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Estrogen receptor alpha Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
EstradiolIC503.2 [1]
EstradiolKi0.21 [1]
RaloxifeneIC501.8 [1]
TamoxifenIC50622.0 [1]
TamoxifenKi31.19 [1]
GenisteinIC509.7 [1], 395.0 [2], 1300.0 [3]
GenisteinKi39.0 [1], 370.0 [2]
FulvestrantIC500.06 [1], 3.4 [2]
FulvestrantKi1.04 [1]
(Z)-4-(1-(4-(2-(Dimethylamino)ethoxy)-phenyl)-2-phenylbut-1-en-1-yl)phenolIC505.6 [1]
(Z)-4-(1-(4-(2-(Dimethylamino)ethoxy)-phenyl)-2-phenylbut-1-en-1-yl)phenolKi0.04 [1], 0.39 [2], 2.51 [3], 5.7 [4]
(2S,3R)-3-(4-Hydroxyphenyl)-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-olIC500.8 [1]
(2E)-3-{4-[(1E)-1,2-Diphenylbut-1-enyl]phenyl}acrylic acidIC504000.0 [1], 12825.0 [2]
(E)-3-[4-[(E)-1-(4-Hydroxyphenyl)-2-phenylbut-1-enyl]phenyl]prop-2-enoic acidIC5012.0 [1], 242.0 [2]
(E)-3-[4-[(E)-1-(4-Hydroxyphenyl)-2-phenylbut-1-enyl]phenyl]prop-2-enoic acidKi2.51 [1]
DiethylstilbestrolIC500.33 [1], 0.77 [2], 3.0 [3], 770.0 [4]
DiethylstilbestrolKi0.26 [1], 0.49 [2]
MifepristoneIC501000.0 [1], 5000.0 [2]
MifepristoneKi200.0 [1], 6754.0 [2], 10000.0 [3]
DaidzeinIC50450.0 [1], 2160.0 [2], 6300.0 [3], 17000.0 [4], 1000000.0 [5]
DaidzeinKi1800.0 [1]
4'-HydroxytamoxifenIC5010.0 [1]
4,4-Bis(3-methyl-4-hydroxyphenyl)heptaneIC504.9 [1], 4.92 [2]
2-Phenyl-1-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-1,2,3,4-tetrahydroisoquinolin-6-olIC5016.5 [1]
BazedoxifeneIC500.6 [1], 3.7 [2], 23.0 [3], 50.0 [4], 31710.0 [5]
BrilanestrantIC500.5 [1], 6.1 [2], 11.1 [3], 24.0 [4]
BrilanestrantKi0.37 [1]
2-(4-Fluorophenyl)-1-methyl-1-[4-(2-piperidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC501.9 [1], 3.0 [2], 38.0 [3], 38.02 [4]
2-Phenyl-1-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}-1,2,3,4-tetrahydroisoquinolin-6-olIC5010.69 [1], 10.7 [2], 11.5 [3], 20.99 [4], 21.0 [5]
(E)-3-[4-[2-Adamantylidene-(4-hydroxyphenyl)methyl]phenyl]prop-2-enoic acidIC5017.0 [1], 500.0 [2]
(E)-3-[4-[2-Adamantylidene-(4-hydroxyphenyl)methyl]phenyl]prop-2-enoic acidKi0.4 [1]
(E)-3-[4-[2-Adamantylidene-(4-hydroxyphenyl)methyl]phenyl]-N-(3-hydroxypropyl)prop-2-enamideIC500.53 [1], 50.0 [2]
(E)-3-[4-[2-Adamantylidene-(4-hydroxyphenyl)methyl]phenyl]-N-(3-hydroxypropyl)prop-2-enamideKi0.43 [1]
PrednisoloneIC5010000.0 [1], 100000.0 [2]
PrednisoloneKi5000.0 [1]
EstroneIC5029.0 [1], 96.0 [2], 210.0 [3]
EstroneKi2.19 [1]
Raloxifene hydrochlorideIC500.72 [1], 2.0 [2], 2.4 [3], 22.0 [4]
AfimoxifeneIC5010.3 [1], 17.0 [2]
AfimoxifeneKi0.25 [1], 0.5 [2]
LasofoxifeneIC501.3 [1], 1.4 [2], 3.1 [3], 4.0 [4]
ErteberelKi2.29 [1], 2.68 [2], 2.7 [3]
2,4-Diisobutylamino-6-isopentylpyrimidineIC503100.0 [1]
2,4-Diisobutylamino-6-isopentylpyrimidineKi2800.0 [1], 29000.0 [2], 30000.0 [3]
2-(4-Fluorophenyl)-1-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC501.6 [1], 30.97 [2], 31.0 [3]
1-Methyl-1-[4-(2-piperidin-1-ylethoxy)phenyl]-2-(3-propan-2-ylphenyl)-3,4-dihydroisoquinolin-6-olIC5016.1 [1], 16.11 [2], 46.0 [3], 46.03 [4]
1-Methyl-2-(4-methylphenyl)-1-[4-(2-piperidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC502.9 [1], 27.99 [2], 28.0 [3]
2-(4-Chlorophenyl)-1-methyl-1-[4-(2-piperidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC503.1 [1], 34.99 [2], 35.0 [3]
2-(3-Hydroxyphenyl)-1-methyl-1-[4-(2-piperidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC500.7 [1], 33.96 [2], 34.0 [3]
2-(3-Chlorophenyl)-1-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC502.9 [1], 66.0 [2], 66.07 [3]
2-(3-Chlorophenyl)-1-methyl-1-[4-(2-piperidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC504.5 [1], 48.98 [2], 49.0 [3]
1-Methyl-2-phenyl-1-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-1,2,3,4-tetrahydroisoquinolin-6-olIC502.6 [1], 28.97 [2], 29.0 [3]
2-(3-Fluorophenyl)-1-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC503.0 [1], 38.99 [2], 39.0 [3]
2-(3-Hydroxyphenyl)-1-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC500.6 [1], 30.97 [2], 31.0 [3]
1-Methyl-2-(4-methylphenyl)-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC503.5 [1], 30.97 [2], 31.0 [3]
2-(4-Chlorophenyl)-1-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC503.3 [1], 26.98 [2], 27.0 [3]
1-{4-[2-(Azepan-1-yl)ethoxy]phenyl}-1-methyl-2-phenyl-1,2,3,4-tetrahydroisoquinolin-6-olIC501.5 [1], 55.98 [2], 56.0 [3]
1-Methyl-2-(4-propan-2-ylphenyl)-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC502.6 [1], 43.95 [2], 44.0 [3]
1-Methyl-1-[4-(2-piperidin-1-ylethoxy)phenyl]-2-(4-propan-2-ylphenyl)-3,4-dihydroisoquinolin-6-olIC505.2 [1], 70.96 [2], 71.0 [3]
1-Methyl-2-phenyl-1-{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}-1,2,3,4-tetrahydroisoquinolin-6-olIC501.8 [1], 38.0 [2], 39.81 [3]
2-[3-(Dimethylamino)phenyl]-1-methyl-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-3,4-dihydroisoquinolin-6-olIC5019.0 [1], 19.01 [2], 93.97 [3], 94.0 [4]
(E)-3-[4-[(7-Hydroxy-2-oxo-3-phenylchromen-4-yl)methyl]phenyl]prop-2-enoic acidIC508.1 [1], 1180.0 [2], 1500.0 [3], 100000.0 [4]
(2R,3S)-3-(4-Hydroxyphenyl)-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-olIC509.6 [1], 23.0 [2], 353.0 [3]
(E)-3-[4-[6-Hydroxy-1-methyl-2-(4-propan-2-ylphenyl)-3,4-dihydroisoquinolin-1-yl]phenyl]prop-2-enoic acidIC500.9 [1], 1.8 [2], 2.1 [3], 30.0 [4]
(E)-3-[4-[3-(4-Fluoro-2-methylphenyl)-7-hydroxy-2-oxochromen-4-yl]oxyphenyl]prop-2-enoic acidIC500.4 [1], 21.0 [2], 27.0 [3]
(E)-3-[4-[7-Hydroxy-3-[2-methyl-4-(trifluoromethoxy)phenyl]-2-oxochromen-4-yl]oxyphenyl]prop-2-enoic acidIC500.5 [1], 2.7 [2], 3.9 [3]
(E)-3-[4-[3-(4-Fluoro-2-methylphenyl)-2-oxochromen-4-yl]oxyphenyl]prop-2-enoic acidIC5072.0 [1], 248.0 [2], 330.0 [3], 3100.0 [4]
(E)-3-[4-[3-[2-Methyl-4-(trifluoromethoxy)phenyl]-2-oxochromen-4-yl]oxyphenyl]prop-2-enoic acidIC5015.0 [1], 100.0 [2], 180.0 [3], 3100.0 [4]
5-[4-[(3S)-1-(3-Fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-(4-methoxy-2-methylphenyl)-8,9-dihydro-7H-benzo[7]annulen-2-olIC500.2 [1], 1.0 [2], 12.0 [3], 16.0 [4]
6-(3-Fluoro-4-methoxyphenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulen-2-olIC500.3 [1], 4.0 [2], 67.0 [3], 120.0 [4]
6-[4-(Difluoromethoxy)-2-fluorophenyl]-1-fluoro-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulen-2-olIC500.2 [1], 2.0 [2], 27.0 [3], 47.0 [4]
CID 130232950IC500.2 [1], 2.0 [2], 29.0 [3], 50.0 [4]
5-[4-[(3S)-1-(3-Fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)-8,9-dihydro-7H-benzo[7]annulen-2-olIC5038.0 [1], 284.0 [2], 728.0 [3], 937.0 [4]
5-[4-[(3S)-1-(3-Fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-(3-hydroxyphenyl)-8,9-dihydro-7H-benzo[7]annulen-2-olIC500.7 [1], 2.0 [2], 3.0 [3], 4.0 [4]
5-[4-[(3S)-1-(3-Fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-6-(2-methyl-1,3-benzoxazol-6-yl)-8,9-dihydro-7H-benzo[7]annulen-2-olIC500.3 [1], 1.0 [2], 11.0 [3], 18.0 [4]
[(5Z)-Cyclodec-5-en-3,7-diyn-1-yl]methyl 3-[(8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl]prop-2-ynoateIC5010000.0 [1], 31000.0 [2], 33000.0 [3], 48000.0 [4]
Ethinyl estradiolIC502.0 [1], 8.04 [2]
Ethinyl estradiolKi0.13 [1]
SpironolactoneIC505702.0 [1], 20000.0 [2]
SpironolactoneKi1100.0 [1]
CoumestrolIC5011.0 [1], 75.7 [2]
PipendoxifeneIC501.5 [1], 14.0 [2], 60.0 [3]
(E)-3-[3,5-Difluoro-4-[(1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]phenyl]prop-2-enoic acidIC500.14 [1], 0.21 [2], 0.68 [3]
(2S,3R)-3-(4-Hydroxyphenyl)-2-[4-[2-[(3R)-3-methylpyrrolidin-1-yl]ethoxy]phenyl]-2,3-dihydro-1,4-benzoxathiin-6-olIC503.0 [1]
(2S,3R)-3-(4-Hydroxyphenyl)-2-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-olIC502.6 [1]
(2S,3R)-3-(3-Hydroxyphenyl)-2-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-olIC500.9 [1], 1.0 [2], 1.7 [3]
(3Ar,4S,9bS)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-olKi4.34 [1], 14.5 [2]
(2S,3R)-3-(3-Hydroxyphenyl)-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-6-olIC504.0 [1], 4.1 [2], 5.4 [3]
6-Butyl-2,4-dipropylaminopyrimidineIC5013000.0 [1]
6-Butyl-2,4-dipropylaminopyrimidineKi16000.0 [1], 32000.0 [2]
(2R,3S)-3-(4-Hydroxyphenyl)-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2,3-dihydro-1,4-benzoxathiin-7-olIC501.6 [1], 1.8 [2], 5.0 [3]
2-N,4-N-Dibenzyl-6-(2-phenylethyl)pyrimidine-2,4-diamineIC501000000.0 [1]
2-N,4-N-Dibenzyl-6-(2-phenylethyl)pyrimidine-2,4-diamineKi49000.0 [1], 1000000.0 [2]
1-[2-[4-[(19R)-5,15-Dimethoxy-8,18-dioxatetracyclo[9.8.0.02,7.012,17]nonadeca-1(11),2(7),3,5,12(17),13,15-heptaen-19-yl]phenoxy]ethyl]piperidineIC5064.0 [1], 1736.0 [2], 10000.0 [3]
Chembl4171598IC500.9 [1], 53.0 [2]
Chembl4171598Ki0.5 [1]
(19R)-15-Methoxy-19-[4-(2-piperidin-1-ylethoxy)phenyl]-8,18-dioxatetracyclo[9.8.0.02,7.012,17]nonadeca-1(11),2(7),3,5,12(17),13,15-heptaen-5-olIC509.0 [1], 10.0 [2], 259.0 [3]
(E)-3-[4-[[2-[2-(1,1-Difluoroethyl)-4-fluorophenyl]-6-hydroxy-1-benzothiophen-3-yl]oxy]phenyl]prop-2-enoic acidIC500.2 [1], 6.0 [2], 8.9 [3]
9a-Benzyl-7-hydroxy-4-methyl-1,2,9,9a-tetrahydro-3H-fluoren-3-oneIC5014.0 [1], 1500.0 [2], 2300.0 [3]



References

This online tool may be cited as follows

MLA

"Quest Database™ Estrogen receptor alpha Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/estrogen-receptor-alpha-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Estrogen receptor alpha Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/estrogen-receptor-alpha-inhibitors-ic50-ki.
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