1.1.1.146 (+/-)-2-((cyclohexylmethyl)amino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74603 1.1.1.146 (+/-)-2-((cyclohexylmethyl)amino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74612 1.1.1.146 (+/-)-2-(1-adamantylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74610 1.1.1.146 (+/-)-2-(1-adamantylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74619 1.1.1.146 (+/-)-2-(cycloheptylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74604 1.1.1.146 (+/-)-2-(cycloheptylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74613 1.1.1.146 (+/-)-2-(cyclohexylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74602 1.1.1.146 (+/-)-2-(cyclohexylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74611 1.1.1.146 (+/-)-2-(cyclooctylamino)-5-ethyl-5-methyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74605 1.1.1.146 (+/-)-2-(cyclooctylamino)-5-methyl-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74614 1.1.1.146 (+/-)-5-ethyl-5-methyl-2-(1-norbornylamino)-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74607 1.1.1.146 (+/-)-5-ethyl-5-methyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74609 1.1.1.146 (+/-)-5-ethyl-5-methyl-2-(7-norbornylamino)-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74608 1.1.1.146 (+/-)-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 74606 1.1.1.146 (+/-)-5-methyl-2-(1-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74616 1.1.1.146 (+/-)-5-methyl-2-(3-noradamantylamino)-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74618 1.1.1.146 (+/-)-5-methyl-2-(7-norbornylamino)-5-propyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74617 1.1.1.146 (+/-)-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 74615 1.1.1.146 (-)-catechin about 98% activity at 0.2 mM 23425 1.1.1.146 (-)-epicatechin about 95% activity at 0.2 mM 1846 1.1.1.146 (-)-epigallocatechin less than 80% activity at 0.2 mM 2241 1.1.1.146 (-)-epigallocatechin 3-gallate potent inhibitor, less than 10% activity at 0.2 mM 166004 1.1.1.146 (-)-gallocatechin less than 30% activity at 0.2 mM 126759 1.1.1.146 (1'-[(adamantan-2-yl)carbamoyl]-7-bromo-2,3-dihydrospiro[indene-1,4'-piperidin]-3-yl)acetic acid selective isoform 11beta-HSD1 inhibitor 256567 1.1.1.146 (1-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]cyclopentyl)acetic acid 11% inhibition at 0.001 mM 150805 1.1.1.146 (1-[2-[(2,4-dichlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid 27% inhibition at 0.001 mM 150801 1.1.1.146 (1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid - 73950 1.1.1.146 (1-[2-[(2-chlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid 22% inhibition at 0.001 mM 150800 1.1.1.146 (1-[2-[(4-methoxypyridin-3-yl)amino]-2-oxoethyl]cyclopentyl)acetic acid 7% inhibition at 0.001 mM 150804 1.1.1.146 (1-[2-[(cyclohexylmethyl)amino]-2-oxoethyl]cyclopentyl)acetic acid 7% inhibition at 0.001 mM 150802 1.1.1.146 (1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)acetic acid - 215851 1.1.1.146 (11beta)-11-hydroxyallopregnanolone - 71012 1.1.1.146 (11beta)-11-hydroxyprogesterone - 71011 1.1.1.146 (1E,4E)-1,5-bis(3-methylthiophen-2-yl)penta-1,4-dien-3-one - 217240 1.1.1.146 (1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one derivative of curcumin, IC50 value in intact cells 93 nM. Not inhibitory to isoform 11beta-HSD2 in kidney at 100 microM 89502 1.1.1.146 (1E,4E)-1,5-bis(thiophen-2-yl) penta-1,4-dien-3-one derivative of curcumin, IC50 value in intact cells 184 nM. Not inhibitory to isoform 11beta-HSD2 in kidney at 100 microM 89502 1.1.1.146 (1E,4E)-1,5-bis(thiophen-2-yl)cyclohexanone - 217242 1.1.1.146 (1E,4E)-1,5-bis(thiophen-2-yl)penta-1,4-dien-3-one - 217241 1.1.1.146 (1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 215860 1.1.1.146 (1r,4s)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215856 1.1.1.146 (1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid - 73969 1.1.1.146 (1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 215874 1.1.1.146 (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 - 215873 1.1.1.146 (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 - 15106 1.1.1.146 (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 - 15105 1.1.1.146 (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 - 15104 1.1.1.146 (1S,3R,4R,7S)-4-[[2-(4-methoxyphenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxamide - 73913 1.1.1.146 (1S,3R,4S,5S,7S)-4-(3-(2-fluorophenylsulfonamido)-3-methylbutanamido) adamantane-1-carboxamide - 217261 1.1.1.146 (1s,4r)-4-[3-[(2,3-dichlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215862 1.1.1.146 (1s,4r)-4-[3-[(2,3-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215863 1.1.1.146 (1s,4r)-4-[3-[(2,4-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215864 1.1.1.146 (1s,4r)-4-[3-[(2,6-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 217101 1.1.1.146 (1s,4r)-4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215849 1.1.1.146 (1s,4r)-4-[3-[(3,5-difluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215870 1.1.1.146 (1s,4r)-4-[3-[(3-chloro-2-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215865 1.1.1.146 (1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215866 1.1.1.146 (1s,4r)-4-[3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid - 215867 1.1.1.146 (1s,4r)-4-[3-[(3-chlorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215868 1.1.1.146 (1s,4r)-4-[3-[(3-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215869 1.1.1.146 (1s,4r)-4-[3-[(4-fluorobenzene-1-sulfonyl)amino]-3-methylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 215871 1.1.1.146 (2-benzyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone - 82870 1.1.1.146 (20R,23E)-eupha-8,23-diene-3beta,25-diol - 217247 1.1.1.146 (24R)-eupha-8,25-diene-3beta,24-diol - 217246 1.1.1.146 (2alpha,3beta,5xi,6beta,9xi,18xi)-2,3,6,23-tetrahydroxyurs-12-en-28-oate - 38726 1.1.1.146 (2alpha,3beta,5xi,9xi,18xi)-2,3,23-trihydroxyurs-12-en-28-oate - 38725 1.1.1.146 (2E,4S)-4-hydroxy-5-[(1S,5S,6S)-6-(hydroxymethyl)-2-methylidenebicyclo[3.1.1]hept-6-yl]-2-methylpent-2-enoic acid - 15097 1.1.1.146 (2R)-1,1,1-trifluoro-2-(3-[(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine-1-sulfonyl]phenyl)propan-2-ol HSD-016 254364 1.1.1.146 (2R)-1-(2-chloro-4-(2-methoxyethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine - 26561 1.1.1.146 (2R)-1-(2-chloro-4-(difluoromethoxy)phenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine - 26559 1.1.1.146 (2R)-1-(2-chloro-4-ethoxyphenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine - 26560 1.1.1.146 (2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxamide - 26548 1.1.1.146 (2R)-1-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)piperidine-4-carboxylic acid - 26547 1.1.1.146 (2R)-1-(3-chloro-4-([4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazin-1-yl]sulfonyl)phenyl)piperidin-4-ol - 38907 1.1.1.146 (2R)-1-(4-bromo-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine - 26540 1.1.1.146 (2R)-1-(4-bromophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)-phenyl)-2-methylpiperazine - 38903 1.1.1.146 (2R)-1-(4-tert-butoxy-2-chlorophenylsulfonyl)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazine - 26556 1.1.1.146 (2R)-1-([2-chloro-4-[(3S)-3-methylpiperazin-1-yl]phenyl]sulfonyl)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 26553 1.1.1.146 (2R)-1-[(2-chloro-4-piperidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 38906 1.1.1.146 (2R)-1-[(2-chloro-4-pyrrolidin-1-ylphenyl)sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 26543 1.1.1.146 (2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazine - 82810 1.1.1.146 (2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-(pyridin-4-ylmethyl)piperazine - 82811 1.1.1.146 (2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[1-(pyridin-4-yl)ethyl]piperazine - 82814 1.1.1.146 (2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine - 82812 1.1.1.146 (2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(pyridin-4-yl)propyl]piperazine - 82813 1.1.1.146 (2R)-1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[phenyl(pyridin-4-yl)methyl]piperazine - 82815 1.1.1.146 (2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-N,N-dimethylpiperidin-4-amine - 26546 1.1.1.146 (2R)-1-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one - 38908 1.1.1.146 (2R)-1-[[2-chloro-4-(1H-1,2,4-triazol-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 26557 1.1.1.146 (2R)-1-[[2-chloro-4-(4,4-difluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 26545 1.1.1.146 (2R)-1-[[2-chloro-4-(4-fluoropiperidin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 26544 1.1.1.146 (2R)-1-[[2-chloro-4-(4-methylpiperazin-1-yl)phenyl]sulfonyl]-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazine - 26552 1.1.1.146 (2R)-1-[[4-(1,1-difluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine - 82823 1.1.1.146 (2R)-1-[[4-(1-fluoroethyl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine - 82822 1.1.1.146 (2R)-1-[[4-(2-fluoropropan-2-yl)phenyl]sulfonyl]-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazine - 82818 1.1.1.146 (2R)-2-(3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenoxy)-N,N-dimethylethanamine - 26562 1.1.1.146 (2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]-1-[[4-(1,1,1,2-tetrafluoropropan-2-yl)phenyl]sulfonyl]piperazine - 82820 1.1.1.146 (2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)-N,N-dimethylaniline - 26542 1.1.1.146 (2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile - 26563 1.1.1.146 (2R)-3-chloro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenol - 26558 1.1.1.146 (2R)-3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)benzamide - 26564 1.1.1.146 (2R)-4-(3-fluoro-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)morpholine - 26550 1.1.1.146 (2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzamide - 26538 1.1.1.146 (2R)-4-(4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methylpiperazin-1-ylsulfonyl)benzonitrile - 26535 1.1.1.146 (2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-1-(4-methoxyphenylsulfonyl)-2-methylpiperazine - 38904 1.1.1.146 (2R)-4-(4-fluoro-2-(trifluoromethyl)phenyl)-2-methyl-1-(4-(trifluoromethoxy)-phenylsulfonyl)-piperazine - 26536 1.1.1.146 (2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-cis-2,6-dimethylmorpholine - 26551 1.1.1.146 (2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine - 26549 1.1.1.146 (2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]piperazin-2-one - 26555 1.1.1.146 (2R)-4-[3-chloro-4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]thiomorpholine-1,1-dioxide - 26554 1.1.1.146 (2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[(4-piperidin-1-ylphenyl)sulfonyl]piperazine - 38905 1.1.1.146 (2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methyl-1-[[4-(1H-tetrazol-5-yl)phenyl]sulfonyl]piperazine - 26539 1.1.1.146 (2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide - 29013 1.1.1.146 (2R)-N-(5-hydroxytricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide treatment of BALB/c mice 15, and 60 m per kg dose-dependently decreases the formation of prednisolone, with respective inhibition ratios of 72 and 88%. The concentration of inhibitor in subcutaneous and celiac adipose as well as liver tissue remains high within 1 h after i.v. treatment, whereas the concentration in plasma dramatically decreases 15 min after administration. The inhibitor is also eliminated moderately in adipose and liver tissue over the subsequent 5 h 29013 1.1.1.146 (2R)-N-(tricyclo[3.3.1.13,7]dec-2-yl)-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide - 29012 1.1.1.146 (2R)-N-cycloheptyl-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide - 29010 1.1.1.146 (2R)-N-[(1R,2S,4R)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]-1-[(3-chloro-2-methylphenyl)sulfonyl]piperidine-2-carboxamide - 29011 1.1.1.146 (2R)-N-[3-chloro-4-([4-[4-fluoro-2-(trifluoromethyl)phenyl]-piperazin-1-yl]sulfonyl)phenyl]morpholine-4-carboxamide - 26541 1.1.1.146 (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 - 26272 1.1.1.146 (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 - 150799 1.1.1.146 (2S)-2-[[(E)-[(1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-3-(4-hydroxyphenyl)propanoic acid - 254429 1.1.1.146 (2S)-5-(acetyloxy)-2-hydroxypentyl acetate - 27981 1.1.1.146 (3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid - 28014 1.1.1.146 (3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid - 28011 1.1.1.146 (3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid - 29027 1.1.1.146 (3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid - 28012 1.1.1.146 (3alpha,5alpha)-3,11,21-trihydroxypregn-11-en-20-one - 38139 1.1.1.146 (3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid - 27957 1.1.1.146 (3beta)-3-hydroxy-11-oxoolean-12-en-30-amide - 27961 1.1.1.146 (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 42543 1.1.1.146 (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 44017 1.1.1.146 (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 42544 1.1.1.146 (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 42545 1.1.1.146 (3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide - 27958 1.1.1.146 (3beta,18alpha)-3-hydroxy-11-oxoolean-12-en-30-oate - 217230 1.1.1.146 (3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid - 28016 1.1.1.146 (3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid - 28015 1.1.1.146 (3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide - 28020 1.1.1.146 (3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid - 28018 1.1.1.146 (3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid - 28017 1.1.1.146 (3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid - 29029 1.1.1.146 (3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide - 29031 1.1.1.146 (3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide - 28019 1.1.1.146 (3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide - 29030 1.1.1.146 (3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide - 28021 1.1.1.146 (3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester - 28010 1.1.1.146 (3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide - 28009 1.1.1.146 (3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid - 29028 1.1.1.146 (3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid - 28013 1.1.1.146 (3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide - 28022 1.1.1.146 (3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide - 28023 1.1.1.146 (3beta,5xi,18xi)-oleana-9(11),12-diene-3,30-diol - 26278 1.1.1.146 (3beta,5xi,9xi)-oleana-11,13(18)-diene-3,30-diol - 26279 1.1.1.146 (3beta,5xi,9xi,18xi)-3,30-dihydroxyolean-12-en-11-one - 26273 1.1.1.146 (3beta,5xi,9xi,18xi)-3-(acetyloxy)-11-oxours-12-en-24-oate - 38724 1.1.1.146 (3beta,5xi,9xi,18xi)-3-(acetyloxy)urs-12-en-24-oate - 38723 1.1.1.146 (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-al - 26274 1.1.1.146 (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate - 26271 1.1.1.146 (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxours-12-en-28-oate - 38722 1.1.1.146 (3beta,5xi,9xi,18xi)-3-hydroxyolean-12-en-28-oate - 38721 1.1.1.146 (3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid - 27960 1.1.1.146 (3E)-3-[[(4-bromo-3-methylphenoxy)acetyl]hydrazono]-N-tricyclo[3.3.1.13,7]dec-1-ylbutanamide - 73947 1.1.1.146 (3R)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide - 215982 1.1.1.146 (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 - 73917 1.1.1.146 (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 - 73916 1.1.1.146 (3R,4R,7S)-4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxamide - 73908 1.1.1.146 (3S)-1-(3-chloro-2-methylbenzene-1-sulfonyl)-N-cyclohexylpiperidine-3-carboxamide INCB-13739, selective inhibitor for isoform 11beta-HSD1 254484 1.1.1.146 (3S)-3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide - 215984 1.1.1.146 (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 42546 1.1.1.146 (4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone - 82866 1.1.1.146 (4-hydroxy-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-3-yl)(phenyl)methanone - 82867 1.1.1.146 (4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decan-1-yl)acetic acid - 216025 1.1.1.146 (4aS,5R,8aR)-5,6-bis(hydroxymethyl)-1,1,4a-trimethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol - 10315 1.1.1.146 (4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-1,2,3,4,4a,5,8,8a-octahydronaphthalen-2-ol - 10314 1.1.1.146 (4aS,5S,8aR)-5-(hydroxymethyl)-1,1,4a,6-tetramethyl-3,4,4a,5,8,8a-hexahydronaphthalen-2(1H)-one - 10313 1.1.1.146 (4R,7S)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one - 217267 1.1.1.146 (4S,7R)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one - 217266 1.1.1.146 (5R)-2-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-5-methyl-5-(trifluoromethyl)-1,3-thiazol-4(5H)-one - 73942 1.1.1.146 (5xi,9xi,18xi)-3,11-dioxoolean-12-en-30-al - 26275 1.1.1.146 (6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)acetic acid - 82847 1.1.1.146 (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 254602 1.1.1.146 (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 89497 1.1.1.146 (6S)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-3-[1-(4'-fluorobiphenyl-4-yl)ethyl]-1,3-oxazinan-2-one - 89498 1.1.1.146 (E)-5-((benzo[d]thiazol-2-ylimino)(methylthio)methylamino)-2-hydroxybenzoic acid - 254616 1.1.1.146 (R)-1-((S)-2-acetamido-3-(2-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254630 1.1.1.146 (R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254631 1.1.1.146 (R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254632 1.1.1.146 (R)-1-((S)-2-acetamido-3-(4-methoxyphenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254633 1.1.1.146 (R)-1-((S)-3-([1,1'-biphenyl]-3-yl)-2-aminopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254634 1.1.1.146 (R)-1-(3-acetamidopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254635 1.1.1.146 (R)-1-(acetyl-L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254636 1.1.1.146 (R)-1-(acetylglycyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254637 1.1.1.146 (R)-1-(L-tryptophyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254638 1.1.1.146 (R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide - 254639 1.1.1.146 (R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one - 41115 1.1.1.146 (R)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one - 41109 1.1.1.146 (R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one - 41114 1.1.1.146 (R)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one - 41110 1.1.1.146 (R)-N-(adamantan-2-yl)-1-((S)-2-(2-aminoacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide - 254642 1.1.1.146 (R)-N-(adamantan-2-yl)-1-((S)-2-(2-hydroxyacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide - 254643 1.1.1.146 (R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(3-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide - 254644 1.1.1.146 (R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide - 254645 1.1.1.146 (S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one - 41113 1.1.1.146 (S)-2-((1R,2R,4S)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one - 41111 1.1.1.146 (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one - 41112 1.1.1.146 (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one - 41108 1.1.1.146 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine] - 73974 1.1.1.146 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine] - 73975 1.1.1.146 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine] - 73977 1.1.1.146 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine] - 73976 1.1.1.146 1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol - 82833 1.1.1.146 1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol - 82835 1.1.1.146 1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-3-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol - 82831 1.1.1.146 1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclobutyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol - 82832 1.1.1.146 1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopentyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol - 82834 1.1.1.146 1,1,1-trifluoro-2-(4-[[(2R)-2-methyl-4-[[1-(pyridin-4-yl)cyclopropyl]methyl]piperazin-1-yl]sulfonyl]phenyl)propan-2-ol - 82830 1.1.1.146 1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-2-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol - 82827 1.1.1.146 1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-3-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol - 82826 1.1.1.146 1,1,1-trifluoro-2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol - 82819 1.1.1.146 1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216167 1.1.1.146 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 - 216168 1.1.1.146 1,7,8,8-tetramethyl-2-(4-methylphenyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216169 1.1.1.146 1,7,8,8-tetramethyl-2-(pyridin-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216170 1.1.1.146 1,7,8,8-tetramethyl-2-[2-(trifluoromethyl)phenyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216172 1.1.1.146 1,7,8,8-tetramethyl-2-[[2-(trifluoromethyl)phenyl]methyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216171 1.1.1.146 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 74639 1.1.1.146 1-(2,4-dichlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)-ethanone - 83268 1.1.1.146 1-(3,4-dimethoxyphenyl)-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone poor stability in liver microsomes 89500 1.1.1.146 1-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)-2-methyl-1H-benzimidazole - 26258 1.1.1.146 1-(3-methoxyphenyl)-2-(phenylsulfonyl)ethanone - 73903 1.1.1.146 1-(4-chlorophenyl)-2-(2-methylbenzo[d]thiazol-5-ylamino)ethanone - 83267 1.1.1.146 1-(5-oxo-2,5-dihydrofuran-3-yl)urea specific for isozyme 11beta-HSD1 132147 1.1.1.146 1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol - 216135 1.1.1.146 1-adamantan-1-yl-2-(2,4-dichloro-benzylsulfanyl)ethanone - 41107 1.1.1.146 1-adamantan-1-yl-2-(2,4-dichloro-phenylmethanesulfonyl)ethanone - 83357 1.1.1.146 1-adamantan-1-yl-2-(2-chloro-benzylsulfanyl)ethanone - 83347 1.1.1.146 1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfinyl)ethanone - 83351 1.1.1.146 1-adamantan-1-yl-2-(2-chloro-phenylmethanesulfonyl)ethanone - 83354 1.1.1.146 1-adamantan-1-yl-2-(2-methylbenzothiazol-5-ylamino)ethanone - 83269 1.1.1.146 1-adamantan-1-yl-2-(2-methylbenzothiazol-5-yloxy)ethanone - 83271 1.1.1.146 1-adamantan-1-yl-2-(3,4-dimethoxy-benzyloxy)ethanone - 83344 1.1.1.146 1-adamantan-1-yl-2-(3,4-dimethoxy-phenoxy)ethanone - 83332 1.1.1.146 1-adamantan-1-yl-2-(3-methylbenzylsulfanyl)ethanone - 83348 1.1.1.146 1-adamantan-1-yl-2-(3-trifluoromethyl-phenoxy)ethanone - 83329 1.1.1.146 1-adamantan-1-yl-2-(3-trifluoromethylbenzyloxy)ethanone - 83341 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-benzenesulfinyl)ethanone - 83335 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-benzenesulfonyl)ethanone - 83337 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-benzyloxy)ethanone - 83345 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-benzylsulfanyl)ethanone - 83346 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-phenoxy)ethanone - 83330 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfinyl)ethanone - 83350 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-phenylmethanesulfonyl)ethanone - 83353 1.1.1.146 1-adamantan-1-yl-2-(4-chloro-phenylsulfanyl)ethanone - 83333 1.1.1.146 1-adamantan-1-yl-2-(4-methoxy-benzyloxy)ethanone - 83343 1.1.1.146 1-adamantan-1-yl-2-(4-methylbenzyloxy)ethanone - 83342 1.1.1.146 1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfinyl)ethanone - 83352 1.1.1.146 1-adamantan-1-yl-2-(4-tert-butyl-phenylmethanesulfonyl)ethanone - 83356 1.1.1.146 1-adamantan-1-yl-2-(4-tert-butylbenzylsulfanyl)ethanone - 83349 1.1.1.146 1-adamantan-1-yl-2-(4-trifluoromethyl-phenoxy)ethanone - 83328 1.1.1.146 1-adamantan-1-yl-2-(4-trifluoromethylbenzyloxy)ethanone - 83340 1.1.1.146 1-adamantan-1-yl-2-(biphenyl-4-ylmethoxy)ethanone - 83339 1.1.1.146 1-adamantan-1-yl-2-(biphenyl-4-yloxy)ethanone - 83327 1.1.1.146 1-adamantan-1-yl-2-(toluene-4-sulfinyl)ethanone - 83336 1.1.1.146 1-adamantan-1-yl-2-(toluene-4-sulfonyl)ethanone - 83338 1.1.1.146 1-adamantan-1-yl-2-m-tolylmethanesulfonyl-ethanone - 83355 1.1.1.146 1-adamantan-1-yl-2-p-tolyloxy-ethanone - 83331 1.1.1.146 1-adamantan-1-yl-2-p-tolylsulfanyl-ethanone - 83334 1.1.1.146 1-benzyl-2-(2,4-difluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216155 1.1.1.146 1-benzyl-2-(2-fluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216154 1.1.1.146 1-benzyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216156 1.1.1.146 1-ethyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216158 1.1.1.146 1-methyl-2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole - 216159 1.1.1.146 1-methyl-4-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole - 26201 1.1.1.146 1-methyl-4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]-1H-indole - 26200 1.1.1.146 1-methyl-5-(4-methyl-5-phenyl-4H-1,2,4-triazol-3-yl)-1H-indole - 26202 1.1.1.146 1-phenyl-2-[(1-phenyl-1H-tetrazol-5-yl)sulfanyl]ethanone poor stability in liver microsomes 89499 1.1.1.146 1-piperidinecarboxylic acid - 132136 1.1.1.146 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 - 73925 1.1.1.146 1-[(2,4-dichlorophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89505 1.1.1.146 1-[(2-chlorobenzyl)oxy]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile compound with a superior metabolic stability profile, but sub-optimal with respect to aqueous solubility 29049 1.1.1.146 1-[(2-chlorobenzyl)sulfanyl]-3-hydroxy-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile good inhibitory activity. Compound undergoes oxidative metabolism at several sites 29046 1.1.1.146 1-[(2-chlorobenzyl)sulfanyl]-7-fluoro-3-hydroxyisoquinoline-4-carbonitrile overall good inhibitory activity and metabolic stability 29048 1.1.1.146 1-[(2-naphthylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89504 1.1.1.146 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide - 29020 1.1.1.146 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide - 29019 1.1.1.146 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide 71% and 62% inhibition of enzyme in adipose and liver tissue at 1 h after administration, short-acting compound displaying a significant drop in potency in the subsequent 3 h 29019 1.1.1.146 1-[(4-methylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 27983 1.1.1.146 1-[(4-nitrophenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89506 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-(4-nitrophenyl)piperazine - 89511 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-(2R)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89509 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-(2S)-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89510 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-2-methyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89508 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-4-(4-nitrophenyl)piperazine - 82809 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-4-(5-nitropyridin-2-yl)piperazine - 82883 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-4-[3-(trifluoromethyl)pyridin-2-yl]piperazine - 89503 1.1.1.146 1-[(4-tert-butylphenyl)sulfonyl]-5-[3-(trifluoromethyl)pyridin-2-yl]-1,5-diazocane - 89507 1.1.1.146 1-[1-(3,4-dimethylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 82884 1.1.1.146 1-[1-(3-methoxy-4-methylbenzoyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 82885 1.1.1.146 1-[1-[(3,4-dimethylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 26267 1.1.1.146 1-[1-[(3-amino-4-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 89525 1.1.1.146 1-[1-[(3-methoxyphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 26266 1.1.1.146 1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 89524 1.1.1.146 1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]ethanol - 82821 1.1.1.146 1-[[(3R)-3-methyl-4-([4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide - 82840 1.1.1.146 1-[[(3R)-3-methyl-4-([4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonyl)piperazin-1-yl]methyl]cyclopropanecarboxamide - 82839 1.1.1.146 1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclobutanecarboxamide - 82837 1.1.1.146 1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropanecarboxamide - 82836 1.1.1.146 1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline - 89517 1.1.1.146 11-dehydrocortisterone - 29017 1.1.1.146 11-deoxycorticosterone IC50: 0.031 mM 1638 1.1.1.146 11-deoxycorticosterone - 1638 1.1.1.146 11-ketotestosterone - 60355 1.1.1.146 11-oxo-3alpha,5alpha-tetrahydrotestosterone - 42548 1.1.1.146 11-oxo-3beta,5alpha-tetrathydrotestosterone - 29014 1.1.1.146 11-oxo-allopregnanolone - 13939 1.1.1.146 11-oxo-androstenedione - 89501 1.1.1.146 11-oxo-progesterone - 11660 1.1.1.146 11-oxo-testosterone - 13940 1.1.1.146 11-oxoandrosterone 0.0021 mM, 50% inhibition of oxido-reductase reaction 122886 1.1.1.146 11-oxoprogesterone 0.0095 mM, 50% inhibition of oxido-reductase reaction 90643 1.1.1.146 11-oxotestosterone 0.018 mM, 50% inhibition of oxido-reductase reaction 34559 1.1.1.146 11alpha-hydroxyprogesterone - 6411 1.1.1.146 11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione i.e. cortisol 3006 1.1.1.146 11beta,17,21-trihydroxy-pregn-4-ene-3,20-dione i.e. cortisol; poor inhibition of corticosterone oxidation 3006 1.1.1.146 11beta,21-dihydroxypregn-4-en-3,20-dione potent inhibition of cortisol oxidation 2895 1.1.1.146 11beta-hydroxy-allopregnanolone - 24047 1.1.1.146 11beta-hydroxy-androstanediol - 38140 1.1.1.146 11beta-hydroxy-testosterone - 23292 1.1.1.146 11beta-hydroxyandrostanediol - 29015 1.1.1.146 11beta-hydroxyandrostenedione - 29016 1.1.1.146 11beta-hydroxyandrosterone 0.07 mM, 50% inhibition of dehydrogenase reaction 122885 1.1.1.146 11beta-hydroxydehydroepiandrosterone 0.003 mM, 50% inhibition of dehydrogenase reaction 122884 1.1.1.146 11beta-hydroxyprogesterone 0.0004 mM, 50% inhibition of dehydrogenase reaction 5889 1.1.1.146 11beta-hydroxyprogesterone - 5889 1.1.1.146 11beta-hydroxytestosterone 0.0017 mM, 50% inhibition of dehydrogenase reaction 5890 1.1.1.146 11beta-hydroxytestosterone - 5890 1.1.1.146 17beta-estradiol non-competitive 745 1.1.1.146 17beta-estradiol - 745 1.1.1.146 17beta-estradiol-3-acetate - 163013 1.1.1.146 18alpha-glycyrrhetinic acid selective inhibition of 11beta-HSD1, does not inhibit 11beta-HSD2 at concentrations up to 0.02 mM 74626 1.1.1.146 18beta-glycyrrhetinic acid inhibits both 11beta-HSD1 and 11beta-HSD2, but preferentially inhibits 11beta-HSD2 11971 1.1.1.146 18beta-glycyrrhetinic acid 11beta-HSD1 inhibitor with submicromolar potency 11971 1.1.1.146 18beta-glycyrrhetinic acid - 11971 1.1.1.146 2'-hydroxyflavanone 0.2 mM, more than 90% inhibition of 7-oxocholesterol reduction in liver homogenates 3736 1.1.1.146 2'-hydroxyflavanone - 3736 1.1.1.146 2,2'-Dihydroxybiphenyl - 6413 1.1.1.146 2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability 29023 1.1.1.146 2,4-dichloro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]naphthalen-1-yl]benzamide - 73907 1.1.1.146 2,4-dichloro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]phenyl]benzamide - 73905 1.1.1.146 2,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzenesulfonamide - 73949 1.1.1.146 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 254944 1.1.1.146 2,6-dichloro-4-[(5,7,7-trimethyl-2-azabicyclo[3.2.1]oct-2-yl)carbonyl]aniline - 73922 1.1.1.146 2,6-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 20.59% inhibition of isoform 11beta-HSD1 at 0.01 mM 254945 1.1.1.146 2,7-dimethyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 17.65% inhibition of isoform 11beta-HSD1 at 0.01 mM 254947 1.1.1.146 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 254948 1.1.1.146 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 74625 1.1.1.146 2-(1-adamantylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74622 1.1.1.146 2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73957 1.1.1.146 2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73954 1.1.1.146 2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73958 1.1.1.146 2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73956 1.1.1.146 2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73952 1.1.1.146 2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73955 1.1.1.146 2-(2,4-dibromophenoxy)-N-[3-(1-hydroxyethyl)phenyl]propanamide - 14599 1.1.1.146 2-(2,4-difluorophenyl)-7,8,8-trimethyl-1-(2-phenylethyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216189 1.1.1.146 2-(2,5-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216190 1.1.1.146 2-(2,6-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216193 1.1.1.146 2-(2-chloro-4-fluorophenoxy)-2-methyl-N-[(1R,2R,7S)-5-(methylsulfonyl)tricyclo[3.3.1.13,7]dec-2-yl]propanamide - 73914 1.1.1.146 2-(2-chloro-4-fluorophenoxy)-2-methyl-N-[(1R,2R,7S)-5-sulfamoyltricyclo[3.3.1.13,7]dec-2-yl]propanamide - 73915 1.1.1.146 2-(2-chlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216183 1.1.1.146 2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine - 89513 1.1.1.146 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 - 216184 1.1.1.146 2-(2-fluorophenyl)-7,8,8-trimethyl-1-(propan-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216185 1.1.1.146 2-(2-fluorophenyl)-7,8,8-trimethyl-1-propyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216186 1.1.1.146 2-(2-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one - 82881 1.1.1.146 2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane - 73984 1.1.1.146 2-(2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-1,3-thiazol-4-yl)-N,N-diethylacetamide - 26265 1.1.1.146 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(4-nitrophenyl)ethanone - 82875 1.1.1.146 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-(biphenyl-4-yl)ethanone - 82874 1.1.1.146 2-(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)-1-phenylethanone - 27979 1.1.1.146 2-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine - 26250 1.1.1.146 2-(3-iodophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216195 1.1.1.146 2-(3-methoxyphenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216196 1.1.1.146 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 74624 1.1.1.146 2-(4-chlorophenoxy)-N-[(1R,2R,7S)-5-(hydroxycarbamimidoyl)tricyclo[3.3.1.13,7]dec-2-yl]-2-methylpropanamide - 73910 1.1.1.146 2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine - 89514 1.1.1.146 2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one - 82882 1.1.1.146 2-(4-methylphenyl)-2-oxoethyl 2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-3-phenylpropanoate - 89520 1.1.1.146 2-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine - 174504 1.1.1.146 2-(6-[[(3-chloro-2-methylphenyl)sulfonyl]amino]pyridin-2-yl)-N,N-diethylacetamide - 82841 1.1.1.146 2-(adamantan-1-yl)-N-methyl-N-(thiophen-3-ylmethyl)acetamide - 74634 1.1.1.146 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 255110 1.1.1.146 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 255111 1.1.1.146 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 255112 1.1.1.146 2-(bicyclo[2.2.1]hept-2-ylamino)-5-(propan-2-yl)-1,3-thiazol-4(5H)-one - 82878 1.1.1.146 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 255132 1.1.1.146 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 255133 1.1.1.146 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 255134 1.1.1.146 2-(cycloheptylamino)-5-methyl-5-(1-methylethyl)-1,3-thiazol-4(5H)-one - 73937 1.1.1.146 2-(cyclooctylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74623 1.1.1.146 2-(cyclooctylamino)-5,5-diethyl-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74620 1.1.1.146 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 255136 1.1.1.146 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 255137 1.1.1.146 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 255138 1.1.1.146 2-adamantan-1-yl-N-methyl-N-thiophen-2-ylmethyl-acetamide - 74632 1.1.1.146 2-benzyl-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one - 216262 1.1.1.146 2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane competitive. Also inhibitory to isoform 11beta-HSD2 29021 1.1.1.146 2-bis(p-hydroxyphenyl)-1,1,1-trichloroethane - 29021 1.1.1.146 2-bis-(4-hydroxyphenyl)-1,1,1-trichloroethane - 256548 1.1.1.146 2-bromo-N-[2-([2-oxo-2-[(2-phenylethyl)amino]ethyl]sulfanyl)-2,3-dihydro-1,3-benzothiazol-6-yl]benzamide - 89522 1.1.1.146 2-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide - 27964 1.1.1.146 2-hydroxy-5-[[(E)-[(5-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid - 255215 1.1.1.146 2-hydroxy-5-[[(E)-[(5-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid - 255216 1.1.1.146 2-hydroxy-5-[[(E)-[(6-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid - 255217 1.1.1.146 2-hydroxy-5-[[(E)-[(6-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid - 255218 1.1.1.146 2-hydroxy-5-[[(E)-[(7-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid - 255219 1.1.1.146 2-hydroxy-5-[[(E)-[(7-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid - 255220 1.1.1.146 2-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one 29.41% inhibition of isoform 11beta-HSD1 at 0.01 mM 255239 1.1.1.146 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 255240 1.1.1.146 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 255241 1.1.1.146 2-oxopentane-1,5-diyl diacetate - 10316 1.1.1.146 2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane - 73985 1.1.1.146 2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane - 73982 1.1.1.146 2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane - 73983 1.1.1.146 2-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-ylamino]-5-methyl-5-(propan-2-yl)-1,3-thiazol-4(5H)-one - 40963 1.1.1.146 2-[(2-chlorobenzyl)sulfanyl]-4-hydroxy-6-phenylpyrimidine-5-carbonitrile lead compound for development of inhibitors, the hydroxypyrimidine may act as a H-bonding pharmacophore. Compound has good cross species 11beta-HSD1 inhibitory activity for the mouse, cynomolgus monkey, and human enzymes 29045 1.1.1.146 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine - 89516 1.1.1.146 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine - 89515 1.1.1.146 2-[(3-benzoyl-2-methyl-1,1-dioxido-2H-1,2-benzothiazin-4-yl)oxy]-1-phenylethanone - 82868 1.1.1.146 2-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylthiazole-4-carboxamide - 27998 1.1.1.146 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylthiazole-4-carboxamide - 28004 1.1.1.146 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylthiazole-4-carboxamide - 28006 1.1.1.146 2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide - 28002 1.1.1.146 2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane - 73981 1.1.1.146 2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane - 73980 1.1.1.146 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 89495 1.1.1.146 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 89496 1.1.1.146 2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73960 1.1.1.146 2-[1-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]cyclopropyl]-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamide - 216231 1.1.1.146 2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73959 1.1.1.146 2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73953 1.1.1.146 2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73964 1.1.1.146 2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide - 73961 1.1.1.146 2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyrazine - 255269 1.1.1.146 2-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine - 255270 1.1.1.146 2-[4-(2,6-difluorobenzenesulfonyl)-[1,4]diazepan-1-yl]-1-(octahydroquinolin-1-yl)-ethanone - 83358 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N,N-dimethyl-acetamide - 83307 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-benzyl-acetamide - 83312 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-ethyl-acetamide - 83309 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-furan-2-ylmethyl-acetamide - 83314 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-isopropyl-acetamide - 83310 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-methyl-acetamide - 83306 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-phenyl-acetamide - 83313 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]-N-tert-butyl-acetamide - 83311 1.1.1.146 2-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide - 83308 1.1.1.146 2-[4-(3,4-dimethoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole - 216236 1.1.1.146 2-[4-(3-methylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzothiazole 89% residual activity at 0.02 mM 216234 1.1.1.146 2-[4-(3-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1,3-benzoxazole 18% residual activity at 0.02 mM 216235 1.1.1.146 2-[4-(3-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole 60% residual activity at 0.02 mM 216233 1.1.1.146 2-[4-(4-methoxy-3-nitrobenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole 75% residual activity at 0.02 mM 217061 1.1.1.146 2-[4-(4-methoxybenzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole - 216238 1.1.1.146 2-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-1H-benzimidazole - 216239 1.1.1.146 2-[4-(4-tert-butylphenyl)sulfonylpiperazin-1-yl]-1-methyl-benzimidazole - 217233 1.1.1.146 2-[4-(4-[[(hydroxyamino)oxy]methyl]benzene-1-sulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole 90% residual activity at 0.02 mM 216237 1.1.1.146 2-[4-(benzenesulfonyl)piperazin-1-yl]-1-methyl-1H-benzimidazole - 216241 1.1.1.146 2-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]propan-2-ol - 82817 1.1.1.146 2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-3-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol - 82829 1.1.1.146 2-[4-([(2R)-4-[2,2-difluoro-2-(pyridin-4-yl)ethyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]-1,1,1-trifluoropropan-2-ol - 82828 1.1.1.146 2-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol - 26219 1.1.1.146 2-[[(1S)-1-(2-fluorophenyl)ethyl]amino]-5-methyl-5-(trifluoromethyl)-1,3-thiazol-4(5H)-one - 73941 1.1.1.146 2-[[(2,6-dichlorophenyl)thio]methyl]-6-[(4-methylpiperidin-1-yl)carbonyl]pyridine - 174488 1.1.1.146 2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane - 73978 1.1.1.146 2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane - 73979 1.1.1.146 3,11-dioxoolean-12-en-30-oic acid - 27959 1.1.1.146 3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide - 73966 1.1.1.146 3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide - 73968 1.1.1.146 3,4-dicyclopropyl-5-[2-(1H-pyrrol-1-yl)propan-2-yl]-4H-1,2,4-triazole - 255312 1.1.1.146 3,4-dicyclopropyl-5-[2-(3,5-dichlorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255313 1.1.1.146 3,4-dicyclopropyl-5-[2-(3-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255314 1.1.1.146 3,4-dicyclopropyl-5-[2-(5-fluorothiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255315 1.1.1.146 3,4-dicyclopropyl-5-[2-(5-methylthiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255316 1.1.1.146 3,4-dicyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255317 1.1.1.146 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 255318 1.1.1.146 3,4-dicyclopropyl-5-[2-[5-(trifluoromethyl)thiophen-2-yl] -propan-2-yl]-4H-1,2,4-triazole - 255319 1.1.1.146 3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability 29024 1.1.1.146 3,5-bis(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole - 26171 1.1.1.146 3,5-bis(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole - 26170 1.1.1.146 3,5-dichloro-N-(2-methyl-1,3-benzothiazol-5-yl)benzamide - 26280 1.1.1.146 3-((3r,5r,7r)-adamantan-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 74 nM, isozyme 11beta-HSD2 IC50: 0.004 mM 29041 1.1.1.146 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 74640 1.1.1.146 3-(1-adamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine - 174495 1.1.1.146 3-(1-fluoronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26205 1.1.1.146 3-(1-methoxy-2-naphthyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 174493 1.1.1.146 3-(1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26204 1.1.1.146 3-(1-phenylcyclobutyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 10208 1.1.1.146 3-(1-phenylcyclohexyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14576 1.1.1.146 3-(1-phenylcyclopentyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14580 1.1.1.146 3-(1-phenylcyclopropyl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14592 1.1.1.146 3-(1-[6-[(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)carbamoyl]pyridin-2-yl]piperidin-4-yl)propanoic acid - 216300 1.1.1.146 3-(2,3-difluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26179 1.1.1.146 3-(2,4-dichlorophenyl)-4-methyl-5-(2-nitrophenyl)-4H-1,2,4-triazole - 26195 1.1.1.146 3-(2,4-dichlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole - 26183 1.1.1.146 3-(2,4-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 174491 1.1.1.146 3-(2,4-dichlorophenyl)-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole - 26178 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethanesulfinyl)-N,N-dimethylbenzamide - 83304 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethanesulfonyl)-N,N-dimethylbenzamide - 83305 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide - 83300 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide - 83296 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide - 83299 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide - 83297 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide - 83295 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide - 83301 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide - 83298 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)benzamide - 83294 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid - 83322 1.1.1.146 3-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester - 83321 1.1.1.146 3-(2-bromophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 174490 1.1.1.146 3-(2-bromophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole - 26169 1.1.1.146 3-(2-bromophenyl)-5-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole - 26172 1.1.1.146 3-(2-chloro-4-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26168 1.1.1.146 3-(2-chloro-4-fluorophenyl)-5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazole - 26175 1.1.1.146 3-(2-chlorophenyl)-4-methyl-5-(4-pentylphenyl)-4H-1,2,4-triazole - 26192 1.1.1.146 3-(2-chlorophenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole - 26182 1.1.1.146 3-(2-chlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26167 1.1.1.146 3-(2-chlorophenyl)-5-(3,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole - 26185 1.1.1.146 3-(2-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26225 1.1.1.146 3-(2-chlorophenyl)-5-[2-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-4H-1,2,4-triazole - 26180 1.1.1.146 3-(3,4,7-trimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 180 nM, isozyme 11beta-HSD2 IC50: 0.004 mM 29036 1.1.1.146 3-(3,4-dimethyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 13 nM, isozyme 11beta-HSD2 IC50: 0.00255 mM 29035 1.1.1.146 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 23932 1.1.1.146 3-(3,5-dichlorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26184 1.1.1.146 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 23931 1.1.1.146 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 23938 1.1.1.146 3-(3,5-dimethyladamantylmethyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 36 nM, isozyme 11beta-HSD2 IC50: 0.0176 mM 29042 1.1.1.146 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 23934 1.1.1.146 3-(3-bromotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 23 nM, isozyme 11beta-HSD2 IC50: 0.004 mM 29038 1.1.1.146 3-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine - 26248 1.1.1.146 3-(3-chlorobiphenyl-4-yl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 14575 1.1.1.146 3-(3-chloronaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26211 1.1.1.146 3-(3-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26226 1.1.1.146 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 23936 1.1.1.146 3-(3-fluorotricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 37 nM, isozyme 11beta-HSD2 IC50: 0.004 mM 29040 1.1.1.146 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 23935 1.1.1.146 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 23933 1.1.1.146 3-(3-phenyltricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 2.3 nM, isozyme 11beta-HSD2 IC50: 23 nM 29037 1.1.1.146 3-(4-benzylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26242 1.1.1.146 3-(4-butyl-2-methylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26190 1.1.1.146 3-(4-butylphenyl)-4-methyl-5-phenyl-4H-1,2,4-triazole - 26193 1.1.1.146 3-(4-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26212 1.1.1.146 3-(4-chloro-2-fluorophenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26177 1.1.1.146 3-(4-chloro-3-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26209 1.1.1.146 3-(4-chlorophenyl)-4-methyl-5-(1-[4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]cyclobutyl)-4H-1,2,4-triazole - 174506 1.1.1.146 3-(4-chlorophenyl)-4-methyl-5-[1-[3'-(methylsulfonyl)biphenyl-4-yl]cyclobutyl]-4H-1,2,4-triazole - 174509 1.1.1.146 3-(4-chlorophenyl)-5-(1-biphenyl-3-ylcyclobutyl)-4-methyl-4H-1,2,4-triazole - 174501 1.1.1.146 3-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole - 26186 1.1.1.146 3-(4-chlorophenyl)-5-[1-(2,4-dichlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 174500 1.1.1.146 3-(4-chlorophenyl)-5-[1-(3-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 174498 1.1.1.146 3-(4-chlorophenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26224 1.1.1.146 3-(4-chlorophenyl)-5-[1-(4-fluorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 174499 1.1.1.146 3-(4-chlorophenyl)-5-[1-[2'-(ethylsulfonyl)biphenyl-4-yl]cyclobutyl]-4-methyl-4H-1,2,4-triazole - 174507 1.1.1.146 3-(4-chlorophenyl)-5-[1-[3'-(ethylsulfonyl)biphenyl-4-yl]cyclobutyl]-4-methyl-4H-1,2,4-triazole - 174508 1.1.1.146 3-(4-chlorophenyl)-5-[1-[4-(1H-imidazol-1-yl)phenyl]cyclobutyl]-4-methyl-4H-1,2,4-triazole - 174505 1.1.1.146 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 - 73936 1.1.1.146 3-(4-pentylbicyclo[2.2.2]oct-1-yl)-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 73930 1.1.1.146 3-(4-tert-butylphenyl)-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26243 1.1.1.146 3-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine - 174502 1.1.1.146 3-(6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepin-3-yl)tricyclo[3.3.1.13,7]decan-1-ol isozyme 11beta-HSD1 IC50: 739 nM, isozyme 11beta-HSD2 IC50: 0.004 mM 29039 1.1.1.146 3-(7-chloro-1-methoxy-2-naphthyl)-4-methyl-5-[2-(methylsulfonyl)phenyl]-4H-1,2,4-triazole - 174494 1.1.1.146 3-(7-chloro-1-methoxy-2-naphthyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 174492 1.1.1.146 3-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26203 1.1.1.146 3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine isozyme 11beta-HSD1 IC50: 7.8 nM, isozyme 11beta-HSD2 IC50: above 0.003 mM 29033 1.1.1.146 3-(adamantan-1-yl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine isozyme 11beta-HSD1 IC50: 98 nM, isozyme 11beta-HSD2 IC50: above 0.01 mM 29033 1.1.1.146 3-(tricyclo[3.3.1.13,7]dec-1-yl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine isozyme 11beta-HSD1 IC50: 7.7 nM, isozyme 11beta-HSD2 IC50: 0.004 mM 29034 1.1.1.146 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 23930 1.1.1.146 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 23929 1.1.1.146 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 23927 1.1.1.146 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 23925 1.1.1.146 3-adamantyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridine IC50: 1112 nM, 11betaHSD1; IC50: above 10000 nM, 11betaHSD2 23923 1.1.1.146 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 23928 1.1.1.146 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 23926 1.1.1.146 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 23924 1.1.1.146 3-adamantyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole IC50: 10000 nM, 11betaHSD2; IC50: 6820 nM, 11betaHSD1 23922 1.1.1.146 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 23937 1.1.1.146 3-benzoyl-1,1-dioxido-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazin-4-yl trifluoromethanesulfonate - 82872 1.1.1.146 3-benzyl-1-cyclohexylpyrrolidin-2-one - 73923 1.1.1.146 3-biphenyl-3-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26240 1.1.1.146 3-biphenyl-4-yl-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26239 1.1.1.146 3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide - 217232 1.1.1.146 3-chloro-2-methyl-N-(6-methylpyridin-2-yl)benzenesulfonamide - 82848 1.1.1.146 3-chloro-2-methyl-N-(9-oxo-9H-fluoren-3-yl)benzenesulfonamide - 82889 1.1.1.146 3-chloro-2-methyl-N-[4-[2-(3-oxomorpholin-4-yl)ethyl]-1,3-thiazol-2-yl]benzene-1-sulfonamide BVT-3498 255401 1.1.1.146 3-chloro-2-methyl-N-[4-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1,3-thiazol-2-yl]benzenesulfonamide - 73901 1.1.1.146 3-chloro-2-methyl-N-[6-(2-morpholin-4-yl-2-oxoethyl)-pyridin-2-yl]-benzenesulfonamide - 83364 1.1.1.146 3-chloro-2-methyl-N-[6-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]benzenesulfonamide - 82843 1.1.1.146 3-chloro-2-methyl-N-[6-[2-oxo-2-(piperidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide - 82842 1.1.1.146 3-chloro-2-methyl-N-[6-[2-oxo-2-(pyrrolidin-1-yl)ethyl]pyridin-2-yl]benzenesulfonamide - 82846 1.1.1.146 3-chloro-2-methyl-N-[6-[2-oxo-2-(thiomorpholin-4-yl)ethyl]pyridin-2-yl]benzenesulfonamide - 82844 1.1.1.146 3-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid - 73944 1.1.1.146 3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-4-fluorobenzenesulfonamide - 27966 1.1.1.146 3-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide - 27962 1.1.1.146 3-chloro-N-([4-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide - 27996 1.1.1.146 3-chloro-N-([4-(piperidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide - 28000 1.1.1.146 3-chloro-N-([4-(pyrrolidine-1-carbonyl)thiazol-2-yl]methyl)benzenesulfonamide - 27994 1.1.1.146 3-chloro-N-([5-((2R,6S)-2,6-dimethylmorpholine-4-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide - 27995 1.1.1.146 3-chloro-N-([5-(piperidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide - 27999 1.1.1.146 3-chloro-N-([5-(pyrrolidine-1-carbonyl)pyridin-2-yl]methyl)benzenesulfonamide - 27993 1.1.1.146 3-chloro-N-[4-(morpholin-4-ylcarbonyl)benzyl]benzenesulfonamide - 27967 1.1.1.146 3-chloro-N-[4-(piperidin-1-ylcarbonyl)benzyl]benzenesulfonamide - 27969 1.1.1.146 3-chloro-N-[4-(pyrrolidin-1-ylcarbonyl)benzyl]benzenesulfonamide - 27970 1.1.1.146 3-chloro-N-[4-[(4-methylpiperazin-1-yl)carbonyl]benzyl]benzenesulfonamide - 27968 1.1.1.146 3-cyclobutyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255403 1.1.1.146 3-cyclohexyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255404 1.1.1.146 3-cyclopentyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255405 1.1.1.146 3-methoxy-7,8,8-trimethyl-2-(4-methylphenyl)-4,5,6,7-tetrahydro-2H-4,7-methanoindazole - 216416 1.1.1.146 3-methylchrysazin - 27992 1.1.1.146 3-monoglucuronyl-glycyrrhetinic acid - 256549 1.1.1.146 3-tert-butyl-4-cyclopropyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255430 1.1.1.146 3-tricyclo[3.3.1.13,7]dec-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine potent and selective inhibitor of 11beta-HSD1 26215 1.1.1.146 3-[(1R,3R,4R,7S)-4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]tricyclo[3.3.1.13,7]dec-1-yl]propanoic acid - 73911 1.1.1.146 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 - 73929 1.1.1.146 3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-1-yl)butanamide - 216337 1.1.1.146 3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-3-methyl-N-(tricyclo[3.3.1.1~3,7~]decan-2-yl)butanamide - 216338 1.1.1.146 3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cycloheptyl-3-methylbutanamide - 216341 1.1.1.146 3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-cyclohexyl-3-methylbutanamide - 216342 1.1.1.146 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 - 216339 1.1.1.146 3-[(3-chloro-2-methylbenzene-1-sulfonyl)amino]-N-[(2s,5r)-5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl]-3-methylbutanamide - 216340 1.1.1.146 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate IC50 in the presence of NADP+: 0.12 mM, IC50 in the presence of NAD+: 5.6 mM; i.e. CHAPS 5106 1.1.1.146 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate i.e. CHAPS; oxidase IC50: 0.17 mM, reductase IC50: 0.82 mM 5106 1.1.1.146 3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate decreased dehydrogenase activity, no effect on reductase activity; i.e. CHAPS 5106 1.1.1.146 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 - 73927 1.1.1.146 3-[1-(2,4-dichlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14594 1.1.1.146 3-[1-(2-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 10209 1.1.1.146 3-[1-(2-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 10207 1.1.1.146 3-[1-(2-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 10210 1.1.1.146 3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one moderate stability in liver microsomes 42547 1.1.1.146 3-[1-(3-chlorophenyl)-1H-tetrazol-5-yl]-1-phenylpropan-1-one displays good levels of inhibition in liver, subcutaneous adipose tissue and brain following an oral dose 42547 1.1.1.146 3-[1-(3-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14586 1.1.1.146 3-[1-(3-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14588 1.1.1.146 3-[1-(3-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14584 1.1.1.146 3-[1-(4-chlorophenyl)-3,3-difluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 14597 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole - 26233 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-(4-phenoxyphenyl)-4H-1,2,4-triazole - 26244 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-phenyl-4H-1,2,4-triazole - 26217 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole - 26222 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26231 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[3-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole - 26223 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1,3-thiazol-2-yl)phenyl]-4H-1,2,4-triazole - 26247 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(1H-pyrrol-1-yl)phenyl]-4H-1,2,4-triazole - 26246 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethoxy)phenyl]-4H-1,2,4-triazole - 26221 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-5-[4-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26230 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine potent inhibitor of 11beta-HSD1 4735 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 4735 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole - 26235 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-fluorophenyl)-4-methyl-4H-1,2,4-triazole - 26228 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(2-methoxyphenyl)-4-methyl-4H-1,2,4-triazole - 26234 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluoro-4-methoxyphenyl)-4-methyl-4H-1,2,4-triazole - 26237 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(3-fluorophenyl)-4-methyl-4H-1,2,4-triazole - 26229 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(4'-fluorobiphenyl-4-yl)-4-methyl-4H-1,2,4-triazole - 26241 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-fluorophenyl)-4-methyl-4H-1,2,4-triazole - 26227 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-(4-iodophenyl)-4-methyl-4H-1,2,4-triazole - 26232 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-[2-chloro-4-[2-(trifluoromethyl)-1H-imidazol-1-yl]phenyl]-4-methyl-4H-1,2,4-triazole - 26255 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(1H-imidazol-1-yl)phenyl]-4-methyl-4H-1,2,4-triazole - 26245 1.1.1.146 3-[1-(4-chlorophenyl)cyclobutyl]-5-[4-(cyclopropyloxy)phenyl]-4-methyl-4H-1,2,4-triazole - 26238 1.1.1.146 3-[1-(4-chlorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14578 1.1.1.146 3-[1-(4-chlorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14582 1.1.1.146 3-[1-(4-chlorophenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14593 1.1.1.146 3-[1-(4-fluorophenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14587 1.1.1.146 3-[1-(4-fluorophenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14577 1.1.1.146 3-[1-(4-fluorophenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14581 1.1.1.146 3-[1-(4-methylphenyl)cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14589 1.1.1.146 3-[1-(4-methylphenyl)cyclohexyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14579 1.1.1.146 3-[1-(4-methylphenyl)cyclopentyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14585 1.1.1.146 3-[1-(4-methylphenyl)cyclopropyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 10211 1.1.1.146 3-[1-(5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocin-3-yl)cyclopentyl]phenol - 14583 1.1.1.146 3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzothiazol-2(3H)-one - 89528 1.1.1.146 3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-benzoxazol-2(3H)-one - 89526 1.1.1.146 3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-indol-2-one - 89527 1.1.1.146 3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one - 89531 1.1.1.146 3-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-4-methyl-1,3-dihydro-2H-benzimidazol-2-one - 89529 1.1.1.146 3-[1-[2-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14590 1.1.1.146 3-[1-[4-(trifluoromethyl)phenyl]cyclobutyl]-5,6,7,8,9,10-hexahydro[1,2,4]triazolo[4,3-a]azocine - 14591 1.1.1.146 3-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenol - 174497 1.1.1.146 3-[2,3-bis(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26176 1.1.1.146 3-[2-(3-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 255458 1.1.1.146 3-[2-(4-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 255462 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 255463 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(2-phenylethyl)-4H-1,2,4-triazole - 255464 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(cyclopropylmethyl)-4H-1,2,4-triazole - 255465 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-(propan-2-yl)-4H-1,2,4-triazole - 255466 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-ethyl-4H-1,2,4-triazole - 255467 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-methyl-4H-1,2,4-triazole - 255468 1.1.1.146 3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4-propyl-4H-1,2,4-triazole - 255469 1.1.1.146 3-[2-(5-chloro-3-fluorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 255470 1.1.1.146 3-[2-(5-chlorothiophen-2-yl)propan-2-yl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 255471 1.1.1.146 3-[2-chloro-4-(1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26251 1.1.1.146 3-[2-chloro-4-(2,4-dimethyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26253 1.1.1.146 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 - 26254 1.1.1.146 3-[2-chloro-4-(2-methyl-1H-imidazol-1-yl)phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26252 1.1.1.146 3-[2-chloro-4-[2-(methylsulfanyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26256 1.1.1.146 3-[2-chloro-4-[2-(methylsulfonyl)-1H-imidazol-1-yl]phenyl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26257 1.1.1.146 3-[2-chloro-4-[3-(ethylsulfonyl)propyl]phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26189 1.1.1.146 3-[3-chloro-2'-(ethylsulfanyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26260 1.1.1.146 3-[3-chloro-2'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26261 1.1.1.146 3-[3-chloro-3'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26262 1.1.1.146 3-[3-chloro-3'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26264 1.1.1.146 3-[3-chloro-4'-(ethylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26259 1.1.1.146 3-[3-chloro-4'-(methylsulfonyl)biphenyl-4-yl]-5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazole - 26263 1.1.1.146 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 - 73933 1.1.1.146 3-[4-chloro-2-(trifluoromethyl)phenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26173 1.1.1.146 3-[4-chloro-2-(trifluoromethyl)phenyl]-5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazole - 26174 1.1.1.146 3-[4-[2-(ethylsulfonyl)ethyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26187 1.1.1.146 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 - 73935 1.1.1.146 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 - 73934 1.1.1.146 3-[4-[3-(ethylsulfonyl)propyl]-2-methylphenyl]-4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26188 1.1.1.146 3-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol - 26220 1.1.1.146 3-[cis-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 14595 1.1.1.146 3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole - 14596 1.1.1.146 3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole MK-0916 14596 1.1.1.146 3-[[(2-chlorophenyl)methyl]sulfanyl]-4-methyl-5-(2-methylphenyl)-4H-1,2,4-triazole - 255492 1.1.1.146 3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N,N-dimethyl benzamide - 83303 1.1.1.146 3-[[2-(adamantan-1-yl)-2-oxoethyl]sulfanyl]-N-methylbenzamide - 83302 1.1.1.146 3alpha,5alpha-tetrahydro-dehydrocortisterone - 29018 1.1.1.146 3alpha,5alpha-tetrahydroaldosterone - 24046 1.1.1.146 3alpha,5alpha-tetrahydrocorticosterone - 11659 1.1.1.146 3alpha,5alpha-tetrahydrocortisol - 16611 1.1.1.146 3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid IC50 in the presence of NAD+: 0.000097 mM, IC50 in the presence of NADP+: 0.0003 mM; i.e. glycyrrhetinic acid 4934 1.1.1.146 3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid i.e. glycyrrhetinic acid; more effective for 11-dehydrogenase than for 11-oxoreductase activity 4934 1.1.1.146 3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid competitive inhibition, Ki: 4 nM; i.e. glycyrrhetinic acid 4934 1.1.1.146 3beta-hydroxy-11-oxo-18beta-olean-12-en-30-oic-acid 50% inhibition of dehydrogenase activity at 5 nM, 50% inhibition of oxoreductase activity at 20 nM; i.e. glycyrrhetinic acid 4934 1.1.1.146 4'-chloro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide - 82857 1.1.1.146 4'-cyano-N-(6-cyclopropylpyridin-2-yl)biphenyl-4-sulfonamide - 82861 1.1.1.146 4'-cyano-N-(6-ethylpyridin-2-yl)biphenyl-4-sulfonamide - 82860 1.1.1.146 4'-cyano-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide - 82859 1.1.1.146 4'-cyano-N-[6-(ethylamino)pyridin-2-yl]biphenyl-4-sulfonamide - 82865 1.1.1.146 4'-cyano-N-[6-(methylamino)pyridin-2-yl]biphenyl-4-sulfonamide - 82864 1.1.1.146 4'-cyano-N-[6-(propan-2-yl)pyridin-2-yl]biphenyl-4-sulfonamide - 82862 1.1.1.146 4'-fluoro-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide - 82856 1.1.1.146 4'-hydroxyflavanone - 13938 1.1.1.146 4'-methyl-N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide - 82858 1.1.1.146 4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate - 255528 1.1.1.146 4-((S)-2-acetamido-3-((R)-2-(adamantan-2-ylcarbamoyl)piperidin-1-yl)-3-oxopropyl)phenyl acetate - 255529 1.1.1.146 4-((S)-2-acetamido-3-((R)-2-(azepane-1-carbonyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate - 255530 1.1.1.146 4-((S)-2-acetamido-3-((S)-2-(adamantan-2-ylcarbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate - 255531 1.1.1.146 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 - 26270 1.1.1.146 4-(1-[[(3R)-3-methyl-4-[[4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl]sulfonyl]piperazin-1-yl]methyl]cyclopropyl)benzamide - 82838 1.1.1.146 4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 217069 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N,N-diethylbenzamide - 83290 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-benzylbenzamide - 83292 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-ethylbenzamide - 83287 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-furan-2-ylmethylbenzamide - 83293 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-isopropylbenzamide - 83288 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-methylbenzamide - 83286 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-phenylbenzamide - 83291 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)-N-tert-butylbenzamide - 83289 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)benzamide - 83285 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid - 83320 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxy)benzoic acid methyl ester - 83319 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N,N-dimethylbenzamide - 83317 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-benzylbenzamide - 83318 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxymethyl)-N-methylbenzamide - 83316 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzamide - 83315 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid - 83326 1.1.1.146 4-(2-adamantan-1-yl-2-oxoethoxymethyl)benzoic acid methyl ester - 83325 1.1.1.146 4-(2-[1-[(2-fluorobenzene-1-sulfonyl)amino]cyclopropyl]-2-methylpropanamido)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216499 1.1.1.146 4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216502 1.1.1.146 4-(3-chloro-4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenyl)pyridine - 26249 1.1.1.146 4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide - 73967 1.1.1.146 4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216510 1.1.1.146 4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216511 1.1.1.146 4-(4-butoxy-3-methylbenzyl)-3-hydroxy-5-(4-methylphenyl)-1-(pyridin-3-ylmethyl)-1,5-dihydro-2H-pyrrol-2-one - 73948 1.1.1.146 4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216509 1.1.1.146 4-(4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenyl)pyridine - 174503 1.1.1.146 4-(cyclopentylsulfanyl)-3-[[1-(2,4-dichlorobenzamido)cyclopropyl]methoxy]-N-[(1R,2s,3S,5s,7s)-5-hydroxyadamantan-2-yl]-1,2-oxazole-5-carboxamide - 255561 1.1.1.146 4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216515 1.1.1.146 4-([(3R)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216484 1.1.1.146 4-([(3R)-4-[(4-tert-butylphenyl)sulfonyl]-3-methylpiperazin-1-yl]methyl)-5,8-dihydroquinoline - 82816 1.1.1.146 4-([(3S)-3-[(2-fluorobenzene-1-sulfonyl)amino]-4-hydroxy-2,2-dimethylbutanoyl]amino)tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216485 1.1.1.146 4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216486 1.1.1.146 4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol - 216487 1.1.1.146 4-([1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methyl)morpholine - 82825 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N,N-diethylbenzamide - 27971 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-(tricyclo[3.3.1.13,7]dec-1-yl)benzamide - 27978 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-methylbenzamide - 27975 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptyl-N-propylbenzamide - 27976 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide - 27974 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclohexylbenzamide - 27972 1.1.1.146 4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cyclopentylbenzamide - 27973 1.1.1.146 4-benzyl-3-[2-(5-bromothiophen-2-yl)propan-2-yl]-5-cyclopropyl-4H-1,2,4-triazole - 255585 1.1.1.146 4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216557 1.1.1.146 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid - 27985 1.1.1.146 4-chloro-N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)benzenesulfonamide - 27963 1.1.1.146 4-chloromercuribenzoate complete inhibition of cortisol oxidation at 0.01 mM 388 1.1.1.146 4-cyclopropyl-3-(cyclopropylmethyl)-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255595 1.1.1.146 4-cyclopropyl-3-propyl-5-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255596 1.1.1.146 4-cyclopropyl-3-[2-(thiophen-2-yl)propan-2-yl]-4H-1,2,4-triazole - 255597 1.1.1.146 4-fluoro-N-[4-[(4aR,8aS)-octahydroquinolin-1(2H)-ylcarbonyl]phenyl]benzamide - 73906 1.1.1.146 4-methoxy-N-(6-methylpyridin-2-yl)benzenesulfonamide - 82851 1.1.1.146 4-methyl-3,5-bis[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 174489 1.1.1.146 4-methyl-3-(2-methylnaphthalen-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26214 1.1.1.146 4-methyl-3-(4-pentylbicyclo[2.2.2]oct-1-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 73931 1.1.1.146 4-methyl-3-(4-pentylphenyl)-5-phenyl-4H-1,2,4-triazole - 26194 1.1.1.146 4-methyl-3-(4-pentylphenyl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26191 1.1.1.146 4-methyl-3-(7-methylnaphthalen-2-yl)-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26208 1.1.1.146 4-methyl-3-naphthalen-2-yl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26206 1.1.1.146 4-methyl-3-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-4H-1,2,4-triazole - 27982 1.1.1.146 4-methyl-3-phenyl-5-tricyclo[3.3.1.13,7]dec-1-yl-4H-1,2,4-triazole - 26216 1.1.1.146 4-methyl-3-phenyl-5-[(3R,5R)-tricyclo[3.3.1.13,7]dec-1-yl]-4H-1,2,4-triazole - 73928 1.1.1.146 4-methyl-3-phenyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole - 26181 1.1.1.146 4-methyl-3-[2-(trifluoromethoxy)phenyl]-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazole potent and selective inhibitor of 11beta-HSD1 26166 1.1.1.146 4-n-nonylphenol - 33319 1.1.1.146 4-n-octylphenol - 22259 1.1.1.146 4-nonylphenol inhibition of liver isozyme 11beta-HSD1 and kidney isozyme 11beta-HSD2, 11beta-HSD1 IC50: 49.3 mM, isozyme 11beta-HSD2 IC50: 0.0203 mM 7529 1.1.1.146 4-nonylphenol - 7529 1.1.1.146 4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216576 1.1.1.146 4-pregnen-11,17-diol-3,20-dione IC50: 0.1 mM 21491 1.1.1.146 4-pregnen-11alpha-ol-3,20-dione IC50: 0.0095 mM 21492 1.1.1.146 4-pregnen-11beta-ol-3,20-dione IC50: 0.011 mM 21493 1.1.1.146 4-pregnen-16alpha-ol-3,20-dione IC50: 0.9 mM 32095 1.1.1.146 4-pregnen-17,21-diol-3,20-dione IC50: 0.07 mM 32096 1.1.1.146 4-pregnen-17alpha,20alpha-diol-3-one IC50: 0.115 mM 32097 1.1.1.146 4-pregnen-17alpha-ol-3,20-dione IC50: 0.19 mM 21494 1.1.1.146 4-pregnen-20alpha-ol-3-one IC50: 0.022 mM 13137 1.1.1.146 4-pregnen-20beta-ol-3-one IC50: 0.031 mM 21495 1.1.1.146 4-pregnen-21-ol-3,20-dione IC50: 0.031 mM 16624 1.1.1.146 4-pregnen-3,11,20-trione IC50: 0.19 mM 21496 1.1.1.146 4-pregnen-3,20-dione IC50: 0.015 mM 5917 1.1.1.146 4-propyl-N-[2-(thiophen-2-yl)ethyl]benzenesulfonamide - 82888 1.1.1.146 4-tert-butyl-N-(6-methylpyridin-2-yl)benzenesulfonamide - 82852 1.1.1.146 4-tert-octylphenol - 71236 1.1.1.146 4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol - 216517 1.1.1.146 4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol - 216518 1.1.1.146 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoic acid - 82877 1.1.1.146 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzonitrile - 27980 1.1.1.146 4-[(E)-[(2Z)-2-[(2-chlorophenyl)imino]-4-oxo-1,3-thiazolidin-5-ylidene]methyl]-2-methoxyphenyl benzoate - 89521 1.1.1.146 4-[(N-[4-[(dimethylamino)methoxy]benzene-1-sulfonyl]-2-methylalanyl)amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216521 1.1.1.146 4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216516 1.1.1.146 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 - 73912 1.1.1.146 4-[1-[5-(4-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]cyclobutyl]phenol - 174496 1.1.1.146 4-[2-(1-[[(2-fluorobenzene-1-sulfonyl)amino]methyl]cyclopropyl)-2-methylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216539 1.1.1.146 4-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]pyridine - 255639 1.1.1.146 4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide - 73965 1.1.1.146 4-[3-(4-methoxyphenoxy)-3-methyl-2-oxobutyl]adamantane-1-carboxamide - 255648 1.1.1.146 4-[3-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylpropanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216542 1.1.1.146 4-[4-(1-methyl-1H-benzimidazol-2-yl)piperazine-1-sulfonyl]benzoic acid 90% residual activity at 0.02 mM 216543 1.1.1.146 4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216549 1.1.1.146 4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol - 216550 1.1.1.146 4-[4-([(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl]sulfonyl)phenyl]morpholine - 26537 1.1.1.146 4-[4-methyl-5-(1-methyl-1H-indol-4-yl)-4H-1,2,4-triazol-3-yl]phenol - 26198 1.1.1.146 4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2,3,3-tetramethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216552 1.1.1.146 4-[4-[(2-fluorobenzene-1-sulfonyl)amino]-2,2-dimethylbutanamido]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216551 1.1.1.146 4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile high metabolic lability 29025 1.1.1.146 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]-1-methyl-1H-indole - 26199 1.1.1.146 4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]-2-fluorophenol - 26236 1.1.1.146 4-[5-[1-(4-chlorophenyl)cyclobutyl]-4-methyl-4H-1,2,4-triazol-3-yl]phenol - 26218 1.1.1.146 4-[[2-(4-chlorophenoxy)-2-methylpropanoyl]amino]bicyclo[2.2.2]octane-1-carboxamide - 73909 1.1.1.146 4-[[2-methyl-N-(2,4,5-trifluorobenzene-1-sulfonyl)alanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216523 1.1.1.146 4-[[N-(2,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216527 1.1.1.146 4-[[N-(2,6-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216528 1.1.1.146 4-[[N-(2-chloro-4-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216524 1.1.1.146 4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216525 1.1.1.146 4-[[N-(2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxylic acid - 216526 1.1.1.146 4-[[N-(3,5-dichlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216531 1.1.1.146 4-[[N-(3,5-difluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216532 1.1.1.146 4-[[N-(3-chloro-2-fluorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216529 1.1.1.146 4-[[N-(3-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216530 1.1.1.146 4-[[N-(4-chlorobenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216533 1.1.1.146 4-[[N-(4-hydroxybenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216534 1.1.1.146 4-[[N-(4-tert-butylbenzene-1-sulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216535 1.1.1.146 4-[[N-(benzenesulfonyl)-2-methylalanyl]amino]tricyclo[3.3.1.1~3,7~]decane-1-carboxamide - 216536 1.1.1.146 5,5-diethyl-2-(3-noradamantylamino)-1,3-thiazol-4-(5H)-one inhibitor for isozyme 11beta-HSD1, but not for isozyme 11beta-HSD2 74621 1.1.1.146 5,5-diethyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1,3-thiazol-4(5H)-one - 73938 1.1.1.146 5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole - 216584 1.1.1.146 5-(3-chloro-2-methylphenoxy)-3-(4-hydroxybicyclo[2.2.2]oct-1-yl)-[1,2,4]triazolo[4,3-a]pyridine potent and metabolically stable inhibitor with about 200fold selectivity for isoform 11beta-HSD-1 versus isoform 11beta-HSD-2 29044 1.1.1.146 5-(adamantan-1-ylcarbonyl)-4H,5H,6H,7H-thieno[3,2-c]pyridine - 74635 1.1.1.146 5-adamantyl-3-benzyl-4-methyl-4H-1,2,4-triazole IC50: 14 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 23943 1.1.1.146 5-adamantyl-3-butyl-4-methyl-4H-1,2,4-triazole IC50: 91 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 23939 1.1.1.146 5-adamantyl-3-ethyl-4-propyl-4H-1,2,4-triazole IC50: 23 nM, 11betaHSD1; IC50: 50 nM, 11betaHSD2 23941 1.1.1.146 5-adamantyl-3-methyl-4-butyl-4H-1,2,4-triazole IC50: 270 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 23942 1.1.1.146 5-adamantyl-3-phenyl-4-methyl-4H-1,2,4-triazole IC50: 109 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 23944 1.1.1.146 5-adamantyl-3-propyl-4-ethyl-4H-1,2,4-triazole IC50: 50 nM, 11betaHSD1; IC50: above 4000 nM, 11betaHSD2 23940 1.1.1.146 5-fluoro-1-[1-[(4-methoxy-3-methylphenyl)carbonyl]piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one - 89530 1.1.1.146 5-hydroxy-4-oxopentyl acetate - 10317 1.1.1.146 5-methyl-4-[(1E)-3-[(3-methylphenoxy)acetyl]triaz-1-en-1-yl]benzene-1,3-diol - 73946 1.1.1.146 5-methyl-5-(1-methylethyl)-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1,3-thiazol-4(5H)-one - 73939 1.1.1.146 5-pregnen-3beta,11beta-diol-20-one IC50: 0.0095 mM 21506 1.1.1.146 5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole - 216590 1.1.1.146 5-[2-(4,5-dicyclopropyl-4H-1,2,4-triazol-3-yl)propan-2-yl]thiophene-2-carbonitrile - 255725 1.1.1.146 5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole - 216592 1.1.1.146 5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole - 216591 1.1.1.146 5-[[(E)-[(5-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255729 1.1.1.146 5-[[(E)-[(5-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255730 1.1.1.146 5-[[(E)-[(5-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255731 1.1.1.146 5-[[(E)-[(6-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255732 1.1.1.146 5-[[(E)-[(6-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255733 1.1.1.146 5-[[(E)-[(6-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255734 1.1.1.146 5-[[(E)-[(7-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255735 1.1.1.146 5-[[(E)-[(7-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255736 1.1.1.146 5-[[(E)-[(7-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid - 255737 1.1.1.146 5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole - 216589 1.1.1.146 5alpha-dihydrocorticosterone - 9902 1.1.1.146 5alpha-pregnan-11alpha-ol-3,20-dione IC50: 0.0027 mM 21509 1.1.1.146 5alpha-pregnan-11beta,17alpha,21-triol-3,20-dione IC50: 0.04 mM 21510 1.1.1.146 5alpha-pregnan-11beta,21-diol-3,20-dione IC50: 0.0075 mM 21511 1.1.1.146 5alpha-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.18 mM 21512 1.1.1.146 5alpha-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.008 mM 21513 1.1.1.146 5alpha-pregnan-3alpha,11beta-diol-20-one IC50: 0.016 mM 21514 1.1.1.146 5alpha-pregnan-3alpha,17alpha,21-triol-11,20-dione IC50: 0.24 mM 21515 1.1.1.146 5alpha-pregnan-3alpha,21-diol-11,20-dione IC50: 0.029 mM 21517 1.1.1.146 5alpha-Pregnan-3alpha,21-diol-20-one IC50: 0.031 mM 8028 1.1.1.146 5alpha-pregnan-3alpha-ol-20-one IC50: 0.014 mM 5704 1.1.1.146 5beta-pregnan-3alpha,11alpha-diol-20-one IC50: 0.08 mM 32112 1.1.1.146 5beta-pregnan-3alpha,11beta,17alpha,21-tetrol-20-one IC50: 0.12 mM 32113 1.1.1.146 5beta-pregnan-3alpha,11beta,21-triol-20-one IC50: 0.14 mM 32114 1.1.1.146 5beta-pregnan-3alpha,11beta-diol-20-one IC50: 0.0 mM 48739 1.1.1.146 5beta-Pregnan-3alpha,21-diol-20-one IC50: 0.003 mM 10548 1.1.1.146 5beta-Pregnan-3alpha-ol-20-one IC50: 0.012 mM 3187 1.1.1.146 6-(4-benzylpiperazin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216688 1.1.1.146 6-(4-hydroxy-4-methylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216692 1.1.1.146 6-(4-hydroxy-4-phenylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216693 1.1.1.146 6-(4-hydroxy-4-propylpiperidin-1-yl)-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216694 1.1.1.146 6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol - 216613 1.1.1.146 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 255763 1.1.1.146 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 255765 1.1.1.146 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 255766 1.1.1.146 6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one - 73973 1.1.1.146 6-hydroxyflavanone - 136192 1.1.1.146 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 - 73924 1.1.1.146 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 - 73926 1.1.1.146 6-[(3-chlorophenylsulfonamido)methyl]-N,N-diethylnicotinamide - 27997 1.1.1.146 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-methylnicotinamide - 28003 1.1.1.146 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptyl-N-propylnicotinamide - 28005 1.1.1.146 6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide - 28001 1.1.1.146 6-[4-(2-amino-2-oxoethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216709 1.1.1.146 6-[4-(3-amino-3-oxopropyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216710 1.1.1.146 6-[4-(4-cyanophenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216711 1.1.1.146 6-[4-(4-hydroxyphenyl)piperazin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216712 1.1.1.146 6-[4-(hydroxymethyl)piperidin-1-yl]-N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)pyridine-2-carboxamide - 216715 1.1.1.146 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 255804 1.1.1.146 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 255805 1.1.1.146 7-chloro-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-ol - 26210 1.1.1.146 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 255814 1.1.1.146 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 255815 1.1.1.146 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 - 82879 1.1.1.146 7-hydroxy-6-(3-methylbut-2-en-1-yl)-3-oxo-2,3-dihydro-1H-isoindol-5-yl 2,4-dihydroxy-6-methylbenzoate - 82880 1.1.1.146 7-keto,25-hydroxycholesterol inhibits the oxoreduction of cortisone to cortisol by the recombinant isoform 11beta-HSD1 256562 1.1.1.146 7-keto,25-hydroxycholesterol - 256562 1.1.1.146 7-keto,27-hydroxycholesterol potent inhibitor of the isoform 11beta-HSD1-dependent oxoreduction of cortisone 256561 1.1.1.146 7-oxo-5alpha-androstane-3beta,17beta-diol mixed type inhibition of cortisone reduction 25819 1.1.1.146 7-oxo-cholesterol - 63161 1.1.1.146 7-oxo-dehydroepiandrosterone mixed type inhibition of cortisone reduction 38141 1.1.1.146 7-oxo-epiandrosterone competitive type inhibition of cortisone reduction 146699 1.1.1.146 7alpha,25-Dihydroxycholesterol - 30623 1.1.1.146 7alpha-hydroxy-dehydroepiandrosterone competitive type inhibition of cortisol oxidation 25608 1.1.1.146 7alpha-hydroxy-epiandrosterone competitive type inhibition of cortisol oxidation 146700 1.1.1.146 7beta,25-dihydroxycholesterol - 256563 1.1.1.146 7beta,27-dihydroxycholesterol potent inhibitor of the isoform 11beta-HSD2-dependent oxidation of cortisol 256560 1.1.1.146 7beta-hydroxy-dehydroepiandrosterone competitive type inhibition of cortisol oxidation 146698 1.1.1.146 7beta-hydroxy-epiandrosterone mixed type inhibition of cortisol oxidation 146701 1.1.1.146 7beta-hydroxycholesterol - 5724 1.1.1.146 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one shows excellent stability against cytochrome P450 metabolism 29009 1.1.1.146 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-(4-chlorophenyl)-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one compound is orally active and shows the same tendency as pioglitazone in diet-induced obesity mice 29009 1.1.1.146 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one methyl substitution at the 8-position achieves an approximately 15fold improvement in potency over the non-substituted compound 29008 1.1.1.146 8,8-dimethyl-5-(1-hydroxytricyclo[3.3.1.13,7]dec-3-yl)-1-phenyl-5,6,7,8-tetrahydropyrazolo[4,3-c]azepin-4(1H)-one compound is orally active and shows the same tendency as pioglitazone in diet-induced obesity mice 29008 1.1.1.146 8-benzyl-2-([(1S)-1-[2-(trifluoromethyl)phenyl]ethyl]amino)-1-thia-3,8-diazaspiro[4.5]dec-2-en-4-one - 73940 1.1.1.146 8-[[(2-cyanopyridin-3-yl)methyl]sulfanyl]-6-hydroxy-3,4-dihydro-1H-pyrano[3,4-c]pyridine-5-carbonitrile - 29047 1.1.1.146 9alpha-Fluorocortisol a competitive inhibitor of the oxidation of cortisol 20090 1.1.1.146 9alpha-Fluorocortisol competitive inhibition, Ki: 0.005 mM 20090 1.1.1.146 A1-tunicamycin 50% inhibition at 50 ng/ml, reductase activity not affected 105341 1.1.1.146 abietic acid weak inhibition 3524 1.1.1.146 abietic acid - 3524 1.1.1.146 ABT-384 - 217263 1.1.1.146 adamantyl triazoles eight derivatives of different ring size, IC50 of 1.4-2180 nM for isozyme 11beta-HSD1, and of 8.7-2000 nM for isozyme 11beta-HSD2, the IC50 value decreases with increasing ring size, overview 29032 1.1.1.146 aloe emodin - 28097 1.1.1.146 Aloe-emodin - 11587 1.1.1.146 alpha-glycyrrhetinic acid oxidase, IC50: 14 nmol, reductase, IC50: 42 nmol 48805 1.1.1.146 AMG-221 - 217237 1.1.1.146 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% 146696 1.1.1.146 arylsulfoamidothiazole - 14000 1.1.1.146 arylsulfoamidothiazoles weak or not binding inhibitors, inhibition mode and profiles 24048 1.1.1.146 arylsulfoamidothiazoles specific, tight-binding inhibitors, inhibition mode and profiles 24048 1.1.1.146 arylsulfoamidothiazoles intermediate binding inhibitors, inhibition mode and profiles 24048 1.1.1.146 arylsulfoamidothiazoles weak or not binding binding inhibitors, inhibition mode and profiles 24048 1.1.1.146 arylsulfonamidothiazole derivatives specific for isozyme 11beta-HSD1 132148 1.1.1.146 AZD-4017 selective inhibitor for isoform 11beta-HSD1 256558 1.1.1.146 AZD-4071 - 217238 1.1.1.146 AZD-8329 - 217265 1.1.1.146 azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone - 89512 1.1.1.146 BDE-100 inhibitor of isoform HSD11B2 217256 1.1.1.146 BDE-153 inhibitor of isoform HSD11B2 217257 1.1.1.146 BDE-3 inhibitor of isoform HSD11B2 217258 1.1.1.146 BDE-47 inhibitor of isoform HSD11B2 217259 1.1.1.146 benzenesulfonamide - 22586 1.1.1.146 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 132145 1.1.1.146 beta-glycyrrhetinic acid oxidase, IC50: 2.9 nmol, reductase, IC50: 13 nmol 48866 1.1.1.146 betulin inhibition at 0.1 mM: oxidase 36%, reductase 34.5% 9522 1.1.1.146 bezafibrate 23% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 6085 1.1.1.146 BI-135585 - 256572 1.1.1.146 bisphenol A - 3723 1.1.1.146 bisphenol A weak inhibition of isoform 11beta-HSD2, 51.16% inhibition at 0.1 mM 3723 1.1.1.146 bisphenol A weak inhibition of isoform 11beta-HSD2, 41.61% inhibition at 0.1 mM 3723 1.1.1.146 BMS-770767 - 217264 1.1.1.146 BMS30 - 217235 1.1.1.146 bortezomib - 4725 1.1.1.146 butylated hydroxyanisole highly selective inhibitor of isoform 11beta-HSD2 11193 1.1.1.146 BVT-14225 isozyme 11beta-HSD1 IC50: 52 nM, 1000fold less potent against isozyme 11beta-HSD2 17999 1.1.1.146 BVT-14225 - 17999 1.1.1.146 BVT-2733 - 60354 1.1.1.146 BVT-2733 mixed-type inhibition pattern 60354 1.1.1.146 BVT-3498 - 256570 1.1.1.146 BVT-4584 - 132134 1.1.1.146 BVT-528 competitive, tight-binding inhibition pattern 132144 1.1.1.146 BVT.2733 - 217262 1.1.1.146 carbenoxolone 0.01 mM, more than 90% inhibition of 7-oxocholesterol reduction in liver homogenates 1844 1.1.1.146 carbenoxolone - 1844 1.1.1.146 carbenoxolone unspecific inhibitor 1844 1.1.1.146 carbenoxolone specific for 11beta-hydroxysteroid dehydrogenase type 1 1844 1.1.1.146 carbenoxolone potent and selective 11beta-HSD1 inhibitor 1844 1.1.1.146 carbenoxolone 89.7% inhibition of isoform 11beta-HSD1 at 0.01 mM 1844 1.1.1.146 chenodeoxycholic acid - 1277 1.1.1.146 cholesterol oxidase: 18.6% inhibition at 0.1 mM, reductase: 7.4% inhibition at 0.1 mM 189 1.1.1.146 clobenzorex - 256565 1.1.1.146 Clofibrate 18% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 1278 1.1.1.146 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 132146 1.1.1.146 curcumin inhibitory against isoform 11beta-HSD1 in intact cells with IC50 value of 2.29 microM 696 1.1.1.146 curcumin inhibitory against isoform 11beta-HSD1 in intact cells with IC50 value of 5.79 microM, competitive. Treatment with curcumin reduces serum glucose, cholesterol, triglyceride, low density lipoprotein levels in high-fat-diet-induced obese rats 696 1.1.1.146 curcumin - 696 1.1.1.146 Cyclobutanone - 8076 1.1.1.146 danazol competitive inhibition 56844 1.1.1.146 dexamethasone dexmethasone inhibits 11beta-HSD1 activity and expression in a time- and concentration-dependent manner, the effect of dexamethasone is mimicked by both cortisol and corticosterone but blocked by the glucocorticoid receptor antagonist RU486 1159 1.1.1.146 di-n-butyl phthalate - 26534 1.1.1.146 dibenzoylmethane - 217249 1.1.1.146 dibutyltin - 217252 1.1.1.146 dicyclohexyl benzene-1,2-dicarboxylate - 217253 1.1.1.146 diethyldithiocarbamate uncompetitive inhibition of isoform 11beta-HSD2 373 1.1.1.146 diethylhexyl adipate inhibition of liver isozyme 11beta-HSD1, IC50: 49.4 mM 60353 1.1.1.146 diethylhexyl adipate - 60353 1.1.1.146 dihydrotestosterone - 2055 1.1.1.146 diphenyltin - 217251 1.1.1.146 dipropyl phthalate - 23842 1.1.1.146 Disulfiram - 986 1.1.1.146 Disulfiram potent inhibitor of isoform 11beta-HSD2 986 1.1.1.146 emodin - 3072 1.1.1.146 endosulfan - 69461 1.1.1.146 enoxolone - 74601 1.1.1.146 epigallocatechin gallate - 1234 1.1.1.146 epigallocatechine-3-gallate - 217248 1.1.1.146 estradiol 50% inhibition, DTT protects at 10 mM, estradiol has a regulatory function on the isozymes in the liver 897 1.1.1.146 ethanone - 132137 1.1.1.146 ethyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate - 26277 1.1.1.146 ethyl 4-hydroxy-2-(2-oxo-2-phenylethyl)-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide - 82873 1.1.1.146 ethyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxide - 82869 1.1.1.146 ethyl 5-[[(2,5-dimethylphenyl)sulfonyl]amino]-2-propyl-1-benzofuran-3-carboxylate - 26268 1.1.1.146 euphane-3beta,20-dihydroxy-24-ene - 217243 1.1.1.146 fenofibrate 82% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 6805 1.1.1.146 fenofibric acid 25% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 49052 1.1.1.146 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 83362 1.1.1.146 fenofibric acid ethylester 85% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 83359 1.1.1.146 fenofibric acid isobutylester 75% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 83361 1.1.1.146 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 83363 1.1.1.146 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 83360 1.1.1.146 flavanone - 3468 1.1.1.146 flavone - 1617 1.1.1.146 fluoxymesterone potent inhibitor of isoform 11beta-HSD2 256552 1.1.1.146 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 146697 1.1.1.146 Fusidic acid - 4245 1.1.1.146 G-strophanthidin inhibition at 0.1 mM: oxidase 4.8%, reductase 6.1% 106109 1.1.1.146 gemfibrozil 19% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 6087 1.1.1.146 glycyrrhetinic acid - 1975 1.1.1.146 glycyrrhetinic acid isozyme 11beta-HSD1 inhibitor, residue Tyr177 is important in binding, molecular modeling 1975 1.1.1.146 glycyrrhetinic acid inhibits both 11beta-hydroxysteroid dehydrogenase and carbonyl reductase activities of the enzyme potently 1975 1.1.1.146 glycyrrhetinic acid 11beta-HSD1 shows 21% residual activity at 0.01 mM, 11beta-HSD2 shows 16% residual activity at 0.01 mM 1975 1.1.1.146 glycyrrhetinic acid inhibitor of isoform 11beta-HSD2 1975 1.1.1.146 glycyrrhizic acid oxidase, IC50: 0.0039 mM, reductase, IC50: 0.013 mM 5309 1.1.1.146 glycyrrhizic acid dose-dependent competitive inhibition, IC50: 1.994 mM 5309 1.1.1.146 glycyrrhizic acid competitive inhibition, Ki: 0.0005 mM 5309 1.1.1.146 glycyrrhizic acid - 5309 1.1.1.146 glycyrrhizin - 4646 1.1.1.146 glycyrrhizinic acid - 7205 1.1.1.146 glycyrrhizininc acid - 15365 1.1.1.146 gossypol - 1825 1.1.1.146 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 32240 1.1.1.146 helvolic acid inhibition at 0.1 mM: oxidase 13%, reductase 18.5% 106248 1.1.1.146 HSD-016 - 256573 1.1.1.146 hydroxyitraconazole - 256568 1.1.1.146 INCB-13739 selective inhibitor for isoform 11beta-HSD1 256557 1.1.1.146 indinavir - 1036 1.1.1.146 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 546 1.1.1.146 interleukin-1beta or tissue necrosis factor-alpha simultaneously increase 11beta-HSD1 expression and down-regulate 11beta-HSD2 - 29022 1.1.1.146 itraconazole - 2302 1.1.1.146 itraconazole 95% residual activity at 0.03 mM 2302 1.1.1.146 kansenone - 217245 1.1.1.146 kansuinone - 217244 1.1.1.146 lanosterol oxidase IC50: 0.00065 mM, reductase IC50: 0.0017 mM 1188 1.1.1.146 lupeol inhibition at 0.1 mM: oxidase 52%, reductase 38.4% 3130 1.1.1.146 maneb - 85388 1.1.1.146 Merck-544 - 217231 1.1.1.146 methoxychlor competitive. Not inhibitory to isoform 11beta-HSD2 32286 1.1.1.146 methoxychlor - 32286 1.1.1.146 methyl (3beta,5xi,9xi,18xi)-3-hydroxy-11-oxoolean-12-en-30-oate - 26276 1.1.1.146 methyl 2-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate - 26196 1.1.1.146 methyl 2-[5-(7-chloro-1-methoxynaphthalen-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate - 26213 1.1.1.146 methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate - 217088 1.1.1.146 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 - 73932 1.1.1.146 methyl 4-[(3-benzoyl-4-hydroxy-1,1-dioxido-2H-1,2-benzothiazin-2-yl)acetyl]benzoate - 82876 1.1.1.146 methyl 4-[5-(2-chlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]benzenesulfinate - 26197 1.1.1.146 methyl jasmonate - 2525 1.1.1.146 methyl {(1S,2S)-3-oxo-2-[(2Z)-pent-2-en-1-yl]cyclopentyl}acetate weak inhibition 47979 1.1.1.146 MK-0916 - 256571 1.1.1.146 Momordica charantia extract - 256569 1.1.1.146 mono(2-ethylhexyl)phthalate - 167144 1.1.1.146 additional information aldosterone, no effect 2 1.1.1.146 additional information all inhibitory compounds tested show competitive inhibition, more effective inhibition of oxidative than reductive activity, inhibition is enhanced by C11-oxygen function and a C7-OH function, inhibition is influenced by steric conformation of inhibitor 2 1.1.1.146 additional information no end-product inhibition 2 1.1.1.146 additional information no inhibition of cortisol oxidation by 0,1 mM o-iodosobenzoate and 2alpha-methylcortisol 2 1.1.1.146 additional information isozyme 11beta-HSD1 expression is about 30% reduced in castrated male rats, while expression of isozyme 11beta-HSD2 is increased, overview 2 1.1.1.146 additional information no inhibition by caffeic acid, chlorogenic acid or trigonelline 2 1.1.1.146 additional information oxidation of the enzymes disulfides with K3Fe(CN)6 reduces the activity 2 1.1.1.146 additional information no inhibition by DETC, flavone, and bisphenol A, molecular docking and modeling of enzyme-inhibitor interactions the model can discriminate between known isozyme 11beta-HSD1 inhibitors or substrates and non-inhibitors, inhibitroy binding mode, overview 2 1.1.1.146 additional information steroid hormones, adrenocorticosteroid derivatives, progesteron and androgen steroid hormones, with 5alpha-ring A reduced-configuration selectively inhibit isozyme 11beta-HSD2, while 5beta-derivatives are inactive 2 1.1.1.146 additional information structure-activity analysis for inhibitor design 2 1.1.1.146 additional information leaf extracts of Eriobotrya japonica preferentially inhibit 11beta-HSD1 over 11beta-HSD2, extracts of roasted but not native coffee beans preferentially inhibit 11beta-HSD1 over 11beta-HSD2 2 1.1.1.146 additional information 11beta-HSD1 mRNA decreases 4fold on day 3 after injection of trehalose-6,6'-dimycolate 2 1.1.1.146 additional information isoform HSD11B1 is not inhibited by 4-bromobiphenyl, BDE-3, BDE-47, BDE-100, and BDE-153 2 1.1.1.146 additional information tea extracts inhibit isoform 11beta-HSD1 mediated cortisone reduction, where green tea exhibits the highest inhibitory potency with an IC50 value of 3.749 mg dried tea leaves per ml 2 1.1.1.146 additional information not inhibited by 2-(allylamino)thiazol-4(5H)-one, 2-(allylamino)-5-methylthiazol-4(5H)-one, 2-(allylamino)-5-ethylthiazol-4(5H)-one, 2-(allylamino)-5-propylthiazol-4(5H)-one, 2-(allylamino)-5-isopropylthiazol-4(5H)-one, 2-(allylamino)-5,5-dimethylthiazol-4(5H)-one, and 2-(allylamino)-5-phenylthiazol-4(5H)-one 2 1.1.1.146 additional information not inhibited by (R)-1-(l-prolyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide trifluoroacetate, (R)-1-(l-histidyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide bis trifluoroacetate, (R)-1-(l-tyrosyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide trifluoroacetate, (R)-1-(l-lysyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide bis trifluoroacetate, (R)-1-(acetylglycyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, (R)-1-(acetyl-l-prolyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, (R)-1-(acetyl-l-tyrosyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, and (R)-1-(acetyl-l-prolyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide 2 1.1.1.146 additional information not inhibited by perfluorobutane sulfonic acid 2 1.1.1.146 additional information 7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD1 activity at concentrations up to 0.01 mM; 7alpha,27-dihydroxycholesterol does not inhibit the enzyme isoform 11beta-HSD2 activity at concentrations up to 0.01 mM 2 1.1.1.146 additional information not inhibited by 7alpha,25-dihydroxycholesterol 2 1.1.1.146 additional information isoform 11beta-HSD2 is not inhibited by 7alpha,25-dihydroxycholesterol 2 1.1.1.146 morpholino antisense oligonucleotide about 50% inhibition at 0.002 mM; about 50% inhibition at 0.002 mM 217260 1.1.1.146 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 - 73945 1.1.1.146 N'-[(1Z)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide - 73943 1.1.1.146 N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2,3-dihydro-1,4-benzodioxine-2-carbohydrazide - 27984 1.1.1.146 N'-[(E)-(2,4-dihydroxy-6-methylphenyl)methylidene]-2-(3-methylphenoxy)acetohydrazide - 82886 1.1.1.146 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 - 82887 1.1.1.146 N,N-bis(3-D-gluconamidopropyl)cholamide i.e. BIGCHAP; oxidase IC50: 0.0026 mM, reductase IC50: 0.0058 mM 32297 1.1.1.146 N,N-bis(3-D-gluconamidopropyl)deoxycholamide i.e. deoxy-BIGCHAP; oxidase IC50: 0.055 mM, reductase IC50: 0.58 mM 32298 1.1.1.146 N-(3-chloro-4-hydroxynaphthalen-1-yl)-2,4-dimethylbenzenesulfonamide - 26269 1.1.1.146 N-(4-biphenyl-4-yl-1,3-oxazol-2-yl)benzenesulfonamide - 73902 1.1.1.146 N-(4-chloro-2-methyl-1,3-benzothiazol-5-yl)adamantane-1-carboxamide - 74627 1.1.1.146 N-(4-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]carbonyl]benzyl)-3-(trifluoromethyl)benzenesulfonamide - 27965 1.1.1.146 N-(5-cyanotricyclo[3.3.1.1~3,7~]decan-2-yl)-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide - 216942 1.1.1.146 N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(4-phenylpiperazin-1-yl)pyridine-2-carboxamide - 217093 1.1.1.146 N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-(piperidin-1-yl)pyridine-2-carboxamide - 216943 1.1.1.146 N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-(pyridin-2-yl)piperazin-1-yl]pyridine-2-carboxamide - 216944 1.1.1.146 N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-hydroxy-4-(trifluoromethyl)piperidin-1-yl]pyridine-2-carboxamide - 216946 1.1.1.146 N-(5-hydroxytricyclo[3.3.1.1~3,7~]decan-2-yl)-6-[4-[(pyridin-3-yl)methyl]piperazin-1-yl]pyridine-2-carboxamide - 216945 1.1.1.146 N-(6-aminopyridin-2-yl)-4'-cyanobiphenyl-4-sulfonamide - 82863 1.1.1.146 N-(6-methylpyridin-2-yl)-2-(trifluoromethyl)benzenesulfonamide - 82850 1.1.1.146 N-(6-methylpyridin-2-yl)-4-(trifluoromethyl)benzenesulfonamide - 82849 1.1.1.146 N-(6-methylpyridin-2-yl)biphenyl-4-sulfonamide - 82855 1.1.1.146 N-(6-methylpyridin-2-yl)naphthalene-1-sulfonamide - 82854 1.1.1.146 N-(6-methylpyridin-2-yl)naphthalene-2-sulfonamide - 82853 1.1.1.146 N-(furan-2-ylmethyl)-N-methyladamantane-1-carboxamide - 74636 1.1.1.146 N-(thiophen-2-ylmethyl)adamantane-1-carboxamide - 74629 1.1.1.146 N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide - 216949 1.1.1.146 N-acetyl-beta-alanyl-N-adamantan-1-yl-D-prolinamide - 256141 1.1.1.146 n-alkyl-substituted adamantyl triazoles substituted with methyl to butyl groups, IC50: of 3-72 nM for isozyme 11beta-HSD1, and of about 0.004 mM for isozyme 11beta-HSD2, overview 29043 1.1.1.146 N-butyl-2-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylthiazole-4-carboxamide - 28008 1.1.1.146 N-butyl-4-([[(3-chlorophenyl)sulfonyl]amino]methyl)-N-cycloheptylbenzamide - 27977 1.1.1.146 N-butyl-6-[(3-chlorophenylsulfonamido)methyl]-N-cycloheptylnicotinamide - 28007 1.1.1.146 N-cyclohexyl-6-(piperidin-1-yl)picolinamide - 217234 1.1.1.146 N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide - 89533 1.1.1.146 N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide - 89532 1.1.1.146 N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide - 73963 1.1.1.146 N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide - 73962 1.1.1.146 N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide - 73972 1.1.1.146 N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide - 73971 1.1.1.146 N-cyclopropyl-N-(cis-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide - 216996 1.1.1.146 N-cyclopropyl-N-(cis-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide - 216997 1.1.1.146 N-cyclopropyl-N-(trans-4-hydroxy-4-methylcyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide - 216998 1.1.1.146 N-cyclopropyl-N-(trans-4-hydroxycyclohexyl)-6-(piperidin-1-yl)pyridine-2-carboxamide - 216999 1.1.1.146 N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide potent 11beta-HSD1 inhibitor 73886 1.1.1.146 N-cyclopropyl-N-[cis-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide - 217000 1.1.1.146 N-cyclopropyl-N-[trans-4-hydroxy-4-(trifluoromethyl)cyclohexyl]-6-(piperidin-1-yl)pyridine-2-carboxamide - 217001 1.1.1.146 N-methyl-2-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]naphthalen-1-amine - 26207 1.1.1.146 N-methyl-N-(thiophen-2-ylmethyl)adamantane-1-carboxamide - 74631 1.1.1.146 N-methyl-N-(thiophen-3-ylmethyl)adamantane-1-carboxamide - 74633 1.1.1.146 N-methyl-N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide - 74638 1.1.1.146 N-methyl-N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide - 74630 1.1.1.146 N-[(1-methyl-1H-pyrrol-2-yl)methyl]adamantane-1-carboxamide - 74637 1.1.1.146 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 - 73919 1.1.1.146 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 - 73918 1.1.1.146 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 - 73921 1.1.1.146 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 - 73920 1.1.1.146 N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide - 73970 1.1.1.146 N-[(5-hydroxy-1,3,3-trimethylcyclohexyl)methyl]dibenzo[b,d]furan-2-sulfonamide - 14598 1.1.1.146 N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73900 1.1.1.146 N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73899 1.1.1.146 N-[2-(thiophen-2-yl)ethyl]adamantane-1-carboxamide - 74628 1.1.1.146 N-[3-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide - 83281 1.1.1.146 N-[3-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide - 83283 1.1.1.146 N-[3-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide - 83273 1.1.1.146 N-[3-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide - 83279 1.1.1.146 N-[3-hydroxy-4-(piperidin-1-ylcarbonyl)phenyl]-3,4,5-trimethoxybenzamide - 73904 1.1.1.146 N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide - 89534 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethanesulfinyl)phenyl]acetamide - 83282 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethanesulfonyl)phenyl]acetamide - 83284 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-chloro-phenyl]acetamide - 83275 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-fluoro-phenyl]acetamide - 83277 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethoxy)-2-methyl-phenyl]acetamide - 83274 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-chloro-phenyl]acetamide - 83276 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethoxy)-3-methyl-phenyl]acetamide - 83278 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetamide - 83272 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethylamino)phenyl]acetamide - 83270 1.1.1.146 N-[4-(2-adamantan-1-yl-2-oxoethylsulfanyl)phenyl]acetamide - 83280 1.1.1.146 N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73894 1.1.1.146 N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide - 89536 1.1.1.146 N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide - 89535 1.1.1.146 N-[4-[(2,6-dimethylpyrimidin-4-yl)sulfamoyl]phenyl]-4-[oxo(phenyl)acetyl]benzamide - 89523 1.1.1.146 N-[5-(2-amino-2-oxoethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide - 216971 1.1.1.146 N-[5-(3-amino-3-oxopropyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide - 216972 1.1.1.146 N-[5-(cyanomethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-N2-(2-fluorobenzene-1-sulfonyl)-2-methylalaninamide - 216973 1.1.1.146 N-[6-[2-(4-benzylpiperazin-1-yl)-2-oxoethyl]pyridin-2-yl]-3-chloro-2-methylbenzenesulfonamide - 82845 1.1.1.146 N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73892 1.1.1.146 N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73890 1.1.1.146 N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73896 1.1.1.146 N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73888 1.1.1.146 N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73893 1.1.1.146 N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73891 1.1.1.146 N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73897 1.1.1.146 N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73889 1.1.1.146 N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73895 1.1.1.146 N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73887 1.1.1.146 N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide - 73898 1.1.1.146 N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydrazinecarbonyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide - 217041 1.1.1.146 N2-(2-fluorobenzene-1-sulfonyl)-N-[5-(hydroxymethyl)tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide - 217042 1.1.1.146 N2-(2-fluorobenzene-1-sulfonyl)-N-[5-[(2-hydroxyhydrazinyl)methyl]tricyclo[3.3.1.1~3,7~]decan-2-yl]-2-methylalaninamide - 217043 1.1.1.146 NADP+ 50% inhibition at 220 nmol 10 1.1.1.146 NSC 112288 - 132138 1.1.1.146 NSC 56412 - 132140 1.1.1.146 NSC 75617 - 132139 1.1.1.146 o-Iodosobenzoate complete inhibition of cortisol oxidation at 1 mM 2092 1.1.1.146 oleanolic acid oxidase IC50: 0.00015 mM, reductase IC50: 0.00055 mM 2975 1.1.1.146 oxymesterone - 256555 1.1.1.146 oxymetholone - 256556 1.1.1.146 p-chloromercuribenzoate complete inhibition of oxidation of cortisol at 0.01 mM 43 1.1.1.146 perfluorohexane sulfonate - 256551 1.1.1.146 perfluorohexanesulfonate - 217255 1.1.1.146 perfluorooctane sulfonate - 7716 1.1.1.146 Perfluorooctanoic acid - 6578 1.1.1.146 perfluorooctyl sulfonate - 217254 1.1.1.146 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 151080 1.1.1.146 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 151081 1.1.1.146 PF-877423 specific 11beta-HSD1 inhibitor 74600 1.1.1.146 PF-877423 - 74600 1.1.1.146 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 151079 1.1.1.146 PF-915275 - 217236 1.1.1.146 posaconazole - 10249 1.1.1.146 progesterone - 286 1.1.1.146 pyrrolidine dithiocarbamate - 34392 1.1.1.146 quercetin - 137 1.1.1.146 resorcinol weak inhibition 2034 1.1.1.146 resveratrol non-competitive inhibitor 799 1.1.1.146 resveratrol - 799 1.1.1.146 Rhein - 10768 1.1.1.146 rheochrysidin - 27991 1.1.1.146 rosiglitazone - 3404 1.1.1.146 saquinavir - 997 1.1.1.146 SAR184841 - 256566 1.1.1.146 sterenin A isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205 25312 1.1.1.146 sterenin B isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205 25313 1.1.1.146 sterenin C isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205 25314 1.1.1.146 sterenin D isoindoline alkaloid inhibitor isolated from Stereum sp. SANK 21205 25315 1.1.1.146 T0504 inhibitor of 11beta-HSD1 5002 1.1.1.146 T0504 - 5002 1.1.1.146 testosterone 0.003 mM, 50% inhibition of oxido-reductase reaction; 0.02 mM, 50% inhibition of dehydrogenase reaction 284 1.1.1.146 testosterone - 284 1.1.1.146 thiram - 6965 1.1.1.146 thiram potent inhibitor of isoform 11beta-HSD2 6965 1.1.1.146 tributyltin - 5717 1.1.1.146 Triphenyltin - 12716 1.1.1.146 TZD 2 - 132135 1.1.1.146 UE2316 selective isoform 11beta-HSD1 inhibitor 217239 1.1.1.146 UE2343 selective inhibitor for isoform 11beta-HSD1 256559 1.1.1.146 WY-14643 22% inhibition at 0.01 mM, cell-based assay, pH not specified in the publication, temperature not specified in the publication 30508 1.1.1.146 zearalenone - 16728 1.1.1.146 zearalenone selective inhibitor of isoform 11beta-HSD2 16728 1.1.1.146 zineb - 217250 1.1.1.146 ziram - 256550 1.1.1.146 [(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 256323 1.1.1.146 [1-[2-(cyclohexylamino)-2-oxoethyl]cyclopentyl]acetic acid 13% inhibition at 0.001 mM 150803 1.1.1.146 [1-[2-(octahydroisoquinolin-2(1H)-yl)-2-oxoethyl]cyclopentyl]acetic acid 34% inhibition at 0.001 mM 150807 1.1.1.146 [1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethyl]cyclopentyl]acetic acid 8% inhibition at 0.001 mM 150806 1.1.1.146 [1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid - 73951 1.1.1.146 [1-[4-([(2R)-2-methyl-4-[2-(pyridin-4-yl)ethyl]piperazin-1-yl]sulfonyl)phenyl]cyclopropyl]methanol - 82824 1.1.1.146 [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid lead compound for high throughput screening of inhibitors. A hydrophobic group at C-2 position dramatically enhances potency 29007 1.1.1.146 [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid - 29007 1.1.1.146 [3-(5H-chromeno[4,3-b]pyridin-3-yl)-5-methyl-1-benzofuran-2-yl](phenyl)methanone - 42549 1.1.1.146 [4-(1H-benzimidazol-2-yl)piperazin-1-yl](4-methylphenyl)methanone 65% residual activity at 0.02 mM 216118 1.1.1.146 [4-(2-adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid - 83324 1.1.1.146 [4-(2-Adamantan-1-yl-2-oxoethoxy)phenyl]acetic acid methyl ester - 83323 1.1.1.146 [4-hydroxy-1,1-dioxido-2-(2-phenylethyl)-2H-1,2-benzothiazin-3-yl](phenyl)methanone - 82871 1.1.1.146 [4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone potent inhibitor with a high permeability value, and low metabolic lability in mouse and human microsomes 29026 1.1.1.146 [4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone potent inhibitor with a high permeability value, and low metabolic lability in mouse and human microsomes, significant inhibition of isoform 11beta-HSD1 in both the liver and fat tissue of mice, 2 h after oral administration at 30 mg/kg 29026 1.1.1.146 [5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid good in vitro potency for the human enzyme while exhibiting enhanced metabolic stability in liver microsomes compared to lead compound [2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid 29006 1.1.1.146 [5-fluoro-2-(4-fluorophenyl)tricyclo[3.3.1.13,7]dec-2-yl]acetic acid - 29006 1.1.1.146 [5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone - 89519 1.1.1.146 [5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone - 89518 1.1.1.146 [9-(4-fluorophenyl)bicyclo[3.3.1]non-9-yl]acetic acid - 29005