Gene-drug interactions (data source: DGIdb)
Gene Name Entrez ID Drug Name Chembl ID Interaction Types Sources publications
ESR1 2099 DIETHYLSTILBESTROL CHEMBL411 agonist TdgClinicalTrial, DrugBank, GuideToPharmacologyInteractions, TEND, TTD, ChemblInteractions 17320868, 17308373, 11752352, 17317669, 17306201, 17314305, 20387803
ESR1 2099 ESTROGENS, CONJUGATED CHEMBL1201649 agonist TdgClinicalTrial, ChemblInteractions, TEND, DrugBank 16876190, 16955786, 16982590, 16884174, 16985877
ESR1 2099 DESOGESTREL CHEMBL1533 agonist TdgClinicalTrial, TEND, DrugBank 10836199, 2175153, 7750284
ESR1 2099 MEDROXYPROGESTERONE ACETATE CHEMBL717 agonist PharmGKB, DrugBank 17094978, 17415709, 17118173, 17203775, 17103262
ESR1 2099 DIENESTROL CHEMBL1018 agonist TdgClinicalTrial, ChemblInteractions, TEND, DrugBank, TTD 18976723, 15276617, 9048584, 11752352, 9558716, 3334987, 3622377
ESR1 2099 ETHINYL ESTRADIOL CHEMBL691 agonist TdgClinicalTrial, GuideToPharmacologyInteractions, ChemblInteractions, TEND, DrugBank, TTD 19434891, 17125913, 11752352, 17142999, 17138652, 17124377, 17095591, 19237207
ESR1 2099 PROPYLPYRAZOLETRIOL CHEMBL441282 agonist GuideToPharmacologyInteractions
ESR1 2099 CHEMBL188528 CHEMBL188528 agonist GuideToPharmacologyInteractions
ESR1 2099 BAZEDOXIFENE CHEMBL46740 agonist, antagonist TdgClinicalTrial, GuideToPharmacologyInteractions, DrugBank 15535430
ESR1 2099 HEXESTROL CHEMBL6615 antagonist GuideToPharmacologyInteractions
ESR1 2099 CHEMBL520107 CHEMBL520107 antagonist GuideToPharmacologyInteractions
ESR1 2099 ALLYLESTRENOL CHEMBL2105618 agonist DrugBank 17415709, 8820988, 17103262, 17203775, 17118173, 17341305
ESR1 2099 CHEMBL304552 CHEMBL304552 DrugBank 17139284, 17016423
ESR1 2099 OSPEMIFENE CHEMBL2105395 agonist, antagonist, modulator TdgClinicalTrial, ChemblInteractions, DrugBank, TTD 15255284, 16153821
ESR1 2099 CHEMBL180517 CHEMBL180517 DrugBank 10592235
ESR1 2099 CHEMBL222501 CHEMBL222501 DrugBank 10592235
ESR1 2099 CHEMBL223026 CHEMBL223026 DrugBank 10592235
ESR1 2099 TIBOLONE CHEMBL2103774 agonist DrugBank 19464167
ESR1 2099 ANASTROZOLE CHEMBL1399 ClearityFoundationBiomarkers, CGI, FDA
ESR1 2099 EXEMESTANE CHEMBL1200374 PharmGKB, CGI, FDA
ESR1 2099 SR16234 (CHEMBL3545210) CHEMBL3545210 antagonist TdgClinicalTrial, ChemblInteractions
ESR1 2099 IODINE CHEMBL1201225 TdgClinicalTrial
ESR1 2099 VINTAFOLIDE CHEMBL3039521 ClearityFoundationClinicalTrial
ESR1 2099 RALOXIFEN CHEMBL1079109 TdgClinicalTrial
ESR1 2099 ESTRONE SODIUM SULFATE CHEMBL2106240 PharmGKB
ESR1 2099 MITOTANE CHEMBL1670 binder TTD
ESR1 2099 GTx-758 CHEMBL3545017 agonist ChemblInteractions
ESR1 2099 CLOMIPHENE CITRATE CHEMBL3185958 modulator ChemblInteractions
ESR1 2099 DIETHYLSTILBESTROL DIPHOSPHATE CHEMBL1200598 agonist ChemblInteractions
ESR1 2099 DIARYLPROPIONITRILE CHEMBL334773 agonist GuideToPharmacologyInteractions
ESR1 2099 ETONOGESTREL CHEMBL1531 agonist TdgClinicalTrial, TEND, DrugBank 17139284, 17016423
ESR1 2099 PROGESTERONE CHEMBL103 agonist TdgClinicalTrial, TEND, DrugBank 17415709, 17118173, 17203775, 17341305, 17103262
ESR1 2099 TOREMIFENE CHEMBL1655 modulator TdgClinicalTrial, TEND, DrugBank, TTD 17503894, 17062721, 11752352, 12870885, 16503765, 16917142, 16595024, 18279543, 11747628, 15369444, 16515478
ESR1 2099 ESTRONE CHEMBL1405 agonist TdgClinicalTrial, GuideToPharmacologyInteractions, ChemblInteractions, TEND, DrugBank, TTD 2011412, 11752352, 12547192
ESR1 2099 FULVESTRANT CHEMBL1358 antagonist DrugBank, GuideToPharmacologyInteractions, TTD, CGI, CIViC, ChemblInteractions, FDA, OncoKB, TALC, PharmGKB, TEND, TdgClinicalTrial 20151846, 11752352, 12542403, 15865850, 15018596, 11922402, 11398912, 12080538, 12113237, 24185510, 27986707, 27269946
ESR1 2099 NORGESTIMATE CHEMBL1200934 agonist TdgClinicalTrial, TEND, DrugBank 14672731, 2175153, 14670645
ESR1 2099 TRILOSTANE CHEMBL1200907 allosteric modulator DrugBank 12209583, 16806905, 17109615
ESR1 2099 CHEMBL201013 CHEMBL201013 antagonist GuideToPharmacologyInteractions
ESR1 2099 MESTRANOL CHEMBL1201151 agonist TdgClinicalTrial, ChemblInteractions, TEND, DrugBank, TTD 20524981, 20497523, 11752352
ESR1 2099 CHF4227 CHEMBL3545355 modulator TdgClinicalTrial, ChemblInteractions, DrugBank
ESR1 2099 CHEMBL184151 CHEMBL184151 DrugBank 10592235
ESR1 2099 CHEMBL180071 CHEMBL180071 DrugBank 10592235
ESR1 2099 CHEMBL391910 CHEMBL391910 DrugBank 10592235
ESR1 2099 2-AMINO-1-METHYL-6- PHENYLIMIDAZO[4,5- B]PYRIDINE CHEMBL1213271 DrugBank 10592235
ESR1 2099 RALOXIFENE CORE CHEMBL431698 DrugBank 10592235
ESR1 2099 ESTROGENS, CONJUGATED SYNTHETIC A CHEMBL1201466 agonist, ligand ChemblInteractions, DrugBank
ESR1 2099 EVEROLIMUS CHEMBL1908360 CGI, FDA
ESR1 2099 PERTUZUMAB CHEMBL2007641 FDA
ESR1 2099 Ribociclib CHEMBL3545110 FDA
ESR1 2099 ESTRADIOL CHEMBL135 agonist TdgClinicalTrial, ChemblInteractions, TEND, TTD
ESR1 2099 ETHYNODIOL DIACETATE CHEMBL1200624 TdgClinicalTrial, TEND
ESR1 2099 MEGESTROL ACETATE CHEMBL1201139 TdgClinicalTrial, TEND
ESR1 2099 ESTROGEN CHEMBL592868 TdgClinicalTrial
ESR1 2099 LEFLUNOMIDE CHEMBL960 PharmGKB
ESR1 2099 CARBOQUONE CHEMBL443014 PharmGKB
ESR1 2099 FISPEMIFENE CHEMBL2107341 modulator TdgClinicalTrial, ChemblInteractions
ESR1 2099 GONADORELIN CHEMBL1007 CGI
ESR1 2099 LY2245461 CHEMBL3545389 modulator ChemblInteractions
ESR1 2099 ESTRADIOL CYPIONATE CHEMBL1200973 agonist ChemblInteractions
ESR1 2099 ESTROGENS, ESTERIFIED CHEMBL1201468 agonist ChemblInteractions
ESR1 2099 BAZEDOXIFENE ACETATE CHEMBL2106615 modulator ChemblInteractions
ESR1 2099 ESTRADIOL ACETATE (CHEMBL1200430) CHEMBL1200430 agonist ChemblInteractions
ESR1 2099 POLYESTRADIOL PHOSPHATE CHEMBL1201477 agonist ChemblInteractions
ESR1 2099 LAPATINIB CHEMBL554 FDA
ESR1 2099 TAMOXIFEN CHEMBL83 agonist, antagonist ClearityFoundationBiomarkers, TdgClinicalTrial, ClearityFoundationClinicalTrial, GuideToPharmacologyInteractions, CGI, CIViC, TEND, DrugBank, TTD, FDA 11752352, 11906441, 20512796, 2011412, 24185512, 24185510, 24398047
ESR1 2099 AFIMOXIFENE (CHEMBL489) CHEMBL489 agonist, antagonist TdgClinicalTrial, GuideToPharmacologyInteractions
ESR1 2099 CHLOROTRIANISENE CHEMBL1200761 agonist, binder TdgClinicalTrial, TEND, DrugBank, TTD 17236558, 11752352, 6872937, 2307235
ESR1 2099 ESTRAMUSTINE CHEMBL1575 agonist DrugBank 6364362, 3314674, 7703721, 3989343
ESR1 2099 ESTRIOL CHEMBL193482 agonist TdgClinicalTrial, GuideToPharmacologyInteractions, TEND, DrugBank, TTD 11752352, 2011412
ESR1 2099 PRINABEREL CHEMBL450940 agonist GuideToPharmacologyInteractions
ESR1 2099 CHEMBL282489 CHEMBL282489 agonist GuideToPharmacologyInteractions
ESR1 2099 LASOFOXIFENE CHEMBL328190 agonist, modulator TdgClinicalTrial, GuideToPharmacologyInteractions, DrugBank, TTD
ESR1 2099 DANAZOL CHEMBL1479 agonist, antagonist TdgClinicalTrial, TEND, DrugBank, TTD 11752352, 7540578, 2326286, 4039467
ESR1 2099 CHEMBL180300 CHEMBL180300 DrugBank 17139284, 17016423
ESR1 2099 ESTROPIPATE CHEMBL1200980 agonist ChemblInteractions, DrugBank 11752352, 17125913, 17138652, 2011412
ESR1 2099 QUINESTROL CHEMBL1201165 agonist, modulator TdgClinicalTrial, ChemblInteractions, TEND, DrugBank, TTD 11752352, 17139284, 17016423, 21075131
ESR1 2099 CUSTIRSEN CHEMBL2108309 DrugBank
ESR1 2099 CHEMBL181936 CHEMBL181936 DrugBank 10592235
ESR1 2099 CHEMBL1213270 CHEMBL1213270 DrugBank 10592235
ESR1 2099 ERTEBEREL CHEMBL278703 DrugBank 10592235
ESR1 2099 TRASTUZUMAB CHEMBL1201585 FDA
ESR1 2099 GDC-0810 CHEMBL3545390 antagonist OncoKB, ChemblInteractions, CGI 24185512, 27410477
ESR1 2099 ARZOXIFENE CHEMBL226267 TdgClinicalTrial
ESR1 2099 RAD1901 CHEMBL3545015 TdgClinicalTrial, ChemblInteractions
ESR1 2099 SIVIFENE CHEMBL307697 TdgClinicalTrial
ESR1 2099 TAMOXIFEN CITRATE CHEMBL786 modulator ChemblInteractions
ESR1 2099 LEVONORGESTREL CHEMBL1389 other TdgClinicalTrial, TEND, DrugBank 16307966, 17634204, 16325240, 16084894, 16609013
ESR1 2099 FLUOXYMESTERONE CHEMBL1445 antagonist DrugBank 7044524, 3058238, 8622076, 10637238, 16538529
ESR1 2099 RALOXIFENE CHEMBL81 agonist, antagonist, modulator TdgClinicalTrial, GuideToPharmacologyInteractions, TEND, TTD
ESR1 2099 CLOMIPHENE CHEMBL2355051 antagonist, modulator GuideToPharmacologyInteractions, TTD
ESR1 2099 GENISTEIN CHEMBL44 DrugBank 10592235
ESR1 2099 PRASTERONE CHEMBL90593 binder DrugBank 15994348
ESR1 2099 CHEMBL193676 CHEMBL193676 DrugBank 10592235
ESR1 2099 CHEMBL236718 CHEMBL236718 DrugBank 10592235
ESR1 2099 CHEMBL236086 CHEMBL236086 DrugBank 10592235
ESR1 2099 SYNTHETIC CONJUGATED ESTROGENS, B CHEMBL1201467 agonist, ligand ChemblInteractions, DrugBank
ESR1 2099 NORGESTREL CHEMBL2107797 TdgClinicalTrial, TEND
ESR1 2099 DIENOGEST CHEMBL1201864 TdgClinicalTrial
ESR1 2099 ENDOXIFEN CHEMBL1093458 ClearityFoundationClinicalTrial
ESR1 2099 MK-6913 CHEMBL3545274 agonist TdgClinicalTrial, ChemblInteractions
ESR1 2099 NORELGESTROMIN CHEMBL1200807 TdgClinicalTrial
ESR1 2099 ABEMACICLIB CHEMBL3301610 CGI
ESR1 2099 IDOXIFENE CHEMBL6318 modulator ChemblInteractions
ESR1 2099 AFIMOXIFENE (CHEMBL10041) CHEMBL10041 modulator ChemblInteractions
ESR1 2099 DROLOXIFENE CHEMBL487 modulator ChemblInteractions
ESR1 2099 ACOLBIFENE CHEMBL68055 modulator ChemblInteractions
ESR1 2099 ESTRADIOL VALERATE CHEMBL1511 agonist ChemblInteractions
ESR1 2099 TOREMIFENE CITRATE CHEMBL1200675 modulator ChemblInteractions
ESR1 2099 LETROZOLE CHEMBL1444 ClearityFoundationBiomarkers, CGI, CIViC, FDA 25524798
ESR1 2099 MELATONIN CHEMBL45 antagonist DrugBank 19796047, 15229223
ESR1 2099 PALBOCICLIB CHEMBL189963 CGI, CIViC, FDA 25524798

Variant-drug associations (data source: PharmGKB)
Gene Name Variant Alleles Chemical Phenotype Category Significance Notes Sentence Publications Annotation ID
ESR1 rs4986936 G morphine "dosage","efficacy" no Haplotype of the three ESR1 variants studied in the paper was also not significantly associated with morphine dose requirements. A stepwise backward linear regression model of age, rs9340799, rs1799971, rs4986936, rs1319339, rs174696, rs677830, rs4680, rs4818, and rs540825 was found to explain 10.7% of variance in morphine dose requirements in the study cohort (p=0.001) Allele G is not associated with dose of morphine in people with Pain, Postoperative as compared to allele A. 26902643 1449295981
ESR1 rs9340799 AA leflunomide efficacy yes rs9340799 and rs2234693 were in linkage disequilibrium: haplotype A-T was associated with better response and haplotype G-C with worse response. Genotype AA is associated with increased response to leflunomide in women with Arthritis, Rheumatoid as compared to genotypes AG + GG. 21174621 827783461
ESR1 rs9340799 G atorvastatin efficacy no Genotypes of this polymorphism (described as ESR1 XbaI) were not associated with change in total cholesterol, LDLC, HDLC, or triglyceride levels after treatment. A haplotype described as PvuII(-)XbaI(+) was significantly associated with greater increases of HDL cholesterol which remained significant only in women, however it was not clear which alleles in the two SNPs this haplotype referred to (rs2234693 and rs9340799). Allele G is not associated with response to atorvastatin in people with Hypercholesterolemia as compared to allele A. 15694942 982045293
ESR1 rs11543791 CC raloxifene efficacy yes This association was reported for rs2234693, which has been merged into rs11543791. Efficacy measured in group x time x genotype interaction, using general PANSS score. Genotype CC is associated with decreased response to raloxifene in women Menopause and Schizophrenia as compared to genotypes CT + TT. 27546373 1448259284
ESR1 rs9340799 A raloxifene efficacy no Efficacy measured in group x time x genotype interaction, using general, positive, negative, and total PANSS score at baseline, 1, 3, and 6 months post-treatment. Allele A is not associated with response to raloxifene in women Menopause and Schizophrenia as compared to allele G. 27546373 1448259292
ESR1 rs1801132 C raloxifene efficacy no Efficacy measured in group x time x genotype interaction, using general, positive, negative, and total PANSS score at baseline, 1, 3, and 6 months post-treatment. Allele C is not associated with response to raloxifene in women Menopause and Schizophrenia as compared to allele G. 27546373 1448259299
ESR1 rs2077647 T glibenclamide efficacy yes No allele was given for the association, so the minor allele from dbSNP at this location was used. Response to treatment was measured as reduction of HbA1c below 6.5% at 1-year of treatment. Allele T is associated with increased response to glibenclamide in people with as compared to allele C. 27403931 1448123605
ESR1 rs2234693 TT leflunomide efficacy yes rs9340799 and rs2234693 were in linkage disequilibrium: haplotype A-T was associated with better response and haplotype G-C with worse response. Genotype TT is associated with increased response to leflunomide in women with Arthritis, Rheumatoid as compared to genotype CC. 21174621 827783469
ESR1 rs2234693 C atorvastatin efficacy no Genotypes of this polymorphism (described as ESR1 PvuII) were not associated with change in total cholesterol, LDLC, HDLC, or triglyceride levels after treatment. A haplotype described as PvuII(-)XbaI(+) was significantly associated with greater increases of HDL cholesterol which remained significant only in women, however it was not clear which alleles in the two SNPs this haplotype referred to (rs2234693 and rs9340799). Allele C is not associated with response to atorvastatin in people with Hypercholesterolemia as compared to allele T. 15694942 982045270
ESR1 rs2234693 C morphine "dosage","efficacy" no Haplotype of the three ESR1 variants studied in the paper was also not significantly associated with morphine dose requirements. Allele C is not associated with dose of morphine in people with Pain, Postoperative as compared to allele T. 26902643 1449295987
ESR1 rs9340799 G morphine "dosage","efficacy" no Haplotype of the three ESR1 variants studied in the paper was also not significantly associated with morphine dose requirements. A stepwise backward linear regression model of age, rs9340799, rs1799971, rs4986936, rs1319339, rs174696, rs677830, rs4680, rs4818, and rs540825 was found to explain 10.7% of variance in morphine dose requirements in the study cohort (p=0.001) Allele G is not associated with dose of morphine in people with Pain, Postoperative as compared to allele A. 26902643 1449295993