Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00242
Target NameEstrogen receptor    
Type of TargetSuccessful target    
Drug Potency against TargetEthinyl EstradiolEC50 = 0.014 nM[1]
DiethylstilbestrolEC50 = 0.06 nM[2]
DienestrolEC50 = 1.1 nM[2]
EstroneEC50 = 1.1 nM[2]
EstriolEC50 = 12 nM[2]
ClomifeneEC50 = 179 nM[3]
MestranolEC50 = 9.1 nM[2]
EstradiolEc50 = 40 nM[4]
LasofoxifeneIC50 = 1.2 nM[5]
ToremifeneIC50 = 1000 nM[6]
TamoxifenIC50 = 174 nM[1]
MitotaneIC50 = 318000 nM[7]
DanazolIC50 = 57400 nM[8]
FulvestrantIC50 = 9.35 nM[9]
RaloxifeneKi = 300 nM[10]
ClomifeneKi = 6500 nM[10]
DiethylstilbestrolKi = 870 nM[11]
TamoxifenKi = 870 nM[11]
DIHYDRORALOXIFENEIC50 = 0.52 nM[12]
Carboron Cluster with phenolIC50 = 0.59 nM[13]
ZK-164015IC50 = 1.4 nM[14]
7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-olIC50 = 1.5 nM[15]
PipendoxifeneIC50 = 1.5 nM[16]
4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenolIC50 = 10 nM[17]
JNJ-26529152IC50 = 10 nM[18]
6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 10 nM[19]
6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 10.3 nM[19]
6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diolIC50 = 101 nM[20]
8-n-undecylnaringeninIC50 = 1017 nM[21]
4',5,7-trihydroxy-6,8-dimethylisoflavoneIC50 = 10200 nM[22]
4,10-dimethyl-6H-benzo[c]chromene-3,8-diolIC50 = 1030 nM[20]
4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenolIC50 = 105 nM[23]
6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 107 nM[19]
JNJ-17148066IC50 = 11 nM[18]
2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-olIC50 = 114 nM[15]
2-phenyl-1,2'-spirobi[1H-indene]-5'-olIC50 = 114 nM[24]
5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-olIC50 = 1140 nM[25]
2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-olIC50 = 117 nM[26]
3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-oneIC50 = 1170 nM[20]
2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-olIC50 = 1200 nM[26]
JNJ-26529126IC50 = 1210 nM[18]
4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diolIC50 = 1210 nM[20]
Estrogen platinum(II) hybrid derivativeIC50 = 12200 nM[27]
2-(4-Hydroxy-phenyl)-benzooxazol-5-olIC50 = 1227 nM[26]
Estrogen platinum(II) hybrid derivativeIC50 = 12300 nM[27]
6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-olIC50 = 1231 nM[19]
2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-olIC50 = 1300 nM[26]
WAY-169916IC50 = 1300 nM[23]
6-butyl-2,4-dipropylaminopyrimidineIC50 = 13000 nM[28]
6-Phenyl-naphthalen-2-olIC50 = 1345 nM[19]
4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamideIC50 = 1371 nM[29]
2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 139 nM[26]
8-(3-methylbutyl)naringeninIC50 = 140 nM[21]
6-(3-Hydroxy-phenyl)-naphthalen-1-olIC50 = 1452 nM[19]
4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenolIC50 = 15 nM[30]
4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenolIC50 = 15 nM[17]
4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenolIC50 = 150 nM[30]
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-olIC50 = 1500 nM[25]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-olIC50 = 153 nM[26]
7-Bromo-2-(4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 155 nM[26]
8-n-propylnaringeninIC50 = 155 nM[21]
Estrogen platinum(II) hybrid derivativeIC50 = 15600 nM[27]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 1570 nM[26]
Estrogen platinum(II) hybrid derivativeIC50 = 15900 nM[27]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-olIC50 = 16 nM[24]
DIADZEINIC50 = 17000 nM[22]
JNJ-19398990IC50 = 1736 nM[18]
6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-olIC50 = 174 nM[19]
2-(4-Hydroxy-phenyl)-benzofuran-5-olIC50 = 176 nM[26]
2-(4-Hydroxy-phenyl)-quinolin-6-olIC50 = 1775 nM[25]
4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenolIC50 = 18 nM[23]
4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenolIC50 = 18 nM[23]
ANDROSTENEDIOLIC50 = 180 nM[31]
4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenolIC50 = 1800 nM[32]
2-Naphthalen-1-yl-benzooxazol-6-olIC50 = 1880 nM[26]
4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diolIC50 = 190 nM[26]
2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-olIC50 = 1900 nM[26]
Estrogen platinum(II) hybrid derivativeIC50 = 19700 nM[27]
HEXESTROLIC50 = 2 nM[33]
Carboron Cluster with phenolIC50 = 2.85 nM[13]
MPrPIC50 = 20 nM[34]
4-[1,2-bis(4-hydroxyphenyl)vinyl]phenolIC50 = 200 nM[17]
ARZOXIFENEIC50 = 21.5 nM[35]
6-(4-Hydroxy-phenyl)-naphthalen-2-olIC50 = 211 nM[25]
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-olIC50 = 212 nM[25]
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-olIC50 = 213 nM[25]
8-(2,2-dimethylpropyl)naringeninIC50 = 216 nM[21]
6-(4-Hydroxy-phenyl)-naphthalen-1-olIC50 = 22 nM[19]
8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-olIC50 = 22 nM[19]
geldanamycin-estradiol hybridIC50 = 220 nM[36]
Carboron Cluster with phenolIC50 = 23.4 nM[13]
6-(3-Hydroxy-phenyl)-naphthalen-2-olIC50 = 230 nM[19]
N-allyl-4-hydroxy-N-phenylbenzenesulfonamideIC50 = 235 nM[29]
3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diolIC50 = 2353 nM[26]
4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diolIC50 = 237 nM[20]
2-phenyl-1,2'-spirobi[1H-indene]-5-olIC50 = 24 nM[24]
4-(2-phenyl-1H-indol-3-yl)phenolIC50 = 24 nM[32]
6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 24 nM[19]
4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenolIC50 = 240 nM[17]
EFFUSOLIC50 = 240 nM[20]
N,N,N-Triisobutyl-pyrimidine-2,4,6-triamineIC50 = 2400 nM[28]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diolIC50 = 2410 nM[26]
4-(1-butyl-7-chloro-1H-indazol-3-yl)phenolIC50 = 25 nM[23]
2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-olIC50 = 2557 nM[26]
7-(3-Hydroxy-phenyl)-naphthalen-2-olIC50 = 2642 nM[19]
1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-olIC50 = 266 nM[19]
6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 27 nM[19]
5-hydroxy-2-phenylisoindoline-1,3-dioneIC50 = 2700 nM[37]
5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-olIC50 = 2765 nM[26]
Estrogen platinum(II) hybrid derivativeIC50 = 2800 nM[27]
6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-olIC50 = 282 nM[19]
Carboron Cluster with phenolIC50 = 3.6 nM[13]
Carboron Cluster with phenolIC50 = 3.92 nM[13]
4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenolIC50 = 30 nM[30]
8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-olIC50 = 30 nM[19]
Doxorubicin-Formaldehyde ConjugateIC50 = 300 nM[38]
3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-olIC50 = 3000 nM[26]
4-hydroxy-N-phenyl-N-propylbenzenesulfonamideIC50 = 303 nM[29]
2,4-diisobutylamino-6-isopentylpyrimidineIC50 = 3100 nM[28]
Estrogen platinum(II) hybrid derivativeIC50 = 3100 nM[27]
N-butyl-4-hydroxy-N-phenylbenzenesulfonamideIC50 = 317 nM[29]
GSK-5182IC50 = 320 nM[39]
2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-olIC50 = 3240 nM[26]
4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diolIC50 = 335 nM[20]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-olIC50 = 34 nM[24]
7-Phenyl-naphthalen-2-olIC50 = 3405 nM[19]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-olIC50 = 35 nM[26]
4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenolIC50 = 37 nM[23]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-olIC50 = 3800 nM[26]
8-n-pentylnaringeninIC50 = 383 nM[21]
2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-olIC50 = 390 nM[26]
8-n-heptylnaringeninIC50 = 392 nM[21]
BITHIONOLIC50 = 3940.88 nM[40]
2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-olIC50 = 4.3 nM[24]
4-(7-methyl-1-propyl-1H-indazol-3-yl)phenolIC50 = 40 nM[23]
4-HYDROXYTAMOXIFENIC50 = 40 nM[41]
6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-olIC50 = 40 nM[19]
NAFOXIDINEIC50 = 40.9 nM[42]
N-ethyl-4-hydroxy-N-phenylbenzenesulfonamideIC50 = 404 nM[29]
4-hydroxy-N,N-diphenylbenzenesulfonamideIC50 = 410 nM[29]
1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-olIC50 = 43 nM[19]
8-n-nonylnaringeninIC50 = 436 nM[21]
7-(4-Hydroxy-phenyl)-naphthalen-2-olIC50 = 442 nM[19]
2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-olIC50 = 447 nM[26]
4,7-dimethyl-6H-benzo[c]chromene-3,8-diolIC50 = 4610 nM[20]
6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 464 nM[26]
4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diolIC50 = 468 nM[20]
7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 481 nM[26]
2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-olIC50 = 483 nM[15]
7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 498 nM[26]
4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenolIC50 = 50 nM[30]
4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenolIC50 = 500 nM[30]
N-benzyl-4-hydroxy-N-phenylbenzenesulfonamideIC50 = 500 nM[29]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-olIC50 = 5000 nM[26]
8-benzylnaringeninIC50 = 503 nM[21]
2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-olIC50 = 504 nM[25]
3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diolIC50 = 5110 nM[26]
4-(7-chloro-1-propyl-1H-indazol-3-yl)phenolIC50 = 52 nM[23]
Estrogen platinum(II) hybrid derivativeIC50 = 5200 nM[27]
8-methylnaringeninIC50 = 5245 nM[21]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 5280 nM[26]
7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 537 nM[26]
SOPHORAFLAVANONE BIC50 = 57 nM[21]
3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-oneIC50 = 585 nM[20]
7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-olIC50 = 6.8 nM[15]
Carboron Cluster with phenolIC50 = 6.88 nM[13]
4-Benzo[d]isoxazol-3-yl-benzene-1,3-diolIC50 = 6100 nM[26]
5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-olIC50 = 632 nM[25]
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-olIC50 = 634 nM[25]
4-Naphthalen-2-yl-phenolIC50 = 638 nM[19]
3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-oneIC50 = 654 nM[20]
2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-olIC50 = 6630 nM[25]
2,3-diphenyl-1H-indoleIC50 = 6950 nM[32]
4-(1,2-Diphenyl-but-1-enyl)-phenolIC50 = 7 nM[30]
4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenolIC50 = 70 nM[17]
6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-olIC50 = 709 nM[19]
Carboron Cluster with phenolIC50 = 71.6 nM[13]
7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-olIC50 = 727 nM[26]
6-ethyl-2,4-diisobutylaminopyrimidineIC50 = 7300 nM[28]
COUMESTROLIC50 = 75.7 nM[43]
1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-olIC50 = 77 nM[19]
2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-olIC50 = 775 nM[26]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-olIC50 = 780 nM[26]
3'-Methoxy-4'HydroxyclomipheneIC50 = 780 nM[44]
8-(2-methylpropyl)naringeninIC50 = 80 nM[21]
geldanamycin-estradiol hybridIC50 = 80 nM[36]
BROUSSONIN AIC50 = 8100 nM[45]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-olIC50 = 815 nM[26]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-olIC50 = 819 nM[26]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diolIC50 = 82 nM[26]
2,4-Dibenzylamino-6-isopentylpyrimidineIC50 = 8300 nM[28]
4-(3-phenyl-1H-indol-2-yl)phenolIC50 = 8310 nM[32]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-olIC50 = 8430 nM[26]
N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamideIC50 = 866 nM[29]
4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamideIC50 = 871 nM[29]
6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-olIC50 = 884 nM[19]
Carboron Cluster with phenolIC50 = 9.57 nM[13]
2-(4-Hydroxy-phenyl)-benzooxazol-6-olIC50 = 902 nM[26]
1-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-olIC50 = 91 nM[19]
6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 92 nM[19]
6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-olIC50 = 92 nM[19]
4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenolIC50 = 94.8 nM[32]
4-benzyl-2,6-diisobutylamino-pyrimidineIC50 = 9500 nM[28]
ONAPRISTONEKi < 20 nM[46]
[1,1';2',1'']Terphenyl-4'-carbaldehyde oximeKi = 0.15 nM[47]
Tamoxifen butyl bromideKi = 13.01 nM[48]
Tamoxifen ethyl bromideKi = 13.66 nM[48]
LTERHKILHRLLQEGSPSDKi = 190 nM[49]
Tamoxifen isopropyl bromideKi = 25.43 nM[48]
3-chloro-4-(4-hydroxyphenyl)salicylaldoximeKi = 310 nM[50]
Tamoxifen methyl iodideKi = 46.29 nM[48]
1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-olKi = 8.5 nM[51]
Action against Disease ModelFulvestrantIC50 in immortalized rat embryonic hypothalamic cell line D12 subclone cells: 0.63 nM[1]
RaloxifeneIC50 in immortalized rat embryonic hypothalamic cell line D12 subclone cells: 1 nM[1]
TamoxifenIC50 in immortalized rat embryonic hypothalamic cell line D12 subclone cells: 174 nM[1]
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National University of Singapore, Singapore


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