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1.1.1.146: 11beta-hydroxysteroid dehydrogenase

This is an abbreviated version!
For detailed information about 11beta-hydroxysteroid dehydrogenase, go to the full flat file.

Word Map on EC 1.1.1.146

Reaction

an 11beta-hydroxysteroid
+
NADP+
=
an 11-oxosteroid
+
NADPH
+
H+

Synonyms

11 beta-hydroxysteroid dehydrogenase type 1, 11-beta hydroxysteroid dehydrogenase type 1, 11-beta-HSD1, 11-beta-HSD1 (oxidase) NADP+, 11-beta-HSD2, 11-beta-hydroxysteroid dehydrogenase type1, 11-DH, 11-DH2, 11-oxoreductase, 11beta hydroxysteroid dehydrogenase type 1, 11beta-HSD, 11beta-HSD 1, 11beta-HSD type 1, 11beta-HSD-1, 11beta-HSD-2, 11beta-HSD1, 11beta-HSD1A, 11beta-HSD2, 11beta-hydroxy steroid dehydrogenase, 11beta-hydroxy steroid dehydrogenase type 2, 11beta-hydroxysteroid dehydrogenase, 11beta-hydroxysteroid dehydrogenase 1, 11beta-hydroxysteroid dehydrogenase 2, 11beta-hydroxysteroid dehydrogenase isoforms 1, 11beta-hydroxysteroid dehydrogenase type 1, 11beta-hydroxysteroid dehydrogenase type 2, 11beta-hydroxysteroid dehydrogenase type I, 11beta-hydroxysteroid dehydrogenase type-1, 11beta-hydroxysteroid dehydrogenase-1, 11beta-hydroxysteroid dehydrogenases type 1, 11beta-hydroxysteroid type 1 dehydrogenase, 11beta-hydroxysteroid-dehydrogenase type I, 11betaHSD1, 11betaHSD2, 11HSD1, beta-hydroxysteroid dehydrogenase, corticosteroid 11-reductase, corticosteroid 11beta-dehydrogenase, dehydrogenase, 11beta-hydroxy steroid, HSD1, HSD11B, HSD11B1, Hsd11B2, HSD2, hydroxysteroid (11-beta) dehydrogenase, isozyme 11beta-HSD1, More, NAD-dependent 11-beta-hydroxysteroid dehydrogenase, NADP(+)-dependent 11beta-dehydrogenase, NADP+-dependent 11beta-hydroxysteroid dehydrogenase 1, type 1 11beta-hydroxysteroid dehydrogenase

ECTree

     1 Oxidoreductases
         1.1 Acting on the CH-OH group of donors
             1.1.1 With NAD+ or NADP+ as acceptor
                1.1.1.146 11beta-hydroxysteroid dehydrogenase

Inhibitors

Inhibitors on EC 1.1.1.146 - 11beta-hydroxysteroid dehydrogenase

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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
(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
(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)-2-[[(E)-[(1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-3-(4-hydroxyphenyl)propanoic acid
-
(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-hydroxyandrost-5-en-17-one
-
treatment of rats induces a shift from isoform 11beta-HSD1 to 11beta-HSD2 expression, increasing conversion from active to inactive glucocorticoids. Dehydroepiandrosterone likely modulates the transcription of 11beta-HSD2 in a phosphatidylinositol-3 kinase/Akt-dependent manner by increasing CCAAT/enhancer-binding protein beta mRNA and protein expression
(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
(4R,7S)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one
-
-
(4S,7R)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-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
-
(E)-5-((benzo[d]thiazol-2-ylimino)(methylthio)methylamino)-2-hydroxybenzoic acid
-
(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
-
-
1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-(2'-methyl[1,1'-biphenyl]-3-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-(4-methylphenyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-(pyridin-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-[2-(trifluoromethyl)phenyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1,7,8,8-tetramethyl-2-[[2-(trifluoromethyl)phenyl]methyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
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-benzyl-2-(2,4-difluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-benzyl-2-(2-fluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-benzyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
1-ethyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
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
1-[(2-chlorobenzyl)sulfanyl]-3-hydroxy-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile
1-[(2-chlorobenzyl)sulfanyl]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile
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-dehydrocortisterone
-
-
11-deoxycorticosterone
11-ketotestosterone
-
-
11-oxo-3alpha,5alpha-tetrahydrotestosterone
-
-
11-oxo-3beta,5alpha-tetrathydrotestosterone
-
-
11-oxo-allopregnanolone
11-oxo-androstenedione
-
-
11-oxo-progesterone
11-oxo-testosterone
11-oxoandrosterone
-
0.0021 mM, 50% inhibition of oxido-reductase reaction
11-oxoprogesterone
-
0.0095 mM, 50% inhibition of oxido-reductase reaction
11-oxotestosterone
-
0.018 mM, 50% inhibition of oxido-reductase reaction
11alpha-hydroxyprogesterone
-
11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione
11beta,21-dihydroxypregn-4-en-3,20-dione
-
potent inhibition of cortisol oxidation
11beta-hydroxy-allopregnanolone
-
-
11beta-hydroxy-androstanediol
-
-
11beta-hydroxy-testosterone
-
-
11beta-hydroxyandrostanediol
-
-
11beta-hydroxyandrostenedione
-
-
11beta-hydroxyandrosterone
-
0.07 mM, 50% inhibition of dehydrogenase reaction
11beta-hydroxydehydroepiandrosterone
-
0.003 mM, 50% inhibition of dehydrogenase reaction
11beta-hydroxyprogesterone
11beta-hydroxytestosterone
17beta-estradiol
17beta-estradiol-3-acetate
-
-
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
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-(2,4-difluorophenyl)-7,8,8-trimethyl-1-(2-phenylethyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2,5-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2,6-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
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)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
-
2-(2-fluorophenyl)-7,8,8-trimethyl-1-(prop-2-en-1-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-fluorophenyl)-7,8,8-trimethyl-1-(propan-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(2-fluorophenyl)-7,8,8-trimethyl-1-propyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
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-iodophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
2-(3-methoxyphenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
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-benzyl-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
-
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-hydroxy-5-[[(E)-[(5-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(5-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(6-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(6-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(7-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
2-hydroxy-5-[[(E)-[(7-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
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
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
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
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
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
3-(3,5,7-trimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 118 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
3-(3,5-dimethyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 104 nM, 11betaHSD1; IC50: above 10000 nM, 11betaHSD2
3-(3,5-dimethyladamantyl)methyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 50 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
3-(3-bromoadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 292 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
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
3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine
3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole
3-(3-fluoroadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 417 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
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
3-(3-hydroxyadamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 1674 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-(3-phenyladamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 365 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
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
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
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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
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
3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
3-adamant-2-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 35 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-adamantyl-5,6,7,8,9,10,11,12,13,14-decahydro[1,2,4]triazolo[4,3-a]azacyclododecine
IC50: 9.2 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-adamantyl-5,6,7,8,9,10,11,12-octahydro[1,2,4]triazolo[4,3-a]azecine
IC50: 4.6 nM, 11betaHSD1; IC50: about 4000 nM, 11betaHSD2
3-adamantyl-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
IC50: 16 nM, 11betaHSD1; IC50: about 10000 nM, 11betaHSD2
3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine
IC50: 1112 nM, 11betaHSD1; IC50: above 10000 nM, 11betaHSD2
3-adamantyl-6,7,8,9,10,11,12,13-octahydro-5H-[1,2,4]triazolo[4,3-a]azacycloundecine
IC50: 11650 nM, 11betaHSD2; IC50: 2.2 nM, 11betaHSD1
3-adamantyl-6,7,8,9,10,11-hexahydro-5H-[1,2,4]triazolo[4,3-a]azonine
IC50: 4563 nM, 11betaHSD2; IC50: 8 nM, 11betaHSD1
3-adamantyl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
IC50: 98 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole
IC50: 10000 nM, 11betaHSD2; IC50: 6820 nM, 11betaHSD1
3-adamantylmethy-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine
IC50: 587 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate
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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
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3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide
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3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide
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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
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3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide
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3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
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3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide
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3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide
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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
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3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
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3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
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3-methoxy-7,8,8-trimethyl-2-(4-methylphenyl)-4,5,6,7-tetrahydro-2H-4,7-methanoindazole
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3-methylchrysazin
3-monoglucuronyl-glycyrrhetinic acid
3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole
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3-tricyclo[3.3.1.13,7]dec-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine
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
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
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
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3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzoxazol-2(3H)-one
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3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-indol-2-one
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3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
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3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-4-methyl-1,3-dihydro-2H-benzimidazol-2-one
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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
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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
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3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
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3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
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3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole
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3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole
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3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole
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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
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3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole
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3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole
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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-tetrahydro-dehydrocortisterone
-
-
3alpha,5alpha-tetrahydroaldosterone
-
-
3alpha,5alpha-tetrahydrocorticosterone
3alpha,5alpha-tetrahydrocortisol
-
-
3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-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-chloromercuribenzoate
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
4-n-nonylphenol
-
-
4-n-octylphenol
-
-
4-nonylphenol
4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
4-pregnen-11,17-diol-3,20-dione
-
IC50: 0.1 mM
4-pregnen-11alpha-ol-3,20-dione
-
IC50: 0.0095 mM
4-pregnen-11beta-ol-3,20-dione
-
IC50: 0.011 mM
4-pregnen-16alpha-ol-3,20-dione
-
IC50: 0.9 mM
4-pregnen-17,21-diol-3,20-dione
-
IC50: 0.07 mM
4-pregnen-17alpha,20alpha-diol-3-one
-
IC50: 0.115 mM
4-pregnen-17alpha-ol-3,20-dione
-
IC50: 0.19 mM
4-pregnen-20alpha-ol-3-one
-
IC50: 0.022 mM
4-pregnen-20beta-ol-3-one
-
IC50: 0.031 mM
4-pregnen-21-ol-3,20-dione
-
IC50: 0.031 mM
4-pregnen-3,11,20-trione
-
IC50: 0.19 mM
4-pregnen-3,20-dione
-
IC50: 0.015 mM
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
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
5-(adamantan-1-ylcarbonyl)-4H,5H,6H,7H-thieno[3,2-c]pyridine
-
-
5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole
IC50: 14 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole
IC50: 91 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole
IC50: 23 nM, 11betaHSD1; IC50: 50 nM, 11betaHSD2
5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole
IC50: 270 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole
IC50: 109 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole
IC50: 50 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2
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-pregnen-3beta,11beta-diol-20-one
-
IC50: 0.0095 mM
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-[[(E)-[(5-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(5-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(5-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(6-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(6-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(6-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(7-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(7-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[(E)-[(7-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
-
5alpha-dihydrocorticosterone
5alpha-pregnan-11alpha-ol-3,20-dione
-
IC50: 0.0027 mM
5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione
-
IC50: 0.04 mM
5alpha-pregnan-11beta,21-diol-3,20-dione
-
IC50: 0.0075 mM
5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
-
IC50: 0.18 mM
5alpha-pregnan-3alpha,11beta,21-triol-20-one
-
IC50: 0.008 mM
5alpha-pregnan-3alpha,11beta-diol-20-one
-
IC50: 0.016 mM
5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione
-
IC50: 0.24 mM
5alpha-pregnan-3alpha,21-diol-11,20-dione
-
IC50: 0.029 mM
5alpha-Pregnan-3alpha,21-diol-20-one
-
IC50: 0.031 mM
5alpha-pregnan-3alpha-ol-20-one
-
IC50: 0.014 mM
5beta-pregnan-3alpha,11alpha-diol-20-one
-
IC50: 0.08 mM
5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one
-
IC50: 0.12 mM
5beta-pregnan-3alpha,11beta,21-triol-20-one
-
IC50: 0.14 mM
5beta-pregnan-3alpha,11beta-diol-20-one
-
IC50: 0.0 mM
5beta-Pregnan-3alpha,21-diol-20-one
-
IC50: 0.003 mM
5beta-Pregnan-3alpha-ol-20-one
-
IC50: 0.012 mM
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
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-cholesterol
-
-
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
7beta-hydroxycholesterol
-
-
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
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
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
9alpha-Fluorocortisol
A1-tunicamycin
-
50% inhibition at 50 ng/ml, reductase activity not affected
abietic acid
adamantyl triazoles
-
aloe emodin
-
-
Aloe-emodin
alpha-glycyrrhetinic acid
-
oxidase, IC50: 14 nmol, reductase, IC50: 42 nmol
AMG-221
antisense oligonucleotide
-
in mice treated with 11beta-hydroxysteroid dehydrogenase type 1-antisense oligonucleotide, plasma blood glucose levels are significantly reduced by up to 54% upon induction of diabetes. Cortisol and other diabetes end products are also reduced, and hepatic 11beta-hydroxysteroid dehydrogenase type 1 mRNA is suppressed by up to 84%
-
arylsulfoamidothiazole
arylsulfoamidothiazoles
-
arylsulfonamidothiazole derivatives
-
specific for isozyme 11beta-HSD1
-
AZD-4017
selective inhibitor for isoform 11beta-HSD1
AZD-8329
-
-
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
BDE-3
-
inhibitor of isoform HSD11B2
BDE-47
-
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
-
beta-glycyrrhetinic acid
-
oxidase, IC50: 2.9 nmol, reductase, IC50: 13 nmol
betulin
-
inhibition at 0.1 mM: oxidase 36%, reductase 34.5%
bezafibrate
-
23% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
BI-135585
-
bisphenol A
BMS-770767
-
-
bortezomib
-
butylated hydroxyanisole
BVT-14225
BVT-2733
BVT-528
competitive, tight-binding inhibition pattern
BVT.2733
-
-
carbenoxolone
chenodeoxycholic acid
-
-
cholesterol
-
oxidase: 18.6% inhibition at 0.1 mM, reductase: 7.4% inhibition at 0.1 mM
Clofibrate
-
18% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
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
dexamethasone
di-n-butyl phthalate
-
-
dibenzoylmethane
-
-
dibutyltin
dicyclohexyl benzene-1,2-dicarboxylate
-
-
diethyldithiocarbamate
uncompetitive inhibition of isoform 11beta-HSD2
diethylhexyl adipate
dihydrotestosterone
-
-
diphenyltin
dipropyl phthalate
-
-
Disulfiram
emodin
endosulfan
-
-
enoxolone
epigallocatechin gallate
-
epigallocatechine-3-gallate
-
-
estradiol
-
50% inhibition, DTT protects at 10 mM, estradiol has a regulatory function on the isozymes in the liver
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
-
-
fenofibrate
-
82% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid
-
25% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid cyclohexyl ester
-
54% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid ethylester
-
85% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid isobutylester
-
75% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid isopropyl amide
-
54% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
fenofibric acid n-butylester
-
64% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
flavanone
-
-
fluoxymesterone
potent inhibitor of isoform 11beta-HSD2
follicular fluid
-
follicular fluid from small antral follicles inhibits the enzyme in kidney homogenates by 50%, follicular fluid from large antral follicles inhibits by 23%, cyst fluid inhibits by 59%. Net cortisol oxidation in granulosa cells decreases by 35-48% when treated with follicular fluid from large antral follicles, and by 45-75% when treated with cyst fluid
-
Fusidic acid
-
-
G-strophanthidin
-
inhibition at 0.1 mM: oxidase 4.8%, reductase 6.1%
gemfibrozil
-
19% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
glycyrrhetinic acid
glycyrrhizic acid
glycyrrhizin
glycyrrhizinic acid
glycyrrhizininc acid
gossypol
-
-
gossypol acetic acid
-
dose-dependent competitive inhibition, IC50: 0.297 mM, (+)-isomer more potent inhibitor than (-)-isomer, mutant hairless strain more sensitive to inhibition than haired strain due to pharmacogenetic differences between the strains
helvolic acid
-
inhibition at 0.1 mM: oxidase 13%, reductase 18.5%
hydroxyitraconazole
INCB-13739
selective inhibitor for isoform 11beta-HSD1
indinavir
-
-
indomethacin
-
significant inhibition at 0.01 mM, the inhibitory effect of indomethacin on HSD11B bioactivity is abolished by 0.001 mM prostaglandin F2alpha, but not by prostaglandin E2
interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2
-
itraconazole
kansenone
-
-
kansuinone
-
-
lanosterol
-
oxidase IC50: 0.00065 mM, reductase IC50: 0.0017 mM
lupeol
-
inhibition at 0.1 mM: oxidase 52%, reductase 38.4%
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
-
-
morpholino antisense oligonucleotide
about 50% inhibition at 0.002 mM; about 50% inhibition at 0.002 mM
-
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,N-bis(3-D-gluconamidopropyl)cholamide
-
i.e. BIGCHAP; oxidase IC50: 0.0026 mM, reductase IC50: 0.0058 mM
N,N-bis(3-D-gluconamidopropyl)deoxycholamide
-
i.e. deoxy-BIGCHAP; oxidase IC50: 0.055 mM, reductase IC50: 0.58 mM
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
-
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
NADP+
NSC 112288
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-
NSC 56412
-
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NSC 75617
-
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o-Iodosobenzoate
-
complete inhibition of cortisol oxidation at 1 mM
oleanolic acid
-
oxidase IC50: 0.00015 mM, reductase IC50: 0.00055 mM
oxymesterone
-
oxymetholone
-
p-chloromercuribenzoate
-
complete inhibition of oxidation of cortisol at 0.01 mM
perfluorohexane sulfonate
perfluorohexanesulfonate
-
-
perfluorooctane sulfonate
Perfluorooctanoic acid
perfluorooctyl sulfonate
-
-
PF-3319913
-
potent and selective 11beta-HSD1 inhibitor, a 1% dose of PF-3319913 inhibits in vivo 11beta-HSD1 enzyme activity in the rabbit eye by 100% at 2 h
-
PF-3859622
-
potent and selective 11beta-HSD1 inhibitor, a 2% dose of PF-3859622 consistently inhibits in vivo 11beta-HSD1 enzyme activity in the rabbit eye by 100% at 6 and 12 h, a 0.2% dose of PF-3859622 causes 81% inhibition of cortisone conversion at 6 h
-
PF-877423
PF-904955
-
potent and selective 11beta-HSD1 inhibitor, a 1% dose of PF-904955 inhibits in vivo 11beta-HSD1 enzyme activity in the rabbit eye by 88% at 2 h
-
PF-915275
posaconazole
progesterone
-
-
pyrrolidine dithiocarbamate
quercetin
-
resorcinol
-
weak inhibition
resveratrol
Rhein
-
-
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
-
-
UE2316
-
selective isoform 11beta-HSD1 inhibitor
UE2343
selective inhibitor for isoform 11beta-HSD1
WY-14643
-
22% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication
zearalenone
zineb
ziram
[(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
[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
[5-fluoro-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
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