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Information on EC 1.1.1.146 - 11beta-hydroxysteroid dehydrogenase and Organism(s) Homo sapiens

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Homo sapiens
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
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, 11betahsd2, beta-hydroxysteroid dehydrogenase, 11betahsd1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
11 beta-hydroxysteroid dehydrogenase type 1
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11-beta-HSD1
11-beta-HSD2
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11-beta-hydroxysteroid dehydrogenase type1
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11-DH
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11-DH2
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-
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11beta-HSD
11beta-HSD 1
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11beta-HSD type 1
11beta-HSD-1
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11beta-HSD-2
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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-hydroxysteroid dehydrogenase
11beta-hydroxysteroid dehydrogenase 1
11beta-hydroxysteroid dehydrogenase 2
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11beta-hydroxysteroid dehydrogenase isoforms 1
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11beta-hydroxysteroid dehydrogenase type 1
11beta-hydroxysteroid dehydrogenase type 2
11beta-hydroxysteroid dehydrogenase type I
11beta-hydroxysteroid type 1 dehydrogenase
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11beta-hydroxysteroid-dehydrogenase type I
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11betaHSD1
11betaHSD2
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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HSD11B1
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isoform
Hsd11B2
isozyme 11beta-HSD1
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NAD-dependent 11-beta-hydroxysteroid dehydrogenase
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type 1 11beta-hydroxysteroid dehydrogenase
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
an 11beta-hydroxysteroid + NADP+ = an 11-oxosteroid + NADPH + H+
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
oxidation
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redox reaction
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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
1,2-dehydrocortisol + NADP+
1,2-dehydrocortisone + NADPH
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
-
-
-
-
r
11alpha-hydroxy-pregn-4-ene-3,20-dione + ?
pregn-4-ene-3,11,20-trione + ?
show the reaction diagram
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + ?
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + ?
show the reaction diagram
-
i.e. cortisol
-
?
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
show the reaction diagram
-
i.e. cortisol
i.e. cortisol
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r
11beta,17beta-dihydroxyandrost-4-ene-3-one + ?
17beta-hydroxyandrost-4-ene-3,11-dione + ?
show the reaction diagram
11beta,20alpha-dihydroxypregn-4-ene-3-one + ?
20alpha-hydroxypregn-4-ene-3,11-dione + ?
show the reaction diagram
11beta,20beta-dihydroxypregn-4-ene-3-one + ?
20beta-hydroxypregn-4-ene-3,11-dione + ?
show the reaction diagram
11beta,21-dihydroxypregn-4-en-3,20-dione + ?
11-dehydro,21-hydroxy-pregn-4-en-3,20-dione + ?
show the reaction diagram
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
show the reaction diagram
11beta-hydroxy-5alpha-androstane-3,17-dione + NAD+
11-keto-5alpha-androstane-3,17-dione + NADH + H+
show the reaction diagram
-
-
-
?
11beta-hydroxy-pregn-4-ene-3,20-dione + ?
pregn-4-ene-3,11,20-trione + ?
show the reaction diagram
11beta-hydroxyandrost-4-ene-3,17-dione + ?
androst-4-ene-3,11,17-trione + ?
show the reaction diagram
11beta-hydroxyandrostenedione + NAD+
11-ketoandrostenedione + NADH + H+
show the reaction diagram
-
-
-
?
11beta-hydroxyandrosterone + NAD+
11-ketoandrosterone + NADH + H+
show the reaction diagram
-
-
-
?
11beta-hydroxydihydrotestosterone + NAD+
11-ketodihydrotestosterone + NADH + H+
show the reaction diagram
-
-
-
?
11beta-hydroxyprogesterone + NAD+
11-ketoprogesterone + NADH + H+
show the reaction diagram
-
-
-
?
11beta-hydroxytestosterone + NAD+
11-ketotestosterone + NADH + H+
show the reaction diagram
-
-
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?
15-deoxy-D12,14-prostaglandin J2 + NADPH
?
show the reaction diagram
-
isozyme 11beta-HSD1
-
-
?
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
2,3-benzoylphenyl-propanoic acid + NADPH
2,3-benzoylphenyl-propanol + NADP+
show the reaction diagram
20alpha-hydroxypregn-4-ene-3-one + ?
20alpha-hydroxypregn-4-ene-3,11-dione + ?
show the reaction diagram
21-deoxycortisol + NAD+
21-deoxycortisone + NADH + H+
show the reaction diagram
-
-
-
?
4-methylnitrosamine-1-(3-pyridiyl)-1-butanone + NADPH
4-methylnitrosamine-1-(3-pyridiyl)-1-butanol + NADP+
show the reaction diagram
-
-
-
-
?
4-methylnitrosamino-1-(3-pyridyl)-1-butanone + NADPH
4-methylnitrosamino-1-(3-pyridyl)-1-butanol + NADP+
show the reaction diagram
-
i.e. NNK, genotoxic compound from tobacco smoke, isozyme 11beta-HSD1, carbonyl reductase activity, EC 1.1.1.184
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r
5,5-dimethyl-3-(3-fluorphenyl)-4-(4-methylsulfonyl)phenyl-2-(5H-furanone)-lactol + NADP+
5,5-dimethyl-3-(3-fluorphenyl)-4-(4-methylsulfonyl)phenyl-2-(5H-furanone)-lactone + NADPH
show the reaction diagram
5alpha-androstane-3beta,7alpha,17beta-triol + NADP+
5alpha-androstane-3beta,7beta,17beta-triol + NADPH
show the reaction diagram
-
interconversion of 7alpha to 7beta isoform, ratio Vmax/Km is 2 pmol min-1 microgramm-1/microMol
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r
5alpha-androstane-3beta,7beta,17beta-triol + NADP+
5alpha-androstane-3beta,7alpha,17beta-triol + NADP
show the reaction diagram
-
interconversion of 7beta to 7alpha isoform, ratio Vmax/Km is 0.5 pmol min-1 microgramm-1/microMol
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r
5alpha-pregnan-11beta,17alpha-diol-3,20-dione + NAD+
5alpha-pregnan-17alpha-ol-3,11,20-trione + NADH + H+
show the reaction diagram
-
-
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?
5alpha-pregnan-3alpha,11beta,17alpha-triol-20-one + NAD+
5alpha-pregnan-3alpha,17alpha-diol-11,20-dione + NADH + H+
show the reaction diagram
-
-
-
?
6-[2-(2-hydroxy-ethylamino)-ethyl]-6H-indeno[1,2-c]isoquinoline-5,11-dione + NADPH
(+)-6-[2-(2-hydroxyethyl)aminoethyl]-5-oxo-11-hydroxy-5,6-dihydro-11H-indeno[1,2-c]isoquinoline + NADP+
show the reaction diagram
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trivial name oracin, cytostatic drug, 11beta-HSD 1 exhibits enzyme cooperativity for the formation of both hydroxy-enantiomers
24% (+)-stereoisomer
-
?
6-[2-(2-hydroxy-ethylamino)-ethyl]-6H-indeno[1,2-c]isoquinoline-5,11-dione + NADPH + H+
(-)-6-[2-(2-hydroxyethyl)aminoethyl]-5-oxo-11-hydroxy-5,6-dihydro-11H-indeno[1,2-c]isoquinoline + NADP+
show the reaction diagram
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trivial name oracin, cytostatic drug
76% (-)-stereoisomer
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?
7-keto,25-hydroxycholesterol + NADPH + H+
7beta,25-dihydroxycholesterol + NADP+
show the reaction diagram
-
-
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?
7-keto,27-hydroxycholesterol + NADP+
7beta,27-dihydroxycholesterol + NADPH + H+
show the reaction diagram
the reaction is catalyzed by isoform 11beta-HSD1
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r
7-ketocholesterol + NADPH + H+
7beta-hydroxycholesterol + NADP+
show the reaction diagram
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-
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?
7-ketodehydroepiandrosterone + 2 NADPH + 2 H+
7alpha-hydroxydehydroepiandrosterone + 7beta-hydroxydehydroepiandrosterone + 2 NADP+
show the reaction diagram
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formation of alpha- and beta-product in almost equal amounts. In presence of hexose-6-phosphate dehydrogenase, the 7keto-substrate is almost fully metabolized and the 7beta-product is preferentially formed
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?
7-oxo-5alpha-androstane-3beta,17beta-diol + NADPH
5alpha-androstane-3beta,7alpha,17beta-triol + 5alpha-androstane-3beta,7alpha,17beta-triol + NADP+
show the reaction diagram
-
-
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r
7-oxo-cholesterol + NADP+
7beta-hydroxycholesterol + NADPH + H+
show the reaction diagram
-
-
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?
7-oxocholesterol + NADPH + H+
7beta-hydroxycholesterol + NADP+
show the reaction diagram
7alpha-hydroxydehydroepiandrosterone + NADP+
7beta-hydroxydehydroepiandrosterone + 7-ketodehydroepiandrosterone + NADPH
show the reaction diagram
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in presence of hexose-6-phosphate dehydrogenase, less substrate is metabolized and accumulation of 7-ketodehydroepiandrosterone is abolished
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?
7beta,25-dihydroxycholesterol + NAD+
7-keto,25-hydroxycholesterol + NADH + H+
show the reaction diagram
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?
7beta,27-dihydroxycholesterol + NADH + H+
7-keto,27-hydroxycholesterol + NAD+
show the reaction diagram
the reaction is catalyzed by isoform 11beta-HSD2
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r
7beta-hydroxycholesterol + NADP+
7-oxocholesterol + NADPH
show the reaction diagram
7beta-hydroxydehydroepiandrosterone + NADP+
7alpha-hydroxydehydroepiandrosterone + 7-ketodehydroepiandrosterone + NADPH
show the reaction diagram
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formation of products in almost equal amounts. In presence of hexose-6-phosphate dehydrogenase, less substrate is metabolized and accumulation of 7-ketodehydroepiandrosterone is abolished
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?
cholestane-3beta,5alpha,6beta-triol + NAD(P)+
6-oxocholestan-3beta,5alpha-diol + NAD(P)H + H+
show the reaction diagram
-
-
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?
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
-
-
-
?
corticosterone + NADPH + H+
corticosterol + NADP+
show the reaction diagram
-
-
-
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r
cortisol + NAD+
cortisone + NADH
show the reaction diagram
-
isoform 11beta-HSD2
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-
?
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
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
show the reaction diagram
dehydrocorticosterone + NADPH
corticosterone + NADP+
show the reaction diagram
dexamethasone + NADP+
11-dehydromethasone + NADPH
show the reaction diagram
metapyrone + NADPH + H+
7alpha-hydroxycholesterol + NADP+
show the reaction diagram
-
-
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r
metyrapone + NADPH
? + NADP+
show the reaction diagram
-
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r
oracin + NADPH + H+
11-dihydrooracin + NADP+
show the reaction diagram
-
the partially purified enzyme catalyzes the reduction of oracin in a stereospecific manner and with higher efficiency and affinity compared to microsomal 11beta-HSD1. The enzyme purified from human liver reduces oracin to (-)-dihydrooracin and (+)-dihydrooracin in a ratio of 76 to 24. Whole human liver microsomes metabolise oracin with different stereospecificity, where the formation of (-)-dihydrooracin (60%) predominates over (+)-dihydrooracin (40%)
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?
oracin + NADPH + H+
dihydrooracin + NADP+
show the reaction diagram
-
a cytostatic drug, isozyme 11beta-HSD1, carbonyl reductase activity, EC 1.1.1.184, stereochemical ratio of 3:1 for R:S enantiomers of the pro-chiral carbonyl centre of oracin, inactivation of the anti-cancer drug
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r
additional information
?
-
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
1,2-dehydrocortisol + NADP+
1,2-dehydrocortisone + NADPH
show the reaction diagram
-
-
-
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r
11-dehydrocorticosterone + NADPH
corticosterone + NADP+
show the reaction diagram
-
isozyme 11beta-HSD1
-
-
?
11alpha-hydroxy-pregn-4-ene-3,20-dione + ?
pregn-4-ene-3,11,20-trione + ?
show the reaction diagram
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + ?
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + ?
show the reaction diagram
-
i.e. cortisol
-
?
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione + NADP+
17,21-dihydroxy-pregn-4-ene-3,11,20-trione + NADPH
show the reaction diagram
-
i.e. cortisol
i.e. cortisol
-
r
11beta,17beta-dihydroxyandrost-4-ene-3-one + ?
17beta-hydroxyandrost-4-ene-3,11-dione + ?
show the reaction diagram
11beta,20alpha-dihydroxypregn-4-ene-3-one + ?
20alpha-hydroxypregn-4-ene-3,11-dione + ?
show the reaction diagram
11beta,20beta-dihydroxypregn-4-ene-3-one + ?
20beta-hydroxypregn-4-ene-3,11-dione + ?
show the reaction diagram
11beta,21-dihydroxypregn-4-en-3,20-dione + ?
11-dehydro,21-hydroxy-pregn-4-en-3,20-dione + ?
show the reaction diagram
11beta,21-dihydroxypregn-4-en-3,20-dione + NADP+
21-hydroxy-pregn-4-en-3,11,20-trione + NADPH
show the reaction diagram
11beta-hydroxy-pregn-4-ene-3,20-dione + ?
pregn-4-ene-3,11,20-trione + ?
show the reaction diagram
11beta-hydroxyandrost-4-ene-3,17-dione + ?
androst-4-ene-3,11,17-trione + ?
show the reaction diagram
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-methylnitrosamino-1-(3-pyridyl)-1-butanone + NADPH
4-methylnitrosamino-1-(3-pyridyl)-1-butanol + NADP+
show the reaction diagram
-
i.e. NNK, genotoxic compound from tobacco smoke, isozyme 11beta-HSD1, carbonyl reductase activity, EC 1.1.1.184
-
-
r
7-keto,27-hydroxycholesterol + NADP+
7beta,27-dihydroxycholesterol + NADPH + H+
show the reaction diagram
the reaction is catalyzed by isoform 11beta-HSD1
-
-
r
7-oxo-cholesterol + NADP+
7beta-hydroxycholesterol + NADPH + H+
show the reaction diagram
-
-
-
?
7beta,27-dihydroxycholesterol + NADH + H+
7-keto,27-hydroxycholesterol + NAD+
show the reaction diagram
the reaction is catalyzed by isoform 11beta-HSD2
-
-
r
7beta-hydroxycholesterol + NADP+
7-oxocholesterol + NADPH
show the reaction diagram
-
-
-
-
r
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
-
-
-
?
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
-
-
-
?
cortisone + NADPH + H+
cortisol + NADP+
show the reaction diagram
dehydrocorticosterone + NADPH
corticosterone + NADP+
show the reaction diagram
-
isozyme 11beta-HSD1, 11beta-hydroxysteroid dehydrogenase activity, EC 1.1.1.146
-
-
r
oracin + NADPH + H+
dihydrooracin + NADP+
show the reaction diagram
-
a cytostatic drug, isozyme 11beta-HSD1, carbonyl reductase activity, EC 1.1.1.184, stereochemical ratio of 3:1 for R:S enantiomers of the pro-chiral carbonyl centre of oracin, inactivation of the anti-cancer drug
-
-
r
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
NADP+
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(+/-)-2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(1-adamantylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(1-adamantylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cycloheptylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cycloheptylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclohexylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclohexylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclooctylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-(1-norbornylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-(7-norbornylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-ethyl-5-methyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-2-(1-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-2-(3-noradamantylamino)-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-2-(7-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(+/-)-5-methyl-5-propyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
(-)-catechin
about 98% activity at 0.2 mM
(-)-epicatechin
about 95% activity at 0.2 mM
(-)-epigallocatechin
less than 80% activity at 0.2 mM
(-)-epigallocatechin 3-gallate
potent inhibitor, less than 10% activity at 0.2 mM
(-)-gallocatechin
less than 30% activity at 0.2 mM
(1'-[(adamantan-2-yl)carbamoyl]-7-bromo-2,3-dihydrospiro[indene-1,4'-piperidin]-3-yl)acetic acid
selective isoform 11beta-HSD1 inhibitor
(1-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]cyclopentyl)acetic acid
11% inhibition at 0.001 mM
(1-[2-[(2,4-dichlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
27% inhibition at 0.001 mM
(1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
-
(1-[2-[(2-chlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
22% inhibition at 0.001 mM
(1-[2-[(4-methoxypyridin-3-yl)amino]-2-oxoethyl]cyclopentyl)acetic acid
7% inhibition at 0.001 mM
(1-[2-[(cyclohexylmethyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
7% inhibition at 0.001 mM
(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid
-
(11beta)-11-hydroxyallopregnanolone
-
-
(11beta)-11-hydroxyprogesterone
-
-
(1E,4E)-1,5-bis(3-methylthiophen-2-yl)penta-1,4-dien-3-one
-
-
(1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one
derivative of curcumin, IC50 value in intact cells 93 nM. Not inhibitory to isoform 11beta-HSD2 in kidney at 100 microM
(1E,4E)-1,5-bis(thiophen-2-yl)cyclohexanone
-
-
(1E,4E)-1,5-bis(thiophen-2-yl)penta-1,4-dien-3-one
-
-
(1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
(1r,4s)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
(1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
-
(1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
(1S)-4-([1-[(4-bromophenyl)methyl]-1H-tetrazol-5-yl]methyl)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-ol
-
(1S,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
-
(2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
-
(20R,23E)-eupha-8,23-diene-3beta,25-diol
-
-
(24R)-eupha-8,25-diene-3beta,24-diol
-
-
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
-
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
-
(2E,4S)-4-hydroxy-5-[(1S,5S,6S)-6-(hydroxymethyl)-2-methylidenebicyclo[3.1.1]hept-6-yl]-2-methylpent-2-enoic acid
-
-
(2R)-1,1,1-trifluoro-2-(3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine-1-sulfonyl]phenyl)propan-2-ol
HSD-016
(2R)-1-(2-chloro-4-(2-methoxyethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(2-chloro-4-(difluoromethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(2-chloro-4-ethoxyphenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxamide
-
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxylic acid
-
(2R)-1-(3-chloro-4-([4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazin-1-yl]sulfonyl)phenyl)piperidin-4-ol
-
(2R)-1-(4-bromo-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-(4-bromophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazine
-
(2R)-1-(4-tert-butoxy-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
-
(2R)-1-([2-chloro-4-[(3S)-3-methylpiperazin-1-yl]phenyl]sulfonyl)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[(2-chloro-4-piperidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[(2-chloro-4-pyrrolidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine
-
-
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine
-
-
(2R)-1-[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)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
-
-
(2R)-2-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenoxy)-N,N-dimethylethanamine
-
(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine
-
-
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)-N,N-dimethylaniline
-
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
-
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenol
-
(2R)-3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)benzamide
-
(2R)-4-(3-fluoro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)morpholine
-
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzamide
-
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
-
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-1-(4-methoxyphenylsulfonyl)-2-methylpiperazine
-
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methyl-1-(4-(trifluoromethoxy)-phenylsulfonyl)-piperazine
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
-
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]thiomorpholine-1,1-dioxide
-
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(4-piperidin-1-ylphenyl)sulfonyl]piperazine
-
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine
-
(2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-(tricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-[(1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
-
(2R)-N-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide
-
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
-
(2R,4aS,6aS,12bR,14aS)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylate
-
(2S)-5-(acetyloxy)-2-hydroxypentyl acetate
-
-
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
(3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid
-
(3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
-
(3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
-
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
-
-
(3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid
-
(3beta)-3-hydroxy-11-oxoolean-12-en-30-amide
-
(3beta)-3-hydroxy-18,29-epoxyolean-12-ene-11,29-dione
IC50 value for isoform 11beta-HSD2 above 25 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-3-[(3-carboxypropanoyl)oxy]urs-12-en-28-oic acid
IC50 value for isoform 11beta-HSD2 above 3 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-30-[hydroxy(methyl)amino]-11,30-dioxoolean-12-en-3-yl acetate
IC50 value for isoform 11beta-HSD1 above 1 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
-
(3beta,18alpha)-3-hydroxy-11-oxoolean-12-en-30-oate
-
(3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
-
(3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
-
(3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
-
(3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
-
(3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
-
(3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
-
(3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
-
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
-
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
-
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
-
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
-
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
-
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
-
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
-
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
-
(3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
-
(3E)-3-[[(4-bromo-3-methylphenoxy)acetyl]hydrazono]-N-tricyclo[3.3.1.13,7]dec-1-ylbutanamide
-
(3R)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
-
(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)-1-(3-chloro-2-methylbenzene-1-sulfonyl)-N-cyclohexylpiperidine-3-carboxamide
INCB-13739, selective inhibitor for isoform 11beta-HSD1
(3S)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
-
(3S,4aR,6aR,6bS,8aS,11S,12aR,14aR,14bS)-4,4,6a,6b,8a,11,14b-heptamethyl-11-[(methylsulfonyl)amino]-14-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,14,14a,14b-icosahydropicen-3-yl acetate
IC50 value for isoform 11beta-HSD1 above 40 microM. Docking studies into isoforms 11beta-HSD1 and 11beta-HSD2 binding sites
(4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
-
(4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
-
-
(4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decan-1-yl)acetic acid
-
-
(4aS,5R,8aR)-5,6-bis(hydroxymethyl)-1,1,4a-trimethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
-
-
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol
-
-
(4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-3,4,4a,5,8,8a-hexahydronaphthalen-2(1H)-one
-
-
(5R)-2-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-5-methyl-5-(trifluoromethyl)-1,3-thiazol-4(5H)-one
-
-
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
-
(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)acetic acid
-
-
(6S)-6-(2-hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(1-methyl-2-oxo-1,2-dihydropyridin-4-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-one
BI-135585
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(2',4'-difluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
displays more than 1000fold selectivity for isoform 11beta-HSD1 over three related hydroxysteroid dehydrogenases, three CYP isozymes, hERG, and three nuclear receptors. When dosed orally at 30 mg/kg to mice, compound is distributed into adipose and liver
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
-
(R)-1-((S)-2-acetamido-3-(2-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-2-acetamido-3-(4-methoxyphenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-((S)-3-([1,1'-biphenyl]-3-yl)-2-aminopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(3-acetamidopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(acetyl-L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(acetylglycyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(L-tryptophyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
(R)-N-(adamantan-2-yl)-1-((S)-2-(2-aminoacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(R)-N-(adamantan-2-yl)-1-((S)-2-(2-hydroxyacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(3-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
-
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine]
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine]
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine]
-
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine]
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
-
-
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydroxypropan-2-yl)phenylsulfonyl)-piperazin-1-yl)methyl)-cyclopropanecarboxamide
substrate competitive inhibitor, specific for 11beta-hydroxysteroid dehydrogenase type 1
1-(2,4-dichlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)-ethanone
-
1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
poor stability in liver microsomes
1-(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-(4-chlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)ethanone
-
1-(5-oxo-2,5-dihydrofuran-3-yl)urea
-
specific for isozyme 11beta-HSD1
1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol
-
1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(2,4-dichloro-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(2-chloro-benzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfinyl)ethanone
-
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-ylamino)ethanone
-
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-yloxy)ethanone
-
1-adamantan-1-yl-2-(3,4-dimethoxy-benzyloxy)ethanone
-
1-adamantan-1-yl-2-(3,4-dimethoxy-phenoxy)ethanone
-
1-adamantan-1-yl-2-(3-methylbenzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(3-trifluoromethyl-phenoxy)ethanone
-
1-adamantan-1-yl-2-(3-trifluoromethylbenzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzenesulfinyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzenesulfonyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-chloro-benzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenoxy)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfinyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(4-chloro-phenylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(4-methoxy-benzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-methylbenzyloxy)ethanone
-
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfinyl)ethanone
-
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfonyl)ethanone
-
1-adamantan-1-yl-2-(4-tert-butylbenzylsulfanyl)ethanone
-
1-adamantan-1-yl-2-(4-trifluoromethyl-phenoxy)ethanone
-
1-adamantan-1-yl-2-(4-trifluoromethylbenzyloxy)ethanone
-
1-adamantan-1-yl-2-(biphenyl-4-ylmethoxy)ethanone
-
1-adamantan-1-yl-2-(biphenyl-4-yloxy)ethanone
-
1-adamantan-1-yl-2-(toluene-4-sulfinyl)ethanone
-
1-adamantan-1-yl-2-(toluene-4-sulfonyl)ethanone
-
1-adamantan-1-yl-2-m-tolylmethanesulfonyl-ethanone
-
1-adamantan-1-yl-2-p-tolyloxy-ethanone
-
1-adamantan-1-yl-2-p-tolylsulfanyl-ethanone
-
1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
-
1-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-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
poor stability in liver microsomes
1-piperidinecarboxylic acid
-
-
1-[(1R,2R,7S)-5-[(aminooxy)methyl]tricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethyl-4-([[5-(1H-1,2,4-triazol-1-yl)pyridin-2-yl]oxy]methyl)pyrrolidin-2-one
-
-
1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(2-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-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
-
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
-
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane
-
-
1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(3,4-dimethylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(3-amino-4-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(3-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol
-
-
1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
-
-
1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
-
-
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide
-
-
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide
-
-
1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
-
-
11-deoxycorticosterone
-
-
11-ketotestosterone
-
-
11-oxo-3alpha,5alpha-tetrahydrotestosterone
-
-
11-oxo-allopregnanolone
-
-
11-oxo-androstenedione
-
-
11-oxo-progesterone
-
-
11-oxo-testosterone
-
-
11alpha-hydroxyprogesterone
-
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione
-
i.e. cortisol
11beta-hydroxy-androstanediol
-
-
11beta-hydroxy-testosterone
-
-
18alpha-glycyrrhetinic acid
selective inhibition of 11beta-HSD1, does not inhibit 11beta-HSD2 at concentrations up to 0.02 mM
18beta-glycyrrhetinic acid
2'-hydroxyflavanone
-
-
2,2'-Dihydroxybiphenyl
-
-
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
2,4-dichloro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]naphthalen-1-yl]benzamide
-
-
2,4-dichloro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]phenyl]benzamide
-
-
2,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzenesulfonamide
-
-
2,6,7-trimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
30.88% inhibition of isoform 11beta-HSD1 at 0.01 mM
2,6-dichloro-4-[(5,7,7-trimethyl-2-azabicyclo[3.2.1]oct-2-yl)carbonyl]aniline
-
-
2,6-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM
2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
17.65% inhibition of isoform 11beta-HSD1 at 0.01 mM
2,7-dimethyl-6-nitro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(1-adamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(1-adamantylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide
2-(2-chloro-4-fluorophenoxy)-2-methyl-N-[(1R,2R,7S)-5-(methylsulfonyl)tricyclo[3.3.1.13,7]dec-2-yl]propanamide
-
-
2-(2-chloro-4-fluorophenoxy)-2-methyl-N-[(1R,2R,7S)-5-sulfamoyltricyclo[3.3.1.13,7]dec-2-yl]propanamide
-
-
2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
-
2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
-
2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane
-
2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide
-
-
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone
-
-
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone
-
-
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
-
-
2-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
-
-
2-(3-noradamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(4-chlorophenoxy)-N-[(1R,2R,7S)-5-(hydroxycarbamimidoyl)tricyclo[3.3.1.13,7]dec-2-yl]-2-methylpropanamide
-
-
2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
-
2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
-
2-(4-methylphenyl)-2-oxoethyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoate
-
-
2-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine
-
-
2-(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)-N,N-diethylacetamide
-
-
2-(adamantan-1-yl)-N-methyl-N-(thiophen-3-ylmethyl)acetamide
-
-
2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one
38.03% inhibition of isoform 11beta-HSD1 at 0.01 mM, 22.6% inhibition of isoform 11beta-HSD2 at 0.01 mM
2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one
71.27% inhibition of isoform 11beta-HSD1 at 0.01 mM, 23.97% inhibition of isoform 11beta-HSD2 at 0.01 mM
2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one
13.46% inhibition of isoform 11beta-HSD1 at 0.01 mM, 1.34% inhibition of isoform 11beta-HSD2 at 0.01 mM
2-(bicyclo[2.2.1]hept-2-ylamino)-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
-
2-(bromomethyl)-6,7-dimethyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
33.82% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(bromomethyl)-7-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(bromomethyl)-7-methyl-6-nitro-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(cycloheptylamino)-5-methyl-5-(1-methylethyl)-1,3-thiazol-4(5H)-one
-
-
2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(cyclooctylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
2-(iodomethyl)-2,3,6,7,8,9-hexahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one
27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(iodomethyl)-2,3,7,8,9,10-hexahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one
23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-(iodomethyl)-6-methyl-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-adamantan-1-yl-N-methyl-N-thiophen-2-ylmethyl-acetamide
-
-
2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane
2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane
-
2-bromo-N-[2-([2-oxo-2-[(2-phenylethyl)amino]ethyl]sulfanyl)-2,3-dihydro-1,3-benzothiazol-6-yl]benzamide
-
-
2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
-
-
2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
29.41% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-methyl-6,7,8,9-tetrahydro-5H-[1,3]thiazolo[2,3-b]quinazolin-5-one
13.24% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-methyl-7,8,9,10-tetrahydrocyclohepta[d][1,3]thiazolo[3,2-a]pyrimidin-5(6H)-one
14.71% inhibition of isoform 11beta-HSD1 at 0.01 mM
2-oxopentane-1,5-diyl diacetate
-
-
2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
-
2-[(2-chlorobenzyl)sulfanyl]-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
lead compound for development of inhibitors, the hydroxypyrimidine may act as a H-bonding pharmacophore. Compound has good cross species 11beta-HSD1 inhibitory activity for the mouse, cynomolgus monkey, and human enzymes
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
-
-
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
-
-
2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone
-
-
2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide
-
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
-
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
-
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
-
2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane
-
2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane
-
2-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
the triazole methyl group fits in a pocket formed by I121, T124 and Y183. The carbonyl group is predicted to form hydrogen bonds to residues Y183 and S170. The adamantyl group is predicted to fit tightly in a hydrophobic pocket formed by L171, Y177 and L217. Half-life in liver microsomes 68 min
2-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfonyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
additionally inhibits cytochrome P450 enzyme 3A4-BFC with an IC50 value of 6.3 microM. Half-life in liver microsomes 34 min
2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide
-
2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine
-
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
-
2-[4-(2,6-difluorobenzenesulfonyl)-[1,4]diazepan-1-yl]-1-(octahydroquinolin-1-yl)-ethanone
-
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N,N-dimethyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-benzyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-ethyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-furan-2-ylmethyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-isopropyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-methyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-phenyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-tert-butyl-acetamide
-
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
-
2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[4-(3-methylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzothiazole
89% residual activity at 0.02 mM
2-[4-(3-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzoxazole
18% residual activity at 0.02 mM
2-[4-(3-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
60% residual activity at 0.02 mM
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
75% residual activity at 0.02 mM
2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
-
2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole
-
2-[4-(4-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
90% residual activity at 0.02 mM
2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
-
2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
-
-
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
-
-
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
-
-
2-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
-
-
2-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-5-methyl-5-(trifluoromethyl)-1,3-thiazol-4(5H)-one
-
-
2-[[(2,6-dichlorophenyl)thio]methyl]-6-[(4-methylpiperidin-1-yl)carbonyl]pyridine
-
-
2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
-
2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
-
3,11-dioxoolean-12-en-30-oic acid
-
3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3,4-dicyclopropyl-5-[2-[3-fluoro-5-(trifluoromethyl)thiophen-2-yl]propan-2-yl]-4H-1,2,4-triazole
potent and selective inhibitor for isoform 11beta-HSD1
3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole
-
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability
3,5-bis(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3,5-bis(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide
-
-
3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(1-(4-fluorophenyl)cyclopropyl)-4-isopropyl-5-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazole
mixed-type inhibitor, specific for 11beta-hydroxysteroid dehydrogenase type 1
3-(1-adamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
-
3-(1-fluoronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(1-methoxy-2-naphthyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid
-
3-(2,3-difluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-4-methyl-5-(2-nitrophenyl)-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2,4-dichlorophenyl)-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-adamantan-1-yl-2-oxoethanesulfinyl)-N,N-dimethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethanesulfonyl)-N,N-dimethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)benzamide
-
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
-
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
-
3-(2-bromophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2-bromophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-bromophenyl)-5-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chloro-4-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2-chloro-4-fluorophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-4-methyl-5-(4-pentylphenyl)-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-5-(3,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(2-chlorophenyl)-5-[2-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM
3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
-
-
3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM
3-(4-benzylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-butyl-2-methylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-butylphenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-(4-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-chloro-2-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-chloro-3-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-4-methyl-5-(1-[4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]cyclobutyl)-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-4-methyl-5-[1-[3'-(methylsulfonyl)biphenyl-4-yl]cyclobutyl]-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-(1-biphenyl-3-ylcyclobutyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(2,4-dichlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(3-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-(4-fluorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-[2'-(ethylsulfonyl)biphenyl-4-yl]cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-[3'-(ethylsulfonyl)biphenyl-4-yl]cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-chlorophenyl)-5-[1-[4-(1H-imidazol-1-yl)phenyl]cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-fluorophenyl)-5-(4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]bicyclo[2.2.2]oct-1-yl)-1,2,4-oxadiazole
-
-
3-(4-pentylbicyclo[2.2.2]oct-1-yl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-(4-tert-butylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine
-
-
3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol
-
isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-(7-chloro-1-methoxy-2-naphthyl)-4-methyl-5-[2-(methylsulfonyl)phenyl]-4H-1,2,4-triazole
-
-
3-(7-chloro-1-methoxy-2-naphthyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
-
isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM
3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM
3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
-
-
3-benzyl-1-cyclohexylpyrrolidin-2-one
-
-
3-biphenyl-3-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-biphenyl-4-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
-
-
3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide
-
3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
-
3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide
-
-
3-chloro-2-methyl-N-[4-[2-(3-oxomorpholin-4-yl)ethyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide
BVT-3498
3-chloro-2-methyl-N-[4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1,3-thiazol-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-(2-morpholin-4-yl-2-oxoethyl)-pyridin-2-yl]-benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
-
3-chloro-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-((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-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-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
3-methylchrysazin
3-monoglucuronyl-glycyrrhetinic acid
-
3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
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-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
-
IC50 in the presence of NADP+: 0.12 mM, IC50 in the presence of NAD+: 5.6 mM; i.e. CHAPS
3-[(3R,5R)-tricyclo[3.3.1.13,7]dec-1-yl]-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
-
-
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one
moderate stability in liver microsomes
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(4-phenoxyphenyl)-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-phenyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[3-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1,3-thiazol-2-yl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1H-pyrrol-1-yl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluoro-4-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4'-fluorobiphenyl-4-yl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-fluorophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-iodophenyl)-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-[2-chloro-4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(cyclopropyloxy)phenyl]-4-methyl-4H-1,2,4-triazole
-
-
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzothiazol-2(3H)-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzoxazol-2(3H)-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-indol-2-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-4-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
-
-
3-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenol
-
-
3-[2,3-bis(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole
-
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole
-
3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
-
3-[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
3-[[(2-chlorophenyl)methyl]sulfanyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
-
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N,N-dimethyl benzamide
-
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N-methylbenzamide
-
3alpha,5alpha-tetrahydrocorticosterone
-
-
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
-
IC50 in the presence of NAD+: 0.000097 mM, IC50 in the presence of NADP+: 0.0003 mM; i.e. glycyrrhetinic acid
4'-chloro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-(6-cyclopropylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-(6-ethylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-cyano-N-[6-(ethylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
-
4'-cyano-N-[6-(methylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
-
4'-cyano-N-[6-(propan-2-yl)pyridin-2-yl]biphenyl-4-sulfonamide
-
-
4'-fluoro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4'-hydroxyflavanone
-
-
4'-methyl-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-((S)-2-acetamido-3-((R)-2-(adamantan-2-ylcarbamoyl)piperidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-((S)-2-acetamido-3-((R)-2-(azepane-1-carbonyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-((S)-2-acetamido-3-((S)-2-(adamantan-2-ylcarbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
4-(1-benzofuran-2-ylcarbonyl)-5-(2-fluorophenyl)-3-hydroxy-1-[5-[(4-methylbenzyl)sulfanyl]-1,3,4-thiadiazol-2-yl]-1,5-dihydro-2H-pyrrol-2-one
4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide
-
-
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N,N-diethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)benzamide
-
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
-
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N,N-dimethylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-benzylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-methylbenzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzamide
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid
-
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid methyl ester
-
4-(2-[1-[(2-fluorobenzene-1-sulfonyl)amino]cyclopropyl]-2-methylpropanamido)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
-
-
4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(4-butoxy-3-methylbenzyl)-3-hydroxy-5-(4-methylphenyl)-1-(pyridin-3-ylmethyl)-1,5-dihydro-2H-pyrrol-2-one
-
4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine
-
-
4-(cyclopentylsulfanyl)-3-[[1-(2,4-dichlorobenzamido)cyclopropyl]methoxy]-N-[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]-1,2-oxazole-5-carboxamide
-
4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-([(3R)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline
-
-
4-([(3S)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol
-
4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N,N-diethylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)benzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-methylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-propylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclohexylbenzamide
-
-
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclopentylbenzamide
-
-
4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole
-
4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
-
-
4-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
-
-
4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
-
4-fluoro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]phenyl]benzamide
-
-
4-methoxy-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
-
4-methyl-3,5-bis[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(2-methylnaphthalen-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(4-pentylbicyclo[2.2.2]oct-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(4-pentylphenyl)-5-phenyl-4H-1,2,4-triazole
-
-
4-methyl-3-(4-pentylphenyl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-(7-methylnaphthalen-2-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-naphthalen-2-yl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-tricyclo[3.3.1.13,7]dec-1-yl-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-[(3R,5R)-tricyclo[3.3.1.13,7]dec-1-yl]-4H-1,2,4-triazole
-
-
4-methyl-3-phenyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
4-methyl-3-[2-(trifluoromethoxy)phenyl]-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
potent and selective inhibitor of 11beta-HSD1
4-n-nonylphenol
-
-
4-n-octylphenol
-
-
4-nonylphenol
4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-propyl-N-[2-(thiophen-2-yl)ethyl]benzenesulfonamide
-
-
4-tert-butyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
-
4-tert-octylphenol
-
-
4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
-
4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
-
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid
-
-
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
-
-
4-[(E)-[(2Z)-2-[(2-chlorophenyl)imino]-4-oxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenyl benzoate
-
-
4-[(N-[4-[(dimethylamino)methoxy]benzene-1-sulfonyl]-2-methylalanyl)amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[([[(1S,3R,4R,7S)-4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]dec-1-yl]carbonyl]amino)methyl]benzoic acid
-
-
4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenol
-
-
4-[2-(1-[[(2-fluorobenzene-1-sulfonyl)amino]methyl]cyclopropyl)-2-methylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
-
4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
4-[3-(4-methoxyphenoxy)-3-methyl-2-oxobutyl]adamantane-1-carboxamide
-
4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
-
-
4-[4-(1-methyl-1H-benzimidazol-2-yl)piperazine-1-sulfonyl]benzoic acid
90% residual activity at 0.02 mM
4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-[4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
-
4-[4-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-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
high metabolic lability
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-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one
inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2
5,5-diethyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1,3-thiazol-4(5H)-one
-
-
5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole
-
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine
potent and metabolically stable inhibitor with about 200fold selectivity for isoform 11beta-HSD-1 versus isoform 11beta-HSD-2
5-(adamantan-1-ylcarbonyl)-4H,5H,6H,7H-thieno[3,2-c]pyridine
-
-
5-fluoro-1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
-
5-hydroxy-4-oxopentyl acetate
-
-
5-methyl-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
-
-
5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole
-
5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile
-
5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
-
5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
-
5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
-
5alpha-dihydrocorticosterone
-
-
6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol
-
6-bromo-2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
2.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
6-bromo-2-(bromomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
25% inhibition of isoform 11beta-HSD1 at 0.01 mM
6-bromo-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
32.35% inhibition of isoform 11beta-HSD1 at 0.01 mM
6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one
-
6-hydroxyflavanone
-
-
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
-
-
6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide
-
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
-
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
-
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
-
7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one
selective inhibitor for isoform 11beta-HSD1, 59.15% inhibition of isoform 11beta-HSD1 at 0.01 mM, 4.74% inhibition of isoform 11beta-HSD2 at 0.01 mM
7-(cyclohexylmethyl)-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
27.94% inhibition of isoform 11beta-HSD1 at 0.01 mM
7-chloro-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-ol
-
-
7-ethyl-2-(iodomethyl)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM
7-ethyl-2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
23.53% inhibition of isoform 11beta-HSD1 at 0.01 mM
7-hydroxy-2-(2-hydroxyethyl)-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
-
-
7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
-
-
7-keto,25-hydroxycholesterol
inhibits the oxoreduction of cortisone to cortisol by the recombinant isoform 11beta-HSD1
7-keto,27-hydroxycholesterol
potent inhibitor of the isoform 11beta-HSD1-dependent oxoreduction of cortisone
7-oxo-5alpha-androstane-3beta,17beta-diol
-
mixed type inhibition of cortisone reduction
7-oxo-dehydroepiandrosterone
-
mixed type inhibition of cortisone reduction
7-oxo-epiandrosterone
-
competitive type inhibition of cortisone reduction
7alpha,25-Dihydroxycholesterol
-
7alpha-hydroxy-dehydroepiandrosterone
-
competitive type inhibition of cortisol oxidation
7alpha-hydroxy-epiandrosterone
-
competitive type inhibition of cortisol oxidation
7beta,25-dihydroxycholesterol
-
7beta,27-dihydroxycholesterol
potent inhibitor of the isoform 11beta-HSD2-dependent oxidation of cortisol
7beta-hydroxy-dehydroepiandrosterone
-
competitive type inhibition of cortisol oxidation
7beta-hydroxy-epiandrosterone
-
mixed type inhibition of cortisol oxidation
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
shows excellent stability against cytochrome P450 metabolism
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
methyl substitution at the 8-position achieves an approximately 15fold improvement in potency over the non-substituted compound
8-benzyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1-thia-3,8-diazaspiro[4.5]dec-2-en-4-one
-
-
8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile
-
abietic acid
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
-
aloe emodin
-
-
Aloe-emodin
-
arylsulfoamidothiazole
-
arylsulfoamidothiazoles
specific, tight-binding inhibitors, inhibition mode and profiles
-
arylsulfonamidothiazole derivatives
-
specific for isozyme 11beta-HSD1
-
AZD-4017
selective inhibitor for isoform 11beta-HSD1
azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
-
-
BDE-100
-
inhibitor of isoform HSD11B2
BDE-153
-
inhibitor of isoform HSD11B2
benzenesulfonamide
-
-
benzothiazole derivatives
-
specific inhibition of isozyme 11beta-HSD1, inhibitory potency and IC50 values, overview, structure-activity relationship, introduction of a chlor atom at position 4 greatly enhances the inhibitory activity, inhibitory mechanism and enzyme/cofactor interaction analysis from molecular docking studies
-
BI-135585
-
bisphenol A
bortezomib
-
butylated hydroxyanisole
highly selective inhibitor of isoform 11beta-HSD2
BVT-14225
BVT-2733
-
-
BVT-528
competitive, tight-binding inhibition pattern
carbenoxolone
chenodeoxycholic acid
-
-
coffee
-
Coffea arabica fruit extract, corresponding to an italian espresso, inhibits recombinant and endogenous isozyme 11beta-HSD1 in HEK-293 cells up by 80% at 2% of extract, the inhibitory component is heat-stable with considerable polarity, extract blocks 11beta-HSD1-dependent cortisol formation in vivo preventing the subsequent nuclear translocation of the glucocorticoid receptor and abolishes glucocorticoid-induced expression of the key gluconeogenic enzyme phosphoenolpyruvate carboxykinase, at least part of the anti-diabetic effects of coffee consumption is due to inhibition of 11beta-HSD1-dependent glucocorticoid reactivation, overview, the inhibitory effect on isozyme 11beta-HSD1 is 7-10fold higher compared to isozyme 11beta-HSD2
-
curcumin
Cyclobutanone
-
-
danazol
competitive inhibition
di-n-butyl phthalate
-
-
dibenzoylmethane
-
-
dibutyltin
dicyclohexyl benzene-1,2-dicarboxylate
-
-
diethyldithiocarbamate
uncompetitive inhibition of isoform 11beta-HSD2
diethylhexyl adipate
diphenyltin
dipropyl phthalate
-
-
Disulfiram
emodin
endosulfan
-
-
enoxolone
-
epigallocatechin gallate
-
epigallocatechine-3-gallate
-
-
ethanone
-
-
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
-
-
ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
-
-
ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate
euphane-3beta,20-dihydroxy-24-ene
-
-
flavanone
-
-
fluoxymesterone
potent inhibitor of isoform 11beta-HSD2
Fusidic acid
-
-
glycyrrhetinic acid
glycyrrhizic acid
-
-
glycyrrhizin
-
glycyrrhizinic acid
-
-
glycyrrhizininc acid
-
-
gossypol
-
-
hydroxyitraconazole
-
INCB-13739
selective inhibitor for isoform 11beta-HSD1
indinavir
-
-
interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2
-
-
-
itraconazole
-
kansenone
-
-
kansuinone
-
-
maneb
methoxychlor
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
-
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'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
-
methyl 4-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)bicyclo[2.2.2]octane-1-carboxylate
-
-
methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate
-
-
methyl 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
-
-
methyl jasmonate
-
-
methyl {(1S,2S)-3-oxo-2-[(2Z)-pent-2-en-1-yl]cyclopentyl}acetate
-
weak inhibition
Momordica charantia extract
-
-
mono(2-ethylhexyl)phthalate
-
-
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'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide
-
-
N'-[(E)-(5-bromo-2-hydroxyphenyl)methylidene]-2-([5-[(phenylamino)methyl]-4-(prop-2-en-1-yl)-4H-1,2,4-triazol-3-yl]sulfanyl)propanehydrazide
-
-
N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide
N-(4-biphenyl-4-yl-1,3-oxazol-2-yl)benzenesulfonamide
-
-
N-(4-chloro-2-methyl-1,3-benzothiazol-5-yl)adamantane-1-carboxamide
-
-
N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-3-(trifluoromethyl)benzenesulfonamide
-
-
N-(5-cyanotricyclo[3.3.1.1~3,7~]decan-2-yl)-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide
-
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide
-
N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide
-
-
N-(6-methylpyridin-2-yl)-2-(trifluoromethyl)benzenesulfonamide
-
-
N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide
-
-
N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
-
N-(6-methylpyridin-2-yl)naphthalene-1-sulfonamide
-
-
N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide
-
-
N-(furan-2-ylmethyl)-N-methyladamantane-1-carboxamide
-
-
N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
-
-
N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-acetyl-beta-alanyl-N-adamantan-1-yl-D-prolinamide
-
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-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
-
-
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
-
N-cyclohexyl-6-(piperidin-1-yl)picolinamide
-
N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
-
N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
-
N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
-
N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
-
N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
potent 11beta-HSD1 inhibitor
N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
-
N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine
-
-
N-methyl-N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
-
-
N-methyl-N-(thiophen-3-ylmethyl)adamantane-1-carboxamide
-
-
N-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
-
-
N-methyl-N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
-
-
N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
-
-
N-[(1R,2R,7S)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]acetamide
-
-
N-[(1R,2R,7S)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamide
-
-
N-[(1S,2R,3R,5S,7R)-1,5-dihydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamide
-
-
N-[(1S,2R,3R,5S,7R)-1,5-dihydroxytricyclo[3.3.1.13,7]dec-2-yl]-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamide
-
-
N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide
-
N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide
N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
-
-
N-[3-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
-
N-[3-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
-
N-[3-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
-
N-[3-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
-
N-[3-hydroxy-4-(piperidin-1-ylcarbonyl)phenyl]-3,4,5-trimethoxybenzamide
-
-
N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-[4-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-chloro-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-fluoro-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-methyl-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-chloro-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-methyl-phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethylamino)phenyl]acetamide
-
N-[4-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
-
N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
N-[4-[(2,6-dimethylpyrimidin-4-yl)sulfamoyl]phenyl]-4-[oxo(phenyl)acetyl]benzamide
-
-
N-[5-(2-amino-2-oxoethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-[5-(3-amino-3-oxopropyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-[5-(cyanomethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
-
-
N-[6-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]-3-chloro-2-methylbenzenesulfonamide
-
-
N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
-
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
-
-
NSC 112288
-
-
NSC 56412
-
-
NSC 75617
-
-
oxymesterone
-
oxymetholone
-
perfluorohexane sulfonate
-
perfluorohexanesulfonate
-
-
perfluorooctane sulfonate
-
Perfluorooctanoic acid
perfluorooctyl sulfonate
-
-
PF-877423
posaconazole
-
progesterone
-
-
pyrrolidine dithiocarbamate
quercetin
-
resorcinol
-
weak inhibition
resveratrol
-
-
rheochrysidin
rosiglitazone
-
-
saquinavir
-
-
sterenin A
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin B
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin C
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
sterenin D
-
isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205
T0504
testosterone
-
thiram
tributyltin
Triphenyltin
TZD 2
-
-
UE2343
selective inhibitor for isoform 11beta-HSD1
zearalenone
zineb
[(1R,3r,5S)-3-hydroxy-3-(pyrimidin-2-yl)-8-azabicyclo[3.2.1]octan-8-yl][5-(1H-pyrazol-4-yl)thiophen-3-yl]methanone
selective inhibitor for isoform 11beta-HSD1
[1-[2-(cyclohexylamino)-2-oxoethyl]cyclopentyl]acetic acid
13% inhibition at 0.001 mM
[1-[2-(octahydroisoquinolin-2(1H)-yl)-2-oxoethyl]cyclopentyl]acetic acid
34% inhibition at 0.001 mM
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethyl]cyclopentyl]acetic acid
8% inhibition at 0.001 mM
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid
-
[1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol
-
-
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
lead compound for high throughput screening of inhibitors. A hydrophobic group at C-2 position dramatically enhances potency
[3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone
-
-
[4-(1H-benzimidazol-2-yl)piperazin-1-yl](4-methylphenyl)methanone
65% residual activity at 0.02 mM
[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid
-
[4-(2-Adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid methyl ester
-
[4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone
-
-
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
potent inhibitor with a high permeability value, and low metabolic lability in mouse and human microsomes
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
good in vitro potency for the human enzyme while exhibiting enhanced metabolic stability in liver microsomes compared to lead compound [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone
-
-
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
-
-
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
D-glucose 6-phosphate
stimulates isoform 11beta-HSD1 reductase activity in liver but not in testis
dexamethasone
-
after application of dexamethasone, 11beta-HSD1 mRNA increases in muscle of both diabetic and control subjects, whereas 11beta-HSD2 mRNA decreases. 11beta-HSD1 activity increases in diabetic subjects, but not in controls, whereas 11beta-HSD2 activity does not change in either group
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
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00031
11-Dehydrocorticosterone
-
37°C, pH 7.4, in HEK-293 lysates expressing 11beta-HSD1
0.0014 - 0.0102
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione
0.000034
11beta,21-dihydroxypregn-4-en-3,20-dione
-
pH and temperature not specified in the publication
0.000685
11beta-hydroxyandrostenedione
isoform 11betaHSD2, pH and temperature not specified in the publication
0.000023
11beta-hydroxyprogesterone
isoform 11betaHSD2, pH and temperature not specified in the publication
0.000147
11beta-hydroxytestosterone
isoform 11betaHSD2, pH and temperature not specified in the publication
0.0038 - 0.0095
17,21-dihydroxy-pregn-4-ene-3,11,20-trione
0.02
2,3-benzoylphenyl-propanoic acid
-
microsomal fraction from transformed Pichia pastoris strain with human enzyme
0.581 - 0.961
5,5-dimethyl-3-(3-fluorphenyl)-4-(4-methylsulphonyl)phenyl-2-(5H-furanone)-lactol
0.0012
5alpha-androstane-3beta,7alpha,17beta-triol
-
pH 7.4, 28°C
0.021
5alpha-androstane-3beta,7beta,17beta-triol
-
pH 7.4, 28°C
0.000039
7-keto,27-hydroxycholesterol
isoform 11beta-HSD1, at pH 7.4, temperature not specified in the publication
0.0051 - 0.0068
7-oxo-5alpha-androstane-3beta,17beta-diol
0.00049
7-oxocholesterol
-
37°C, pH 7.4, in HEK-293 lysates expressing 11beta-HSD1
0.000029 - 0.000556
7beta,25-dihydroxycholesterol
0.000056
7beta,27-dihydroxycholesterol
isoform 11beta-HSD2, at pH 7.4, temperature not specified in the publication
0.00074
7beta-hydroxycholesterol
-
37°C, pH 7.4, in HEK-293 lysates expressing 11beta-HSD1
0.0003 - 0.043
corticosterone
0.00034 - 0.1
cortisol
0.0003 - 0.1
cortisone
0.02
dehydrocorticosterone
-
37°C, pH 7.4, Hill coefficient of 2.7
0.37
metapyrone
-
microsomal fraction from transformed Pichia pastoris strain with human enzyme
0.0000102
NAD+
-
isoform 11beta-HSD2, kidney homogenate
0.0000063 - 0.00042
NADP+
0.042
oracin
-
-
additional information
additional information
-
the glucocorticoid and xenobiotic reductase activities show cooperative kinetics
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.042 - 0.19
cortisol
0.4
cortisone
-
37°C, pH 7.4, recombinant 11beta-HSD1 expressed in Escherichia coli
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000064
(+/-)-2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000034
(+/-)-2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000024
(+/-)-2-(1-adamantylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000024
(+/-)-2-(1-adamantylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000082
(+/-)-2-(cycloheptylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000032
(+/-)-2-(cycloheptylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000126
(+/-)-2-(cyclohexylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000055
(+/-)-2-(cyclohexylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000047
(+/-)-2-(cyclooctylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000028
(+/-)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000073
(+/-)-5-ethyl-5-methyl-2-(1-norbornylamino)-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000013
(+/-)-5-ethyl-5-methyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000372
(+/-)-5-ethyl-5-methyl-2-(7-norbornylamino)-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000058
(+/-)-5-ethyl-5-methyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000025
(+/-)-5-methyl-2-(1-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000012
(+/-)-5-methyl-2-(3-noradamantylamino)-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000149
(+/-)-5-methyl-2-(7-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000038
(+/-)-5-methyl-5-propyl-2-[(2,2,3,3-tetramethylcyclopropyl)amino]-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.01874 - 0.02268
(-)-epigallocatechin 3-gallate
0.0000472
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.00077
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.0000306
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.000329
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.0000278
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.000227
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.0000128
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.000012
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.000028
2-(1-adamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
pH and temperature not specified in the publication
0.00002
2-(1-adamantylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.000003
2-(3-noradamantylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
pH and temperature not specified in the publication
0.000287
2-(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)-N,N-diethylacetamide
-
pH not specified in the publication, temperature not specified in the publication
0.000058
2-(bicyclo[2.2.1]hept-2-ylamino)-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.000014
2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one
pH and temperature not specified in the publication
0.000026
2-(cyclooctylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.0000173
2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
pH not specified in the publication, temperature not specified in the publication
0.000169
3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.000169
3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.0000058
4'-chloro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.0000019
4'-cyano-N-(6-cyclopropylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.0000066
4'-cyano-N-(6-ethylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.000004
4'-cyano-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.0000048
4'-cyano-N-[6-(ethylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.0000098
4'-cyano-N-[6-(methylamino)pyridin-2-yl]biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.0000017
4'-cyano-N-[6-(propan-2-yl)pyridin-2-yl]biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.00002
4'-fluoro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.000062
4'-methyl-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.000013
5,5-diethyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one
pH and temperature not specified in the publication
0.00005
arylsulfoamidothiazole
-
0.0000049 - 0.000014
glycyrrhetinic acid
0.000108
N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.000048
N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
0.000084
N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide
-
pH not specified in the publication, temperature not specified in the publication
additional information
N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide
-
Ki below 0.000001 mM, pH not specified in the publication, temperature not specified in the publication
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.05799 - 0.1312
(-)-epigallocatechin 3-gallate
0.0012
(1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
Homo sapiens
-
0.000018
(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid
Homo sapiens
at 37°C, pH not specified in the publication
0.003
(11beta)-11-hydroxyallopregnanolone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.0056
(11beta)-11-hydroxyprogesterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.0000037
(1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.001
(1r,4s)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
(1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
Homo sapiens
IC50 above 0.001 mM, in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000015
(1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000002
(1S,3R,4S,5S,7S)-4-(3-(2-fluorophenylsulfonamido)-3-methylbutanamido) adamantane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(2,3-dichlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(2,3-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(2,4-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001 - 0.000002
(1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
0.000002
(1s,4r)-4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000007
(1s,4r)-4-[3-[(3,5-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(3-chloro-2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000057
(1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(3-chlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
(1s,4r)-4-[3-[(3-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000001
(1s,4r)-4-[3-[(4-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000254
(2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.003 - 0.112
(2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate
0.005 - 0.2
(2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate
0.000031
(2R)-1-(2-chloro-4-(2-methoxyethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000018
(2R)-1-(2-chloro-4-(difluoromethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000063
(2R)-1-(2-chloro-4-ethoxyphenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000017
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxamide
Homo sapiens
at 37°C
0.00001
(2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxylic acid
Homo sapiens
at 37°C
0.00001
(2R)-1-(3-chloro-4-([4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazin-1-yl]sulfonyl)phenyl)piperidin-4-ol
Homo sapiens
at 37°C
0.00001
(2R)-1-(4-bromo-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000028
(2R)-1-(4-bromophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.00004
(2R)-1-(4-tert-butoxy-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000639
(2R)-1-([2-chloro-4-[(3S)-3-methylpiperazin-1-yl]phenyl]sulfonyl)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000097
(2R)-1-[(2-chloro-4-piperidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000011
(2R)-1-[(2-chloro-4-pyrrolidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000003
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000113
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000034
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000053
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000001
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000094
(2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000015
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-N,N-dimethylpiperidin-4-amine
Homo sapiens
at 37°C
0.000018
(2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
Homo sapiens
at 37°C
0.00001
(2R)-1-[[2-chloro-4-(1H-1,2,4-triazol-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000074
(2R)-1-[[2-chloro-4-(4,4-difluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.00005
(2R)-1-[[2-chloro-4-(4-fluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.000136
(2R)-1-[[2-chloro-4-(4-methylpiperazin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine
Homo sapiens
at 37°C
0.00003
(2R)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000016
(2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000036
(2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000092
(2R)-2-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenoxy)-N,N-dimethylethanamine
Homo sapiens
at 37°C
0.000004
(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000015
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)-N,N-dimethylaniline
Homo sapiens
at 37°C
0.000016
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
Homo sapiens
at 37°C
0.00005
(2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenol
Homo sapiens
at 37°C
0.00001
(2R)-3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)benzamide
Homo sapiens
at 37°C
0.000011
(2R)-4-(3-fluoro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)morpholine
Homo sapiens
at 37°C
0.000063
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzamide
Homo sapiens
at 37°C
0.00001
(2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile
Homo sapiens
at 37°C
0.00002
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-1-(4-methoxyphenylsulfonyl)-2-methylpiperazine
Homo sapiens
at 37°C
0.000023
(2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methyl-1-(4-(trifluoromethoxy)-phenylsulfonyl)-piperazine
Homo sapiens
at 37°C
0.000185
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine
Homo sapiens
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
Homo sapiens
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one
Homo sapiens
at 37°C
0.00001
(2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]thiomorpholine-1,1-dioxide
Homo sapiens
at 37°C
0.000019
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(4-piperidin-1-ylphenyl)sulfonyl]piperazine
Homo sapiens
at 37°C
0.000674
(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine
Homo sapiens
at 37°C
0.0000012
(2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000015
(2R)-N-(tricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000037
(2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000031
(2R)-N-[(1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000115
(2R)-N-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide
Homo sapiens
at 37°C
0.000056 - 0.012
(2R,4aR,6aS,6bR,10S,12aS)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-1,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,14b-octadecahydropicen-13(2H)-one
0.0000619
(3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.0007 - 0.008
(3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one
0.007138
(3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000049
(3beta)-3-hydroxy-18,29-epoxyolean-12-ene-11,29-dione
Homo sapiens
pH 7.4, 37°C
0.000025
(3beta)-3-[(3-carboxypropanoyl)oxy]urs-12-en-28-oic acid
Homo sapiens
pH 7.4, 37°C
0.001157
(3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
Homo sapiens
pH not specified in the publication, 37°C
0.000825
(3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000626
(3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
Homo sapiens
pH not specified in the publication, 37°C
0.001012
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
Homo sapiens
pH not specified in the publication, 37°C
0.000929
(3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
Homo sapiens
pH not specified in the publication, 37°C
0.0000427
(3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.002 - 0.2
(3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol
0.002 - 0.2
(3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol
0.000049 - 0.016
(3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one
0.011 - 0.074
(3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate
0.009 - 0.2
(3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate
0.000122 - 0.025
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al
0.000008 - 0.000012
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.001 - 0.068
(3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate
0.2
(3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate
0.001508
(3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000053
(3R)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.000089
(3S)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.0148
(4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000388
(4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001
(4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decan-1-yl)acetic acid
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000074 - 0.016
(5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al
0.0000008
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(2',4'-difluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
Homo sapiens
pH 7.4, 22°C, microsomal assay
0.0000005
(6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one
Homo sapiens
pH 7.4, 22°C, microsomal assay
0.000197
(R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.000266
(R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.000902
(R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.000062
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.001505
(R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000568
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000885
(R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000373
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
Homo sapiens
at pH 7.4 and 37°C
0.0000286
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000931
(S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000101
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000153
(S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000094
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000025
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000022
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0021
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine]
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000005
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000006
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000005
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000006
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000008
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000004
1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00001
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000013
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000022
1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000012
1-(((R)-3-methyl-4-(4-((S)-1,1,1-trifluoro-2-hydroxypropan-2-yl)phenylsulfonyl)-piperazin-1-yl)methyl)-cyclopropanecarboxamide
Homo sapiens
in PBS buffer, at 37°C
0.0058
1-(2,4-dichlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)-ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000116
1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
Homo sapiens
pH 7.0, 22°C, cellular assay
0.000012
1-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)-2-methyl-1H-benzimidazole
Homo sapiens
-
-
0.0064
1-(4-chlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000008
1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol
Homo sapiens
pH and temperature not specified in the publication
0.002975
1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000171
1-adamantan-1-yl-2-(2,4-dichloro-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000122
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000128
1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000302
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-ylamino)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.004755
1-adamantan-1-yl-2-(2-methylbenzothiazol-5-yloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000339
1-adamantan-1-yl-2-(3,4-dimethoxy-benzyloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.009379
1-adamantan-1-yl-2-(3,4-dimethoxy-phenoxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.001438
1-adamantan-1-yl-2-(4-chloro-benzenesulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.001
1-adamantan-1-yl-2-(4-chloro-phenoxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000231
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00135
1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00081
1-adamantan-1-yl-2-(4-chloro-phenylsulfanyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000296
1-adamantan-1-yl-2-(4-methoxy-benzyloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.002069
1-adamantan-1-yl-2-(4-methylbenzyloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.002017
1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.005236
1-adamantan-1-yl-2-(4-trifluoromethyl-phenoxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.0049
1-adamantan-1-yl-2-(biphenyl-4-yloxy)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000443
1-adamantan-1-yl-2-(toluene-4-sulfinyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.000668
1-adamantan-1-yl-2-(toluene-4-sulfonyl)ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00251
1-adamantan-1-yl-2-p-tolyloxy-ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.00672
1-adamantan-1-yl-2-p-tolylsulfanyl-ethanone
Homo sapiens
pH not specified in the publication, 37°C
0.0007
1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.000012
1-methyl-4-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
Homo sapiens
-
-
0.00000098
1-methyl-4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]-1H-indole
Homo sapiens
-
-
0.000963
1-methyl-5-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole
Homo sapiens
-
-
0.000257
1-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone
Homo sapiens
pH 7.0, 22°C, cellular assay
0.000007
1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
1-[(2-chlorobenzyl)oxy]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000005
1-[(2-chlorobenzyl)sulfanyl]-3-hydroxy-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000002
1-[(2-chlorobenzyl)sulfanyl]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000013
1-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.00000003
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.0000004
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000016
1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
0.00001
1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000004
1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000004
1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00011
1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0001
1-[1-[(3,4-dimethylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
1-[1-[(3-amino-4-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0003
1-[1-[(3-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000079
1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000007
1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000003
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000017
1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000002
1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
Homo sapiens
-
pH and temperature not specified in the publication
0.00065 - 0.05
11-oxo-3alpha,5alpha-tetrahydrotestosterone
0.0008
11-oxo-allopregnanolone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.021
11-oxo-androstenedione
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.0095
11-oxo-progesterone
Homo sapiens
-
pH 8.4, 37°C
0.018
11-oxo-testosterone
Homo sapiens
-
reductase reaction, pH 8.4, 37°C
0.005 - 0.0115
11beta-hydroxy-androstanediol
0.009
11beta-hydroxy-testosterone
Homo sapiens
-
dehydrogenase reaction, pH 8.4, 37°C
0.002214
18alpha-glycyrrhetinic acid
Homo sapiens
37°C, pH not specified in the publication
0.000779
18beta-glycyrrhetinic acid
Homo sapiens
37°C, pH not specified in the publication
0.000027
2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0032
2,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzenesulfonamide
Homo sapiens
-
at 37°C
0.000016
2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000009
2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000009
2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000018
2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000017
2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000048
2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000029
2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.01
2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000015
2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000052
2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00003
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000028
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000031
2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000001
2-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Homo sapiens
-
-
0.0000011
2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.034
2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00026
2-(4-methylphenyl)-2-oxoethyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoate
Homo sapiens
-
pH and temperature not specified in the publication
0.00035
2-(adamantan-1-yl)-N-methyl-N-(thiophen-3-ylmethyl)acetamide
Homo sapiens
-
-
0.036
2-(allylamino)-1-thia-3-azaspiro[4.3]oct-2-en-4-one
Homo sapiens
isoform 11beta-HSD1, at pH 7.4 and 37°C
0.0025
2-(allylamino)-1-thia-3-azaspiro[4.5]dec-2-en-4-one
Homo sapiens
isoform 11beta-HSD1, at pH 7.4 and 37°C
0.05
2-(allylamino)-5-(4-bromophenyl)thiazol-4(5H)-one
Homo sapiens
IC50 above 0.05 mM, isoform 11beta-HSD1, at pH 7.4 and 37°C
0.000308
2-adamantan-1-yl-N-methyl-N-thiophen-2-ylmethyl-acetamide
Homo sapiens
-
-
0.00888
2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane
Homo sapiens
37°C, pH not specified in the publication, microsomal assay
0.05557
2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane
Homo sapiens
pH and temperature not specified in the publication
0.00357
2-bromo-N-[2-([2-oxo-2-[(2-phenylethyl)amino]ethyl]sulfanyl)-2,3-dihydro-1,3-benzothiazol-6-yl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00113
2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000005
2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000092
2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000252
2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000126
2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000027
2-[(2-chlorobenzyl)sulfanyl]-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.0000001
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000011
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000547
2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000006
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000078
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000222
2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.00045
2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00141
2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000019
2-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
Homo sapiens
37°C, pH not specified in the publication, cellular assay
0.000031
2-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfonyl]-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
Homo sapiens
37°C, pH not specified in the publication, cellular assay
0.000048
2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000012
2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide
Homo sapiens
pH and temperature not specified in the publication
0.00016
2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000019
2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00034
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00006
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.003
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine
Homo sapiens
IC50 above 0.003 mM, isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000591
2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000017
2-[4-(2,6-difluorobenzenesulfonyl)-[1,4]diazepan-1-yl]-1-(octahydroquinolin-1-yl)-ethanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000058
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N,N-dimethyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000472
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-benzyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000912
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-ethyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000094
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-methyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.002194
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-phenyl-acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000204
2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.0185
2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0272
2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0042
2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.02
2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0048
2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.0064
2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole
Homo sapiens
pH and temperature not specified in the publication
0.000005
2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000011
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000009
2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000018
2-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000006
2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000003
2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000619
3,11-dioxoolean-12-en-30-oic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000057
3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000008
3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000134
3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000013
3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000012
3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000011
3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000019
3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000023
3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000024
3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000007
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000021
3,5-bis(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000029
3,5-bis(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0032
3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide
Homo sapiens
-
at 37°C
0.0000016
3-(1-(4-fluorophenyl)cyclopropyl)-4-isopropyl-5-(4-(trifluoromethoxy)phenyl)-4H-1,2,4-triazole
Homo sapiens
in PBS buffer, at 37°C
0.0000043
3-(1-fluoronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
IC50 below 0.000001 mM
0.000001 - 0.000008
3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000013 - 0.0001
3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000012
3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000008 - 0.000172
3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.0000087
3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid
Homo sapiens
at 37°C, pH not specified in the publication
0.000032
3-(2,3-difluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000013
3-(2,4-dichlorophenyl)-4-methyl-5-(2-nitrophenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.00009
3-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00002
3-(2,4-dichlorophenyl)-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000057
3-(2-adamantan-1-yl-2-oxoethanesulfinyl)-N,N-dimethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000069
3-(2-adamantan-1-yl-2-oxoethanesulfonyl)-N,N-dimethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000527
3-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000343
3-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000229
3-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.001222
3-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000068
3-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000876
3-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.001047
3-(2-adamantan-1-yl-2-oxoethoxy)benzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000153
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000078
3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester
Homo sapiens
pH not specified in the publication, 37°C
0.000002
3-(2-bromophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(2-bromophenyl)-5-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000026
3-(2-chloro-4-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000058
3-(2-chloro-4-fluorophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000077
3-(2-chlorophenyl)-4-methyl-5-(4-pentylphenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.000043
3-(2-chlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000031
3-(2-chlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0002
3-(2-chlorophenyl)-5-(3,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000028
3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000088
3-(2-chlorophenyl)-5-[2-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000089
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Homo sapiens
-
-
0.000001
3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000029
3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000068
3-(4-benzylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(4-butyl-2-methylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
IC50 below 0.000001 mM
0.00026
3-(4-butylphenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000023
3-(4-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000015
3-(4-chloro-2-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000027
3-(4-chloro-3-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.00063
3-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000027
3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000014
3-(4-tert-butylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
IC50 below 0.000001 mM
0.00074
3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000043
3-biphenyl-3-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000011
3-biphenyl-4-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.002631
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-4-fluorobenzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001672
3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.01449
3-chloro-N-[4-(morpholin-4-ylcarbonyl)benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000647
3-chloro-N-[4-(piperidin-1-ylcarbonyl)benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001733
3-chloro-N-[4-(pyrrolidin-1-ylcarbonyl)benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0159
3-chloro-N-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000013
3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00001
3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000014
3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00354
3-methylchrysazin
Homo sapiens
pH 7.4, 37°C
0.000016
3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000078
3-tricyclo[3.3.1.13,7]dec-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
Homo sapiens
-
-
0.00008
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-1-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.000004
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide
Homo sapiens
pH and temperature not specified in the publication
0.00019
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cycloheptyl-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.00039
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cyclohexyl-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.000054
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-(methanesulfonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.000004
3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide
Homo sapiens
pH and temperature not specified in the publication
0.12
3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate
Homo sapiens
-
pH and temperature not specified in the publication
0.000002 - 0.000199
3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000016
3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000027
3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000078
3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000114
3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one
Homo sapiens
pH 7.0, 22°C, cellular assay
0.000002 - 0.000019
3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000052
3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.00001 - 0.000057
3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000035 - 0.000107
3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
0.000005
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.000026
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(4-phenoxyphenyl)-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000017
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000023
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000002
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[3-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000044
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1,3-thiazol-2-yl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000003
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1H-pyrrol-1-yl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000013
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000093
3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001 - 0.000014
3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000002
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000027
3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000003
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluoro-4-methoxyphenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000011
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4'-fluorobiphenyl-4-yl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000015
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-fluorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000038
3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-iodophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[1-(4-chlorophenyl)cyclobutyl]-5-[2-chloro-4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000035
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000022
3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(cyclopropyloxy)phenyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000032 - 0.000454
3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000041
3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.00023
3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000003 - 0.000037
3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000027 - 0.000494
3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000008 - 0.000018
3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000019
3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000015 - 0.000374
3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000025
3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000001 - 0.000332
3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000043 - 0.000061
3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol
0.00017
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzothiazol-2(3H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00027
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzoxazol-2(3H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00024
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-indol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00014
3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-4-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000005 - 0.000355
3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.000002 - 0.000115
3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
0.0000036
3-[2,3-bis(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000014
3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000012
3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000079
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000043
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000012
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000014
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000096
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000048
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000086
3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000087
3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000015
3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000001
3-[2-chloro-4-(1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000069
3-[2-chloro-4-(2,4-dimethyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000098
3-[2-chloro-4-(2-cyclopropyl-4-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000026
3-[2-chloro-4-(2-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000039
3-[2-chloro-4-[2-(methylsulfanyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000014
3-[2-chloro-4-[2-(methylsulfonyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000028
3-[2-chloro-4-[3-(ethylsulfonyl)propyl]phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000011
3-[3-chloro-2'-(ethylsulfanyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[3-chloro-2'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[3-chloro-3'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[3-chloro-3'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000021
3-[3-chloro-4'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000017
3-[3-chloro-4'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.00000098
3-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000013
3-[4-chloro-2-(trifluoromethyl)phenyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000028
3-[4-[2-(ethylsulfonyl)ethyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000034
3-[4-[3-(ethylsulfonyl)propyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000001
3-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000005 - 0.000016
3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
0.000022 - 0.000038
3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole
0.000146
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N,N-dimethyl benzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000124
3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N-methylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.0013 - 0.05
3alpha,5alpha-tetrahydrocorticosterone
0.0003
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000496
4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
Homo sapiens
at pH 7.4 and 37°C
0.0000012
4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000002 - 0.0000026
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000798
4-(2-adamantan-1-yl-2-oxoethoxy)-N,N-diethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.001959
4-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000382
4-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000594
4-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000283
4-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.00114
4-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000117
4-(2-adamantan-1-yl-2-oxoethoxy)benzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000074
4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000056
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N,N-dimethylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.00025
4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-methylbenzamide
Homo sapiens
pH not specified in the publication, 37°C
0.000359
4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid
Homo sapiens
pH not specified in the publication, 37°C
0.000025
4-(2-[1-[(2-fluorobenzene-1-sulfonyl)amino]cyclopropyl]-2-methylpropanamido)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
Homo sapiens
-
-
0.000012
4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00001
4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000008
4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000026
4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000107
4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.001
4-([(3R)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000073
4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001
4-([(3S)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.00064
4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000152
4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol
Homo sapiens
pH and temperature not specified in the publication
0.000008
4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.002106
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N,N-diethylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000014
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)benzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000638
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-methylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000002
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-propylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000049
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000411
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclohexylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.008512
4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclopentylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000022
4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.00408
4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.002698
4-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000051
4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000051
4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.003
4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
Homo sapiens
IC50 above 0.003 mM, isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0000046
4-methyl-3-(2-methylnaphthalen-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.00025
4-methyl-3-(4-pentylphenyl)-5-phenyl-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000052
4-methyl-3-(4-pentylphenyl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000009
4-methyl-3-(7-methylnaphthalen-2-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.000026
4-methyl-3-naphthalen-2-yl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000078
4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000037
4-methyl-3-phenyl-5-tricyclo[3.3.1.13,7]dec-1-yl-4H-1,2,4-triazole
Homo sapiens
-
-
0.000027
4-methyl-3-phenyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
0.0000013
4-methyl-3-[2-(trifluoromethoxy)phenyl]-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
Homo sapiens
-
-
49.3
4-nonylphenol
Homo sapiens
-
inhibition of liver isozyme 11beta-HSD1, pH 7.4, 37°C
0.00019
4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000008
4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.0000023
4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.00072
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00004
4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00195
4-[(E)-[(2Z)-2-[(2-chlorophenyl)imino]-4-oxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenyl benzoate
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[(N-[4-[(dimethylamino)methoxy]benzene-1-sulfonyl]-2-methylalanyl)amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000282
4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000006
4-[2-(1-[[(2-fluorobenzene-1-sulfonyl)amino]methyl]cyclopropyl)-2-methylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000343
4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.0002
4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.001
4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000102
4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.000014
4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
Homo sapiens
pH and temperature not specified in the publication
0.00001
4-[4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine
Homo sapiens
at 37°C
0.0000039
4-[4-methyl-5-(1-methyl-1H-indol-4-yl)-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000009
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2,3,3-tetramethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000037
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00000098
4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indole
Homo sapiens
-
-
0.000002
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]-2-fluorophenol
Homo sapiens
-
-
0.00000034
4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol
Homo sapiens
-
-
0.000014
4-[[2-methyl-N-(2,4,5-trifluorobenzene-1-sulfonyl)alanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
4-[[N-(2,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
4-[[N-(2,6-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000001
4-[[N-(2-chloro-4-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000006
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000002
4-[[N-(3,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[[N-(3,5-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[[N-(3-chloro-2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000001
4-[[N-(3-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
4-[[N-(4-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000044
4-[[N-(4-hydroxybenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
4-[[N-(4-tert-butylbenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
4-[[N-(benzenesulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000449
5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.000012
5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000435
5-(adamantan-1-ylcarbonyl)-4H,5H,6H,7H-thieno[3,2-c]pyridine
Homo sapiens
-
-
0.0002
5-fluoro-1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000085
5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.000095
5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile
Homo sapiens
isoform 11beta-HSD1, at pH 6.6 and 25°C
0.000052
5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.0000048
5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.000002
5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
Homo sapiens
pH and temperature not specified in the publication
0.0021 - 0.0063
5alpha-dihydrocorticosterone
0.0000068
6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000039
6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000032
6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000032
6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.001929
6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol
Homo sapiens
pH and temperature not specified in the publication
0.0025
6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000057
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide
Homo sapiens
pH 7.4, 37°C
0.000375
6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide
Homo sapiens
pH 7.4, 37°C
0.0000066
6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000041
6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000028
6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000031
6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000019
6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0069
7-(cyclohexylmethyl)-2-iodomethyl-2,3-dihydrothiazolo[3,2-a]pyrimidin-5-one
Homo sapiens
isoform 11beta-HSD1, at pH 7.4 and 37°C
0.000089
7-chloro-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-ol
Homo sapiens
-
-
0.00024
7-hydroxy-2-(2-hydroxyethyl)-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00023
7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000049 - 0.000405
7-keto,25-hydroxycholesterol
0.000015 - 0.000357
7-keto,27-hydroxycholesterol
0.000091 - 0.003
7beta,25-dihydroxycholesterol
0.000011 - 0.003
7beta,27-dihydroxycholesterol
0.000003
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000089
8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000012
8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile
Homo sapiens
22°C, pH not specified in the publication, assay on microsomes
0.000879
Aloe-emodin
Homo sapiens
pH 7.4, 37°C
0.000007
AMG-221
Homo sapiens
pH and temperature not specified in the publication
0.0000025
azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.01197
BDE-100
Homo sapiens
-
pH and temperature not specified in the publication
0.00441
BDE-153
Homo sapiens
-
pH and temperature not specified in the publication
0.01481
bisphenol A
Homo sapiens
pH and temperature not specified in the publication
0.01399
butylated hydroxyanisole
Homo sapiens
pH and temperature not specified in the publication
0.000052
BVT-14225
Homo sapiens
-
isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2, pH and temperature not specified in the publication
0.0005
carbenoxolone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00074
danazol
Homo sapiens
pH and temperature not specified in the publication
0.00195
dibutyltin
Homo sapiens
pH and temperature not specified in the publication
0.0017
diethyldithiocarbamate
Homo sapiens
pH and temperature not specified in the publication
49.4
diethylhexyl adipate
Homo sapiens
-
inhibition of liver isozyme 11beta-HSD1, pH 7.4, 37°C
0.00142
diphenyltin
Homo sapiens
pH and temperature not specified in the publication
0.000128
Disulfiram
Homo sapiens
pH and temperature not specified in the publication
0.000186
emodin
Homo sapiens
pH 7.4, 37°C
0.000068 - 0.2
ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.003
ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0045
ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00006
fluoxymesterone
Homo sapiens
pH and temperature not specified in the publication
0.000256 - 0.000778
glycyrrhetinic acid
0.00001
glycyrrhizic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000186
glycyrrhizinic acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0000186
glycyrrhizininc acid
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000187
hydroxyitraconazole
Homo sapiens
at pH 7.4 and 37°C
0.000122
itraconazole
Homo sapiens
at pH 7.4 and 37°C
0.000753
maneb
Homo sapiens
pH and temperature not specified in the publication
0.00191
methoxychlor
Homo sapiens
37°C, pH not specified in the publication, microsomal assay
0.000061 - 0.2
methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate
0.000038
methyl 2-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Homo sapiens
-
-
0.0000019
methyl 2-[5-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Homo sapiens
-
-
0.000005 - 0.00002
methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
0.000031
methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00005
methyl 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate
Homo sapiens
-
-
0.00528
N-(4-chloro-2-methyl-1,3-benzothiazol-5-yl)adamantane-1-carboxamide
Homo sapiens
-
-
0.001208
N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-3-(trifluoromethyl)benzenesulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.001
N-(5-cyanotricyclo[3.3.1.1~3,7~]decan-2-yl)-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000038 - 0.0000072
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide
0.0000017
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000037
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000027
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000095
N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000249
N-(furan-2-ylmethyl)-N-methyladamantane-1-carboxamide
Homo sapiens
-
-
0.000403
N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
Homo sapiens
-
-
0.000027
N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000084
N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide
Homo sapiens
pH 7.4, 37°C
0.000047
N-butyl-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000143
N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide
Homo sapiens
pH 7.4, 37°C
0.000058
N-cyclohexyl-6-(piperidin-1-yl)picolinamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000008
N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000017
N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00015
N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.001
N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
Homo sapiens
IC50 above 0.001 mM, in 30 mM HEPES buffer, pH 7.4, at 37°C
0.00055
N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000008
N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.0000046
N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000018
N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000064
N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.000021
N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000014
N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000013
N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000037
N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide
Homo sapiens
at 37°C, pH not specified in the publication
0.0000014
N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine
Homo sapiens
-
-
0.000229
N-methyl-N-(thiophen-2-ylmethyl)adamantane-1-carboxamide
Homo sapiens
-
-
0.000125
N-methyl-N-(thiophen-3-ylmethyl)adamantane-1-carboxamide
Homo sapiens
-
-
0.000113
N-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.000448
N-methyl-N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.0017
N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.000008
N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000014
N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000011
N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000679
N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide
Homo sapiens
-
-
0.000105
N-[3-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000167
N-[3-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000285
N-[3-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.002037
N-[3-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.0000007
N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.000151
N-[4-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000058
N-[4-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000894
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-fluoro-phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000897
N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-methyl-phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000211
N-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.00009
N-[4-(2-adamantan-1-yl-2-oxoethylamino)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000313
N-[4-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide
Homo sapiens
pH not specified in the publication, 37°C
0.000036
N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000007
N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000014
N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00069
N-[4-[(2,6-dimethylpyrimidin-4-yl)sulfamoyl]phenyl]-4-[oxo(phenyl)acetyl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
N-[5-(2-amino-2-oxoethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.001
N-[5-(3-amino-3-oxopropyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
N-[5-(cyanomethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000002
N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000028
N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.000011
N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000076
N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000006
N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.00000088
N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000038
N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000007
N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000024
N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000055
N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.0000017
N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
Homo sapiens
-
0.001
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydrazinecarbonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000002
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydroxymethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000055
N2-(2-fluorobenzene-1-sulfonyl)-N-[5-[(2-hydroxyhydrazinyl)methyl]tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00096
oxymesterone
Homo sapiens
pH and temperature not specified in the publication
0.00071
oxymetholone
Homo sapiens
pH and temperature not specified in the publication
0.00001897
perfluorohexane sulfonate
Homo sapiens
pH and temperature not specified in the publication
0.000000048
perfluorooctane sulfonate
Homo sapiens
pH and temperature not specified in the publication
0.00002441
Perfluorooctanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000512
posaconazole
Homo sapiens
at pH 7.4 and 37°C
0.0063
pyrrolidine dithiocarbamate
Homo sapiens
pH and temperature not specified in the publication
0.000542
rheochrysidin
Homo sapiens
pH 7.4, 37°C
0.00023
sterenin A
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.0066
sterenin B
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.00024
sterenin C
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.0026
sterenin D
Homo sapiens
-
value above, pH not specified in the publication, 26°C
0.00137
testosterone
Homo sapiens
pH and temperature not specified in the publication
0.000132
thiram
Homo sapiens
pH and temperature not specified in the publication
0.0019
tributyltin
Homo sapiens
pH and temperature not specified in the publication
0.00319
Triphenyltin
Homo sapiens
pH and temperature not specified in the publication
0.031
zineb
Homo sapiens
pH and temperature not specified in the publication
0.0018
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid
Homo sapiens
in 30 mM HEPES buffer, pH 7.4, at 37°C
0.000004
[1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000012
[2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00077 - 0.00185
[3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone
0.0004
[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid
Homo sapiens
pH not specified in the publication, 37°C
0.00258
[4-(2-Adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid methyl ester
Homo sapiens
pH not specified in the publication, 37°C
0.000234
[4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000043
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000013
[5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000017
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
[9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
additional information
(1S,2R,3S,5R,6R)-4-methylidene-1-([(1S,4aS,8aS)-2,5,5,8a-tetramethyl-1,4,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]methyl)-7-oxabicyclo[4.1.0]heptane-2,3,5-triol
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
1.44
-
purified recombinant His6-tagged isozyme 11beta-HSD1
3.84
-
purified by detergent/polymer two-phase system, i.e. Tween20/dextran 500
91.36
-
-
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.5
-
assay at
8
-
assay at
8.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at room temperature
26
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
11beta-HSD1 activity is increased in visceral adipose tissue in prepubertal children with normal weight
Manually annotated by BRENDA team
-
rectum, sigmoid colon
Manually annotated by BRENDA team
-
samples from hepatic, renal and peripheral veins
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
chorionic trophoblast cell
Manually annotated by BRENDA team
-
isoform 11betaHSD1
Manually annotated by BRENDA team
isoform 11beta-HSD1 is clearly expressed while isoform 11beta-HSD2 is much less prominent, 11beta-HSD1 protein expression predominates in endothelial cells and varies during periods of growth
Manually annotated by BRENDA team
-
isoform 11betaHSD2
Manually annotated by BRENDA team
-
lung epithelial cell line, isozymes HSD1 and 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
-
significant expression of isoform 11beta-HSD2 protein is found at single cell level in thymus parenchyma, at perivascular sites of capillaries and small vessels penetrating the thymus lobuli and within Hassall's bodies
Manually annotated by BRENDA team
-
chorionic trophoblast cell
Manually annotated by BRENDA team
-
amnion-derived cell line
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
metabolism
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
DHI1_HUMAN
292
1
32401
Swiss-Prot
Secretory Pathway (Reliability: 2)
DHI2_HUMAN
405
0
44127
Swiss-Prot
-
R4GN04_HUMAN
58
0
6264
TrEMBL
other Location (Reliability: 1)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
32000
-
x * 32000, SDS-PAGE
32386
-
2 * 32386, deduced from nucleotide sequence
33500
-
calculated from amino acid sequence
34000
40000
67400
-
gel filtration
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
monomer
-
1 * 40000, isozyme HSD1, SDS-PAGE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
11beta-HSD1 (24-292) C272S mutant, hanging drop vapour diffusion method, using 25% (w/v) PEG 3350, 0.2 M ammonium acetate, and 0.1 M sodium citrate buffer (pH 5.6)
11beta-HSD1 residues 24-292 C272S, hanging drop vapour diffusion method, using 100 mM HEPES pH 6.8-7.1 and 16-18% (w/v) PEG 3350
analysis of substratebinding by threedimensional modeling. There are favorable interactions between the C7-hydroxyl group of substrate and the catalytic site when the A ring of substrate is oriented towards the interior of the enzyme
-
co-crystal structure of inhibitor 8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile with enzyme and cofactor NADP+. Structure shows a critical H-bonding interaction between the OH pharmacophore of the inhibitor and the side chains of S170 and Y183 residues at the catalytic site of the enzyme
docking of cortisone into the catalytic site of wild type and mutant Y177A, PDB entry 2BEL. The catalytic site is stabilised in the enzyme dimer. Residues K44, N123, and T222 at the bottom of the cavity define a small functional back-door that allows water to enter or exit, making it easier for the substrate to leave or occupy the site. Residue Y177 is involved in stabilising interactions with the A ring of the substrate
in complex with inhibitor 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine. The carbonyl oxygen of the inhibitor is within hydrogen bonding distance to active site residues S170 and Y183, the inhibitor also forms hydrophobic interactions with the protein
-
purified recombinant isozyme 11beta-HSD1 catalytic domain mutant C272S, the nanovolume crystallization method, the reservoir solution contains 20% PEG 3350, and 0.1 M MES, pH 6.2, soaking of crystals in 1 mM lutetium acetate reservoir solution, two crystal forms, X-ray diffraction structure determination and analysis at 1.55-2.45 A resolution
-
sitting drop vapour diffusion method, using 16-18% (w/v) PEG3350 and 0.1 M MES buffer (pH 6.2-6.4)
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C272S
-
ability to form disulfide bonds abolished, but no change in activity or Km
E25K
-
88% of wild type cortisone reduction activity
E25K/E26K
-
20% of wild type cortisone reduction activity
E25K/E26Q
-
45% of wild type cortisone reduction activity
E25Q
-
82% of wild type cortisone reduction activity
E25Q/E26Q
-
57% of wild type cortisone reduction activity
E26K
-
65% of wild type cortisone reduction activity
K35S/K36S
-
no activity
K5S/K6S
-
93% of wild type cortisone reduction activity, no reduction of 7-oxocholesterol in intact HEK-293 cells transfected with 11beta-HSD1
K5S/K6S/E25K/E26K
-
21% of wild type cortisone reduction activity
K6S/E25K
-
86% of wild type cortisone reduction activity
K6S/E25K/E26K
-
31% of wild type cortisone reduction activity
K6S/E25K/E26Q
-
30% of wild type cortisone reduction activity
K6S/E25Q/E26Q
-
43% of wild type cortisone reduction activity
L150R
-
also lacking the first 30 n-terminal amino acids, gains activity in microsomal fraction after solubilization with Emulgen
V148R
-
also lacking the first 30 N-terminal amino acids, no activity
V149E
V149R
Y177A
-
site-directed mutagenesis, the mutant shows increased Km for cortisone compared to the wild-type enzyme, the mutation reduces the sensitivity to glycyrrhetinic acid inhibition 6-10fold, but not to carbenoxolone
Y177F
-
site-directed mutagenesis, the mutant shows kinetics similar to the wild-type enzyme
Y177Q
-
site-directed mutagenesis, the mutant shows increased Km for cortisone compared to the wild-type enzyme, the mutation reduces the sensitivity to glycyrrhetinic acid inhibition 6-10fold, but not to carbenoxolone
Y280A
wild-type and mutant enzyme exhibit similar Km values for either cortisone or 11-dehydrocorticosterone. About 10fold increase in IC50-value for glycyrrhetinic acid
Y280F
wild-type and mutant enzyme exhibit similar Km values for either cortisone or 11-dehydrocorticosterone. About 6fold increase in IC50-value for glycyrrhetinic acid
Y280S
wild-type and mutant enzyme exhibit similar Km values for either cortisone or 11-dehydrocorticosterone. 100% increase in IC50-value for glycyrrhetinic acid
additional information
a cytoplasmic localized mutant of isozyme 11beta-HSD1 catalyzes the oxoreduction of cortisone, but not of 7-oxocholesterol
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
affinity partitioning of His-tagged 11beta-HSD1 in polymer/detergent aqueous two-phase system
-
native enzyme from liver microsomes to homogeneity
-
near homogeneity, recombinant enzyme
-
octyl-Sepharose, Mono Q-sepharose, Red Sepharose A
-
Octyl-Sepharose, Mono Q-Sepharose, Red-Sepharose
-
purified in the presence of CHAPS by Ni+-NTA column chromatography and Superdex 200 gel filtration
recombinant His-tagged-11beta-HSD1 expressed in Escherichia coli
-
recombinant His6-tagged isozyme 11beta-HSD1 from membrane by microsome preparation, in situ solubilization, partitioning and batch metal affinity adsorption in aqueous two-phase systems, optimization of solubilization using different detergents at 1% w/v, overview
-
recombinant isozyme 11beta-HSD1 catalytic domain mutant C272S from Escherichia coli strain DH10b-Tir by affinity chromatography
-
solubilization, partially purifed by gel filtration, 73fold
-
solubilized microsomes, octyl-Sepharose, Mono Q-Sepharose, Red Sepharose A
-
to homogeneity, recombinant catalytic domain
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
Baculovirus-produced recombinant protein
-
cloning from clone 5193867, ATCC clone 7277078, expression of isozyme 11beta-HSD1 catalytic domain mutant C272S, comprising residues 24-292 proceeded by a 17-amino acid-affinity tag, in Escherichia coli strain DH10b-Tir
-
cloning of cDNA
-
expressed in Escherichia coli
-
expressed in HEK-293 cell
expressed in HEK-293 cells
expressed in HEK-293 cells, co-expression of hexose-6-phosphate dehydrogenase is not required for the enzyme to function effectively as an oxo-reductase
-
expressed in in Hi5 cells via a baculovirus protein expression system and in Escherichia coli Rosetta1(DE3) cells
expression in CHO cells
expression in Escherichia coli and Pichia pastoris
-
expression in Escherichia coli, catalytic domain
-
expression in HEK-293 cell
expression in HEK-293 cell of 11beta-hydroxysteroid dehydrogenase alone or together with hexose-6-phosphate dehydrogenase
-
expression in HEK-293 cells
expression in HEK293 cells
-
expression in Pichia pastoris
-
expression in Saccharomyces cerevisiae
-
expression inEscherichia coli of N-terminally deleted gene, amino acids 24-292, with an N-terminal His-tag
expression of 11beta-HSD1 in Pichia pastoris, COS cells and Escherichia coli
-
expression of His-tagged 11beta-HSD1 in Pichia pastoris
-
expression of isozyme 11beta-HSD1 in HEK-293 cells
-
expression of N-terminally His6-tagged isozyme 11beta-HSD1 in Pichia pastoris strain GS115 membranes
-
expression Pichia pastoris
-
isoform 11beta-HSD1, expression in HEK-293 cell
-
isozyme 11beta-HSD1 is expressed in Pichia pastoris
overexpressed in HEK-293 cell
-
stable expression of isozymes 11beta-HSD1 and 11beta-HSD2 in CHO cells
-
the 11beta-HSD1 enzyme is expressed in Escherichia coli
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
continuous exposure to glucocorticoid indirectly inhibits the activity of isoform 11beta-HSD1
-
enzyme expression of isoform 11beta-HSD2 is dysregulated in malignant cells
epidermal isoform 11beta-HSD1 expression is decreased in the lesional skin of patients with atopic dermatitis
expression of isoform 11beta-HSD1 is induced by UV-B irradiation and in response to the pro-inflammatory cytokines, interleukin-1beta and tumor necrosis factor alpha
-
isoform 11beta-HSD1 enzyme activity is decreased in diabetic subjects
isoform 11beta-HSD1 expression does not vary in patients with inflammatory bowel disease compared with controls
isoform 11beta-HSD1 mRNA expression and enzyme activity is up-regulated by physiological concentrations of cortisol. After treatment with dexamethasone, isoform 11beta-HSD1 mRNA expression increases in both diabetics and controls
isoform 11beta-HSD2 expression is downregulated in patients with inflammatory bowel disease compared with controls
isozyme 11beta-HSD1, expression analysis
-
short-term exposure to glucocorticoid increases the activity of isoform 11beta-HSD1
-
the enzyme is upregulated in rheumatoid arthritis
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
analysis
drug development
medicine
pharmacology
-
isozyme 11beta-HSD1 is a target in treatment of metabolic diseases such as diabetes mellitus type 2 or obesity
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Hult, M.; Nobel, C.S.I.; Abrahmsen, L.; Nicoll-Griffith, D.A.; Jrnvall, H.; Oppermann, U.C.T.
Novel enzymological profiles of human 11beta-hydroxysteroid dehydrogenase type 1
Chem. Biol. Interact.
130-132
805-8014
2001
Homo sapiens
Manually annotated by BRENDA team
Walker, E.A.; Clarks, A.M.; Hewison, M.; Ride, J.P.; Steward, P.M.
Functional expression, characterization, and purification of the catalytic domain of human 11-beta-hydroxysteroid dehydrogenase type 1
J. Biol. Chem.
276
21343-21350
2001
Homo sapiens
Manually annotated by BRENDA team
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
Ferrari, P.; Smith, R.E.; Funder, J.W.; Krozowski, Z.S.
Substrate and inhibitor specificity of the clones human 11beta-hydroxysteroid dehydrogenase type 2 isoform
Am. J. Physiol.
270
E900-904
1996
Homo sapiens
Manually annotated by BRENDA team
Blum , S.; Buhler, H.
Characterization of human placental 11beta-hydroxysteroid dehydrogenase, a key enzyme of cortocosteroid metabolism
Cell. Physiol. Biochem.
5
167-175
1995
Homo sapiens
-
Manually annotated by BRENDA team
Lakshim, V.; Nath, N.; Muneyyirci-Delale, O.
Characterization of 11beta-hydroxysteroid dehydrogenase of human placenta: Evidence for the existence of two species of 11beta-hydroxysteroid dehydrogenases
J. Steroid Biochem. Mol. Biol.
45
391-397
1993
Homo sapiens
Manually annotated by BRENDA team
Pearson Murphy, B.E.
Specificity of human 11beta-hydroxysteroid dehydrogenase
J. Steroid Biochem.
14
807-809
1981
Homo sapiens
Manually annotated by BRENDA team
Maser, E.; Volker, B.; Friebertshauser, J.
11 beta-Hydroxysteroid dehydrogenase type 1 from human liver: dimerization and enzyme cooperativity support its postulated role as glucocorticoid reductase
Biochemistry
41
2459-2465
2002
Homo sapiens
Manually annotated by BRENDA team
Blum, A.; Raum, A.; Maser, E.
Functional characterization of the human 11 beta-hydroxysteroid dehydrogenase 1B (11 beta-HSD 1B) variant
Biochemistry
42
4108-4117
2003
Homo sapiens
Manually annotated by BRENDA team
Zbankova, S.; Bryndova, J.; Kment, M.; Pacha, J.
Expression of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in colorectal cancer
Cancer Lett.
210
95-100
2004
Homo sapiens
Manually annotated by BRENDA team
Maser, E.; Friebertshauser, J.; Volker, B.
Purification, characterization and NNK carbonyl reductase activities of 11beta-hydroxysteroid dehydrogenase type 1 from human liver: enzyme cooperativity and significance in the detoxification of a tobacco-derived carcinogen
Chem. Biol. Interact.
143-144
435-448
2003
Homo sapiens
Manually annotated by BRENDA team
Blum, A.; Maser, E.
The critical role of the N-terminus of 11beta-hydroxysteroid dehydrogenase type 1, as being encoded by exon 1, for enzyme stabilization and activity
Chem. Biol. Interact.
143-144
469-480
2003
Homo sapiens
Manually annotated by BRENDA team
Shafqat, N.; Elleby, B.; Svensson, S.; Shafqat, J.; Jornvall, H.; Abrahmsen, L.; Oppermann, U.
Comparative enzymology of 11beta -hydroxysteroid dehydrogenase type 1 from glucocorticoid resistant (guinea pig) versus sensitive (human) species
J. Biol. Chem.
278
2030-2035
2003
Cavia porcellus, Homo sapiens
Manually annotated by BRENDA team
Schweizer, R.A.; Zurcher, M.; Balazs, Z.; Dick, B.; Odermatt, A.
Rapid hepatic metabolism of 7-ketocholesterol by 11beta-hydroxysteroid dehydrogenase type 1: species-specific differences between the rat, human, and hamster enzyme
J. Biol. Chem.
279
18415-18424
2004
Homo sapiens, Rattus norvegicus, Mesocricetus auratus (Q6R0J2)
Manually annotated by BRENDA team
Frick, C.; Atanasov, A.G.; Arnold, P.; Ozols, J.; Odermatt, A.
Appropriate function of 11beta-hydroxysteroid dehydrogenase type 1 in the endoplasmic reticulum lumen is dependent on its N-terminal region sharing similar topological determinants with 50-kDa esterase
J. Biol. Chem.
279
31131-31138
2004
Homo sapiens
Manually annotated by BRENDA team
Roobol-Boza, M.; Dolby, V.; Doverskog, M.; Barrefelt, A.; Lindqvist, F.; Oppermann, U.C.; Kohler Van Alstine, K.; Tjerneld, F.
Membrane protein isolation by in situ solubilization, partitioning and affinity adsorption in aqueous two-phase systems. Purification of the human type 1 11beta-hydroxysteroid dehydrogenase
J. Chromatogr. A
1043
217-223
2004
Homo sapiens
Manually annotated by BRENDA team
Nobel, C.S.I.; Dunas, F.; Abrahmsen, L.B.
Purification of full-length recombinant human and rat type 1 11beta-hydroxysteroid dehydrogenases with retained oxidoreductase activities
Protein Expr. Purif.
26
349-356
2002
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Wsol, V.; Szotakova, B.; Skalova, L.; Maser, E.
The novel anticancer drug oracin: different stereospecificity and cooperativity for carbonyl reduction by purified human liver 11beta-hydroxysteroid dehydrogenase type 1
Toxicology
197
253-261
2004
Homo sapiens
Manually annotated by BRENDA team
Garbrecht, M.R.; Schmidt, T.J.; Krozowski, Z.S.; Snyder, J.M.
11beta-Hydroxysteroid dehydrogenase type 2 and the regulation of surfactant protein A by dexamethasone metabolites
Am. J. Physiol. Endocrinol. Metab.
290
E653-E660
2006
Homo sapiens
Manually annotated by BRENDA team
Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.
The role of tyrosine 177 in human 11beta-hydroxysteroid dehydrogenase type 1 in substrate and inhibitor binding: an unlikely hydrogen bond donor for the substrate
Biochim. Biophys. Acta
1764
824-830
2006
Homo sapiens
Manually annotated by BRENDA team
Xiang, J.; Ipek, M.; Suri, V.; Massefski, W.; Pan, N.; Ge, Y.; Tam, M.; Xing, Y.; Tobin, J.F.; Xu, X.; Tam, S.
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
15
2865-2869
2005
Homo sapiens
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
Mai, K.; Kullmann, V.; Bobbert, T.; Maser-Gluth, C.; Moehlig, M.; Baehr, V.; Pfeiffer, A.F.; Spranger, J.; Diederich, S.
In vivo activity of 11beta-hydroxysteroid dehydrogenase type 1 and free fatty acid-induced insulin resistance
Clin. Endocrinol. (Oxf.)
63
442-449
2005
Homo sapiens
Manually annotated by BRENDA team
Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Alford, F.P.; Inder, W.J.
11beta Hydroxysteroid dehydrogenase type 1 is expressed and is biologically active in human skeletal muscle
Clin. Endocrinol. (Oxf.)
65
800-805
2006
Homo sapiens
Manually annotated by BRENDA team
Li, W.; Gao, L.; Wang, Y.; Duan, T.; Myatt, L.; Sun, K.
Enhancement of cortisol-induced 11beta-hydroxysteroid dehydrogenase type 1 expression by interleukin 1beta in cultured human chorionic trophoblast cells
Endocrinology
147
2490-2495
2006
Homo sapiens
Manually annotated by BRENDA team
Ohshima, M.; Ohno, S.; Nakajin, S.
Inhibitory effects of some possible endocrine-disrupting chemicals on the isozymes of human 11beta-hydroxysteroid dehydrogenase and expression of their mRNA in gonads and adrenal glands
Environ. Sci.
12
219-230
2005
Homo sapiens
Manually annotated by BRENDA team
Atanasov, A.G.; Dzyakanchuk, A.A.; Schweizer, R.A.; Nashev, L.G.; Maurer, E.M.; Odermatt, A.
Coffee inhibits the reactivation of glucocorticoids by 11beta-hydroxysteroid dehydrogenase type 1: a glucocorticoid connection in the anti-diabetic action of coffee?
FEBS Lett.
580
4081-4085
2006
Homo sapiens
Manually annotated by BRENDA team
Hosfield, D.J.; Wu, Y.; Skene, R.J.; Hilgers, M.; Jennings, A.; Snell, G.P.; Aertgeerts, K.
Conformational flexibility in crystal structures of human 11beta-hydroxysteroid dehydrogenase type I provide insights into glucocorticoid interconversion and enzyme regulation
J. Biol. Chem.
280
4639-4648
2005
Homo sapiens
Manually annotated by BRENDA team
Miguet, L.; Zhang, Z.; Barbier, M.; Grigorov, M.G.
Comparison of a homology model and the crystallographic structure of human 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) in a structure-based identification of inhibitors
J. Comput. Aided Mol. Des.
20
67-81
2006
Homo sapiens
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
Ayachi, S.E.; Paulmyer-Lacroix, O.; Verdier, M.; Alessi, M.C.; Dutour, A.; Grino, M.
11beta-Hydroxysteroid dehydrogenase type 1-driven cortisone reactivation regulates plasminogen activator inhibitor type 1 in adipose tissue of obese women
J. Thromb. Haemost.
4
621-627
2006
Homo sapiens
Manually annotated by BRENDA team
Latif, S.A.; Pardo, H.A.; Hardy, M.P.; Morris, D.J.
Endogenous selective inhibitors of 11beta-hydroxysteroid dehydrogenase isoforms 1 and 2 of adrenal origin
Mol. Cell. Endocrinol.
243
43-50
2005
Ovis aries, Homo sapiens
Manually annotated by BRENDA team
Odermatt, A.; Atanasov, A.G.; Balazs, Z.; Schweizer, R.A.; Nashev, L.G.; Schuster, D.; Langer, T.
Why is 11beta-hydroxysteroid dehydrogenase type 1 facing the endoplasmic reticulum lumen? Physiological relevance of the membrane topology of 11beta-HSD1
Mol. Cell. Endocrinol.
248
15-23
2006
Homo sapiens (P28845)
Manually annotated by BRENDA team
Su, X.; Vicker, N.; Ganeshapillai, D.; Smith, A.; Purohit, A.; Reed, M.J.; Potter, B.V.
Benzothiazole derivatives as novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
248
214-217
2006
Homo sapiens
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
Maser, E.; Wsol, V.; Martin, H.J.
11beta-Hydroxysteroid dehydrogenase type 1: purification from human liver and characterization as carbonyl reductase of xenobiotics
Mol. Cell. Endocrinol.
248
34-37
2006
Homo sapiens
Manually annotated by BRENDA team
Ito-Kobayashi, M.; Aoyagi, A.; Tanaka, I.; Muramatsu, Y.; Umetani, M.; Takatsu, T.
Sterenin A, B, C and D, novel 11beta-hydroxysteroid dehydrogenase type 1 inhibitors from Stereum sp. SANK 21205
J. Antibiot.
61
128-135
2008
Homo sapiens
Manually annotated by BRENDA team
Jang, C.; Obeyesekere, V.R.; Dilley, R.J.; Krozowski, Z.; Inder, W.J.; Alford, F.P.
Altered activity of 11beta-hydroxysteroid dehydrogenase types 1 and 2 in skeletal muscle confers metabolic protection in subjects with type 2 diabetes
J. Clin. Endocrinol. Metab.
92
3314-3320
2007
Homo sapiens
Manually annotated by BRENDA team
Gong, R.; Morris, D.J.; Brem, A.S.
Human renal 11beta-hydroxysteroid dehydrogenase 1 functions and co-localizes with COX-2
Life Sci.
82
631-637
2008
Homo sapiens
Manually annotated by BRENDA team
Sun, L.; Stenken, J.A.; Yang, A.Y.; Zhao, J.J.; Musson, D.G.
An in vitro microdialysis methodology to study 11beta-hydroxysteroid dehydrogenase type 1 enzyme activity in liver microsomes
Anal. Biochem.
370
26-37
2007
Canis lupus, Homo sapiens
Manually annotated by BRENDA team
Flyren, K.; Bergquist, L.O.; Castro, V.M.; Fotsch, C.; Johansson, L.; St Jean, D.J.; Sutin, L.; Williams, M.
Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
Bioorg. Med. Chem. Lett.
17
3421-3425
2007
Homo sapiens
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
Wang, H.; Ruan, Z.; Li, J.J.; Simpkins, L.M.; Smirk, R.A.; Wu, S.C.; Hutchins, R.D.; Nirschl, D.S.; Van Kirk, K.; Cooper, C.B.; Sutton, J.C.; Ma, Z.; Golla, R.; Seethala, R.; Salyan, M.E.; Nayeem, A.; Krystek, S.R.; Sheriff, S.; Camac, D.M.; Morin, P.E.; Carpenter, B.; Robl, J.A.; Zahler, R.; Gordon, D.A.; Hamann, L.G.
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem. Lett.
18
3168-3172
2008
Homo sapiens
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
Ahmed, A.; Saksena, S.; Sherlock, M.; Olliff, S.P.; Elias, E.; Stewart, P.M.
Induction of hepatic 11beta-hydroxysteroid dehydrogenase type 1 in patients with alcoholic liver disease
Clin. Endocrinol. (Oxf.)
68
898-903
2008
Homo sapiens
Manually annotated by BRENDA team
Kim, K.W.; Wang, Z.; Busby, J.; Tsuruda, T.; Chen, M.; Hale, C.; Castro, V.M.; Svensson, S.; Nybo, R.; Xiong, F.; Wang, M.
The selectivity of tyrosine 280 of human 11beta-hydroxysteroid dehydrogenase type 1 in inhibitor binding
FEBS Lett.
581
995-999
2007
Homo sapiens (P28845), Homo sapiens
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
Bujalska, I.J.; Durrani, O.M.; Abbott, J.; Onyimba, C.U.; Khosla, P.; Moosavi, A.H.; Reuser, T.T.; Stewart, P.M.; Tomlinson, J.W.; Walker, E.A.; Rauz, S.
Characterisation of 11beta-hydroxysteroid dehydrogenase 1 in human orbital adipose tissue: a comparison with subcutaneous and omental fat
J. Endocrinol.
192
279-288
2007
Homo sapiens
Manually annotated by BRENDA team
Johansson, L.; Fotsch, C.; Bartberger, M.D.; Castro, V.M.; Chen, M.; Emery, M.; Gustafsson, S.; Hale, C.; Hickman, D.; Homan, E.; Jordan, S.R.; Komorowski, R.; Li, A.; McRae, K.; Moniz, G.; Matsumoto, G.; Orihuela, C.; Palm, G.; Veniant, M.; Wang, M.; Williams, M.; Zhang, J.
2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice
J. Med. Chem.
51
2933-2943
2008
Homo sapiens (P28845), Homo sapiens
Manually annotated by BRENDA team
Julian, L.D.; Wang, Z.; Bostick, T.; Caille, S.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Hungate, R.W.; Jaen, J.C.; Liu, J.; Monshouwer, M.; McMinn, D.; Rew, Y.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model
J. Med. Chem.
51
3953-3960
2008
Macaca fascicularis, Homo sapiens, Homo sapiens (P28845)
Manually annotated by BRENDA team
Munoz, R.; Carvajal, C.; Escalona, A.; Boza, C.; Perez, G.; Ibanez, L.; Fardella, C.
11beta-Hydroxysteroid dehydrogenase type 1 is overexpressed in subcutaneous adipose tissue of morbidly obese patients
Obes. Surg.
19
764-770
2008
Homo sapiens
Manually annotated by BRENDA team
Nashev, L.G.; Chandsawangbhuwana, C.; Balazs, Z.; Atanasov, A.G.; Dick, B.; Frey, F.J.; Baker, M.E.; Odermatt, A.
Hexose-6-phosphate dehydrogenase modulates 11beta-hydroxysteroid dehydrogenase type 1-dependent metabolism of 7-keto- and 7beta-hydroxy-neurosteroids
PLoS ONE
2
e561
2007
Homo sapiens
Manually annotated by BRENDA team
Hennebert, O.; Le Mee, S.; Pernelle, C.; Morfin, R.
5Alpha-androstane-3beta,7alpha,17beta-triol and 5alpha-androstane-3beta,7beta,17beta-triol as substrates for the human 11beta-hydroxysteroid dehydrogenase type 1
Steroids
72
855-864
2007
Homo sapiens
Manually annotated by BRENDA team
Rew, Y.; McMinn, D.L.; Wang, Z.; He, X.; Hungate, R.W.; Jaen, J.C.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Villemure, E.; Walker, N.P.; Yan, X.; Ye, Q.; Powers, J.P.
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors
Bioorg. Med. Chem. Lett.
19
1797-1801
2009
Homo sapiens (P28845)
Manually annotated by BRENDA team
Roche, D.; Carniato, D.; Leriche, C.; Lepifre, F.; Christmann-Franck, S.; Graedler, U.; Charon, C.; Bozec, S.; Doare, L.; Schmidlin, F.; Lecomte, M.; Valeur, E.
Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I
Bioorg. Med. Chem. Lett.
19
2674-2678
2009
Homo sapiens (P28845), Homo sapiens
Manually annotated by BRENDA team
Lepifre, F.; Christmann-Franck, S.; Roche, D.; Leriche, C.; Carniato, D.; Charon, C.; Bozec, S.; Doare, L.; Schmidlin, F.; Lecomte, M.; Valeur, E.
Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold
Bioorg. Med. Chem. Lett.
19
3682-3685
2009
Homo sapiens (P28845), Homo sapiens
Manually annotated by BRENDA team
Tu, H.; Powers, J.P.; Liu, J.; Ursu, S.; Sudom, A.; Yan, X.; Xu, H.; Meininger, D.; Degraffenreid, M.; He, X.; Jaen, J.C.; Sun, D.; Labelle, M.; Yamamoto, H.; Shan, B.; Walker, N.P.; Wang, Z.
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Med. Chem.
16
8922-8931
2008
Homo sapiens (P28845), Homo sapiens
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
Mericq, V.; Medina, P.; Kakarieka, E.; Marquez, L.; Johnson, M.C.; Iniguez, G.
Differences in expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 and 2 in human placentas of term pregnancies according to birth weight and gender
Eur. J. Endocrinol.
161
419-425
2009
Homo sapiens
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
Gumy, C.; Thurnbichler, C.; Aubry, E.M.; Balazs, Z.; Pfisterer, P.; Baumgartner, L.; Stuppner, H.; Odermatt, A.; Rollinger, J.M.
Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 by plant extracts used as traditional antidiabetic medicines
Fitoterapia
80
200-205
2009
Homo sapiens
Manually annotated by BRENDA team
Mericq, V.; Medina, P.; Bouwman, C.; Johnson, M.C.; Godoy, J.; Lopez, T.; Iniguez, G.
Expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 enzyme in subcutaneous and visceral adipose tissue of prepubertal children
Horm. Res.
71
89-93
2009
Homo sapiens
Manually annotated by BRENDA team
Cooper, M.S.
11beta-Hydroxysteroid dehydrogenase: a regulator of glucocorticoid response in osteoporosis
J. Endocrinol. Invest.
31 (7 Suppl)
16-21
2008
Homo sapiens
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
Chen, B.B.; Lin, H.; Hu, G.X.; Su, Y.; Zhou, H.Y.; Lian, Q.Q.; Cai, H.; Hardy, D.O.; Gu, D.Y.; Ge, R.S.
The (+)- and (-)-gossypols potently inhibit human and rat 11beta-hydroxysteroid dehydrogenase type 2
J. Steroid Biochem. Mol. Biol.
113
177-181
2009
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Classen-Houben, D.; Schuster, D.; Da Cunha, T.; Odermatt, A.; Wolber, G.; Jordis, U.; Kueenburg, B.
Selective inhibition of 11beta-hydroxysteroid dehydrogenase 1 by 18alpha-glycyrrhetinic acid but not 18beta-glycyrrhetinic acid
J. Steroid Biochem. Mol. Biol.
113
248-252
2009
Homo sapiens (P28845), Homo sapiens
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
Blum, A.; Favia, A.D.; Maser, E.
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors with oleanan and ursan scaffolds
Mol. Cell. Endocrinol.
301
132-136
2009
Homo sapiens (P28845), Homo sapiens
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
Su, X.; Vicker, N.; Trusselle, M.; Halem, H.; Culler, M.D.; Potter, B.V.
Discovery of novel inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
Mol. Cell. Endocrinol.
301
169-173
2009
Homo sapiens
Manually annotated by BRENDA team
Gong, R.; Morris, D.J.; Brem, A.S.
Variable expression of 11beta Hydroxysteroid dehydrogenase (11beta-HSD) isoforms in vascular endothelial cells
Steroids
73
1187-1196
2008
Homo sapiens, Homo sapiens (P80365), Rattus norvegicus
Manually annotated by BRENDA team
Mondok, A.; Varga, I.; Glaz, E.; Szucs, N.; Toth, M.; Patocs, A.; Beko, G.; Racz, K.
11beta-hydroxysteroid dehydrogenase activity in acromegalic patients with normal or impaired carbohydrate metabolism
Steroids
74
725-729
2009
Homo sapiens
Manually annotated by BRENDA team
Skarydova, L.; Skarka, A.; Novotna, R.; Zivna, L.; Martin, H.J.; Wsol, V.; Maser, E.
Partial purification and characterization of a new human membrane-bound carbonyl reductase playing a role in the deactivation of the anticancer drug oracin
Toxicology
264
52-60
2009
Homo sapiens
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
Sun, D.; Wang, Z.; Cardozo, M.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Jaen, J.C.; Labelle, M.; Liu, J.; Ma, J.; Miao, S.; Sudom, A.; Tang, L.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1)
Bioorg. Med. Chem. Lett.
19
1522-1527
2009
Homo sapiens
Manually annotated by BRENDA team
Siu, M.; Johnson, T.O.; Wang, Y.; Nair, S.K.; Taylor, W.D.; Cripps, S.J.; Matthews, J.J.; Edwards, M.P.; Pauly, T.A.; Ermolieff, J.; Castro, A.; Hosea, N.A.; LaPaglia, A.; Fanjul, A.N.; Vogel, J.E.
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275
Bioorg. Med. Chem. Lett.
19
3493-3497
2009
Homo sapiens
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
Stanetty, C.; Czollner, L.; Koller, I.; Shah, P.; Gaware, R.; Cunha, T.D.; Odermatt, A.; Jordis, U.; Kosma, P.; Classen-Houben, D.
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11beta-hydroxysteroid dehydrogenase 2 inhibitors
Bioorg. Med. Chem.
18
7522-7541
2010
Homo sapiens (P28845)
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
Su, X.; Pradaux-Caggiano, F.; Thomas, M.P.; Szeto, M.W.; Halem, H.A.; Culler, M.D.; Vicker, N.; Potter, B.V.
Discovery of adamantyl ethanone derivatives as potent 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors
ChemMedChem
5
1026-1044
2010
Homo sapiens (P28845), Homo sapiens
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
Torres-Piedra, M.; Ortiz-Andrade, R.; Villalobos-Molina, R.; Singh, N.; Medina-Franco, J.L.; Webster, S.P.; Binnie, M.; Navarrete-Vazquez, G.; Estrada-Soto, S.
A comparative study of flavonoid analogues on streptozotocin-nicotinamide induced diabetic rats: quercetin as a potential antidiabetic agent acting via 11beta-hydroxysteroid dehydrogenase type 1 inhibition
Eur. J. Med. Chem.
45
2606-2612
2010
Homo sapiens (P28845)
Manually annotated by BRENDA team
Odermatt, A.
Diazepane-acetamide derivatives as selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
Expert Opin. Ther. Pat.
19
1477-1483
2009
Homo sapiens
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
Veniant, M.M.; Hale, C.; Hungate, R.W.; Gahm, K.; Emery, M.G.; Jona, J.; Joseph, S.; Adams, J.; Hague, A.; Moniz, G.; Zhang, J.; Bartberger, M.D.; Li, V.; Syed, R.; Jordan, S.; Komorowski, R.; Chen, M.M.; Cupples, R.; Kim, K.W.; St Jean, D.J.; Johansson, L.; Henriksson, M.A.; Williams, M.; Vallgarda, J.; Fots, F.o.t.s.c.
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221)
J. Med. Chem.
53
4481-4487
2010
Homo sapiens (P28845)
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
Su, X.; Vicker, N.; Thomas, M.P.; Pradaux-Caggiano, F.; Halem, H.; Culler, M.D.; Potter, B.V.
Discovery of adamantyl heterocyclic ketones as potent 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
ChemMedChem
6
1439-1451
2011
Homo sapiens (P28845)
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
Xu, Z.; Tice, C.M.; Zhao, W.; Cacatian, S.; Ye, Y.J.; Singh, S.B.; Lindblom, P.; McKeever, B.M.; Krosky, P.M.; Kruk, B.A.; Berbaum, J.; Harrison, R.K.; Johnson, J.A.; Bukhtiyarov, Y.; Panemangalore, R.; Scott, B.B.; Zhao, Y.; Bruno, J.G.; Togias, J.; Guo, J.; Guo, R.; Carroll, P.J.; McGeehan, G.M.; Zhuang, L. et al.
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
J. Med. Chem.
54
6050-6062
2011
Homo sapiens (P28845)
Manually annotated by BRENDA team
Kratschmar, D.V.; Vuorinen, A.; Da Cunha, T.; Wolber, G.; Classen-Houben, D.; Doblhoff, O.; Schuster, D.; Odermatt, A.
Characterization of activity and binding mode of glycyrrhetinic acid derivatives inhibiting 11beta-hydroxysteroid dehydrogenase type 2
J. Steroid Biochem. Mol. Biol.
125
129-142
2011
Homo sapiens (P28845)
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
Favia, A.; Masetti, M.; Recanatini, M.; Cavalli, A.
Substrate binding process and mechanistic functioning of type 1 11beta-hydroxysteroid dehydrogenase from enhanced sampling methods
PLoS ONE
6
e25375
2011
Homo sapiens (P28845)
Manually annotated by BRENDA team
Hu, G.; Lin, H.; Lian, Q.; Zhou, S.; Guo, J.; Zhou, H.; Chu, Y.; Ge, R.
Curcumin as a potent and selective inhibitor of 11beta-hydroxysteroid dehydrogenase 1: improving lipid profiles in high-fat-diet-treated rats
PLoS ONE
8
e49976
2013
Rattus norvegicus (P16232), Homo sapiens (P28845)
Manually annotated by BRENDA team
Guo, J.; Deng, H.; Li, H.; Zhu, Q.; Zhao, B.; Chen, B.; Chu, Y.; Ge, R.S.
Effects of methoxychlor and its metabolite 2,2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane on 11beta-hydroxysteroid dehydrogenase activities in vitro
Toxicol. Lett.
218
18-23
2013
Homo sapiens (P28845), Rattus norvegicus (P16232)
Manually annotated by BRENDA team
Itoi, S.; Terao, M.; Murota, H.; Katayama, I.
11beta-Hydroxysteroid dehydrogenase 1 contributes to the pro-inflammatory response of keratinocytes
Biochem. Biophys. Res. Commun.
440
265-270
2013
Homo sapiens
Manually annotated by BRENDA team
Hofer, S.; Kratschmar, D.V.; Schernthanner, B.; Vuorinen, A.; Schuster, D.; Odermatt, A.; Easmon, J.
Synthesis and biological analysis of benzazol-2-yl piperazine sulfonamides as 11beta-hydroxysteroid dehydrogenase 1 inhibitors
Bioorg. Med. Chem. Lett.
23
5397-5400
2013
Homo sapiens (P28845)
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
Ye, X.Y.; Yoon, D.; Chen, S.Y.; Nayeem, A.; Golla, R.; Seethala, R.; Wang, M.; Harper, T.; Sleczka, B.G.; Apedo, A.; Li, Y.X.; He, B.; Kirby, M.; Gordon, D.A.; Robl, J.A.
Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
Bioorg. Med. Chem. Lett.
24
654-660
2014
Homo sapiens (P28845)
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
Ryu, J.H.; Kim, S.; Han, H.Y.; Son, H.J.; Lee, H.J.; Shin, Y.A.; Kim, J.S.; Park, H.G.
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
Bioorg. Med. Chem. Lett.
25
695-700
2015
Homo sapiens (P28845)
Manually annotated by BRENDA team
Morelli, V.; Polledri, E.; Mercadante, R.; Zhukouskaya, V.; Palmieri, S.; Beck-Peccoz, P.; Spada, A.; Fustinoni, S.; Chiodini, I.
The activity of 11beta-hydroxysteroid dehydrogenase type 2 enzyme and cortisol secretion in patients with adrenal incidentalomas
Endocrine
53
809-815
2016
Homo sapiens
Manually annotated by BRENDA team
Dube, S.; Norby, B.J.; Pattan, V.; Carter, R.E.; Basu, A.; Basu, R.
11beta-hydroxysteroid dehydrogenase types 1 and 2 activity in subcutaneous adipose tissue in humans: implications in obesity and diabetes
J. Clin. Endocrinol. Metab.
100
E70-E76
2015
Homo sapiens
Manually annotated by BRENDA team
Scott, J.S.; Goldberg, F.W.; Turnbull, A.V.
Medicinal chemistry of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1)
J. Med. Chem.
57
4466-4486
2014
Homo sapiens (P28845)
Manually annotated by BRENDA team
Vitku, J.; Starka, L.; Bicikova, M.; Hill, M.; Heracek, J.; Sosvorova, L.; Hampl, R.
Endocrine disruptors and other inhibitors of 11beta-hydroxysteroid dehydrogenase 1 and 2: Tissue-specific consequences of enzyme inhibition
J. Steroid Biochem. Mol. Biol.
155
207-216
2016
Homo sapiens
Manually annotated by BRENDA team
Schmidt, M.; Straub, R.H.
11beta-Hydroxysteroid dehydrogenase enzymes modulate effects of glucocorticoids in rheumatoid arthritis synovial cells
Neuroimmunomodulation
22
40-45
2015
Homo sapiens
Manually annotated by BRENDA team
Chen, X.; Dong, Y.; Cao, S.; Li, X.; Wang, Z.; Chen, R.; Ge, R.S.
Effects of polybrominated diphenyl ethers on rat and human 11beta-hydroxysteroid dehydrogenase 1 and 2 activities
Pharmacology
98
115-123
2016
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Li, X.; Hu, G.; Li, X.; Wang, Y.Y.; Hu, Y.Y.; Zhou, H.; Latif, S.A.; Morris, D.J.; Chu, Y.; Zheng, Z.; Ge, R.S.
Metabolic coupling determines the activity: comparison of 11beta-hydroxysteroid dehydrogenase 1 and its coupling between liver parenchymal cells and testicular Leydig cells
PLoS ONE
10
e0141767
2015
Rattus norvegicus, Homo sapiens (P28845), Homo sapiens
Manually annotated by BRENDA team
Hintzpeter, J.; Stapelfeld, C.; Loerz, C.; Martin, H.J.; Maser, E.
Green tea and one of its constituents, epigallocatechine-3-gallate, are potent inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1
PLoS ONE
9
e84468
2014
Homo sapiens (P28845)
Manually annotated by BRENDA team
Almanzar, G.; Mayerl, C.; Seitz, J.C.; Hoefner, K.; Brunner, A.; Wild, V.; Jahn, D.; Geier, A.; Fassnacht, M.; Prelog, M.
Expression of 11beta-hydroxysteroid-dehydrogenase type 2 in human thymus
Steroids
110
35-40
2016
Homo sapiens
Manually annotated by BRENDA team
Voisin, M.; de Medina, P.; Mallinger, A.; Dalenc, F.; Huc-Claustre, E.; et, al.
Identification of a tumor-promoter cholesterol metabolite in human breast cancers acting through the glucocorticoid receptor
Proc. Natl. Acad. Sci. USA
114
E9346-E9355
2017
Homo sapiens (P80365)
Manually annotated by BRENDA team
Huebner, H.; Heussner, K.; Ruebner, M.; Schmid, M.; Nadal, J.; Woelfle, J.; Hartner, A.; Menendez-Castro, C.; Rauh, M.; Beckmann, M.W.; Kehl, S.; Fahlbusch, F.B.
Influence of labor on direct and indirect determinants of placental 11beta-hydroxysteroid dehydrogenase activity
Arch. Gynecol. Obstet.
303
401-408
2021
Homo sapiens (P80365), Homo sapiens
Manually annotated by BRENDA team
Studzinska, R.; Kolodziejska, R.; Kupczyk, D.; Plazinski, W.; Kosmalski, T.
A novel derivatives of thiazol-4(5H)-one and their activity in the inhibition of 11beta-hydroxysteroid dehydrogenase type 1
Bioorg. Chem.
79
115-121
2018
Homo sapiens (P28845)
Manually annotated by BRENDA team
Studzinska, R.; Kupczyk, D.; Plazinska, A.; Kolodziejska, R.; Kosmalski, T.; Modzelewska-Banachiewicz, B.
Thiazolo[3,2-a]pyrimidin-5-one derivatives as a novel class of 11beta-hydroxysteroid dehydrogenase inhibitors
Bioorg. Chem.
81
21-26
2018
Homo sapiens (P28845)
Manually annotated by BRENDA team
Boudon, S.; Heidl, M.; Vuorinen, A.; Wandeler, E.; Campiche, R.; Odermatt, A.; Jackson, E.
Design, synthesis, and biological evaluation of novel selective peptide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
Bioorg. Med. Chem.
26
5128-5139
2018
Homo sapiens (P28845)
Manually annotated by BRENDA team
Cirillo, N.; Morgan, D.J.; Pedicillo, M.C.; Celentano, A.; Lo Muzio, L.; McCullough, M.J.; Prime, S.S.
Characterisation of the cancer-associated glucocorticoid system key role of 11beta-hydroxysteroid dehydrogenase type 2
Br. J. Cancer
117
984-993
2017
Homo sapiens (P80365)
Manually annotated by BRENDA team
Dammann, C.; Stapelfeld, C.; Maser, E.
Expression and activity of the cortisol-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 is tissue and species-specific
Chem. Biol. Interact.
303
57-61
2019
Homo sapiens (P28845)
Manually annotated by BRENDA team
Koike, T.; Shiraki, R.; Sasuga, D.; Hosaka, M.; Kawano, T.; Fukudome, H.; Kurosawa, K.; Moritomo, A.; Mimasu, S.; Ishii, H.; Yoshimura, S.
Discovery and biological evaluation of potent and orally active human 11beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of type 2 diabetes mellitus
Chem. Pharm. Bull.
67
824-838
2019
Homo sapiens (P28845)
Manually annotated by BRENDA team
Han, J.; Sun, W.; Gao, F.
Role of 11beta-hydroxysteroid dehydrogenase in bone metabolism
Chinese J. Tissue Eng. Res.
21
5203-5208
2017
Homo sapiens
-
Manually annotated by BRENDA team
Hussey, M.; Holleran, G.; Smith, S.; Sherlock, M.; McNamara, D.
The role and regulation of the 11 beta-hydroxysteroid dehydrogenase enzyme system in patients with inflammatory bowel disease
Digest. Dis. Sci.
62
3385-3390
2017
Homo sapiens (P28845), Homo sapiens (P80365)
Manually annotated by BRENDA team
Zhou, C.; Ye, F.; Wu, H.; Ye, H.; Chen, Q.
Recent advances in the study of 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) inhibitors
Environ. Toxicol. Pharmacol.
52
47-53
2017
Rattus norvegicus (A0A1B0GWP2), Homo sapiens (P80365)
Manually annotated by BRENDA team
Ganjoo, A.; Tripathi, A.; Chetti, P.
Structural assessment and identification of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors
J. Biomol. Struct. Dyn.
38
4928-4937
2020
Homo sapiens (P28845)
Manually annotated by BRENDA team
Beck, K.R.; Inderbinen, S.G.; Kanagaratnam, S.; Kratschmar, D.V.; Jetten, A.M.; Yamaguchi, H.; Odermatt, A.
11beta-Hydroxysteroid dehydrogenases control access of 7beta,27-dihydroxycholesterol to retinoid-related orphan receptor gamma
J. Lipid Res.
60
1535-1546
2019
Homo sapiens (P28845), Homo sapiens (R4GN04)
Manually annotated by BRENDA team
Loerz, C.; Maser, E.
The cortisol-activating enzyme 11beta-hydroxysteroid dehydrogenase type 1 in skeletal muscle in the pathogenesis of the metabolic syndrome
J. Steroid Biochem. Mol. Biol.
174
65-71
2017
Homo sapiens (P28845)
Manually annotated by BRENDA team
Gent, R.; du Toit, T.; Bloem, L.M.; Swart, A.C.
The 11beta-hydroxysteroid dehydrogenase isoforms pivotal catalytic activities yield potent C11-oxy C19 steroids with 11betaHSD2 favouring 11-ketotestosterone, 11-ketoandrostenedione and 11-ketoprogesterone biosynthesis
J. Steroid Biochem. Mol. Biol.
189
116-126
2019
Homo sapiens (P80365)
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
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