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11-beta-hydroxysteroid dehydrogenase 1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
N-[4-(2-Cyanoethyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC501.4 [1]
(6S)-3-[(1S)-1-[4-(2,4-Difluorophenyl)phenyl]ethyl]-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-1,3-oxazinan-2-oneIC502.5 [1]
N-Cyclopropyl-N-(4-pyridin-3-ylcyclohexyl)-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC503.0 [1]
EnoxoloneIC5013.0 [1]
2-(2-(3-Chloro-2-methylphenylsulfonamido)thiazol-4-yl)-N,N-diethylacetamideIC5052.0 [1]
N-Cyclopropyl-N-(4-phenylcyclohexyl)-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC509.8 [1]
(6R)-3-[(1S)-1-[4-(2,4-Difluorophenyl)phenyl]ethyl]-6-(3-hydroxypropyl)-6-phenyl-1,3-oxazinan-2-oneIC500.72 [1]
(R)-3-((S)-1-(4'-Fluorobiphenyl-4-yl)ethyl)-6-(3-hydroxypropyl)-6-phenyl-1,3-oxazinan-2-oneIC500.6 [1]
(S)-3-((S)-1-(4'-Fluorobiphenyl-4-yl)ethyl)-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-1,3-oxazinan-2-oneIC501.5 [1]
3-[(6R)-3-[(1S)-1-[4-(2,4-Difluorophenyl)phenyl]ethyl]-6-(4-fluorophenyl)-2-oxo-1,3-oxazinan-6-yl]propanamideIC505.0 [1]
N-[3-[(6R)-3-[(1S)-1-[4-(2,4-Difluorophenyl)phenyl]ethyl]-6-(4-fluorophenyl)-2-oxo-1,3-oxazinan-6-yl]propyl]methanesulfonamideIC503.7 [1]
{(3s)-1-[5-(Cyclohexylcarbamoyl)-6-(Propylsulfanyl)pyridin-2-Yl]piperidin-3-Yl}acetic AcidIC502.0 [1]
1-[[(3R)-3-Methyl-4-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonylpiperazin-1-yl]methyl]cyclopropane-1-carboxamideIC500.7 [1], 0.83 [2], 1.2 [3], 7.3 [4], 14.0 [5]
1-[[(3R)-3-Methyl-4-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]phenyl]sulfonylpiperazin-1-yl]methyl]cyclopropane-1-carboxamideKi1.1 [1], 2.7 [2]
N-Cyclopropyl-N-(4-cyclopropyl-4-hydroxycyclohexyl)-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC5052.0 [1]
(6S)-3-[(1S)-1-(4-Bromophenyl)ethyl]-6-(4-fluorophenyl)-6-(2-hydroxy-2-methylpropyl)-1,3-oxazinan-2-oneIC501.9 [1]
Amg-221IC507.0 [1], 10.1 [2], 10000.0 [3]
Amg-221Ki12.8 [1]
N-[4-(4-Cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC503.4 [1]
9-[[2-Methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanoyl]amino]bicyclo[3.3.1]nonane-3-carboxamideIC5088.0 [1]
N-[4-(2-Cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC502.0 [1]
N-Cyclopropyl-N-(4-hydroxy-4-phenylcyclohexyl)-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC50150.0 [1]
N-(4-Cyano-4-pyridin-2-ylcyclohexyl)-N-cyclopropyl-4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC5039.0 [1]
N-[4-(3-Amino-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC5017.0 [1]
N-[4-Cyano-4-(4-fluorophenyl)cyclohexyl]-N-cyclopropyl-4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC5048.0 [1]
N-[4-(Cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(2R)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC5016.0 [1]
CarbenoxoloneIC5083.0 [1], 330.0 [2], 500.0 [3]
3-(1-Adamantyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepineIC507.5 [1], 7.8 [2], 8.0 [3]
N-Adamantan-2-Yl-1-Ethyl-D-ProlinamideIC504.0 [1], 4.1 [2], 4.15 [3], 90.0 [4]
N-Adamantan-2-Yl-1-Ethyl-D-ProlinamideKi1.4 [1]
N-[(E)-5-Hydroxy-2-adamantyl]-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}acetamideIC50130.0 [1], 15000.0 [2]
N-[(E)-5-Hydroxy-2-adamantyl]-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}acetamideKi8.0 [1], 67.0 [2]
(6S)-3-[3-(2,4-Difluorophenyl)phenyl]-6-(2-hydroxyethyl)-6-phenyl-1,3-oxazinan-2-oneIC500.77 [1], 11.97 [2]
(6S)-3-[(1S)-1-[4-(4-Fluorophenyl)phenyl]ethyl]-6-(2-hydroxy-2-methylpropyl)-6-phenyl-1,3-oxazinan-2-oneIC501.08 [1], 19.54 [2]
(S)-3-((S)-1-(4-Bromophenyl)ethyl)-6-(2-hydroxy-2-methylpropyl)-6-phenyl-1,3-oxazinan-2-oneIC500.79 [1], 8.94 [2]
(6S)-3-[6-(4-Fluorophenyl)pyridin-2-yl]-6-(2-hydroxyethyl)-6-phenyl-1,3-oxazinan-2-oneIC501.44 [1], 15.24 [2]
(6S)-3-[(1S)-1-[4-(Difluoromethoxy)phenyl]ethyl]-6-(4-fluorophenyl)-6-(2-hydroxyethyl)-1,3-oxazinan-2-oneIC501.3 [1], 8.94 [2]
3-[6-(2,4-Difluorophenyl)pyridin-2-yl]-6-(2-fluorophenyl)-6-(2-hydroxyethyl)-1,3-oxazinan-2-oneIC501.8 [1], 14.16 [2]
(6S)-3-[(1S)-1-[4-(2,4-Difluorophenyl)phenyl]ethyl]-6-(4-fluorophenyl)-6-(2-hydroxy-2-methylpropyl)-1,3-oxazinan-2-oneIC501.48 [1], 37.58 [2]
3-((R)-3-((S)-1-(4'-Fluorobiphenyl-4-yl)ethyl)-2-oxo-6-phenyl-1,3-oxazinan-6-yl)propanamideIC500.55 [1], 13.4 [2]
AcetoxoloneIC50800.0 [1], 3450.0 [2], 7100.0 [3], 7138.0 [4]
3-(4-Fluorophenyl)-5-[4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-1,2,4-triazol-3-yl]-1-bicyclo[2.2.2]octanyl]-1,2,4-oxadiazoleIC502.0 [1], 2.2 [2], 2200.0 [3]
N-(2-Adamantyl)piperidine-1-carboxamideIC5016.0 [1], 16.1 [2], 32.0 [3], 873.0 [4]
(5s)-2-{[(1s)-1-(2-Fluorophenyl)ethyl]amino}-5-Methyl-5-(Trifluoromethyl)-1,3-Thiazol-4(5h)-OneIC5033.0 [1], 10000.0 [2]
(5s)-2-{[(1s)-1-(2-Fluorophenyl)ethyl]amino}-5-Methyl-5-(Trifluoromethyl)-1,3-Thiazol-4(5h)-OneKi22.0 [1]
[4-[Cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-(4-fluorophenyl)cyclohexyl]methyl carbamateIC500.5 [1], 12.0 [2], 15.0 [3], 34.0 [4]
(2R)-1-[(4-Tert-butylphenyl)sulfonyl]-2-methyl-4-(4-nitrophenyl)piperazineIC503.0 [1], 57.0 [2]
9-[[2-(4-Chlorophenoxy)-2-methylpropanoyl]amino]bicyclo[3.3.1]nonane-3-carboxamideIC505.0 [1], 5.01 [2], 8.0 [3], 21.88 [4]
(6R)-6-(2-Aminoethyl)-3-[(1S)-1-[4-(2,4-difluorophenyl)phenyl]ethyl]-6-(4-fluorophenyl)-1,3-oxazinan-2-oneIC502.7 [1], 66.0 [2], 66.5 [3]
6-[4-(4-Cyanophenyl)piperazin-1-yl]-N-(5-hydroxy-2-adamantyl)pyridine-2-carboxamideIC502.8 [1], 6.7 [2]
4-[[1-[4-[5-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]cyclopropanecarbonyl]amino]adamantane-1-carboxylic acidIC5045.0 [1], 1900.0 [2]
4-[[1-[4-[5-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]cyclopropanecarbonyl]amino]adamantane-1-carboxylic acidKi7.0 [1], 250.0 [2]
N-[(E)-5-Fluoro-2-adamantyl]-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}acetamideIC50450.0 [1], 550.0 [2]
N-[(E)-5-Fluoro-2-adamantyl]-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}acetamideKi26.0 [1], 32.0 [2]
N-(5-Hydroxy-2-adamantyl)-1-piperidin-1-ylcyclopropane-1-carboxamideIC507.0 [1], 390.0 [2]
N-(5-Hydroxy-2-adamantyl)-1-piperidin-1-ylcyclopropane-1-carboxamideKi2.0 [1], 6.0 [2]
4-[[1-[4-[5-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]cyclopropanecarbonyl]amino]adamantane-1-carboxamideIC5022.0 [1], 490.0 [2]
4-[[1-[4-[5-(Trifluoromethyl)pyridin-2-yl]piperazin-1-yl]cyclopropanecarbonyl]amino]adamantane-1-carboxamideKi8.0 [1], 13.0 [2]
(S)-N-(trans-4-Fluorocyclohexyl)-4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)-N-cyclopropylbenzamideIC504.1 [1], 6.6 [2], 36.0 [3], 140.0 [4]
9-[4-[(5-Cyanopyridin-2-yl)oxymethyl]-3,3-dimethyl-2-oxopyrrolidin-1-yl]bicyclo[3.3.1]nonane-3-carboxamideIC505.0 [1], 39.0 [2], 510.0 [3]
9-[4-[(5-Cyanopyridin-2-yl)oxymethyl]-3,3-dimethyl-2-oxopyrrolidin-1-yl]bicyclo[3.3.1]nonane-3-carboxamideKi29.0 [1]
N-[4-(3-Amino-3-oxopropyl)-4-phenylcyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC500.8 [1], 3.9 [2], 17.0 [3], 37.0 [4]
N-(5-Fluoro-7-hydroxy-2-adamantyl)-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamideIC50120.0 [1], 3400.0 [2]
N-(5-Fluoro-7-hydroxy-2-adamantyl)-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanamideKi12.0 [1], 46.0 [2]
(6S)-6-(2-Hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(1-methyl-6-oxopyridin-3-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-oneIC501.6 [1], 1.67 [2], 3.3 [3], 6.44 [4]
(6S)-6-(2-Hydroxy-2-methylpropyl)-3-[(1S)-1-[4-(1-methyl-2-oxopyridin-4-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-oneIC501.62 [1], 1.7 [2], 4.3 [3], 5.54 [4]
[4-[Cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-(5-fluoropyridin-2-yl)cyclohexyl]methyl carbamateIC502.4 [1], 30.0 [2], 31.0 [3], 93.0 [4]
N-[4-(3-Amino-3-oxopropyl)-4-(4-fluorophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC501.8 [1], 12.0 [2], 24.0 [3], 55.0 [4]
[4-[Cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-phenylcyclohexyl]methyl carbamateIC501.0 [1], 4.6 [2], 8.8 [3], 20.0 [4]
N-Cyclopropyl-N-[4-(2-hydroxyethyl)-4-phenylcyclohexyl]-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC501.9 [1], 12.0 [2], 15.0 [3], 35.0 [4]
N-[4-(Acetamidomethyl)-4-phenylcyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC502.2 [1], 6.7 [2], 17.0 [3], 129.0 [4]
[4-[Cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-(1,3-thiazol-4-yl)cyclohexyl]methyl carbamateIC501.8 [1], 16.0 [2], 18.0 [3], 63.0 [4]
[4-[Cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-(2-fluorophenyl)cyclohexyl]methyl carbamateIC500.6 [1], 5.7 [2], 14.0 [3], 135.0 [4]
[4-[Cyclopropyl-[4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzoyl]amino]-1-pyridin-2-ylcyclohexyl]methyl carbamateIC503.5 [1], 19.0 [2], 25.0 [3], 74.0 [4]
N-Cyclopropyl-N-[4-(methanesulfonamidomethyl)-4-phenylcyclohexyl]-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC501.7 [1], 20.0 [2], 86.0 [3], 259.0 [4]
N-[4-(3-Amino-3-oxopropyl)-4-(2-fluorophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamideIC501.3 [1], 7.0 [2], 36.0 [3], 109.0 [4]
(6R)-6-(3-Hydroxypropyl)-3-[(1S)-1-[4-(1-methyl-6-oxopyridin-3-yl)phenyl]ethyl]-6-phenyl-1,3-oxazinan-2-oneIC501.4 [1], 1.44 [2], 3.42 [3], 5.7 [4]
Glycyrrhizic acidIC506.0 [1], 10.0 [2], 18.6 [3]
3-Chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamideIC503341.0 [1], 10000.0 [2]
3-(1-Adamantyl)-4-methyl-5-phenyl-1,2,4-triazoleIC5037.0 [1], 109.0 [2]
4-Methyl-3-(4-pentyl-1-bicyclo[2.2.2]octanyl)-5-[2-(trifluoromethyl)phenyl]-1,2,4-triazoleIC501.8 [1], 2.0 [2]
3-(1-(4-Chlorophenyl)cyclobutyl)-5,6,7,8,9,10-hexahydro-[1,2,4]triazolo[4,3-a]azocineIC501.0 [1], 1.3 [2]
2-(Phenylsulfonyl)-1-(4-(trifluoromethyl)phenyl)ethanoneIC50187.0 [1], 190.0 [2]
N-[(E)-5-Hydroxy-2-adamantyl]-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}propionamideIC505.0 [1], 29.0 [2]
N-[(E)-5-Hydroxy-2-adamantyl]-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}propionamideKi5.0 [1]
1-(3-Hydroxyazetidin-1-yl)-2-(6-hydroxy-2-phenyl-2-adamantyl)ethanoneIC5010.0 [1], 37.3 [2]
1-(3-Hydroxyazetidin-1-yl)-2-(6-hydroxy-2-phenyl-2-adamantyl)ethanoneKi3.8 [1]
3-Biphenyl-4-yl-5-[1-(4-chloro-phenyl)-cyclobutyl]-4-methyl-4H-[1,2,4]triazoleIC5011.0 [1]
2-(2-Chloro-4-fluorophenoxy)-2-methyl-N-[5-(2H-tetrazol-5-yl)-2-adamantyl]propanamideIC5010.96 [1], 11.0 [2], 54.0 [3]
4-[[2-(4-Chlorophenoxy)-2-methylpropanoyl]amino]adamantane-1-carboxylic acidIC5021.88 [1], 22.0 [2], 220.0 [3]
E-4-[(2-Methyl-2-phenoxypropanoyl)amino]adamantane-1-carboxamideIC505.0 [1], 5.01 [2], 24.0 [3]
4-[[2-(4-Methoxyphenoxy)-2-methylpropanoyl]amino]adamantane-1-carboxamideIC506.0 [1], 6.03 [2], 21.0 [3]
4-[[2-(4-Chlorophenoxy)-2-methylpropanoyl]amino]adamantane-1-carboxamideIC506.0 [1], 6.03 [2], 22.0 [3]
4-[[2-(2-Chlorophenoxy)-2-methylpropanoyl]amino]adamantane-1-carboxylic acidIC507.94 [1], 8.0 [2], 59.0 [3]
4-(2-(4-Chlorophenoxy)-2-methylpropanamido)bicyclo[2.2.2]octane-1-carboxamideIC5012.88 [1], 13.0 [2], 450.0 [3]
1-Naphthalen-2-ylsulfonyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazineIC5011.0 [1], 13.0 [2], 547.0 [3]
1-(Phenylsulfonyl)-4-[3-(trifluoromethyl)pyridin-2-yl]piperazineIC5045.0 [1], 724.0 [2]
1-Naphthalen-1-ylsulfonyl-4-[3-(trifluoromethyl)pyridin-2-yl]piperazineIC5013.0 [1], 329.0 [2]
9-[[2-(4-Chlorophenoxy)-2-methylpropanoyl]amino]-3-oxabicyclo[3.3.1]nonane-7-carboxamideIC5025.0 [1], 25.12 [2], 2400.0 [3]
2-(4-Chlorophenoxy)-N-(1-hydroxy-2-oxatricyclo[3.3.1.13,7]decan-6-yl)-2-methylpropanamideIC5015.0 [1], 15.14 [2], 199.0 [3]



References

This online tool may be cited as follows

MLA

"Quest Database™ 11-beta-hydroxysteroid dehydrogenase 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/11-beta-hydroxysteroid-dehydrogenase-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ 11-beta-hydroxysteroid dehydrogenase 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/11-beta-hydroxysteroid-dehydrogenase-1-inhibitors-ic50-ki.
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