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Glucocorticoid receptor Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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▼
MifepristoneIC501.6 [1]
MifepristoneKi1.2 [1]
DexamethasoneIC502.51 [1]
PrednisoloneIC507.7 [1]
ProgesteroneIC501000.0 [1]
Medroxyprogesterone acetateIC5010.0 [1]
Medroxyprogesterone acetateKi13.2 [1]
(3R,4S)-5,7-Difluoro-6-(1H-indol-7-yl)-2,2,4-trimethyl-3,4-dihydro-1H-quinolin-3-olIC501.5 [1], 11.0 [2]
(3R,4S)-5,7-Difluoro-6-(1H-indol-7-yl)-2,2,4-trimethyl-3,4-dihydro-1H-quinolin-3-olKi2.5 [1]
4-(5-Fluoro-2-hydroxyphenyl)-4-methyl-1-(2-methylquinolin-5-ylamino)-2-(trifluoromethyl)-pentan-2-olIC503.16 [1], 5.01 [2]
5-(3,5-Dichlorophenyl)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC501.3 [1], 16.0 [2], 67.0 [3], 107.0 [4], 139.0 [5]
5-(3,5-Dichlorophenyl)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneKi3.3 [1], 7.1 [2]
N-(3-Dibenzylamino-2-methyl-phenyl)-methanesulfonamideIC5028.0 [1], 250.0 [2]
N-{3-[Benzyl-(4-phenoxy-benzyl)-amino]-2-methyl-phenyl}-methanesulfonamideIC502.7 [1]
10-Methoxy-2,2,4-trimethyl-5-(3-methylsulfanylmethoxy-phenyl)-2,5-dihydro-1H-6-oxa-1-aza-chryseneIC504.0 [1], 9.0 [2], 16.0 [3], 140.0 [4]
10-Methoxy-2,2,4-trimethyl-5-(3-methylsulfanylmethoxy-phenyl)-2,5-dihydro-1H-6-oxa-1-aza-chryseneKi4.0 [1]
2-[(1-Ethyl-3,4-dihydro-2H-naphthalen-1-yl)methyl]-3,3,3-trifluoro-2-hydroxy-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)propanamideIC506.17 [1], 199.53 [2]
5-Chloro-6-(1H-indol-7-yl)-2,2,4,8-tetramethyl-1,2,3,4-tetrahydroquinolineIC509.4 [1], 10.0 [2], 59.0 [3], 1000.0 [4]
5-Chloro-6-(1H-indol-7-yl)-2,2,4,8-tetramethyl-1,2,3,4-tetrahydroquinolineKi0.3 [1], 0.6 [2]
(3R,4S)-5-Chloro-6-(1H-indol-7-yl)-2,2,4,8-tetramethyl-3,4-dihydro-1H-quinolin-3-olIC501.1 [1], 7.8 [2], 16.0 [3]
(3R,4S)-5-Chloro-6-(1H-indol-7-yl)-2,2,4,8-tetramethyl-3,4-dihydro-1H-quinolin-3-olKi1.7 [1]
10-Methoxy-2,2,4-trimethyl-5-phenyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC5030.0 [1], 51.0 [2], 123.0 [3], 164.0 [4], 300.0 [5]
10-Methoxy-2,2,4-trimethyl-5-phenyl-2,5-dihydro-1H-1-aza-6-oxachryseneKi240.0 [1]
SpironolactoneIC501400.0 [1], 4100.0 [2], 6920.0 [3]
SpironolactoneKi32.6 [1], 864.8 [2]
BudesonideIC500.5 [1], 1.57 [2], 3.8 [3]
BudesonideKi1.3 [1], 2.03 [2]
Fluticasone propionateIC500.04 [1], 0.07 [2], 0.5 [3], 0.9 [4]
3,3,3-Trifluoro-2-hydroxy-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-[(1-pentan-3-yl-3,4-dihydro-2H-naphthalen-1-yl)methyl]propanamideIC501.2 [1], 5.25 [2], 66.07 [3]
(2R,3S)-3-(2-Chloro-3-fluoro-4-methoxyphenyl)-2-(ethylsulfanylmethyl)-1,1,1-trifluoro-3-[(2-methylquinolin-5-yl)amino]propan-2-olIC500.16 [1], 0.47 [2], 0.63 [3], 31.62 [4]
5-[[(1S,2R,4R)-4-Ethyl-6,7-difluoro-2,5-dihydroxy-2-(trifluoromethyl)-3,4-dihydro-1H-naphthalen-1-yl]amino]-1H-quinolin-2-oneIC501.15 [1], 6.31 [2], 10.0 [3], 63.1 [4]
[(4Ar)-1-(4-fluorophenyl)-6-[4-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-pyridin-2-ylmethanoneKi0.16 [1], 0.28 [2], 12.0 [3], 14.0 [4], 100.0 [5]
5-[3-(Dimethylcarbamoyloxy)phenyl]-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC506.0 [1], 12.0 [2], 26.0 [3], 216.0 [4]
5-[3-(Dimethylcarbamoyloxy)phenyl]-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneKi2.4 [1]
10-Methoxy-2,2,4-trimethyl-5-(3-trifluoromethyl-phenyl)-2,5-dihydro-1H-6-oxa-1-aza-chryseneIC5032.0 [1], 44.0 [2], 57.0 [3], 105.0 [4]
10-Methoxy-2,2,4-trimethyl-5-(3-trifluoromethyl-phenyl)-2,5-dihydro-1H-6-oxa-1-aza-chryseneKi11.0 [1]
OnapristoneIC5027.0 [1]
OnapristoneKi41.8 [1]
10-Methoxy-2,2,4-trimethyl-5-prop-2-enyl-1,5-dihydrochromeno[3,4-f]quinolineIC5013.0 [1], 33.0 [2]
10-Methoxy-2,2,4-trimethyl-5-prop-2-enyl-1,5-dihydrochromeno[3,4-f]quinolineKi2.5 [1]
ZK-216348IC503.0 [1], 6.31 [2], 19.95 [3], 31.62 [4]
2-[(4R)-4-[(5-Ethylsulfonyl-1H-pyrrolo[2,3-c]pyridin-2-yl)methyl]-5,5,5-trifluoro-4-hydroxy-2-methylpentan-2-yl]-5-fluorobenzamideIC5019.0 [1], 23.0 [2], 55.0 [3], 84.0 [4]
N-[(1R,2S)-1-[1-(4-Fluorophenyl)indazol-5-yl]oxy-1-(6-methoxypyridin-3-yl)propan-2-yl]cyclopropanecarboxamideIC500.24 [1], 0.4 [2], 2.8 [3], 6.3 [4]
(2R,4As,10aR)-4a-benzyl-2-prop-1-ynyl-1,3,4,9,10,10a-hexahydrophenanthrene-2,7-diolKi0.17 [1], 0.6 [2], 4.0 [3], 5.5 [4]
N-{3-[Benzyl-(4-chloro-2-fluoro-benzyl)-amino]-2-methyl-phenyl}-methanesulfonamideIC505.7 [1], 210.0 [2]
3-[5-[(1R,2S)-2-(2,2-Difluoropropanoylamino)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)propoxy]indazol-1-yl]-N-[(3R)-oxolan-3-yl]benzamideIC500.06 [1], 0.43 [2], 0.9 [3], 0.91 [4]
1,1,1-Trifluoro-4-(5-fluoro-2-methoxyphenyl)-2-(1H-indol-2-ylmethyl)-4-methylpentan-2-olIC506.6 [1], 21.0 [2], 22.0 [3], 96.0 [4]
4-[4-[3-[4-[[N-Benzyl-3-(methanesulfonamido)-2-methylanilino]methyl]phenoxy]phenoxy]butanoylamino]butanoic acidIC500.6 [1], 86.0 [2]
5-Benzyl-6-(4-phenylpiperidin-1-yl)pyrimidine-2,4(1H,3H)-dioneKi8.0 [1], 8.1 [2], 93.0 [3]
CID 11640164IC504.0 [1], 4.4 [2], 9.8 [3], 10.0 [4]
CID 11661172IC5010.0 [1], 38.0 [2]
N-[(2s)-1-[[1-(4-Fluorophenyl)indazol-4-Yl]amino]propan-2-Yl]-2,4,6-Trimethyl-BenzenesulfonamideIC501.47 [1], 1.5 [2], 4.9 [3], 14.0 [4]
3-(4-{4-[(Benzyl{2-methyl-3-[(methylsulfonyl)amino]phenyl}amino)methyl]phenoxy}phenyl)propanoic AcidIC5034.0 [1], 500.0 [2]
N-(3-Dibenzylamino-2-ethyl-phenyl)-methanesulfonamideIC5012.0 [1], 270.0 [2]
N-{3-[Benzyl-(2,4-difluoro-benzyl)-amino]-2-methyl-phenyl}-methanesulfonamideIC5015.0 [1], 100.0 [2]
4-(4-{4-[(Benzyl{2-methyl-3-[(methylsulfonyl)amino]phenyl}amino)methyl]phenoxy}phenyl)butanoic AcidIC508.8 [1], 670.0 [2]
N-{3-[(2,4-Difluoro-benzyl)-(4-phenoxy-benzyl)-amino]-2-methyl-phenyl}-methanesulfonamideIC5021.0 [1], 95.0 [2], 385.0 [3], 1800.0 [4]
4-(5-Fluoro-2-hydroxyphenyl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamideIC503.16 [1], 4.0 [2], 10.0 [3], 50.12 [4]
2,2,2-Trifluoro-N-[(1r,2s)-1-{[1-(4-Fluorophenyl)-1h-Indazol-5-Yl]oxy}-1-Phenylpropan-2-Yl]acetamideIC500.13 [1], 0.5 [2], 2.7 [3]
(2R,4Ar,10aR)-4a-ethyl-2-phenyl-1,3,4,9,10,10a-hexahydrophenanthrene-2,7-diolIC5021.0 [1], 5000.0 [2]
(2R,3R,4Ar,10aR)-4a-ethyl-2-phenyl-1,3,4,9,10,10a-hexahydrophenanthrene-2,3,7-triolIC503.8 [1], 5000.0 [2]
(8S,9S,10R,11S,13S,14S,17R)-17-[2-(1,3-Benzothiazol-2-ylsulfanyl)acetyl]-11,17-dihydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-3-oneIC504.8 [1], 36.0 [2]
4-Methyl-5-(2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline-6-yl)thiophene-2-carbonitrileIC5073.0 [1], 113.0 [2], 1000.0 [3]
4-Methyl-5-(2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline-6-yl)thiophene-2-carbonitrileKi43.0 [1]
(R)-8a-Benzyl-2-(4-tert-butylphenylsulfonyl)-1,2,3,4,8,8a-hexahydroisoquinolin-6(7H)-oneKi4.0 [1], 200.0 [2]
[(4Ar)-6-(3,4-difluorophenyl)sulfonyl-1-(4-fluorophenyl)-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-pyridin-2-ylmethanoneKi0.22 [1], 7.5 [2]
[(4Ar)-1-(4-fluorophenyl)-6-(3-methylphenyl)sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-pyridin-2-ylmethanoneKi0.14 [1], 6.8 [2]
[(4Ar)-1-(4-fluorophenyl)-6-[3-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-pyridin-2-ylmethanoneKi0.1 [1], 14.0 [2]
3-[[(4Ar)-1-(4-fluorophenyl)-4a-(pyridine-2-carbonyl)-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-6-yl]sulfonyl]benzonitrileKi0.14 [1], 15.0 [2]
[(4Ar)-1-(4-fluorophenyl)-6-[3-fluoro-4-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolin-4a-yl]-pyridin-2-ylmethanoneKi0.29 [1], 11.0 [2]
5-(3,5-Difluorophenyl)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC509.0 [1], 10.0 [2], 11.0 [3], 56.0 [4]
5-[3-(Methoxymethoxy)phenyl]-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC5023.0 [1], 28.0 [2], 49.0 [3], 131.0 [4]
5-(3,5-Dimethylphenyl)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC509.2 [1], 18.0 [2], 24.0 [3], 146.0 [4]
(8R,9S,10R,11S,13S,14S,17S)-17-(3,3-Dimethylbut-1-ynyl)-17-hydroxy-13-methyl-11-[4-[methyl(propan-2-yl)amino]phenyl]-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-oneIC505.6 [1], 17.2 [2], 19.5 [3], 24.9 [4]
(5S,6R,8R)-8-Ethyl-2-fluoro-5-[(2-methylquinolin-5-yl)amino]-6-(trifluoromethyl)-7,8-dihydro-5H-naphthalene-1,6-diolIC505.01 [1], 12.59 [2]
5-[[(1S,2R)-1-(5-Bromo-2-hydroxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pent-4-enyl]amino]-2H-isoquinolin-1-oneIC5019.95 [1], 63.1 [2], 158.49 [3]
5-[[(1S,2R)-6-Fluoro-2,5-dihydroxy-4,4-dimethyl-2-(trifluoromethyl)-1,3-dihydronaphthalen-1-yl]amino]-2H-isoquinolin-1-oneIC506.31 [1], 12.59 [2], 19.95 [3]
5-[[(1S,2R)-6-Fluoro-2,5-dihydroxy-4,4-dimethyl-2-(trifluoromethyl)-1,3-dihydronaphthalen-1-yl]amino]-1H-quinolin-2-oneIC5015.85 [1], 25.12 [2]
(5S,6R,8R)-8-Ethyl-2-fluoro-5-[(7-fluoro-2-methylquinazolin-5-yl)amino]-6-(trifluoromethyl)-7,8-dihydro-5H-naphthalene-1,6-diolIC506.31 [1], 25.12 [2], 125.89 [3]
(5S,6R,8R)-2-Fluoro-8-methyl-5-[(2-methylquinolin-5-yl)amino]-6-(trifluoromethyl)-7,8-dihydro-5H-naphthalene-1,6-diolIC5015.85 [1], 19.95 [2], 39.81 [3]
DagrocoratIC500.69 [1], 1.31 [2], 7.2 [3], 8.9 [4]
3-[5-[(1R,2S)-1-(4H-1,3-Benzodioxin-7-yl)-2-(2,2-difluoropropanoylamino)propoxy]indazol-1-yl]-N-(pyridin-3-ylmethyl)benzamideIC500.06 [1], 0.38 [2], 0.8 [3], 0.82 [4]
3-[5-[(1R,2S)-2-(2,2-Difluoropropanoylamino)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)propoxy]indazol-1-yl]-N-(pyridin-3-ylmethyl)benzamideIC500.04 [1], 0.17 [2], 0.77 [3], 1.0 [4]
3-[5-[(1R,2S)-2-(2,2-Difluoropropanoylamino)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)propoxy]indazol-1-yl]-N-[(3R)-1,1-dioxothiolan-3-yl]benzamideIC500.17 [1], 0.54 [2], 1.5 [3], 1.6 [4]
(5S,6R)-2-Fluoro-5-[(7-fluoro-2-methylquinazolin-5-yl)amino]-8,8-dimethyl-6-(trifluoromethyl)-5,7-dihydronaphthalene-1,6-diolIC5039.81 [1], 125.89 [2], 158.49 [3]
5-[[4-(3-Fluoro-2-hydroxyphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)pentyl]amino]-2H-isoquinolin-1-oneIC502.51 [1], 3.98 [2], 25.12 [3]
3,5-Dibromo-4-[5-isopropyl-4-methoxy-2-(3-methylbenzoyl)phenoxy]-phenylacetic acidIC5019.0 [1], 20.0 [2], 400.0 [3], 410.0 [4]
5-(3-Bromo-5-methylphenyl)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-1-aza-6-oxachryseneIC5012.0 [1], 18.0 [2], 29.0 [3], 314.0 [4]
EplerenoneIC508940.0 [1], 10000.0 [2], 18000.0 [3]
(4Ar)-4a-(ethoxymethyl)-1-(4-fluorophenyl)-6-[4-(trifluoromethyl)phenyl]sulfonyl-4,5,7,8-tetrahydropyrazolo[3,4-g]isoquinolineKi0.9 [1], 6.8 [2]
CID 24825740IC500.05 [1], 0.16 [2], 0.9 [3]
Glucocorticoid receptor agonistIC502.1 [1], 3.3 [2], 80.0 [3]
(1S)-1-[(4Ar,5S)-1-(4-fluorophenyl)-4a-methyl-5,6,7,8-tetrahydro-4H-benzo[f]indazol-5-yl]-1-thiophen-3-ylethanolIC500.8 [1]
(1S)-1-[(4Ar,5S)-1-(4-fluorophenyl)-4a-methyl-5,6,7,8-tetrahydro-4H-benzo[f]indazol-5-yl]-1-thiophen-3-ylethanolKi0.8 [1]
(R)-[(4Ar,5S)-1-(4-fluorophenyl)-4a-methyl-5,6,7,8-tetrahydro-4H-benzo[f]indazol-5-yl]-(4-fluorophenyl)methanolIC505.3 [1], 6.2 [2]
CID 121248172IC503.8 [1], 7.0 [2], 160.0 [3]
4-(5-Fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-2,3-benzoxazin-6-yl)-2-(trifluoromethyl)pentanamideIC501.0 [1], 8.0 [2]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Glucocorticoid receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Dec. 2024, https://www.aatbio.com/data-sets/glucocorticoid-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, December 21). Quest Database™ Glucocorticoid receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/glucocorticoid-receptor-inhibitors-ic50-ki.
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