homo sapiens (P28845)
brenda
Xia, G.; Liu, L.; Xue, M.; Liu, H.; Yu, J.; Li, P.; Chen, Q.; Xiong, B.; Liu, X.; Shen, J.
Discovery of novel sulfonamides as potent and selective inhibitors against human and mouse 11beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
358
46-52
2012
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Favia, A.; Masetti, M.; Recanatini, M.; Cavalli, A.
Substrate binding process and mechanistic functioning of type 1 11beta-hydroxysteroid dehydrogenase from enhanced sampling methods
PLoS ONE
6
e25375
2011
Homo sapiens (P28845)
brenda
Hu, G.; Lin, H.; Lian, Q.; Zhou, S.; Guo, J.; Zhou, H.; Chu, Y.; Ge, R.
Curcumin as a potent and selective inhibitor of 11beta-hydroxysteroid dehydrogenase 1: improving lipid profiles in high-fat-diet-treated rats
PLoS ONE
8
e49976
2013
Rattus norvegicus (P16232), Homo sapiens (P28845)
brenda
Guo, J.; Deng, H.; Li, H.; Zhu, Q.; Zhao, B.; Chen, B.; Chu, Y.; Ge, R.S.
Effects of methoxychlor and its metabolite 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane on 11beta-hydroxysteroid dehydrogenase activities in vitro
Toxicol. Lett.
218
18-23
2013
Homo sapiens (P28845), Rattus norvegicus (P16232)
brenda
Itoi, S.; Terao, M.; Murota, H.; Katayama, I.
11beta-Hydroxysteroid dehydrogenase 1 contributes to the pro-inflammatory response of keratinocytes
Biochem. Biophys. Res. Commun.
440
265-270
2013
Homo sapiens
brenda
Hofer, S.; Kratschmar, D.V.; Schernthanner, B.; Vuorinen, A.; Schuster, D.; Odermatt, A.; Easmon, J.
Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11beta-hydroxysteroid dehydrogenase 1 inhibitors
Bioorg. Med. Chem. Lett.
23
5397-5400
2013
Homo sapiens (P28845)
brenda
Lee, Y.; Shin, Y.J.; Ahn, S.K.
3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitor
Bioorg. Med. Chem. Lett.
24
1421-1425
2014
Mus musculus, Homo sapiens (P28845)
brenda
Ye, X.Y.; Yoon, D.; Chen, S.Y.; Nayeem, A.; Golla, R.; Seethala, R.; Wang, M.; Harper, T.; Sleczka, B.G.; Apedo, A.; Li, Y.X.; He, B.; Kirby, M.; Gordon, D.A.; Robl, J.A.
Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
Bioorg. Med. Chem. Lett.
24
654-660
2014
Homo sapiens (P28845)
brenda
Hong, S.P.; Nam, K.Y.; Shin, Y.J.; Kim, K.W.; Ahn, S.K.
Discovery of 11beta-hydroxysteroid dehydrogenase type 1 inhibitor
Bioorg. Med. Chem. Lett.
25
3501-3506
2015
Homo sapiens, Mus musculus
brenda
Ryu, J.H.; Kim, S.; Han, H.Y.; Son, H.J.; Lee, H.J.; Shin, Y.A.; Kim, J.S.; Park, H.G.
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
Bioorg. Med. Chem. Lett.
25
695-700
2015
Homo sapiens (P28845)
brenda
Morelli, V.; Polledri, E.; Mercadante, R.; Zhukouskaya, V.; Palmieri, S.; Beck-Peccoz, P.; Spada, A.; Fustinoni, S.; Chiodini, I.
The activity of 11beta-hydroxysteroid dehydrogenase type 2 enzyme and cortisol secretion in patients with adrenal incidentalomas
Endocrine
53
809-815
2016
Homo sapiens
brenda
Dube, S.; Norby, B.J.; Pattan, V.; Carter, R.E.; Basu, A.; Basu, R.
11beta-hydroxysteroid dehydrogenase types 1 and 2 activity in subcutaneous adipose tissue in humans: implications in obesity and diabetes
J. Clin. Endocrinol. Metab.
100
E70-E76
2015
Homo sapiens
brenda
Scott, J.S.; Goldberg, F.W.; Turnbull, A.V.
Medicinal chemistry of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
J. Med. Chem.
57
4466-4486
2014
Homo sapiens (P28845)
brenda
Vitku, J.; Starka, L.; Bicikova, M.; Hill, M.; Heracek, J.; Sosvorova, L.; Hampl, R.
Endocrine disruptors and other inhibitors of 11beta-hydroxysteroid dehydrogenase 1 and 2: Tissue-specific consequences of enzyme inhibition
J. Steroid Biochem. Mol. Biol.
155
207-216
2016
Homo sapiens
brenda
Schmidt, M.; Straub, R.H.
11beta-Hydroxysteroid dehydrogenase enzymes modulate effects of glucocorticoids in rheumatoid arthritis synovial cells
Neuroimmunomodulation
22
40-45
2015
Homo sapiens
brenda
Chen, X.; Dong, Y.; Cao, S.; Li, X.; Wang, Z.; Chen, R.; Ge, R.S.
Effects of polybrominated diphenyl ethers on rat and human 11beta-hydroxysteroid dehydrogenase 1 and 2 activities
Pharmacology
98
115-123
2016
Homo sapiens, Rattus norvegicus
brenda
Li, X.; Hu, G.; Li, X.; Wang, Y.Y.; Hu, Y.Y.; Zhou, H.; Latif, S.A.; Morris, D.J.; Chu, Y.; Zheng, Z.; Ge, R.S.
Metabolic coupling determines the activity: comparison of 11beta-hydroxysteroid dehydrogenase 1 and its coupling between liver parenchymal cells and testicular Leydig cells
PLoS ONE
10
e0141767
2015
Rattus norvegicus, Homo sapiens (P28845), Homo sapiens
brenda
Hintzpeter, J.; Stapelfeld, C.; Loerz, C.; Martin, H.J.; Maser, E.
Green tea and one of its constituents, epigallocatechine-3-gallate, are potent inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
PLoS ONE
9
e84468
2014
Homo sapiens (P28845)
brenda
Almanzar, G.; Mayerl, C.; Seitz, J.C.; Hoefner, K.; Brunner, A.; Wild, V.; Jahn, D.; Geier, A.; Fassnacht, M.; Prelog, M.
Expression of 11beta-hydroxysteroid-dehydrogenase type 2 in human thymus
Steroids
110
35-40
2016
Homo sapiens
brenda
Voisin, M.; de Medina, P.; Mallinger, A.; Dalenc, F.; Huc-Claustre, E.; et, al.
Identification of a tumor-promoter cholesterol metabolite in human breast cancers acting through the glucocorticoid receptor
Proc. Natl. Acad. Sci. USA
114
E9346-E9355
2017
Homo sapiens (P80365)
brenda
Huebner, H.; Heussner, K.; Ruebner, M.; Schmid, M.; Nadal, J.; Woelfle, J.; Hartner, A.; Menendez-Castro, C.; Rauh, M.; Beckmann, M.W.; Kehl, S.; Fahlbusch, F.B.
Influence of labor on direct and indirect determinants of placental 11beta-hydroxysteroid dehydrogenase activity
Arch. Gynecol. Obstet.
303
401-408
2021
Homo sapiens (P80365), Homo sapiens
brenda
Studzinska, R.; Kolodziejska, R.; Kupczyk, D.; Plazinski, W.; Kosmalski, T.
A novel derivatives of thiazol-4(5H)-one and their activity in the inhibition of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Chem.
79
115-121
2018
Homo sapiens (P28845)
brenda
Studzinska, R.; Kupczyk, D.; Plazinska, A.; Kolodziejska, R.; Kosmalski, T.; Modzelewska-Banachiewicz, B.
Thiazolo[3,2-a]pyrimidin-5-one derivatives as a novel class of 11beta-hydroxysteroid dehydrogenase inhibitors
Bioorg. Chem.
81
21-26
2018
Homo sapiens (P28845)
brenda
Boudon, S.; Heidl, M.; Vuorinen, A.; Wandeler, E.; Campiche, R.; Odermatt, A.; Jackson, E.
Design, synthesis, and biological evaluation of novel selective peptide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
Bioorg. Med. Chem.
26
5128-5139
2018
Homo sapiens (P28845)
brenda
Cirillo, N.; Morgan, D.J.; Pedicillo, M.C.; Celentano, A.; Lo Muzio, L.; McCullough, M.J.; Prime, S.S.
Characterisation of the cancer-associated glucocorticoid system key role of 11beta-hydroxysteroid dehydrogenase type 2
Br. J. Cancer
117
984-993
2017
Homo sapiens (P80365)
brenda
Dammann, C.; Stapelfeld, C.; Maser, E.
Expression and activity of the cortisol-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 is tissue and species-specific
Chem. Biol. Interact.
303
57-61
2019
Homo sapiens (P28845)
brenda
Koike, T.; Shiraki, R.; Sasuga, D.; Hosaka, M.; Kawano, T.; Fukudome, H.; Kurosawa, K.; Moritomo, A.; Mimasu, S.; Ishii, H.; Yoshimura, S.
Discovery and biological evaluation of potent and orally active human 11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes mellitus
Chem. Pharm. Bull.
67
824-838
2019
Homo sapiens (P28845)
brenda
Han, J.; Sun, W.; Gao, F.
Role of 11beta-hydroxysteroid dehydrogenase in bone metabolism
Chinese J. Tissue Eng. Res.
21
5203-5208
2017
Homo sapiens
-
brenda
Hussey, M.; Holleran, G.; Smith, S.; Sherlock, M.; McNamara, D.
The role and regulation of the 11 beta-hydroxysteroid dehydrogenase enzyme system in patients with inflammatory bowel disease
Digest. Dis. Sci.
62
3385-3390
2017
Homo sapiens (P28845), Homo sapiens (P80365)
brenda
Zhou, C.; Ye, F.; Wu, H.; Ye, H.; Chen, Q.
Recent advances in the study of 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) inhibitors
Environ. Toxicol. Pharmacol.
52
47-53
2017
Rattus norvegicus (A0A1B0GWP2), Homo sapiens (P80365)
brenda
Ganjoo, A.; Tripathi, A.; Chetti, P.
Structural assessment and identification of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
J. Biomol. Struct. Dyn.
38
4928-4937
2020
Homo sapiens (P28845)
brenda
Beck, K.R.; Inderbinen, S.G.; Kanagaratnam, S.; Kratschmar, D.V.; Jetten, A.M.; Yamaguchi, H.; Odermatt, A.
11beta-Hydroxysteroid dehydrogenases control access of 7beta,27-dihydroxycholesterol to retinoid-related orphan receptor gamma
J. Lipid Res.
60
1535-1546
2019
Homo sapiens (P28845), Homo sapiens (R4GN04)
brenda
Loerz, C.; Maser, E.
The cortisol-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 in skeletal muscle in the pathogenesis of the metabolic syndrome
J. Steroid Biochem. Mol. Biol.
174
65-71
2017
Homo sapiens (P28845)
brenda
Gent, R.; du Toit, T.; Bloem, L.M.; Swart, A.C.
The 11beta-hydroxysteroid dehydrogenase isoforms pivotal catalytic activities yield potent C11-oxy C19 steroids with 11betaHSD2 favouring 11-ketotestosterone, 11-ketoandrostenedione and 11-ketoprogesterone biosynthesis
J. Steroid Biochem. Mol. Biol.
189
116-126
2019
Homo sapiens (P80365)
brenda
Beck, K.R.; Kanagaratnam, S.; Kratschmar, D.V.; Birk, J.; Yamaguchi, H.; Sailer, A.W.; Seuwen, K.; Odermatt, A.
Enzymatic interconversion of the oxysterols 7beta,25-dihydroxycholesterol and 7-keto,25-hydroxycholesterol by 11beta-hydroxysteroid dehydrogenase type 1 and 2
J. Steroid Biochem. Mol. Biol.
190
19-28
2019
Homo sapiens (P28845), Homo sapiens (P80365), Mus musculus (P50172), Mus musculus (P51661)
brenda
Lee, N.R.; Kim, B.J.; Lee, C.H.; Lee, Y.B.; Lee, S.; Hwang, H.J.; Kim, E.; Kim, S.H.; Lee, M.G.; Lee, S.E.; Lavery, G.G.; Choi, E.H.
Role of 11beta-hydroxysteroid dehydrogenase type 1 in the development of atopic dermatitis
Sci. Rep.
10
20237
2020
Homo sapiens (P28845), Mus musculus (P50172)
brenda
Inderbinen, S.G.; Zogg, M.; Kley, M.; Smiesko, M.; Odermatt, A.
Species-specific differences in the inhibition of 11beta-hydroxysteroid dehydrogenase 2 by itraconazole and posaconazole
Toxicol. Appl. Pharmacol.
412
115387
2021
Rattus norvegicus (P50233), Mus musculus (P51661), Homo sapiens (P80365), Danio rerio (Q6P0H9)
brenda