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(1'-[(adamantan-2-yl)carbamoyl]-7-bromo-2,3-dihydrospiro[indene-1,4'-piperidin]-3-yl)acetic acid
selective isoform 11beta-HSD1 inhibitor
(2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
treatment of BALB/c mice 15, and 60 m per kg dose-dependently decreases the formation of prednisolone, with respective inhibition ratios of 72 and 88%. The concentration of inhibitor in subcutaneous and celiac adipose as well as liver tissue remains high within 1 h after i.v. treatment, whereas the concentration in plasma dramatically decreases 15 min after administration. The inhibitor is also eliminated moderately in adipose and liver tissue over the subsequent 5 h
(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
-
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
71% and 62% inhibition of enzyme in adipose and liver tissue at 1 h after administration, short-acting compound displaying a significant drop in potency in the subsequent 3 h
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-[(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
-
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-((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-(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-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 118 nM, 11betaHSD1
3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 104 nM, 11betaHSD1
3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 50 nM, 11betaHSD1
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-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 292 nM, 11betaHSD1
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-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 417 nM, 11betaHSD1
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-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 1674 nM, 11betaHSD1
3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 365 nM, 11betaHSD1
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-(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-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
isozyme 11beta-HSD1 IC50: 98 nM, isozyme 11beta-HSD2 IC50: above 0.01 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-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 35 nM, 11betaHSD1
3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
IC50: 9.2 nM, 11betaHSD1
3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
IC50: 4.6 nM, 11betaHSD1
3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
IC50: 16 nM, 11betaHSD1
3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
IC50: 1112 nM, 11betaHSD1
3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine
IC50: 2.2 nM, 11betaHSD1
3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
IC50: 8 nM, 11betaHSD1
3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 98 nM, 11betaHSD1
3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
IC50: 6820 nM, 11betaHSD1
3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
IC50: 587 nM, 11betaHSD1
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-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one
displays good levels of inhibition in liver, subcutaneous adipose tissue and brain following an oral dose
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
high metabolic lability
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-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
IC50: 14 nM, 11betaHSD1
5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
IC50: 91 nM, 11betaHSD1
5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
IC50: 23 nM, 11betaHSD1
5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
IC50: 270 nM, 11betaHSD1
5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
IC50: 109 nM, 11betaHSD1
5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
IC50: 50 nM, 11betaHSD1
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
-
7-keto,25-hydroxycholesterol
-
7beta,25-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
compound is orally active and shows the same tendency as pioglitazone in diet-induced obesity mice
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
compound is orally active and shows the same tendency as pioglitazone in diet-induced obesity mice
8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile
-
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
-
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-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
-
[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, significant inhibition of isoform 11beta-HSD1 in both the liver and fat tissue of mice, 2 h after oral administration at 30 mg/kg
[5-fluoro-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
-
(1r,4s)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
(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
-
-
(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
-
-
(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-(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
-
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(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
-
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(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-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide
-
-
(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
-
-
(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
-
-
(3S)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
-
-
(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
-
-
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-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-[(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-[1-[(3,4-dimethylphenyl)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
-
-
17beta-estradiol
-
non-competitive
17beta-estradiol-3-acetate
-
-
18beta-glycyrrhetinic acid
-
11beta-HSD1 inhibitor with submicromolar potency
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
-
-
2,6-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-[[(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-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-(cycloheptylamino)-5-methyl-5-(1-methylethyl)-1,3-thiazol-4(5H)-one
-
-
2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
-
-
2-oxopentane-1,5-diyl diacetate
-
-
2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide
-
-
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
-
-
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-(1-fluoronaphthalen-2-yl)-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)-5-(2-fluorophenyl)-4-methyl-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-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 10000 nM, 11betaHSD2
3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
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-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
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)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)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-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
IC50: above 4000 nM, 11betaHSD2
3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
IC50: about 4000 nM, 11betaHSD2
3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
IC50: about 10000 nM, 11betaHSD2
3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
IC50: above 10000 nM, 11betaHSD2
3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine
IC50: 11650 nM, 11betaHSD2
3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
IC50: 4563 nM, 11betaHSD2
3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: above 4000 nM, 11betaHSD2
3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
IC50: 10000 nM, 11betaHSD2
3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
IC50: above 4000 nM, 11betaHSD2
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-[4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1,3-thiazol-2-yl]benzenesulfonamide
-
-
3-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
-
-
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-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-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-[(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-[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-[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
-
-
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-[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-butoxy-3-methylbenzyl)-3-hydroxy-5-(4-methylphenyl)-1-(pyridin-3-ylmethyl)-1,5-dihydro-2H-pyrrol-2-one
-
-
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-([(3S)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
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-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-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
-
-
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-[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-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
-
-
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-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
IC50: 50 nM, 11betaHSD2
5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
IC50: above 4000 nM, 11betaHSD2
5-hydroxy-4-oxopentyl acetate
-
-
5-methyl-4-[(1E)-3-[(3-methylphenoxy)acetyl]triaz-1-en-1-yl]benzene-1,3-diol
-
-
5-methyl-5-(1-methylethyl)-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1,3-thiazol-4(5H)-one
-
-
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-keto,25-hydroxycholesterol
-
7beta,25-dihydroxycholesterol
-
7beta-hydroxycholesterol
-
-
8-benzyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1-thia-3,8-diazaspiro[4.5]dec-2-en-4-one
-
-
antisense oligonucleotide
-
in mice treated with 11beta-hydroxysteroid dehydrogenase type 1-antisense oligonucleotide, plasma blood glucose levels are significantly reduced by up to 54% upon induction of diabetes. Cortisol and other diabetes end products are also reduced, and hepatic 11beta-hydroxysteroid dehydrogenase type 1 mRNA is suppressed by up to 84%
-
arylsulfoamidothiazoles
-
intermediate binding inhibitors, inhibition mode and profiles
-
bezafibrate
-
23% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
BVT-2733
-
mixed-type inhibition pattern
Clofibrate
-
18% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
dexamethasone
-
dexmethasone inhibits 11beta-HSD1 activity and expression in a time- and concentration-dependent manner, the effect of dexamethasone is mimicked by both cortisol and corticosterone but blocked by the glucocorticoid receptor antagonist RU486
ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate
-
-
fenofibrate
-
82% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid
-
25% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid cyclohexyl ester
-
54% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid ethylester
-
85% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid isobutylester
-
75% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid isopropyl amide
-
54% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid n-butylester
-
64% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
gemfibrozil
-
19% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2
-
-
-
itraconazole
95% residual activity at 0.03 mM
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-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
-
-
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'-[(E)-(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-(4-biphenyl-4-yl-1,3-oxazol-2-yl)benzenesulfonamide
-
-
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-butyl-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
-
-
N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine
-
-
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-[3-hydroxy-4-(piperidin-1-ylcarbonyl)phenyl]-3,4,5-trimethoxybenzamide
-
-
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
-
-
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
-
-
PF-877423
-
specific 11beta-HSD1 inhibitor
UE2316
-
selective isoform 11beta-HSD1 inhibitor
WY-14643
-
22% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
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
carbenoxolone
-
-
carbenoxolone
-
unspecific inhibitor
additional information
-
structure-activity analysis for inhibitor design
-
additional information
-
11beta-HSD1 mRNA decreases 4fold on day 3 after injection of trehalose-6,6'-dimycolate
-
additional information
isoform 11beta-HSD2 is not inhibited by 7alpha,25-dihydroxycholesterol
-
additional information
isoform 11beta-HSD2 is not inhibited by 7alpha,25-dihydroxycholesterol
-
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0.000015
(2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000013
(2R)-N-(tricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000032
(2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000024
(2R)-N-[(1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000021
1-[(2-chlorobenzyl)oxy]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
Mus musculus
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
Mus musculus
22°C, pH not specified in the publication, assay on microsomes
0.000007
1-[(2-chlorobenzyl)sulfanyl]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
Mus musculus
22°C, pH not specified in the publication, assay on microsomes
0.000123
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
Mus musculus
pH 7.4, 37°C
0.000018
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
Mus musculus
pH 7.4, 37°C
0.00049
2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000058
2-[(2-chlorobenzyl)sulfanyl]-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
Mus musculus
22°C, pH not specified in the publication, assay on microsomes
0.000307
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
Mus musculus
pH 7.4, 37°C
0.000279
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
Mus musculus
pH 7.4, 37°C
0.001055
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
Mus musculus
pH 7.4, 37°C
0.000055
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000118
3-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 118 nM, 11betaHSD1
0.000104
3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 104 nM, 11betaHSD1
0.00005
3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 50 nM, 11betaHSD1
0.000292
3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 292 nM, 11betaHSD1
0.000417
3-(3-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 417 nM, 11betaHSD1
0.001674
3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 1674 nM, 11betaHSD1
0.000365
3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 365 nM, 11betaHSD1
0.000035
3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 35 nM, 11betaHSD1
0.0000092
3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
Mus musculus
IC50: 9.2 nM, 11betaHSD1
0.0000046
3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
Mus musculus
IC50: 4.6 nM, 11betaHSD1
0.000016
3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
IC50: 16 nM, 11betaHSD1
0.001112
3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
Mus musculus
IC50: 1112 nM, 11betaHSD1
0.0000022
3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine
Mus musculus
IC50: 2.2 nM, 11betaHSD1
0.000008
3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
Mus musculus
IC50: 8 nM, 11betaHSD1
0.000098
3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: 98 nM, 11betaHSD1
0.00682
3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
Mus musculus
IC50: 6820 nM, 11betaHSD1
0.000587
3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
IC50: 587 nM, 11betaHSD1
0.000075
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.00103
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000014
5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
Mus musculus
IC50: 14 nM, 11betaHSD1
0.000091
5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
Mus musculus
IC50: 91 nM, 11betaHSD1
0.000023
5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
Mus musculus
IC50: 23 nM, 11betaHSD1
0.00027
5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
Mus musculus
IC50: 270 nM, 11betaHSD1
0.000109
5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
Mus musculus
IC50: 109 nM, 11betaHSD1
0.00005
5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
Mus musculus
IC50: 50 nM, 11betaHSD1
0.000045
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
Mus musculus
pH 7.4, 37°C
0.00008
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
Mus musculus
pH 7.4, 37°C
0.000849
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
Mus musculus
pH 7.4, 37°C
0.000053
7-keto,25-hydroxycholesterol
Mus musculus
recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C
0.000119
7beta,25-dihydroxycholesterol
Mus musculus
recombinant isoform 11beta-HSD1, at pH 7.4 and 37°C
0.000035
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
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.0000098
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
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000105
8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile
Mus musculus
22°C, pH not specified in the publication, assay on microsomes
0.00021
N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
Mus musculus
pH 7.4, 37°C
0.000024
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
Mus musculus
pH 7.4, 37°C
0.00012
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000049
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.001616
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000184
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
Mus musculus
pH not specified in the publication, temperature not specified in the publication
0.000021
(1S,3R,4S,5S,7S)-4-(3-(2-fluorophenylsulfonamido)-3-methylbutanamido) adamantane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000009
(1s,4r)-4-[3-[(2,3-dichlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000009
(1s,4r)-4-[3-[(2,3-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000022
(1s,4r)-4-[3-[(2,4-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000016 - 0.000196
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
0.000021
(1s,4r)-4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000099
(1s,4r)-4-[3-[(3,5-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.00001
(1s,4r)-4-[3-[(3-chloro-2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000012
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.001
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000046
(1s,4r)-4-[3-[(3-chlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000028
(1s,4r)-4-[3-[(3-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000024
(1s,4r)-4-[3-[(4-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.00001
(2R)-1-(2-chloro-4-(2-methoxyethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Mus musculus
-
at 37°C
0.00001
(2R)-1-(2-chloro-4-(difluoromethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Mus musculus
-
at 37°C
0.000012
(2R)-1-(2-chloro-4-ethoxyphenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Mus musculus
-
at 37°C
0.00001
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxamide
Mus musculus
-
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
Mus musculus
-
at 37°C
0.00001
(2R)-1-(4-bromo-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Mus musculus
-
at 37°C
0.000013
(2R)-1-(4-tert-butoxy-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Mus musculus
-
at 37°C
0.00001
(2R)-1-([2-chloro-4-[(3S)-3-methylpiperazin-1-yl]phenyl]sulfonyl)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Mus musculus
-
at 37°C
0.000012
(2R)-1-[(2-chloro-4-pyrrolidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Mus musculus
-
at 37°C
0.00001
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-N,N-dimethylpiperidin-4-amine
Mus musculus
-
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
Mus musculus
-
at 37°C
0.000017
(2R)-1-[[2-chloro-4-(4,4-difluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Mus musculus
-
at 37°C
0.000015
(2R)-1-[[2-chloro-4-(4-fluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Mus musculus
-
at 37°C
0.000128
(2R)-1-[[2-chloro-4-(4-methylpiperazin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Mus musculus
-
at 37°C
0.00001
(2R)-2-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenoxy)-N,N-dimethylethanamine
Mus musculus
-
at 37°C
0.00001
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)-N,N-dimethylaniline
Mus musculus
-
at 37°C
0.00001
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
Mus musculus
-
at 37°C
0.000012
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenol
Mus musculus
-
at 37°C
0.00001
(2R)-3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)benzamide
Mus musculus
-
at 37°C
0.00001
(2R)-4-(3-fluoro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)morpholine
Mus musculus
-
at 37°C
0.00001
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzamide
Mus musculus
-
at 37°C
0.000636
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
Mus musculus
-
at 37°C
0.000016
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methyl-1-(4-(trifluoromethoxy)-phenylsulfonyl)-piperazine
Mus musculus
-
at 37°C
0.000088
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine
Mus musculus
-
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
Mus musculus
-
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
Mus musculus
-
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
Mus musculus
-
at 37°C
0.002337
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine
Mus musculus
-
at 37°C
0.000071
(2R)-N-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide
Mus musculus
-
at 37°C
0.001
(4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decan-1-yl)acetic acid
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000057
1-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)-2-methyl-1H-benzimidazole
Mus musculus
-
-
0.000091
1-methyl-4-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
Mus musculus
-
-
0.0000013
1-methyl-4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]-1H-indole
Mus musculus
-
-
0.000346
1-methyl-5-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
Mus musculus
-
-
0.0078
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000014
2-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Mus musculus
-
-
0.005843
2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000094
2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide
Mus musculus
-
pH and temperature not specified in the publication
0.000017
2-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Mus musculus
-
-
0.000089
3,5-bis(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000022
3,5-bis(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000028
3-(1-fluoronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000001
3-(1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
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
0.00026
3-(2,3-difluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.00014
3-(2,4-dichlorophenyl)-4-methyl-5-(2-nitrophenyl)-4H-1,2,4-triazole
Mus musculus
-
-
0.00085
3-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00018
3-(2,4-dichlorophenyl)-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000012
3-(2-bromophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000008
3-(2-bromophenyl)-5-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000042
3-(2-chloro-4-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000071
3-(2-chloro-4-fluorophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00001
3-(2-chlorophenyl)-4-methyl-5-(4-pentylphenyl)-4H-1,2,4-triazole
Mus musculus
-
-
0.00019
3-(2-chlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000086
3-(2-chlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.00041
3-(2-chlorophenyl)-5-(3,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000035
3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00014
3-(2-chlorophenyl)-5-[2-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.004
3-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.0013
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.01
3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 10000 nM, 11betaHSD2
0.004
3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.0000013
3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Mus musculus
-
-
0.0000014
3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000098
3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000034
3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.004
3-(3-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.000018
3-(4-benzylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000001
3-(4-butyl-2-methylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
IC50 below 0.000001 mM
0.000068
3-(4-butylphenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000023
3-(4-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0001
3-(4-chloro-2-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.00002
3-(4-chloro-3-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0015
3-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000043
3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000018
3-(4-tert-butylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000001
3-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
IC50 below 0.000001 mM
0.004
3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
Mus musculus
IC50: about 4000 nM, 11betaHSD2
0.01
3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
IC50: about 10000 nM, 11betaHSD2
0.01
3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
Mus musculus
IC50: above 10000 nM, 11betaHSD2
0.01165
3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine
Mus musculus
IC50: 11650 nM, 11betaHSD2
0.004563
3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
Mus musculus
IC50: 4563 nM, 11betaHSD2
0.004
3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.01
3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
Mus musculus
IC50: 10000 nM, 11betaHSD2
0.004
3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.000056
3-biphenyl-3-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000004
3-biphenyl-4-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.001024
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-4-fluorobenzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000576
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.003379
3-chloro-N-[4-(morpholin-4-ylcarbonyl)benzyl]benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000131
3-chloro-N-[4-(piperidin-1-ylcarbonyl)benzyl]benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.00048
3-chloro-N-[4-(pyrrolidin-1-ylcarbonyl)benzyl]benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.001319
3-chloro-N-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0004
3-methylchrysazin
Mus musculus
-
pH 7.4, 37°C
0.000098
3-tricyclo[3.3.1.13,7]dec-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Mus musculus
-
-
0.00064
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-1-yl)butanamide
Mus musculus
-
pH and temperature not specified in the publication
0.00013
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Mus musculus
-
pH and temperature not specified in the publication
0.001
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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.00007
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
Mus musculus
-
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
0.000021
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
Mus musculus
-
-
0.0000037
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(4-phenoxyphenyl)-4H-1,2,4-triazole
Mus musculus
-
-
0.000052
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-phenyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000041
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000004
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000036
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[3-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0000031
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1,3-thiazol-2-yl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0000054
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1H-pyrrol-1-yl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0000069
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000026
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000001 - 0.000014
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000013
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000021
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000078
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000042
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluoro-4-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000163
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000091
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4'-fluorobiphenyl-4-yl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000101
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000082
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-iodophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00000096
3-[1-(4-chlorophenyl)cyclobutyl]-5-[2-chloro-4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000046
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(cyclopropyloxy)phenyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
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
0.000005 - 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
0.000022
3-[2,3-bis(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0000028
3-[2-chloro-4-(1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000072
3-[2-chloro-4-(2,4-dimethyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000006
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
Mus musculus
-
-
0.0000096
3-[2-chloro-4-(2-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
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
Mus musculus
-
-
0.0000094
3-[2-chloro-4-[2-(methylsulfonyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000084
3-[2-chloro-4-[3-(ethylsulfonyl)propyl]phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0000047
3-[3-chloro-2'-(ethylsulfanyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000012
3-[3-chloro-2'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00000098
3-[3-chloro-3'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00000098
3-[3-chloro-3'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.00000098
3-[3-chloro-4'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000012
3-[3-chloro-4'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000071
3-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000011
3-[4-chloro-2-(trifluoromethyl)phenyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000064
3-[4-[2-(ethylsulfonyl)ethyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000011
3-[4-[3-(ethylsulfonyl)propyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000019
3-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Mus musculus
-
-
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
0.000193
4-(2-[1-[(2-fluorobenzene-1-sulfonyl)amino]cyclopropyl]-2-methylpropanamido)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000002
4-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Mus musculus
-
-
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
Mus musculus
-
IC50 above 0.001 mM, pH and 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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000395
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N,N-diethylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.00001
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)benzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000002
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-methylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000002
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-propylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000015
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000302
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclohexylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000732
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclopentylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.001404
4-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000046
4-methyl-3-(2-methylnaphthalen-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000054
4-methyl-3-(4-pentylphenyl)-5-phenyl-4H-1,2,4-triazole
Mus musculus
-
-
0.0000029
4-methyl-3-(4-pentylphenyl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.00001
4-methyl-3-(7-methylnaphthalen-2-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000015
4-methyl-3-naphthalen-2-yl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.000098
4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.000109
4-methyl-3-phenyl-5-tricyclo[3.3.1.13,7]dec-1-yl-4H-1,2,4-triazole
Mus musculus
-
-
0.00012
4-methyl-3-phenyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.0000045
4-methyl-3-[2-(trifluoromethoxy)phenyl]-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Mus musculus
-
-
0.009
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.00013
4-[(N-[4-[(dimethylamino)methoxy]benzene-1-sulfonyl]-2-methylalanyl)amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000013
4-[2-(1-[[(2-fluorobenzene-1-sulfonyl)amino]methyl]cyclopropyl)-2-methylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000069
4-[4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
Mus musculus
-
at 37°C
0.0000066
4-[4-methyl-5-(1-methyl-1H-indol-4-yl)-4H-1,2,4-triazol-3-yl]phenol
Mus musculus
-
-
0.000204
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2,3,3-tetramethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000012
4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indole
Mus musculus
-
-
0.000061
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]-2-fluorophenol
Mus musculus
-
-
0.000019
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Mus musculus
-
-
0.000207
4-[[2-methyl-N-(2,4,5-trifluorobenzene-1-sulfonyl)alanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000172
4-[[N-(2,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000012
4-[[N-(2,6-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.00001
4-[[N-(2-chloro-4-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000026
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000008
4-[[N-(3,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000018
4-[[N-(3,5-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000013
4-[[N-(3-chloro-2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000012
4-[[N-(3-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.00013
4-[[N-(4-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000084
4-[[N-(4-hydroxybenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000056
4-[[N-(4-tert-butylbenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000028
4-[[N-(benzenesulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.004
5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.00005
5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
Mus musculus
IC50: 50 nM, 11betaHSD2
0.004
5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.004
5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
Mus musculus
IC50: above 4000 nM, 11betaHSD2
0.000019
7-chloro-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-ol
Mus musculus
-
-
0.002
7-keto,25-hydroxycholesterol
Mus musculus
IC50 of more than 0.002 mM, recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C
0.0194
7-oxo-cholesterol
Mus musculus
-
recombinant enzyme, at pH 7.4 and 37°C
0.003
7beta,25-dihydroxycholesterol
Mus musculus
recombinant isoform 11beta-HSD2, at pH 7.4 and 37°C
0.0022
7beta-hydroxycholesterol
Mus musculus
-
recombinant enzyme, at pH 7.4 and 37°C
0.000098
Aloe-emodin
Mus musculus
-
pH 7.4, 37°C
0.00047
AMG-221
Mus musculus
-
pH and temperature not specified in the publication
0.000281
carbenoxolone
Mus musculus
-
cell-based assay, pH not specified in the publication, temperature not specified in the publication
0.000086
emodin
Mus musculus
-
pH 7.4, 37°C
0.000008
glycyrrhizic acid
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000295
glycyrrhizinic acid
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000295
glycyrrhizininc acid
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0119
hydroxyitraconazole
Mus musculus
at pH 7.4 and 37°C
0.0015
methyl 2-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Mus musculus
-
-
0.0000019
methyl 2-[5-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Mus musculus
-
-
0.003
methyl 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Mus musculus
-
-
0.005614
N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-3-(trifluoromethyl)benzenesulfonamide
Mus musculus
-
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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000002
N-butyl-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
Mus musculus
-
pH not specified in the publication, temperature not specified in the publication
0.0000023
N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine
Mus musculus
-
-
0.000301
N-[5-(2-amino-2-oxoethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Mus musculus
-
pH and temperature not specified in the publication
0.000543
N-[5-(3-amino-3-oxopropyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Mus musculus
-
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
Mus musculus
-
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
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000021
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydroxymethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Mus musculus
-
pH and temperature not specified in the publication
0.001
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-[(2-hydroxyhydrazinyl)methyl]tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Mus musculus
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.008212
posaconazole
Mus musculus
at pH 7.4 and 37°C
0.00284
Rhein
Mus musculus
-
pH 7.4, 37°C
0.000081
rheochrysidin
Mus musculus
-
pH 7.4, 37°C
additional information
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
0.000016
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000028
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000196
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Mus musculus
-
pH and temperature not specified in the publication
0.000001
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000008
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000008
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
pH and temperature not specified in the publication
0.000013
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.0001
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000012
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000008
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000172
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000199
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000001
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000016
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000016
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
pH and temperature not specified in the publication
0.000001
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000027
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000027
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
pH and temperature not specified in the publication
0.000001
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000078
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000078
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
pH and temperature not specified in the publication
0.000002
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000019
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000052
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.00001
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000057
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000035
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000107
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000001
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.0000135
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.0000135
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
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
Mus musculus
-
-
0.000014
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
pH and temperature not specified in the publication
0.000032
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000454
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000041
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.00023
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000003
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000037
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000027
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000494
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000008
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000018
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000019
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000015
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000374
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000025
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000001
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000332
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000332
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
pH and temperature not specified in the publication
0.000043
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
Mus musculus
-
-
0.000061
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
Mus musculus
-
-
0.000005
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000355
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000002
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000115
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
Mus musculus
-
-
0.000005
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000016
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000022
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Mus musculus
-
-
0.000038
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Mus musculus
-
-
additional information
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
Mus musculus
27.68% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
Mus musculus
-
27.68% 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
Mus musculus
21.8% 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
Mus musculus
-
21.8% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Mus musculus
31.44% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Mus musculus
-
31.44% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Mus musculus
8.49% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide
Mus musculus
-
8.49% 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
Mus musculus
40.43% 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
Mus musculus
-
40.43% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Mus musculus
40.43% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Mus musculus
-
40.43% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Mus musculus
8.42% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide
Mus musculus
-
8.42% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
Mus musculus
28.0% inhibition at 0.001 mM, pH 7.4, 37°C
additional information
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
Mus musculus
-
28.0% inhibition at 0.001 mM, pH 7.4, 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
Mus musculus
-
IC50 = 0.0933 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
Mus musculus
-
IC50 = 0.0548 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
Mus musculus
-
IC50 = 0.0363 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
Mus musculus
-
IC50 = 0.0197 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
Mus musculus
-
IC50 = 0.0241 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
Mus musculus
-
IC50 = 0.0194 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
Mus musculus
-
IC50 = 0.0107 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide
Mus musculus
-
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication
additional information
2-oxopentane-1,5-diyl diacetate
Mus musculus
-
IC50 = 0.0304 mg/ml, pH not specified in the publication, temperature not specified in the publication
additional information
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
Mus musculus
-
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication
additional information
5-hydroxy-4-oxopentyl acetate
Mus musculus
-
IC50 = 0.1492 mg/ml, 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
Mus musculus
-
IC50 value between 0.00044 to 0.00848 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
Mus musculus
-
IC50 value between 0.00044 to 0.00848 mM, pH not specified in the publication, temperature not specified in the publication
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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
Holmes, M.C.; Yau, J.L.W.; Kotelevtsev, Y.; Mullins, J.J.; Seckl, J.R.
11beta-Hydroxysteroid dehydrogenases in the brain: two enzymes two roles
Ann. N. Y. Acad. Sci.
1007
357-366
2003
Mus musculus
brenda
Wsol, V.; Szotakova, B.; Skalova, L.; Maser, E.
Stereochemical aspects of carbonyl reduction of the original anticancer drug oracin by mouse liver microsomes and purified 11beta-hydroxysteroid dehydrogenase type 1
Chem. Biol. Interact.
143-144
459-468
2003
Mus musculus
brenda
Zhang, J.; Osslund, T.D.; Plant, M.H.; Clogston, C.L.; Nybo, R.E.; Xiong, F.; Delaney, J.M.; Jordan, S.R.
Crystal structure of murine 11 beta-hydroxysteroid dehydrogenase 1: an important therapeutic target for diabetes
Biochemistry
44
6948-6957
2005
Mus musculus (P50172), Mus musculus
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
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
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
Arai, N.; Masuzaki, H.; Tanaka, T.; Ishii, T.; Yasue, S.; Kobayashi, N.; Tomita, T.; Noguchi, M.; Kusakabe, T.; Fujikura, J.; Ebihara, K.; Hirata, M.; Hosoda, K.; Hayashi, T.; Sawai, H.; Minokoshi, Y.; Nakao, K.
Ceramide and adenosine 5-monophosphate-activated protein kinase are two novel regulators of 11beta-hydroxysteroid dehydrogenase type 1 expression and activity in cultured preadipocytes
Endocrinology
148
5268-5277
2007
Mus musculus
brenda
De Sousa Peixoto, R.A.; Turban, S.; Battle, J.H.; Chapman, K.E.; Seckl, J.R.; Morton, N.M.
Preadipocyte 11beta-hydroxysteroid dehydrogenase type 1 is a keto-reductase and contributes to diet-induced visceral obesity in vivo
Endocrinology
149
1861-1868
2008
Mus musculus
brenda
Bhat, B.G.; Younis, H.; Herrera, J.; Palacio, K.; Pascual, B.; Hur, G.; Jessen, B.; Ogilvie, K.M.; Rejto, P.A.
Antisense inhibition of 11betahydroxysteroid dehydrogenase type 1 improves diabetes in a novel cortisone-induced diabetic KK mouse model
Biochem. Biophys. Res. Commun.
365
740-745
2008
Mus musculus
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
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
Kim, J.; Temple, K.A.; Jones, S.A.; Meredith, K.N.; Basko, J.L.; Brady, M.J.
Differential modulation of 3T3-L1 adipogenesis mediated by 11beta-hydroxysteroid dehydrogenase-1 levels
J. Biol. Chem.
282
11038-11046
2007
Mus musculus
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
Hong, D.; Li, X.W.; Lian, Q.Q.; Lamba, P.; Bernard, D.J.; Hardy, D.O.; Chen, H.X.; Ge, R.S.
Mono-(2-ethylhexyl) phthalate (MEHP) regulates glucocorticoid metabolism through 11beta-hydroxysteroid dehydrogenase 2 in murine gonadotrope cells
Biochem. Biophys. Res. Commun.
389
305-309
2009
Mus musculus
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
Balachandran, A.; Guan, H.; Sellan, M.; van Uum, S.; Yang, K.
Insulin and dexamethasone dynamically regulate adipocyte 11beta-hydroxysteroid dehydrogenase type 1
Endocrinology
149
4069-4079
2008
Mus musculus, Rattus norvegicus
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
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
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
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
Abbott, A.N.; Guidry, T.V.; Welsh, K.J.; Thomas, A.M.; Kling, M.A.; Hunter, R.L.; Actor, J.K.
11beta-hydroxysteroid dehydrogenases are regulated during the pulmonary granulomatous response to the mycobacterial glycolipid trehalose-6,6-dimycolate
Neuroimmunomodulation
16
147-154
2009
Mus musculus
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
Cho, Y.S.; Kim, C.H.; Cheon, H.G.
Cell-based assay for screening 11beta-hydroxysteroid dehydrogenase 1 inhibitors
Anal. Biochem.
392
110-116
2009
Mus musculus
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
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
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
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
Tagawa, N.; Yuda, R.; Kubota, S.; Wakabayashi, M.; Yamaguchi, Y.; Kiyonaga, D.; Mori, N.; Minamitani, E.; Masuzaki, H.; Kobayashi, Y.
17Beta-estradiol inhibits 11beta-hydroxysteroid dehydrogenase type 1 activity in rodent adipocytes
J. Endocrinol.
202
131-139
2009
Mus musculus, Rattus norvegicus
brenda
Kim, C.H.; Ramu, R.; Ahn, J.H.; Bae, M.A.; Cho, Y.S.
Fenofibrate but not fenofibric acid inhibits 11beta-hydroxysteroid dehydrogenase 1 in C2C12 myotubes
Mol. Cell. Biochem.
344
91-98
2010
Mus musculus
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
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
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
Mitic, T.; Shave, S.; Semjonous, N.; McNae, I.; Cobice, D.F.; Lavery, G.G.; Webster, S.P.; Hadoke, P.W.; Walker, B.R.; Andrew, R.
11beta-Hydroxysteroid dehydrogenase type 1 contributes to the balance between 7-keto- and 7-hydroxy-oxysterols in vivo
Biochem. Pharmacol.
86
146-153
2013
Mus musculus
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
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
Coutinho, A.E.; Kipari, T.M.; Zhang, Z.; Esteves, C.L.; Lucas, C.D.; Gilmour, J.S.; Webster, S.P.; Walker, B.R.; Hughes, J.; Savill, J.S.; Seckl, J.R.; Rossi, A.G.; Chapman, K.E.
11beta-Hydroxysteroid dehydrogenase type 1 is expressed in neutrophils and restrains an inflammatory response in male mice
Endocrinology
157
2928-2936
2016
Mus musculus
brenda
Odermatt, A.; Klusonova, P.
11beta-Hydroxysteroid dehydrogenase 1: Regeneration of active glucocorticoids is only part of the story
J. Steroid Biochem. Mol. Biol.
151
85-92
2015
Mus musculus
brenda
Penno, C.A.; Morgan, S.A.; Rose, A.J.; Herzig, S.; Lavery, G.G.; Odermatt, A.
11beta-Hydroxysteroid dehydrogenase-1 is involved in bile acid homeostasis by modulating fatty acid transport protein-5 in the liver of mice
Mol. Metab.
3
554-564
2014
Mus musculus
brenda
Hardy, R.S.; Fenton, C.; Croft, A.P.; Naylor, A.J.; Begum, R.; Desanti, G.; Buckley, C.D.; Lavery, G.; Cooper, M.S.; Raza, K.
11 Beta-hydroxysteroid dehydrogenase type 1 regulates synovitis, joint destruction, and systemic bone loss in chronic polyarthritis
J. Autoimmun.
92
104-113
2018
Mus musculus (P50172)
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
Shearer, F.J.G.; Wyrwoll, C.S.; Holmes, M.C.
The role of 11beta-hydroxy steroid dehydrogenase type 2 in glucocorticoid programming of affective and cognitive behaviours
Neuroendocrinology
109
257-265
2019
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