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Information on EC 1.1.1.146 - 11beta-hydroxysteroid dehydrogenase and Organism(s) Mus musculus and UniProt Accession P50172

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Mus musculus
UNIPROT: P50172 not found.
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Word Map
The taxonomic range for the selected organisms is: Mus musculus
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
Synonyms
11beta-hsd1, 11beta-hsd2, hsd11b2, hsd11b1, 11beta-hydroxysteroid dehydrogenase, 11beta-hsd, 11beta-hydroxysteroid dehydrogenase type 1, beta-hydroxysteroid dehydrogenase, 11betahsd2, 11betahsd1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
11 beta-hydroxysteroid dehydrogenase type 1
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11beta-hydroxysteroid dehydrogenase 1
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11beta-hydroxysteroid dehydrogenase type 1
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11 beta-hydroxysteroid dehydrogenase type 1
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11-beta-HSD1
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11-beta-HSD1 (oxidase) NADP+
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11-beta-HSD2
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11-DH
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11-DH2
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11-oxoreductase
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11beta-HSD
11beta-HSD1
11beta-HSD1A
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-
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11beta-HSD2
11beta-hydroxy steroid dehydrogenase
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-
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11beta-hydroxy steroid dehydrogenase type 2
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11beta-hydroxysteroid dehydrogenase 1
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11beta-hydroxysteroid dehydrogenase 2
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11beta-hydroxysteroid dehydrogenase type 1
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11beta-hydroxysteroid dehydrogenase type 2
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11beta-hydroxysteroid dehydrogenase type I
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11beta-hydroxysteroid dehydrogenase-1
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11betaHSD1
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beta-hydroxysteroid dehydrogenase
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corticosteroid 11-reductase
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corticosteroid 11beta-dehydrogenase
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dehydrogenase, 11beta-hydroxy steroid
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NAD-dependent 11-beta-hydroxysteroid dehydrogenase
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type 1 11beta-hydroxysteroid dehydrogenase
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additional information
-
the enzyme belongs to the short-chain dehydrogenase/reductase superfamily
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+
show the reaction diagram
substrate binding site structure, reaction mechanism involving Lys187 and Tyr183, active site structure involving a S-Y-K catalytic triad
an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+
show the reaction diagram
active site variability of isozyme 11beta-HSD1, structure-activity analysis, catalytic mechanism
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
redox reaction
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oxidation
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reduction
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SYSTEMATIC NAME
IUBMB Comments
11beta-hydroxysteroid:NADP+ 11-oxidoreductase
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CAS REGISTRY NUMBER
COMMENTARY hide
9041-46-7
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SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
show the reaction diagram
isozyme 11beta-HSD1 catalyzes the forward reaction with cofactor NADPH
-
-
ir
11-dehydrocorticosterone + NADPH + H+
corticosterone + NADP+
show the reaction diagram
-
-
-
?
7-keto,25-hydroxycholesterol + NADPH + H+
7beta,25-dihydroxycholesterol + NADP+
show the reaction diagram
-
-
-
?
7-ketocholesterol + NADPH + H+
7beta-hydroxycholesterol + NADP+
show the reaction diagram
-
-
-
?
corticosterone + NAD+
11-dehydrocorticosterone + NADH + H+
show the reaction diagram
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-
-
?
cortisol + NAD+
cortisone + NADH + H+
show the reaction diagram
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
show the reaction diagram
(+)-11-dihydrooracin + NADP+
?
show the reaction diagram
-
-
-
-
r
1,2-dehydrocortisone + NADPH
1,2-dehydrocortisol + NADP+
show the reaction diagram
-
-
-
-
?
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
show the reaction diagram
11-dehydrocorticosterone + NADPH + H+
corticosterone + NADP+
show the reaction diagram
11-oxotestosterone + NADPH + H+
?
show the reaction diagram
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-
-
-
?
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
show the reaction diagram
4-nitroacetophenone + NADPH + H+
?
show the reaction diagram
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-
-
-
?
4-nitrobenzaldehyde + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
7-oxo-cholesterol + NADP+
7beta-hydroxycholesterol + NADPH + H+
show the reaction diagram
-
-
-
-
r
7-oxocholesterol + NADPH + H+
7alpha-hydroxycholesterol + NADP+
show the reaction diagram
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-
-
-
?
7-oxolithocholic acid + NADPH + H+
?
show the reaction diagram
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-
-
-
?
7beta,25-dihydroxycholesterol + NAD+
7-keto,25-hydroxycholesterol + NADH + H+
show the reaction diagram
-
-
-
?
7beta-hydroxycholesterol + NADPH + H+
7-oxo-cholesterol + NADP+
show the reaction diagram
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-
-
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r
bupropion + NADPH + H+
threohydrobupropion
show the reaction diagram
-
-
-
-
?
corticosterone + NAD+
11-dehydrocorticosterone + NADH + H+
show the reaction diagram
-
-
-
?
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
show the reaction diagram
corticosterone + NADP+
11-dehydrocorticosterone + NADPH + H+
show the reaction diagram
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-
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r
cortisol + NAD+
cortisone + NADH
show the reaction diagram
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
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ir
cortisol + NAD+
cortisone + NADH + H+
show the reaction diagram
cortisol + NADP+
cortisone + NADPH
show the reaction diagram
cortisol + NADP+
cortisone + NADPH + H+
show the reaction diagram
-
-
-
-
?
cortisone + NADH + H+
cortisol + NAD+
show the reaction diagram
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-
-
?
cortisone + NADPH + H+
cortisol + NADP+
show the reaction diagram
DFU-lactol + NADPH + H+
?
show the reaction diagram
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-
-
-
?
itrosamineketone + NADPH + H+
?
show the reaction diagram
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-
?
ketoprofen + NADPH + H+
?
show the reaction diagram
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-
?
metyrapone + NADPH + H+
7alpha-hydroxycholesterol + NADP+
show the reaction diagram
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-
-
-
?
oracin + NADPH + H+
11-dihydrooracin + NADP+
show the reaction diagram
-
trivial name oracin, anticancer drug
93% (+)-11-dihydrooracin
-
?
oracin + NADPH + H+
?
show the reaction diagram
-
-
-
-
?
triadimefon + NADPH + H+
?
show the reaction diagram
-
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-
?
additional information
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
11-dehydrocorticosterone + NADPH + H+
corticosterone + NADP+
show the reaction diagram
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
show the reaction diagram
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
show the reaction diagram
-
isozyme 11beta-HSD1
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-
?
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
show the reaction diagram
corticosterone + NADP+
11-dehydrocorticosterone + NADPH
show the reaction diagram
cortisol + NAD+
cortisone + NADH
show the reaction diagram
isozyme 11beta-HSD2 catalyzes the reverse reaction with cofactor NAD+
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-
ir
cortisol + NAD+
cortisone + NADH + H+
show the reaction diagram
cortisol + NADP+
cortisone + NADPH + H+
show the reaction diagram
-
-
-
-
?
cortisone + NADH + H+
cortisol + NAD+
show the reaction diagram
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
NADPH
11beta-HSD1
NADP+
NADPH
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
1 mM used in assay conditions
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
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(2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
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(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
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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
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2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
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2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
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2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
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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
-
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine
-
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
-
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
-
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]thiomorpholine-1,1-dioxide
-
-
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(4-piperidin-1-ylphenyl)sulfonyl]piperazine
-
-
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine
-
-
(2R)-N-[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-methylchrysazin
-
-
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
-
7-oxo-cholesterol
-
-
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
-
-
Aloe-emodin
-
-
AMG-221
-
-
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
carbenoxolone
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
dihydrotestosterone
-
-
emodin
-
-
enoxolone
-
-
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
glycyrrhizic acid
-
-
glycyrrhizinic acid
-
-
glycyrrhizininc acid
-
-
hydroxyitraconazole
-
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
posaconazole
-
Rhein
-
-
rheochrysidin
-
-
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
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
5-aminoimidazole-4-carboxamide ribonucleoside
-
treatment augments the induction of enzyme expression and activity by C2 ceramide
bacterial sphingomyelinase
-
-
-
C2 ceramide
-
treatment of 3T3-L1 preadipocytes robustly induces the expression of isoform 11beta-HSD1 via induction of CCAAT/enhancer-binding protein beta and its binding to the 11beta-HSD1 promoter
glucose
-
coexpression with hexose-6-phosphate dehydrogenase potentiates 11beta-HSD1 reductase activity at high glucose, this effect is significantly decreased at low glucose, with concomitantly increased 11beta-HSD1 dehydrogenase activity
Insulin
-
insulin stimulates 11beta-HSD1 activity and expression in a time- and concentration-dependent manner, the p38 MAPK inhibitor SB-220025, but not the ERK inhibitor U-0126 or the phosphatidylinositol 3-kinase inhibitor LY294002, prevent insulin stimulation of 11beta-HSD1 activity
-
sphingosine 1-phosphate
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.79
(+)-11-dihydrooracin
-
37°C, pH 10.8-11.0
-
0.0002 - 0.0013
11-Dehydrocorticosterone
1.269
7-oxo-cholesterol
-
recombinant enzyme, at pH 7.4 and 37°C
0.3176 - 3.5
7beta-hydroxycholesterol
0.00178 - 0.0042
corticosterone
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0016
fenofibrate
-
82% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
0.0091
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
0.0034
fenofibric acid ethylester
-
85% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
0.0031
fenofibric acid isobutylester
-
75% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
0.009
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
0.0041
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
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
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
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
peripheral lymph nodes and mesenteric lymph nodes
Manually annotated by BRENDA team
-
derived from bone-marrow, peritoneal macrophages, expression of isozyme 11beta-HSD1, not isozyme 11beta-HSD2
Manually annotated by BRENDA team
-
11beta-HSD1 co-localises with glucagon in the periphery of pancreatic islets, but not with insulin or somatostatin
Manually annotated by BRENDA team
-
isoform 11beta-HSD1 is highly expressed in freshly isolated omental adipose stromal vascular cells, predominantly in preadipocytes
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
associated, isozyme 11beta-HSD1
Manually annotated by BRENDA team
-
isozyme 11beta-HSD1 is anchored through an N-terminal transmembrane domain
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
malfunction
feto-placental deletion of isoform HSD2 results in a reduced birthweight and the development of anxiety- and depression-like behaviours in adult mice. Brain-specific HSD2 removal also generates adult phenotypes of depressive-like behaviour and memory deficits
metabolism
-
11beta-hydroxysteroid dehydrogenase-1 is involved in bile acid homeostasis by modulating fatty acid transport protein-5 in the liver of mice
physiological function
isoform HSD2 expression protects the serotonin system in development
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
DHI1_MOUSE
292
1
32364
Swiss-Prot
Secretory Pathway (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
34000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
-
2 * 34000, SDS-PAGE
additional information
-
comparison of primary structures, three-dimensional structure around the substrate binding site, and active site amino acid sequences of several mammalia
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
-
-
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
purified recombinant His6-tagged enzyme, hanging drop vapour diffusion method, 25 mg/ml protein in 20 mM Tris-HCl, pH 8.0, 0.2 M NaCl, 0.1% Triton, 5% glycerol, and 2 mM EDTA, mixed with equal volume of well solution containing 1.8 M Li2O4, and 0.1 M HEOES, pH 7.5, at room temperature, derivatization with 1 mM ethylmercuric chloride, soaking of crystals with NADH and corticoserone containing solution, X-ray diffraction structure determination and analysis at 3.0 A resolution
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant His6-tagged enzyme from Escherichia coli by nickel affinity chromatography and gel filtration
octyl-Sepharose, Mono Q-sepharose, Red Sepharose A
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in HEK-293 cell
expression in HEK-293 cell
expression of His6-tagged enzyme in Escherichia coli
expressed in CHO cells
-
expressed in HEK-293 cell
-
expressed in HEK-293 cells
-
expressed in rat H4IIE hepatoma cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
the expression of isoform 11beta-HSD1 in the epidermis of atopic dermatitis lesions is higher than that in the epidermis of healthy controls
the enzyme is highly expressed in immune cells elicited to the mouse peritoneum during thioglycollate-induced peritonitis
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pharmacology
the enzyme is an important therapeutic target for diabetes in humans
analysis
-
high-throughput screening for potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
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
-
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team