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Androgen Receptor Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
BicalutamideIC50330.0 [1]
BicalutamideKi19.0 [1], 35.0 [2], 64.0 [3]
AndrostanoloneIC502.1 [1], 13.1 [2], 10000.0 [3]
HydroxyflutamideIC5043.0 [1]
HydroxyflutamideKi2.0 [1], 43.0 [2]
MifepristoneIC507.8 [1]
MifepristoneKi0.65 [1]
ProgesteroneIC5037.0 [1]
TestosteroneIC502.7 [1], 3.9 [2], 4.27 [3]
TestosteroneKi29.0 [1]
FlutamideIC50580.0 [1]
FlutamideKi1300.0 [1], 3700.0 [2]
(R)-BicalutamideIC50270.0 [1], 490.0 [2]
(R)-BicalutamideKi70.0 [1], 151.0 [2], 3700.0 [3]
6-(Bis-(2,2,2-trifluoroethyl)amino)-4-trifluoromethyl-1H-quinolin-2-oneIC5010000.0 [1]
6-(Bis-(2,2,2-trifluoroethyl)amino)-4-trifluoromethyl-1H-quinolin-2-oneKi1.5 [1], 4.6 [2]
Medroxyprogesterone acetateIC506.1 [1]
Medroxyprogesterone acetateKi2.9 [1]
EnzalutamideIC5050.0 [1], 90.0 [2], 361.0 [3], 1260.0 [4], 100000.0 [5]
EnzalutamideKi28.2 [1]
(2R,6S)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dioneIC507.0 [1], 127.0 [2], 152.0 [3], 205.0 [4]
(2R,6S)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dioneKi3.4 [1], 319.0 [2], 360.0 [3]
SpironolactoneIC50120.0 [1], 523.0 [2], 670.0 [3]
SpironolactoneKi39.4 [1]
4-(3-(4-Hydroxybutyl)-4,4-dimethyl-2,5-dioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrileIC5032.0 [1], 40.0 [2]
6-Ethyl-4-(trifluoromethyl)-6,7,8,9-tetrahydro-1H-pyrido[3,2-g]quinolin-2-oneIC504580.0 [1], 7481.0 [2], 10000.0 [3]
6-Ethyl-4-(trifluoromethyl)-6,7,8,9-tetrahydro-1H-pyrido[3,2-g]quinolin-2-oneKi7.0 [1], 11.0 [2], 17.0 [3]
8,8-Dimethyl-4-trifluoromethyl-6,7,8,9-tetrahydro-1H-pyrido[3,2-g]quinolin-2-oneIC5027.0 [1]
8,8-Dimethyl-4-trifluoromethyl-6,7,8,9-tetrahydro-1H-pyrido[3,2-g]quinolin-2-oneKi26.0 [1]
(2S,6R)-4-[4-Nitro-3-(trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dioneIC5012.0 [1], 114.0 [2]
(2S,6R)-4-[4-Nitro-3-(trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]decane-3,5-dioneKi2.0 [1], 5.0 [2], 117.0 [3]
DexamethasoneIC501000.0 [1], 4000.0 [2], 20000.0 [3]
DexamethasoneKi1410.0 [1]
PrednisoloneIC502000.0 [1], 34000.0 [2]
PrednisoloneKi2520.0 [1], 2760.0 [2], 2762.0 [3]
Bms-564929Ki1.4 [1], 2.1 [2], 2.11 [3], 14.0 [4]
1-Imidazolidinepropanesulfonamide, 3-(3-chloro-4-cyanophenyl)-5,5-dimethyl-4-oxo-2-thioxo-IC5010.0 [1], 12.0 [2], 200.0 [3], 410.0 [4], 440.0 [5]
(2S,6R)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5035.0 [1], 410.0 [2], 744.0 [3]
(2S,6R)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi7.0 [1], 632.0 [2]
(2R,6S)-4-(8-Hydroxyquinolin-5-yl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC50418.0 [1], 1790.0 [2], 3639.0 [3]
(2R,6S)-4-(8-Hydroxyquinolin-5-yl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi32.0 [1], 162.0 [2]
(2S,6R)-4-[3,5-Bis(trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5072.0 [1], 198.0 [2], 1746.0 [3]
(2S,6R)-4-[3,5-Bis(trifluoromethyl)phenyl]-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi24.0 [1], 401.0 [2]
(2R,6S)-4-(3,5-Dichlorophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5041.0 [1], 180.0 [2], 307.0 [3]
(2R,6S)-4-(3,5-Dichlorophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi6.0 [1], 158.0 [2]
(2S,6R)-4-Naphthalen-2-yl-4-azatricyclo[5.2.1.02,6]decane-3,5-dioneIC5084.0 [1], 265.0 [2], 1200.0 [3]
(2S,6R)-4-Naphthalen-2-yl-4-azatricyclo[5.2.1.02,6]decane-3,5-dioneKi11.0 [1], 284.0 [2]
(2R,6S)-4-(4-Nitrophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5030.0 [1], 179.0 [2], 664.0 [3]
(2R,6S)-4-(4-Nitrophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi12.0 [1], 192.0 [2]
(2S,6R)-4-Quinolin-7-yl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5052.0 [1], 234.0 [2], 1038.0 [3]
(2S,6R)-4-Quinolin-7-yl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi13.0 [1], 530.0 [2]
(2S,6R)-4-Naphthalen-2-yl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5084.0 [1], 265.0 [2], 1210.0 [3]
(2S,6R)-4-Naphthalen-2-yl-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi11.0 [1], 284.0 [2]
(2R,6S)-4-(3-Chloro-4-fluorophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5033.0 [1], 132.0 [2], 517.0 [3]
(2R,6S)-4-(3-Chloro-4-fluorophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi2.0 [1], 177.0 [2]
(2S,6R)-4-(3,4-Dimethylphenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5010.0 [1], 96.0 [2], 2014.0 [3]
(2S,6R)-4-(3,4-Dimethylphenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi3.4 [1], 400.0 [2]
(2R,6R)-8-Methyl-4-(4-nitronaphthalen-1-yl)-4,8-diazatricyclo[5.2.2.02,6]undec-10-ene-3,5,9-trioneIC50631.0 [1], 4030.0 [2], 8460.0 [3]
(2R,6R)-8-Methyl-4-(4-nitronaphthalen-1-yl)-4,8-diazatricyclo[5.2.2.02,6]undec-10-ene-3,5,9-trioneKi115.0 [1], 5000.0 [2]
(2R,6S,8S,10R)-4-[3-(Trifluoromethyl)phenyl]-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-ene-3,5-dioneIC5030.0 [1], 148.0 [2], 1700.0 [3]
(2R,6S,8S,10R)-4-[3-(Trifluoromethyl)phenyl]-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-ene-3,5-dioneKi9.0 [1], 3200.0 [2]
(2R,6S)-4-(3,4-Dichlorophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneIC5041.0 [1], 180.0 [2], 307.0 [3]
(2R,6S)-4-(3,4-Dichlorophenyl)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dioneKi6.0 [1], 158.0 [2]
(2R,6S)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dioneIC500.4 [1], 66.0 [2], 196.0 [3]
(2R,6S)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dioneKi19.0 [1], 100.0 [2]
(2S,6R)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.3.2.02,6]dodecane-3,5-dioneIC5023.0 [1], 179.0 [2], 658.0 [3]
(2S,6R)-4-[3-(Trifluoromethyl)phenyl]-4-azatricyclo[5.3.2.02,6]dodecane-3,5-dioneKi20.0 [1], 2810.0 [2]
EplerenoneIC5010000.0 [1], 20000.0 [2]
OnapristoneIC50269.0 [1]
OnapristoneKi100.0 [1]
4-(((1R,2S)-2-Cyanocyclohexyl)oxy)-2-(trifluoromethyl)benzonitrileIC5012.0 [1], 60.0 [2]
4-[(7r,7As)-7-Hydroxy-1,3-Dioxotetrahydro-1h-Pyrrolo[1,2-C]imidazol-2(3h)-Yl]-1-NaphthonitrileKi3.2 [1]
(2R)-2-Methyl-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-3,6-dihydro-2H-pyrido[3,2-g][1,4]benzoxazin-7-oneIC5070.0 [1]
(2R)-2-Methyl-1-(2,2,2-trifluoroethyl)-9-(trifluoromethyl)-3,6-dihydro-2H-pyrido[3,2-g][1,4]benzoxazin-7-oneKi0.9 [1], 7.1 [2]
6-{Methyl[(1R)-1-phenylethyl]amino}-4-(trifluoromethyl)pyridine-3-carbonitrileIC5020.0 [1], 45.0 [2]
4-(2-Hydroxyphenyl)-2-(trifluoromethyl)benzonitrileIC500.02 [1], 39.9 [2]
2,2-Dimethyl-6-(trifluoromethyl)-1,9-dihydropyrido[3,2-g]quinolin-8-oneIC5027.0 [1], 58.0 [2]
2,2-Dimethyl-6-(trifluoromethyl)-1,9-dihydropyrido[3,2-g]quinolin-8-oneKi73.0 [1], 86.0 [2]
3-Chloro-4-(o-tolyloxy)benzonitrileIC5046.0 [1], 64.0 [2]
4-(Trifluoromethyl)-6-(diethylamino)quinoline-2(1H)-oneIC501000.0 [1], 10000.0 [2]
4-(Trifluoromethyl)-6-(diethylamino)quinoline-2(1H)-oneKi4.4 [1]
6-(Dipropylamino)-4-(trifluoromethyl)-1,2-dihydroquinolin-2-oneIC5010000.0 [1]
6-(Dipropylamino)-4-(trifluoromethyl)-1,2-dihydroquinolin-2-oneKi64.0 [1]
1-[2-(4-Methylphenoxy)ethyl]-2-(2-phenoxyethylsulfanyl)benzimidazoleIC5010000.0 [1], 13100.0 [2], 50000.0 [3]
4-(2-Fluorophenylthio)-2-(trifluoromethyl)benzonitrileIC5054.0 [1], 184.0 [2]
6-[Ethyl(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-oneIC5010000.0 [1]
6-[Ethyl(2,2,2-trifluoroethyl)amino]-4-(trifluoromethyl)-1,2-dihydroquinolin-2-oneKi7.1 [1]
(2S,6R,10S,11R)-4-(4-Bromo-3-methylphenyl)-10,11-dihydroxy-4-azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dioneIC5059.0 [1], 5240.0 [2]
(2S,6R,10S,11R)-4-(4-Bromo-3-methylphenyl)-10,11-dihydroxy-4-azatricyclo[5.2.2.02,6]undec-8-ene-3,5-dioneKi33.0 [1], 432.0 [2]
EstradiolIC5019.1 [1], 26.0 [2]
Nordihydroguaiaretic acidIC5010000.0 [1], 38800.0 [2], 50000.0 [3]
MethyltrienoloneIC500.3 [1], 7.0 [2]
MethyltrienoloneKi0.4 [1]
6-[(2R,5R)-2-Methyl-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-4-(trifluoromethyl)-1H-quinolin-2-oneIC5010000.0 [1]
6-[(2R,5R)-2-Methyl-5-[(1R)-2,2,2-trifluoro-1-hydroxyethyl]pyrrolidin-1-yl]-4-(trifluoromethyl)-1H-quinolin-2-oneKi1.5 [1]
4-[(1S,7S,7Ar)-1-ethyl-7-hydroxy-3-oxo-5,6,7,7a-tetrahydro-1H-pyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrileKi0.9 [1]
1,8-Dichloro-10-[(3-hydroxy-2,4-dimethoxyphenyl)methylidene]anthracen-9-oneIC50170.0 [1], 1135.0 [2], 10000.0 [3]
10-[(2-Hydroxy-4-methoxyphenyl)methylidene]anthracen-9-oneIC50100.0 [1], 231.8 [2], 10000.0 [3]



References

This online tool may be cited as follows

MLA

"Quest Database™ Androgen Receptor Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/androgen-receptor-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Androgen Receptor Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/androgen-receptor-inhibitors-ic50-ki.
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