Target Validation Information
TTD ID T89534
Target Name Estrogen receptor (ESR)
Type of Target
Successful
Drug Potency against Target Clomifene Drug Info EC50 = 179 nM [46]
Conjugated Estrogens Drug Info EC50 = 1.1 nM [44]
Danazol Drug Info IC50 = 57400 nM
Dienestrol Drug Info EC50 = 1.1 nM [44]
Diethylstilbestrol Drug Info Ki = 870 nM [45]
Estradiol Drug Info Ec50 = 40 nM [47]
Estriol Drug Info EC50 = 12 nM [44]
Fulvestrant Drug Info IC50 = 9.35 nM
Lasofoxifene Drug Info IC50 = 1.2 nM [42]
Mestranol Drug Info EC50 = 9.1 nM [44]
Mitotane Drug Info IC50 = 318000 nM [43]
Tamoxifen Drug Info IC50 = 174 nM [41]
Toremifene Drug Info IC50 = 1000 nM [29]
Drug Info IC50 = 2800 nM [14]
1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol Drug Info Ki = 8.5 nM [19]
1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 43 nM [17]
1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 266 nM [17]
1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL Drug Info IC50 = 91 nM [17]
1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 77 nM [17]
2,3-diphenyl-1H-indole Drug Info IC50 = 6950 nM [20]
2,4-Dibenzylamino-6-isopentylpyrimidine Drug Info IC50 = 8300 nM [31]
2,4-diisobutylamino-6-isopentylpyrimidine Drug Info IC50 = 3100 nM [31]
2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 139 nM [13]
2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info IC50 = 3240 nM [13]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 5280 nM [13]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info IC50 = 5000 nM [13]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 1570 nM [13]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info IC50 = 8430 nM [13]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Drug Info IC50 = 34 nM [6]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol Drug Info IC50 = 16 nM [6]
2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info IC50 = 1900 nM [13]
2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol Drug Info IC50 = 6630 nM [18]
2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Drug Info IC50 = 504 nM [18]
2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol Drug Info IC50 = 1200 nM [13]
2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol Drug Info IC50 = 483 nM [12]
2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol Drug Info IC50 = 2557 nM [13]
2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol Drug Info IC50 = 114 nM [12]
2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol Drug Info IC50 = 1300 nM [13]
2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol Drug Info IC50 = 775 nM [13]
2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol Drug Info IC50 = 390 nM [13]
2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol Drug Info IC50 = 447 nM [13]
2-(4-Hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 1227 nM [13]
2-(4-Hydroxy-phenyl)-benzooxazol-6-ol Drug Info IC50 = 902 nM [13]
2-(4-Hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 1775 nM [18]
2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL Drug Info IC50 = 176 nM [13]
2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Drug Info IC50 = 4.3 nM [6]
2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info IC50 = 117 nM [13]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol Drug Info IC50 = 153 nM [13]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info IC50 = 35 nM [13]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol Drug Info IC50 = 3800 nM [13]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol Drug Info IC50 = 780 nM [13]
2-Naphthalen-1-yl-benzooxazol-6-ol Drug Info IC50 = 1880 nM [13]
2-phenyl-1,2'-spirobi[1H-indene]-5'-ol Drug Info IC50 = 114 nM [6]
3'-Methoxy-4'Hydroxyclomiphene Drug Info IC50 = 780 nM [38]
3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one Drug Info IC50 = 654 nM [23]
3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one Drug Info IC50 = 1170 nM [23]
3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Drug Info IC50 = 3000 nM [13]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol Drug Info IC50 = 819 nM [13]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Drug Info IC50 = 815 nM [13]
3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info IC50 = 5110 nM [13]
3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info IC50 = 2353 nM [13]
3-chloro-4-(4-hydroxyphenyl)salicylaldoxime Drug Info Ki = 310 nM [30]
3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one Drug Info IC50 = 585 nM [23]
4',5,7-trihydroxy-6,8-dimethylisoflavone Drug Info IC50 = 10200 nM [5]
4,10-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 1030 nM [23]
4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 1210 nM [23]
4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 468 nM [23]
4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 237 nM [23]
4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 335 nM [23]
4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 4610 nM [23]
4-(1,2-Diphenyl-but-1-enyl)-phenol Drug Info IC50 = 7 nM [4]
4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenol Drug Info IC50 = 105 nM [15]
4-(1-butyl-7-chloro-1H-indazol-3-yl)phenol Drug Info IC50 = 25 nM [15]
4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenol Drug Info IC50 = 18 nM [15]
4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol Drug Info IC50 = 1800 nM [20]
4-(2-phenyl-1H-indol-3-yl)phenol Drug Info IC50 = 24 nM [20]
4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol Drug Info IC50 = 94.8 nM [20]
4-(3-phenyl-1H-indol-2-yl)phenol Drug Info IC50 = 8310 nM [20]
4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Drug Info IC50 = 190 nM [13]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info IC50 = 2410 nM [13]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Drug Info IC50 = 82 nM [13]
4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenol Drug Info IC50 = 37 nM [15]
4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenol Drug Info IC50 = 18 nM [15]
4-(7-chloro-1-propyl-1H-indazol-3-yl)phenol Drug Info IC50 = 52 nM [15]
4-(7-methyl-1-propyl-1H-indazol-3-yl)phenol Drug Info IC50 = 40 nM [15]
4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol Drug Info IC50 = 6100 nM [13]
4-benzyl-2,6-diisobutylamino-pyrimidine Drug Info IC50 = 9500 nM [31]
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 212 nM [18]
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 213 nM [18]
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 634 nM [18]
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 1500 nM [18]
4-hydroxy-N,N-diphenylbenzenesulfonamide Drug Info IC50 = 410 nM [21]
4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamide Drug Info IC50 = 871 nM [21]
4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamide Drug Info IC50 = 1371 nM [21]
4-hydroxy-N-phenyl-N-propylbenzenesulfonamide Drug Info IC50 = 303 nM [21]
4-Naphthalen-2-yl-phenol Drug Info IC50 = 638 nM [17]
4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol Drug Info IC50 = 10 nM [7]
4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol Drug Info IC50 = 240 nM [7]
4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol Drug Info IC50 = 70 nM [7]
4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol Drug Info IC50 = 200 nM [7]
4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenol Drug Info IC50 = 15 nM [4]
4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenol Drug Info IC50 = 500 nM [4]
4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenol Drug Info IC50 = 50 nM [4]
4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenol Drug Info IC50 = 30 nM [4]
4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenol Drug Info IC50 = 150 nM [4]
4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol Drug Info IC50 = 15 nM [7]
5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 1140 nM [18]
5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info IC50 = 2765 nM [13]
5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info IC50 = 632 nM [18]
5-hydroxy-2-phenylisoindoline-1,3-dione Drug Info IC50 = 2700 nM [24]
6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 27 nM [17]
6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 10.3 nM [17]
6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 10 nM [17]
6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 24 nM [17]
6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 92 nM [17]
6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 107 nM [17]
6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 92 nM [17]
6-(3-Hydroxy-phenyl)-naphthalen-1-ol Drug Info IC50 = 1452 nM [17]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 230 nM [17]
6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 174 nM [17]
6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol Drug Info IC50 = 40 nM [17]
6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol Drug Info IC50 = 884 nM [17]
6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol Drug Info IC50 = 282 nM [17]
6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol Drug Info IC50 = 709 nM [17]
6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol Drug Info IC50 = 1231 nM [17]
6-(4-Hydroxy-phenyl)-naphthalen-1-ol Drug Info IC50 = 22 nM [17]
6-(4-Hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 211 nM [18]
6-butyl-2,4-dipropylaminopyrimidine Drug Info IC50 = 13000 nM [31]
6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 464 nM [13]
6-ethyl-2,4-diisobutylaminopyrimidine Drug Info IC50 = 7300 nM [31]
6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info IC50 = 101 nM [23]
6-Phenyl-naphthalen-2-ol Drug Info IC50 = 1345 nM [17]
7-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 2642 nM [17]
7-(4-Hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 442 nM [17]
7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 727 nM [13]
7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol Drug Info IC50 = 1.5 nM [12]
7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 498 nM [13]
7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol Drug Info IC50 = 6.8 nM [12]
7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 537 nM [13]
7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info IC50 = 481 nM [13]
7-Phenyl-naphthalen-2-ol Drug Info IC50 = 3405 nM [17]
8-(2,2-dimethylpropyl)naringenin Drug Info IC50 = 216 nM [25]
8-(2-methylpropyl)naringenin Drug Info IC50 = 80 nM [25]
8-(3-methylbutyl)naringenin Drug Info IC50 = 140 nM [25]
8-benzylnaringenin Drug Info IC50 = 503 nM [25]
8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 30 nM [17]
8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info IC50 = 22 nM [17]
8-methylnaringenin Drug Info IC50 = 5245 nM [25]
8-n-heptylnaringenin Drug Info IC50 = 392 nM [25]
8-n-nonylnaringenin Drug Info IC50 = 436 nM [25]
8-n-pentylnaringenin Drug Info IC50 = 383 nM [25]
8-n-propylnaringenin Drug Info IC50 = 155 nM [25]
8-n-undecylnaringenin Drug Info IC50 = 1017 nM [25]
Afimoxifene Drug Info IC50 = 40 nM [32]
ARZOXIFENE Drug Info IC50 = 21.5 nM [26]
BITHIONOL Drug Info IC50 = 3940.88 nM [37]
BROUSSONIN A Drug Info IC50 = 8100 nM [35]
Carboron Cluster with phenol Drug Info IC50 = 0.59 nM [9]
COUMESTROL Drug Info IC50 = 75.7 nM [16]
daidzein Drug Info IC50 = 17000 nM [5]
DIHYDRORALOXIFENE Drug Info IC50 = 0.52 nM [1]
Doxorubicin-Formaldehyde Conjugate Drug Info IC50 = 300 nM [10]
EFFUSOL Drug Info IC50 = 240 nM [23]
ERA-923 Drug Info IC50 = 1.5 nM [3]
Geldanamycin-estradiol hybrid Drug Info IC50 = 80 nM [2]
GSK-5182 Drug Info IC50 = 320 nM [22]
HE2100 Drug Info IC50 = 180 nM [28]
HEXESTROL Drug Info IC50 = 2 nM
JNJ-17148066 Drug Info IC50 = 11 nM [34]
JNJ-19398990 Drug Info IC50 = 1736 nM [34]
JNJ-26529126 Drug Info IC50 = 1210 nM [34]
JNJ-26529152 Drug Info IC50 = 10 nM [34]
LTERHKILHRLLQEGSPSD Drug Info Ki = 190 nM [27]
MPrP Drug Info IC50 = 20 nM [33]
N,N,N-Triisobutyl-pyrimidine-2,4,6-triamine Drug Info IC50 = 2400 nM [31]
N-allyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info IC50 = 235 nM [21]
N-benzyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info IC50 = 500 nM [21]
N-butyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info IC50 = 317 nM [21]
N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info IC50 = 866 nM [21]
N-ethyl-4-hydroxy-N-phenylbenzenesulfonamide Drug Info IC50 = 404 nM [21]
Nafoxidine Drug Info IC50 = 40.9 nM [40]
ONAPRISTONE Drug Info Ki < 20 nM [39]
SOPHORAFLAVANONE B Drug Info IC50 = 57 nM [25]
Tamoxifen butyl bromide Drug Info Ki = 13.01 nM [36]
Tamoxifen ethyl bromide Drug Info Ki = 13.66 nM [36]
Tamoxifen isopropyl bromide Drug Info Ki = 25.43 nM [36]
Tamoxifen methyl iodide Drug Info Ki = 46.29 nM [36]
WAY-169916 Drug Info IC50 = 1300 nM [15]
WAY200070 Drug Info IC50 = 155 nM [13]
ZK-164015 Drug Info IC50 = 1.4 nM [11]
[1,1':2',1'']Terphenyl-4'-carbaldehyde oxime Drug Info Ki = 0.15 nM [8]
Action against Disease Model Fulvestrant Drug Info IC50 in immortalized rat embryonic hypothalamic cell line D12 subclone cells: 0.63 nM [41]
Tamoxifen Drug Info IC50 in immortalized rat embryonic hypothalamic cell line D12 subclone cells: 174 nM [41]
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