DGIdb - ESR1 Gene Record

ESR1 2099 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

2099
ESTROGEN RECEPTOR 1
ESR1
ER
ESR
ESRA
ESTRR
Era
NR3A1
133430
3467
ENSG00000091831
OTTHUMG00000016103
ESTROGEN RECEPTOR (ER) (ESTRADIOL RECEPTOR) (ER-ALPHA). [SOURCE:UNIPROT/SWISSPROT;ACC:P03372]
P03372
ESR1_HUMAN
21
Nuclear receptor subfamily 3 group A member 1
Estradiol receptor
ER-alpha
Estrogen receptor
PA156
T89534

Gene Info:

Human Readable Name	NUCLEAR HORMONE RECEPTOR
Human Readable Name	DRUGGABLE GENOME
Target Main Class	Receptors
Target Subclass	Nuclear receptor
Initial Gene Query	NR3A1
Counted Citations from 1950-2000	29833
Target Class	Receptors
Uniprot Evidence	1: Evidence at protein level
Interpro Short Name	Nucl_hrmn_rcpt_lig-bd_core
Interpro Type	Domain
Interpro Name	Nuclear hormone receptor, ligand-binding, core
Interpro Acc	IPR000536
Uniprot Status	Swiss-Prot
Gene Biotype	PROTEIN_CODING

(22 More Sources)

Gene Categories: Category Details

TRANSCRIPTION FACTOR COMPLEX
KINASE
DRUG RESISTANCE
NUCLEAR HORMONE RECEPTOR
DRUGGABLE GENOME
CLINICALLY ACTIONABLE
TRANSCRIPTION FACTOR

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Dulos et al., 2010, Suppression of the inflammatory response in experimental arthritis is mediated via estrogen receptor alpha but not estrogen receptor beta., Arthritis Res. Ther.
Cleuren et al., 2010, 17α-Ethinylestradiol rapidly alters transcript levels of murine coagulation genes via estrogen receptor α., J. Thromb. Haemost.
Fujii S et al., 2013, Increased hydrophobicity and estrogenic activity of simple phenols with silicon and germanium-containing substituents., J Med Chem
Oesterreich S et al., 2015, Associations between genetic variants and the effect of letrozole and exemestane on bone mass and bone turnover., Breast Cancer Res Treat
Dang Z, 2010, Comparison of relative binding affinities to fish and mammalian estrogen receptors: the regulatory implications., Toxicol Lett
Finn et al., 2015, The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study., Lancet Oncol.
Rivera-Guevara C et al., 2010, Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-alpha., Bioorg Med Chem
Lin HR et al., 2007, Identification of a series of tetrahydroisoquinoline derivatives as potential therapeutic agents for breast cancer., Bioorg Med Chem Lett
Agouridas V et al., 2009, Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells., J Med Chem
Lai A et al., 2015, Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts., J Med Chem
Calogeropoulou T et al., 2009, Novel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activity., J Med Chem
De Savi C et al., 2015, Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist., J Med Chem
Jacquot Y et al., 2007, Synthesis, structure, and estrogenic activity of 4-amino-3-(2-methylbenzyl)coumarins on human breast carcinoma cells., Bioorg Med Chem
Toy et al., 2013, ESR1 ligand-binding domain mutations in hormone-resistant breast cancer., Nat. Genet.
Robinson et al., 2013, Activating ESR1 mutations in hormone-resistant metastatic breast cancer., Nat. Genet.
Bundred et al., 2002, Fulvestrant (Faslodex): current status in the therapy of breast cancer., Expert Rev Anticancer Ther
Dow, 2002, Existing and emerging endocrine therapies for breast cancer., Cancer Nurs
Curran et al., 2001, Fulvestrant., Drugs
Elkak et al., 2001, Pure antiestrogens and breast cancer., Curr Med Res Opin
McKeage et al., 2004, Fulvestrant: a review of its use in hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy., Drugs
Jones et al., 2005, Effectiveness and tolerability of fulvestrant in postmenopausal women with hormone receptor-positive breast cancer., Clin. Breast Cancer
Morris et al., 2002, Fulvestrant ('Faslodex')--a new treatment option for patients progressing on prior endocrine therapy., Endocr. Relat. Cancer
Kabos et al., 2010, Fulvestrant: a unique antiendocrine agent for estrogen-sensitive breast cancer., Expert Opin Pharmacother
Jeselsohn et al., 2014, Emergence of constitutively active estrogen receptor-α mutations in pretreated advanced estrogen receptor-positive breast cancer., Clin. Cancer Res.
Ogawa T et al., 2006, m-Carborane bisphenol structure as a pharmacophore for selective estrogen receptor modulators., Bioorg Med Chem Lett
Jain D et al., 2010, A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements., Bioorg Med Chem Lett
Sasson, 1991, Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor., Pathol. Biol.
Cyrus et al., 2010, Jostling for position: optimizing linker location in the design of estrogen receptor-targeting PROTACs., ChemMedChem
Fabian et al., Chemoprevention for high-risk women: tamoxifen and beyond., Breast J
Ntukidem NI et al., 2008, Estrogen receptor genotypes, menopausal status, and the lipid effects of tamoxifen., Clin Pharmacol Ther
Maximov PY et al., 2010, Structure-function relationships of estrogenic triphenylethylenes related to endoxifen and 4-hydroxytamoxifen., J Med Chem
Maximov PY et al., 2014, Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells., J Med Chem
Reed et al., 2005, Dose-dependent effects of 4-hydroxytamoxifen, the active metabolite of tamoxifen, on estrogen receptor-alpha expression in the rat uterus., Anticancer Drugs
Matsumoto, 2006, [Selective estrogen receptor modulators (SERMs)]., Clin Calcium
Moen et al., 2008, Raloxifene: a review of its use in the prevention of invasive breast cancer., Drugs
Bryant et al., An estrogen receptor basis for raloxifene action in bone., J. Steroid Biochem. Mol. Biol.
Khovidhunkit et al., 1999, Clinical effects of raloxifene hydrochloride in women., Ann. Intern. Med.
Scott et al., 1999, Raloxifene: a selective estrogen receptor modulator., Am Fam Physician
Schafer et al., 1999, The interaction of raloxifene and the active metabolite of the antiestrogen EM-800 (SC 5705) with the human estrogen receptor., Cancer Res.
Figtree et al., 1999, Raloxifene acutely relaxes rabbit coronary arteries in vitro by an estrogen receptor-dependent and nitric oxide-dependent mechanism., Circulation
Cummings et al., 1999, The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation., JAMA
Labad J et al., 2016, Pharmacogenetic study of the effects of raloxifene on negative symptoms of postmenopausal women with schizophrenia: A double-blind, randomized, placebo-controlled trial., Eur Neuropsychopharmacol
Margeat et al., 2003, Ligands differentially modulate the protein interactions of the human estrogen receptors alpha and beta., J. Mol. Biol.
Grove et al., 1987, Estrogen stimulation of phosphatidylinositol metabolism in mouse uterine tissue., Endocrinology
Juriansz et al., 1988, Interactions of putative estrogens with the intracellular receptor complex in mouse Leydig cells: relationship to preneoplastic hyperplasia., Cancer Res.
Chae et al., 1998, Estrogen-dependent gene regulation by an oxidative metabolite of diethylstilbestrol, diethylstilbestrol-4',4"-quinone., Steroids
Kuiper et al., 1997, Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta., Endocrinology
Bovee et al., 2004, Rapid yeast estrogen bioassays stably expressing human estrogen receptors alpha and beta, and green fluorescent protein: a comparison of different compounds with both receptor types., J. Steroid Biochem. Mol. Biol.
Maru et al., 2009, Potential use of an estrogen-glucocorticoid receptor chimera as a drug screen for tissue selective estrogenic activity., Bone
Wurz et al., 2005, Ospemifene inhibits the growth of dimethylbenzanthracene-induced mammary tumors in Sencar mice., J. Steroid Biochem. Mol. Biol.
Komi et al., 2004, Effects of ospemifene, a novel SERM, on biochemical markers of bone turnover in healthy postmenopausal women., Gynecol. Endocrinol.
Lehnes et al., 2007, The effect of estradiol on in vivo tumorigenesis is modulated by the human epidermal growth factor receptor 2/phosphatidylinositol 3-kinase/Akt1 pathway., Endocrinology
Brama et al., 2007, Cadmium induces mitogenic signaling in breast cancer cell by an ERalpha-dependent mechanism., Mol. Cell. Endocrinol.
Chang FR et al., 2005, The transgenic Arabidopsis plant system, pER8-GFP, as a powerful tool in searching for natural product estrogen-agonists/antagonists., J Nat Prod
Bologa et al., 2006, Virtual and biomolecular screening converge on a selective agonist for GPR30., Nat. Chem. Biol.
Renner S et al., 2009, Bioactivity-guided mapping and navigation of chemical space., Nat Chem Biol
Banerjee M et al., 2013, Modulation of xenobiotic receptors by steroids., Molecules
Paterni I et al., 2014, Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential., Steroids
Ariazi et al., 2006, Estrogen receptors as therapeutic targets in breast cancer., Curr Top Med Chem
Jones et al., 2004, A review of adjuvant hormonal therapy in breast cancer., Endocr. Relat. Cancer
Locci et al., 2001, Synthesis and secretion of transforming growth factor-beta1 by human desmoid fibroblast cell line and its modulation by toremifene., J. Interferon Cytokine Res.
Shelly et al., 2008, Selective estrogen receptor modulators: an update on recent clinical findings., Obstet Gynecol Surv
Goldstein, 2006, Controversies in adjuvant endocrine treatment of premenopausal women., Clin. Breast Cancer
Lewis-Wambi et al., Treatment of Postmenopausal Breast Cancer with Selective Estrogen Receptor Modulators (SERMs)., Breast Dis
Taneja et al., 2006, Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy., Expert Opin Investig Drugs
Liu et al., 2003, Antiestrogenic and DNA damaging effects induced by tamoxifen and toremifene metabolites., Chem. Res. Toxicol.
Smith, 2006, Treatment-related osteoporosis in men with prostate cancer., Clin. Cancer Res.
Gennari et al., 2007, Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development., Drugs Aging
Kwok et al., 2010, Measuring binding kinetics of ligands with tethered receptors by fluorescence polarization and total internal reflection fluorescence., Anal. Chem.
Hart et al., 2007, Estrogen mobilizes a subset of estrogen receptor-alpha-immunoreactive vesicles in inhibitory presynaptic boutons in hippocampal CA1., J. Neurosci.
Muñoz et al., Association with litter size of new polymorphisms on ESR1 and ESR2 genes in a Chinese-European pig line., Genet. Sel. Evol.
Baron et al., 2007, Estrogen receptor alpha and the activating protein-1 complex cooperate during insulin-like growth factor-I-induced transcriptional activation of the pS2/TFF1 gene., J. Biol. Chem.
Dixon et al., 2007, Renoprotective effects of a selective estrogen receptor modulator, raloxifene, in an animal model of diabetic nephropathy., Am. J. Nephrol.
Bains et al., 2007, Neuroprotection by estrogen against MPP+-induced dopamine neuron death is mediated by ERalpha in primary cultures of mouse mesencephalon., Exp. Neurol.
Hodnik Ž et al., 2015, Diethylstilbestrol-scaffold-based pregnane X receptor modulators., Eur J Med Chem
Kupfer et al., 1990, Inactivation of the uterine estrogen receptor binding of estradiol during P-450 catalyzed metabolism of chlorotrianisene (TACE). Speculation that TACE antiestrogenic activity involves covalent binding to the estrogen receptor., FEBS Lett.
Jordan et al., 1983, Inhibition of the uterotropic activity of estrogens and antiestrogens by the short acting antiestrogen LY117018., Endocrinology
Wang et al., 2006, [Clinical characteristics and potential prognostic factors of breast cancer patients with liver metastases]., Zhonghua Zhong Liu Za Zhi
Shyu et al., 2011, Computational estimation of rainbow trout estrogen receptor binding affinities for environmental estrogens., Toxicol. Appl. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Jung J et al., 2004, Anti-estrogenic activity of fifty chemicals evaluated by in vitro assays., Life Sci
Poutiainen PK et al., 2010, Synthesis and biological evaluation of phenolic 4,5-dihydroisoxazoles and 3-hydroxy ketones as estrogen receptor alpha and beta agonists., Bioorg Med Chem
Kumar et al., 2007, Type and duration of exogenous hormone use affects breast cancer histology., Ann. Surg. Oncol.
Montero Girard et al., 2007, Association of estrogen receptor-alpha and progesterone receptor A expression with hormonal mammary carcinogenesis: role of the host microenvironment., Breast Cancer Res.
Yuri et al., Effects of different durations of estrogen and progesterone treatment on development of N-methyl-N-nitrosourea-induced mammary carcinomas in female Lewis rats., In Vivo
Lessey et al., 2006, Estrogen receptor-alpha (ER-alpha) and defects in uterine receptivity in women., Reprod. Biol. Endocrinol.
Ghebeh et al., 2007, Expression of B7-H1 in breast cancer patients is strongly associated with high proliferative Ki-67-expressing tumor cells., Int. J. Cancer
Jayaraman A et al., 2009, Progesterone attenuates oestrogen neuroprotection via downregulation of oestrogen receptor expression in cultured neurones., J Neuroendocrinol
Mohammed H et al., 2015, Progesterone receptor modulates ERα action in breast cancer., Nature
Tessier C et al., 2000, Estrogen receptors alpha and beta in rat decidua cells: cell-specific expression and differential regulation by steroid hormones and prolactin., Endocrinology
Ravdin PM et al., 1987, Estrogenic effects of phenolphthalein on human breast cancer cells in vitro., Breast Cancer Res Treat
Vijayanathan et al., 2006, Physiologic levels of 2-methoxyestradiol interfere with nongenomic signaling of 17beta-estradiol in human breast cancer cells., Clin. Cancer Res.
Mirkin et al., 2005, Effect of 17 beta-estradiol, progesterone, synthetic progestins, tibolone, and tibolone metabolites on vascular endothelial growth factor mRNA in breast cancer cells., Fertil. Steril.
Vereide et al., 2006, Effect of levonorgestrel IUD and oral medroxyprogesterone acetate on glandular and stromal progesterone receptors (PRA and PRB), and estrogen receptors (ER-alpha and ER-beta) in human endometrial hyperplasia., Gynecol. Oncol.
Sun et al., 2007, Contribution of epoxyeicosatrienoic acids to flow-induced dilation in arteries of male ERalpha knockout mice: role of aromatase., Am. J. Physiol. Regul. Integr. Comp. Physiol.
Abdel-Aleem et al., 2005, Tamoxifen treatment of bleeding irregularities associated with Norplant use., Contraception
Lv XH et al., 2011, Effects of levonorgestrel on reproductive hormone levels and their receptor expression in Mongolian gerbils (Meriones unguiculatus)., Exp Anim
Lemus AE et al., 1992, Mechanism of action of levonorgestrel: in vitro metabolism and specific interactions with steroid receptors in target organs., J Steroid Biochem Mol Biol
García-Becerra R et al., 2002, The intrinsic transcriptional estrogenic activity of a non-phenolic derivative of levonorgestrel is mediated via the estrogen receptor-alpha., J Steroid Biochem Mol Biol
Micevych et al., 2007, Estradiol stimulates progesterone synthesis in hypothalamic astrocyte cultures., Endocrinology
Bennink, Reprint of Are all estrogens the same?, Maturitas
Garcia-Segura et al., 2006, Cross-talk between IGF-I and estradiol in the brain: focus on neuroprotection., Neuroendocrinology
Notch et al., 2009, 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells., Aquat. Toxicol.
Mukai et al., 2006, Local neurosteroid production in the hippocampus: influence on synaptic plasticity of memory., Neuroendocrinology
Kojima H et al., 2003, Effects of a diphenyl ether-type herbicide, chlornitrofen, and its amino derivative on androgen and estrogen receptor activities., Environ Health Perspect
Gruber et al., 2004, Bazedoxifene (Wyeth)., Curr Opin Investig Drugs
Shen J et al., 2012, Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening., Eur J Med Chem
Sanfilippo et al., 1985, Evaluation of danazol influence upon the uterus using scanning electron microscopic morphometric and biochemical analyses., Surg Gynecol Obstet
Snyder et al., 1990, Danazol suppression of luteinizing hormone in the rat: evidence for mediation by both androgen and estrogen receptors., Proc. Soc. Exp. Biol. Med.
Fujimoto et al., 1995, Danazol decreases transcription of estrogen receptor gene in human monocytes., Gen. Pharmacol.
Vajdos FF et al., 2007, The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene., Protein Sci
Kieser KJ et al., 2010, Characterization of the pharmacophore properties of novel selective estrogen receptor downregulators (SERDs)., J Med Chem
Hughes et al., 2010, Clomiphene citrate for unexplained subfertility in women., Cochrane Database Syst Rev
Homburg, 2008, Oral agents for ovulation induction--clomiphene citrate versus aromatase inhibitors., Hum Fertil (Camb)
Homburg, 2005, Clomiphene citrate--end of an era? A mini-review., Hum. Reprod.
2006, Use of clomiphene citrate in women., Fertil. Steril.
Kurosawa et al., 2010, Clomiphene citrate elicits estrogen agonistic/antagonistic effects differentially via estrogen receptors alpha and beta., Endocr. J.
Overbeek et al., 2009, Pharmacogenomics of ovulation induction: facilitating decisions on who, when and how to treat., Pharmacogenomics
Brown et al., 2009, Clomiphene and anti-oestrogens for ovulation induction in PCOS., Cochrane Database Syst Rev
Pasqualini, 2003, Differential effects of progestins on breast tissue enzymes., Maturitas
Juchem et al., 1990, Binding of oral contraceptive progestogens to serum proteins and cytoplasmic receptor., Am. J. Obstet. Gynecol.
Shields-Botella et al., 2003, An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone-dependent cancer cells., J. Steroid Biochem. Mol. Biol.
Paris F et al., 2015, Molecular action of norgestimate: new developments., Gynecol Endocrinol
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Kishi T et al., 2009, A functional polymorphism in estrogen receptor alpha gene is associated with Japanese methamphetamine induced psychosis., Prog Neuropsychopharmacol Biol Psychiatry
Fuhrmann et al., 1995, Characterization of the novel progestin gestodene by receptor binding studies and transactivation assays., Contraception
Rabe et al., 2000, Induction of estrogen receptor-alpha and -beta activities by synthetic progestins., Gynecol. Endocrinol.
Deng HW et al., 1998, Change of bone mass in postmenopausal Caucasian women with and without hormone replacement therapy is associated with vitamin D receptor and estrogen receptor genotypes., Hum Genet
Romerius P et al., 2011, Estrogen receptor α single nucleotide polymorphism modifies the risk of azoospermia in childhood cancer survivors., Pharmacogenet Genomics
Huang R et al., 2014, Profiling of the Tox21 10K compound library for agonists and antagonists of the estrogen receptor alpha signaling pathway., Sci Rep
Scippo ML et al., 2004, Recombinant human estrogen, androgen and progesterone receptors for detection of potential endocrine disruptors., Anal Bioanal Chem
Dziedziejko V et al., 2011, The effect of ESR1 and ESR2 gene polymorphisms on the outcome of rheumatoid arthritis treatment with leflunomide., Pharmacogenomics
Spannhoff A et al., 2007, Target-based approach to inhibitors of histone arginine methyltransferases., J Med Chem
Zhou J et al., 2000, Testosterone inhibits estrogen-induced mammary epithelial proliferation and suppresses estrogen receptor expression., FASEB J
Lappano R et al., 2009, Structure-activity relationships of resveratrol and derivatives in breast cancer cells., Mol Nutr Food Res

ENDOXIFEN ESR1

Interaction Score: 1.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24805199

Sources:
DTC ClearityFoundationClinicalTrial TTD
CLOMIPHENE ESR1

Interaction Score: 1.27

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name Androxal

Novel drug target Established target

PMIDs:
20091498 18320435 15878925 17055820 20379036 19761360 2011412 11752352 19821295

Sources:
TdgClinicalTrial TEND TTD
LEVONORGESTREL ESR1

Interaction Score: 1.06

Interaction Types & Directionality:

other/unknown

Interaction Info:

Trial Name ethinyl estradiol + levonorgestrel,Seasonale, Lo Seasonale, Seasonique

Novel drug target Established target

Trial Name AG-200-15

PMIDs:
16609013 16084894 16325240 17634204 16307966 21791876 1562565 12589940

Sources:
TdgClinicalTrial TEND
LASOFOXIFENE ESR1

Interaction Score: 0.96

Interaction Types & Directionality:

negative modulator (inhibitory)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name lasofoxifene,Fablyn, Oporia

Novel drug target Established target

PMIDs:
17456742

Sources:
TdgClinicalTrial TTD
ESTRIOL ESR1

Interaction Score: 0.8

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2011412 11752352

Sources:
TdgClinicalTrial TEND TTD
TOREMIFENE ESR1

Interaction Score: 0.73

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name Acapodene

Novel drug target Established target

Trial Name atamestane-plus-toremifene

PMIDs:
16515478 15369444 11747628 18279543 16595024 16917142 16503765 12870885 11752352 17062721 17503894

Sources:
TdgClinicalTrial TEND PharmGKB TTD FDA
FULVESTRANT ESR1

Interaction Score: 0.69

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fulvestrant,Faslodex

Mechanism of Interaction Estrogen receptor antagonist

PMIDs:
20621492 17337183 19133777 25879485 19845386 26407012 17275315 24185512 24185510 12113237 12080538 11398912 11922402 15018596 15865850 12542403 11752352 20151846

Sources:
TALC DTC TdgClinicalTrial ChemblInteractions TEND CIViC PharmGKB TTD FDA OncoKB
CHEMBL2313445 ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23214428

Sources:
DTC
4-TRIETHYLGERMYLPHENOL ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23214428

Sources:
DTC
GLYCITEIN ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16038533

Sources:
DTC
ESTROPIPATE ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
2011412 17138652 17125913 11752352

Sources:
ChemblInteractions TTD
BRILANESTRANT ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor alpha antagonist

PMIDs:
None found

Sources:
ChemblInteractions TTD
RAD1901 ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name RAD1901

Novel drug target Established target

Mechanism of Interaction Estrogen receptor alpha degrader

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
AZD-9496 ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD OncoKB
NORGESTIMATE ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14670645 2175153 14672731 25970022

Sources:
TdgClinicalTrial TEND
CHEMBL195515 ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20334372

Sources:
DTC
CHEMBL2071180 ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22647217

Sources:
DTC
1-HYDROXY-6-(4-HYDROXY-PHENYL)-1-PHENYL-HEXAN-3-ONE (ENANTIOMERIC MIX) ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20430632

Sources:
DTC
CHEMBL2313444 ESR1

Interaction Score: 0.64

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23214428

Sources:
DTC
DIENESTROL ESR1

Interaction Score: 0.55

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

Novel drug target Established target

PMIDs:
3622377 3334987 9558716 11752352 9048584 15276617 18976723

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND TTD
QUINESTROL ESR1

Interaction Score: 0.51

Interaction Types & Directionality:

agonist (activating)

modulator

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
21075131 17016423 17139284 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
CHLOROTRIANISENE ESR1

Interaction Score: 0.51

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2307235 6872937 11752352 17236558

Sources:
DTC TdgClinicalTrial TEND TTD
DESOGESTREL ESR1

Interaction Score: 0.4

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
7750284 2175153 10836199

Sources:
TdgClinicalTrial TEND
OSPEMIFENE ESR1

Interaction Score: 0.4

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

Novel drug target Established target

PMIDs:
16153821 15255284

Sources:
TdgClinicalTrial ChemblInteractions TTD
SULFENTRAZONE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1222035 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20659801

Sources:
DTC
POLYESTRADIOL PHOSPHATE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEGESTROL ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
IODINE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name molecular iodine,IoGen

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
BORIC ACID ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ETHYLENEDIAMINE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALFADEX ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROMESTRIENE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PUERARIN ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16038533

Sources:
DTC
4-METHYLBENZOIC ACID METHYL ESTER ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL354663 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL384441 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ESTETROL ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ELACESTRANT ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
N-PROPYL BROMIDE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DIETHYLSTILBESTROL DIPHOSPHATE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CLOMIPHENE CITRATE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FISPEMIFENE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name fispemifene, HM-101

Novel drug target Established target

Mechanism of Interaction Estrogen receptor modulator

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
ARZOXIFENE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name Arzoxifene, LY353381

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
ETONOGESTREL ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name etonogestrel implant,Implanon

Novel drug target Established target

Trial Name etonogestrel/ethinyl estradiol vaginal ring,Nuvaring

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
ICARITIN ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
METHYLISOTHIOCYANATE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHF4227 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CHEMBL1432305 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SR16234 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha antagonist

Direct Interaction yes

Trial Name TAS-108

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
ESTROGEN ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name conjugated estrogens/medroxyprogesterone acetate,Prempro, Premphase

Novel drug target Established target

Trial Name oral contraceptive,Pill-Plus

PMIDs:
None found

Sources:
TdgClinicalTrial TTD
MONOETHANOLAMINE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ACRYLAMIDE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MK-6913 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

Trial Name MK-6913

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
ESTRADIOL ACETATE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PALMITIC ACID ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ESTRONE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

Trial Name -

PMIDs:
12547192 11752352 2011412

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND TTD
ACOLBIFENE ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
CENESTIN ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

ligand

Interaction Info:

PMIDs:
None found

Sources:
TTD
GTX-758 ESR1

Interaction Score: 0.32

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
ETHINYL ESTRADIOL ESR1

Interaction Score: 0.26

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
17125913 17095591 17138652 19434891 17124377 19237207 11752352 17142999

Sources:
ChemblInteractions
MESTRANOL ESR1

Interaction Score: 0.25

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor alpha agonist

Trial Name -

PMIDs:
11752352 20497523 20524981

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD
BAZEDOXIFENE ESR1

Interaction Score: 0.24

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name bazedoxifene, bazedoxifene/conjugated estrogens, TSE-424,Viviant, Aprela, Conbriza

Novel drug target Established target

PMIDs:
15535430

Sources:
TdgClinicalTrial TTD
CHEMBL221047 ESR1

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17432842

Sources:
DTC
ESTRADIOL ESR1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor alpha agonist

Trial Name transdermal estradiol,Divigel

PMIDs:
2011412 17138652 17125913 11752352 20659801 20334368 16038533 16520733 19561619 25879485 24805199 23884115 24971815

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND TTD
RALOXIFENE ESR1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
16951478 18778124 10418979 10068418 10507743 10485477 11752352 10477535 10376571 27546373 20659801

Sources:
DTC TdgClinicalTrial TEND PharmGKB TTD FDA
HYDROXYPROGESTERONE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GESTRINONE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
TTD
LY2245461 ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ARSANILIC ACID ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CAMPHOR ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL503990 ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DIENOGEST ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name estradiol valerate + dienogest,Natazia, Qlaira

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
BENZODODECINIUM CHLORIDE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SYNTHETIC CONJUGATED ESTROGENS, B ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
METHIOCARB ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALFATRADIOL ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ESTROGENS, ESTERIFIED ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
ESTROGENS, CONJUGATED ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RALOXIFEN ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Evista

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
TRIADIMEFON ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DANAZOL ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
4039467 2326286 7540578 11752352

Sources:
DTC TdgClinicalTrial TEND TTD
ESTRADIOL CYPIONATE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DIETHYLSTILBESTROL DIPROPIONATE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
SIVIFENE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name A-007

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ESTROGENS, CONJUGATED SYNTHETIC A ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
VINTAFOLIDE ESR1

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
AFIMOXIFENE ESR1

Interaction Score: 0.15

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
20334368 24805199 15846122

Sources:
DTC ChemblInteractions TTD
DIETHYLSTILBESTROL ESR1

Interaction Score: 0.14

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
20387803 17314305 17306201 17317669 11752352 17308373 17320868 26408814

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND TTD
LETROZOLE ESR1

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26536870 25524798

Sources:
ClearityFoundationBiomarkers CIViC PharmGKB FDA
METHYLTESTOSTERONE ESR1

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25012808

Sources:
DTC
TAMOXIFEN ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
24185510 24398047 24185512 16735120 20659801 20621492 2011412 20512796 11906441 11752352 17713466

Sources:
DTC ClearityFoundationBiomarkers TdgClinicalTrial ClearityFoundationClinicalTrial TEND CIViC PharmGKB TTD FDA
ESTRADIOL VALERATE ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor alpha agonist

PMIDs:
None found

Sources:
ChemblInteractions
ALACHLOR ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CUMENE HYDROPEROXIDE ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BAZEDOXIFENE ACETATE ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ERIBULIN ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
TRIS(2,3-DIBROMOPROPYL)PHOSPHATE ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
NORGESTREL ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
CYCLOFENIL ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PHENYLALANINE ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
STANOLONE ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12676605

Sources:
DTC
CHEMBL259327 ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GOSERELIN ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
NORELGESTROMIN ESR1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name norelgestromin/ethinyl estradiol,Ortho Evra

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ZERANOL ESR1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19913605

Sources:
DTC
HYDRAMETHYLNON ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1579130 ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MITOTANE ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14579009

Sources:
TTD
ALOE-EMODIN ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1523215 ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BISPHENOL A ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PERTUZUMAB ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
ORTHOTOLIDINE ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PHENOLPHTHALEIN ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
3620717

Sources:
DTC
IDOXIFENE ESR1

Interaction Score: 0.08

Interaction Types & Directionality:

modulator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor modulator

PMIDs:
None found

Sources:
ChemblInteractions
ANASTROZOLE ESR1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationBiomarkers PharmGKB FDA
EXEMESTANE ESR1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26536870

Sources:
PharmGKB FDA
GUGGULSTERONE ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ACETOCHLOR ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ENDOSULFAN ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CETRIMONIUM BROMIDE ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TESTOSTERONE PROPIONATE ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROPYLPARABEN ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
4-NONYLPHENOL ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIPHENYLSTANNANOL ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
NERATINIB ESR1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
DOXYCYCLINE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24185512

Sources:
PharmGKB
LEFLUNOMIDE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21174621

Sources:
PharmGKB
DROLOXIFENE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROGESTERONE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

negative modulator (inhibitory)

agonist (activating)

inhibitor (inhibitory)

Interaction Info:

Trial Name conjugated estrogens/medroxyprogesterone acetate,Prempro, Premphase

Novel drug target Established target

Trial Name BHR-100

PMIDs:
17103262 17341305 17203775 17118173 17415709 19094096 26153859 11014241

Sources:
TdgClinicalTrial TEND
RETINAL ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOMIPHEN BROMIDE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MEDROXYPROGESTERONE ACETATE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9860300

Sources:
PharmGKB
OXYTETRACYCLINE HYDROCHLORIDE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOREMIFENE CITRATE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

modulator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor modulator

PMIDs:
None found

Sources:
ChemblInteractions
PROPACHLOR ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ABEMACICLIB ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
PROTOAPIGENONE ESR1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16038533

Sources:
DTC
RIBOCICLIB ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
METHOXSALEN ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TESTOSTERONE ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
16038533 12676605 10973921

Sources:
DTC
CHEMBL85826 ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
3R14S-OCHRATOXIN A ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
OXYMETHOLONE ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
COUMESTROL ESR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TAMOXIFEN CITRATE ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha modulator

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
DAIDZEIN ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16038533

Sources:
DTC
TRASTUZUMAB ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
IXABEPILONE ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
CHEMBL329673 ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CADMIUM DICHLORIDE ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROPYLPYRAZOLETRIOL ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
DTC
PALBOCICLIB ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25524798

Sources:
CIViC PharmGKB FDA
CHOLECALCIFEROL ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KEPONE ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GUTHION ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RETINOL ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PENTABROMOPHENOL ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZIRAM ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
METHAMPHETAMINE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19386276

Sources:
PharmGKB
CAPTAN ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ZEARALENONE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LAPATINIB ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
OLAPARIB ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
PYRITHIONE ZINC ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL184450 ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHLORANIL ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PYROGALLOL ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BENZETHONIUM CHLORIDE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DACTINOMYCIN ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PHENAZOPYRIDINE HYDROCHLORIDE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ALPELISIB ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
GENISTEIN ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16038533 10592235

Sources:
DTC
GENTIAN VIOLET ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
KAEMPFEROL ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRIAMTERENE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DICHLOROPHEN ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
EVEROLIMUS ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
MERCURIC CHLORIDE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PHENYLMERCURIC ACETATE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
HEXACHLOROPHENE ESR1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15081572

Sources:
DTC
CATECHOL ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
RESVERATROL ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19496085

Sources:
DTC
BITHIONOL ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
FENRETINIDE ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
APIGENIN ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
GW7647 ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DAUNORUBICIN HYDROCHLORIDE ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOXORUBICIN HYDROCHLORIDE ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
NORDIHYDROGUAIARETIC ACID ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DOCETAXEL ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB FDA
GOSSYPOL ESR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CISPLATIN ESR1

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21430602

Sources:
PharmGKB

Ensembl: ENSG00000091831
- Version: 101_38
Alternate Names:

ESR1 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
RussLampel: ENSG00000091831
- Version: 26-July-2011
Alternate Names:

ENSG00000091831 Ensembl Gene Id

ESTROGEN RECEPTOR (ER) (ESTRADIOL RECEPTOR) (ER-ALPHA). [SOURCE:UNIPROT/SWISSPROT;ACC:P03372] Description

ESR1 Display Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
BaderLabGenes: ESR1
- Version: February-2014
Alternate Names:

2099 Entrez Gene ID

Gene Info:

Initial Gene Query NR3A1

Counted Citations from 1950-2000 29833

Gene Categories:

NUCLEAR HORMONE RECEPTOR

Publications:
HopkinsGroom: P03372
- Version: 11-September-2012
Alternate Names:

P03372 Uniprot Accession

ENSG00000091831 Ensembl Gene Id

ESR1 Uniprot Gene Name

Gene Info:

Human Readable Name DRUGGABLE GENOME

Uniprot Evidence 1: Evidence at protein level

Interpro Short Name Nucl_hrmn_rcpt_lig-bd_core

Gene Categories:

NUCLEAR HORMONE RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P03372
- Version: 01-August-2011
Alternate Names:

2099 Entrez Gene Id

ENSG00000091831 Ensembl Gene Id

ESR1_HUMAN Uniprot Id

Gene Info:

Target Subclass Nuclear receptor

Target Main Class Receptors

Publications:
TdgClinicalTrial: P03372
- Version: January-2014
Alternate Names:

ESR1 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass Nuclear receptor

Publications:

PharmGKB: ESR1

Version: 18-August-2020

Alternate Names:

PA156 PharmGKB ID

Gene Info:

Publications:

Toy et al., 2013, ESR1 ligand-binding domain mutations in hormone-resistant breast cancer., Nat. Genet.

Robinson et al., 2013, Activating ESR1 mutations in hormone-resistant metastatic breast cancer., Nat. Genet.

Oesterreich S et al., 2015, Associations between genetic variants and the effect of letrozole and exemestane on bone mass and bone turnover., Breast Cancer Res Treat

CIViC: ESR1

Version: 14-September-2020

Alternate Names:

2099 Entrez Gene ID

21 CIViC Gene ID

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Toy et al., 2013, ESR1 ligand-binding domain mutations in hormone-resistant breast cancer., Nat. Genet.

Robinson et al., 2013, Activating ESR1 mutations in hormone-resistant metastatic breast cancer., Nat. Genet.

Finn et al., 2015, The cyclin-dependent kinase 4/6 inhibitor palbociclib in combination with letrozole versus letrozole alone as first-line treatment of oestrogen receptor-positive, HER2-negative, advanced breast cancer (PALOMA-1/TRIO-18): a randomised phase 2 study., Lancet Oncol.

TTD: Estrogen receptor
- Version: 2020.06.01
Alternate Names:

ESR TTD Gene Abbreviation

T89534 TTD Target ID

Gene Info:

Publications:

Fugh-Berman AJ, 2010, The haunting of medical journals: how ghostwriting sold "HRT"., PLoS Med

DTC: ESR1

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Shen J et al., 2012, Discovery and structure-activity analysis of selective estrogen receptor modulators via similarity-based virtual screening., Eur J Med Chem

Jain D et al., 2010, A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements., Bioorg Med Chem Lett

Maximov PY et al., 2010, Structure-function relationships of estrogenic triphenylethylenes related to endoxifen and 4-hydroxytamoxifen., J Med Chem

TALC: ESR1
- Version: 12-May-2016
Alternate Names:

ESR1 Gene Symbol

Gene Info:

Publications:
HingoraniCasas: ENSG00000091831
- Version: 31-May-2017
Alternate Names:

ENSG00000091831 Gene Symbol

ESR1 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: ESR
- Version: chembl_23
Alternate Names:

NR3A1 GENE_SYMBOL

ESR1 GENE_SYMBOL

Estrogen receptor UNIPROT

Gene Info:

Publications:
OncoKB: ESR1
- Version: 23-July-2020
Alternate Names:

2099 OncoKB Entrez Id

ESR OncoKB Gene Synonym

ESTRR OncoKB Gene Synonym

Gene Info:

Publications:
GO: ESR1
- Version: 01-February-2022
Alternate Names:

ESR GO Gene Synonym

NR3A1 GO Gene Synonym

Gene Info:

Gene Categories:

TRANSCRIPTION FACTOR COMPLEX, NUCLEAR HORMONE RECEPTOR

Publications:
Tempus: ESR1
- Version: 11-November-2018
Alternate Names:

ESR1 Gene Symbol

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
dGene: ESR1
- Version: 27-Jun-2013
Alternate Names:

2099 Gene ID

ER dGene Synonym

ESR dGene Synonym

Gene Info:

Gene Categories:

NUCLEAR HORMONE RECEPTOR

Publications:
Pharos: ESR1
- Version: 01-February-2022
Alternate Names:

Estrogen receptor Gene Name

P03372 UniProt ID

Gene Info:

Gene Categories:

KINASE, TRANSCRIPTION FACTOR

Publications:
ClearityFoundationClinicalTrial: ESR1
- Version: 15-June-2013
Alternate Names:

Gene Info:

Publications:
ClearityFoundationBiomarkers: ESR1
- Version: 26-July-2013
Alternate Names:

Gene Info:

Publications:
MskImpact: ESR1
- Version: May-2015
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FoundationOneGenes: ESR1
- Version: 03-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
CarisMolecularIntelligence: ESR1
- Version: 04-September-2020
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
FDA: ESR
- Version: 04-September-2020
Alternate Names:

Gene Info:

Publications:
Oncomine: ESR1
- Version: v3
Alternate Names:

Gene Info:

Gene Categories:

CLINICALLY ACTIONABLE

Publications:
COSMIC: ESR1
- Version: 4-Sep-2020
Alternate Names:

Gene Info:

Gene Categories:

DRUG RESISTANCE

Publications:

Trial Name	ethinyl estradiol + levonorgestrel,Seasonale, Lo Seasonale, Seasonique
Novel drug target	Established target
Trial Name	AG-200-15

Trial Name	lasofoxifene,Fablyn, Oporia
Novel drug target	Established target

Trial Name	Acapodene
Novel drug target	Established target
Trial Name	atamestane-plus-toremifene

Mechanism of Interaction	Estrogen receptor alpha agonist
Direct Interaction	yes

Direct Interaction	yes
Mechanism of Interaction	Estrogen receptor alpha antagonist

Trial Name	RAD1901
Novel drug target	Established target
Mechanism of Interaction	Estrogen receptor alpha degrader

Mechanism of Interaction	Estrogen receptor modulator
Direct Interaction	yes
Novel drug target	Established target

Trial Name	molecular iodine,IoGen
Novel drug target	Established target

Mechanism of Interaction	Estrogen receptor agonist
Direct Interaction	yes

Mechanism of Interaction	Estrogen receptor alpha modulator
Direct Interaction	yes

agonist (activating)
antagonist (inhibitory)

Trial Name	fispemifene, HM-101
Novel drug target	Established target
Mechanism of Interaction	Estrogen receptor modulator

Trial Name	etonogestrel implant,Implanon
Novel drug target	Established target
Trial Name	etonogestrel/ethinyl estradiol vaginal ring,Nuvaring

Trial Name	conjugated estrogens/medroxyprogesterone acetate,Prempro, Premphase
Novel drug target	Established target
Trial Name	oral contraceptive,Pill-Plus

Trial Name	bazedoxifene, bazedoxifene/conjugated estrogens, TSE-424,Viviant, Aprela, Conbriza
Novel drug target	Established target

Trial Name	estradiol valerate + dienogest,Natazia, Qlaira
Novel drug target	Established target

Trial Name	norelgestromin/ethinyl estradiol,Ortho Evra
Novel drug target	Established target

ENSG00000091831	Ensembl Gene Id
ESTROGEN RECEPTOR (ER) (ESTRADIOL RECEPTOR) (ER-ALPHA). [SOURCE:UNIPROT/SWISSPROT;ACC:P03372]	Description
ESR1	Display Id

P03372	Uniprot Accession
ENSG00000091831	Ensembl Gene Id
ESR1	Uniprot Gene Name

2099	Entrez Gene Id
ENSG00000091831	Ensembl Gene Id
ESR1_HUMAN	Uniprot Id

2099	OncoKB Entrez Id
ESR	OncoKB Gene Synonym
ESTRR	OncoKB Gene Synonym

ESR1 Gene Record

ESR1 2099 Druggable GenomeClinically ActionableDrug Resistance

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24805199

Sources: DTC ClearityFoundationClinicalTrial TTD

Interaction Types & Directionality: agonist (activating) antagonist (inhibitory)

Interaction Info: Trial Name Androxal Novel drug target Established target

PMIDs: 20091498 18320435 15878925 17055820 20379036 19761360 2011412 11752352 19821295

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: other/unknown

Interaction Info: Trial Name ethinyl estradiol + levonorgestrel,Seasonale, Lo Seasonale, Seasonique Novel drug target Established target Trial Name AG-200-15

PMIDs: 16609013 16084894 16325240 17634204 16307966 21791876 1562565 12589940

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: negative modulator (inhibitory) agonist (activating) antagonist (inhibitory)

Interaction Info: Trial Name lasofoxifene,Fablyn, Oporia Novel drug target Established target

PMIDs: 17456742

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2011412 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: modulator

Interaction Info: Trial Name Acapodene Novel drug target Established target Trial Name atamestane-plus-toremifene

PMIDs: 16515478 15369444 11747628 18279543 16595024 16917142 16503765 12870885 11752352 17062721 17503894

Sources: TdgClinicalTrial TEND PharmGKB TTD FDA

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name fulvestrant,Faslodex Mechanism of Interaction Estrogen receptor antagonist

PMIDs: 20621492 17337183 19133777 25879485 19845386 26407012 17275315 24185512 24185510 12113237 12080538 11398912 11922402 15018596 15865850 12542403 11752352 20151846

Sources: TALC DTC TdgClinicalTrial ChemblInteractions TEND CIViC PharmGKB TTD FDA OncoKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23214428

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23214428

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16038533

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Mechanism of Interaction Estrogen receptor alpha agonist Direct Interaction yes

PMIDs: 2011412 17138652 17125913 11752352

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Estrogen receptor alpha antagonist

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name RAD1901 Novel drug target Established target Mechanism of Interaction Estrogen receptor alpha degrader

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD OncoKB

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 14670645 2175153 14672731 25970022

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20334372

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22647217

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20430632

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
24805199

Sources:
DTC ClearityFoundationClinicalTrial TTD

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name Androxal

Novel drug target Established target

PMIDs:
20091498 18320435 15878925 17055820 20379036 19761360 2011412 11752352 19821295

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

other/unknown

Interaction Info:

Trial Name ethinyl estradiol + levonorgestrel,Seasonale, Lo Seasonale, Seasonique

Novel drug target Established target

Trial Name AG-200-15

PMIDs:
16609013 16084894 16325240 17634204 16307966 21791876 1562565 12589940

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

negative modulator (inhibitory)

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Trial Name lasofoxifene,Fablyn, Oporia

Novel drug target Established target

PMIDs:
17456742

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2011412 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name Acapodene

Novel drug target Established target

Trial Name atamestane-plus-toremifene

PMIDs:
16515478 15369444 11747628 18279543 16595024 16917142 16503765 12870885 11752352 17062721 17503894

Sources:
TdgClinicalTrial TEND PharmGKB TTD FDA

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name fulvestrant,Faslodex

Mechanism of Interaction Estrogen receptor antagonist

PMIDs:
20621492 17337183 19133777 25879485 19845386 26407012 17275315 24185512 24185510 12113237 12080538 11398912 11922402 15018596 15865850 12542403 11752352 20151846

Sources:
TALC DTC TdgClinicalTrial ChemblInteractions TEND CIViC PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

n/a

PMIDs:
23214428

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23214428

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
16038533

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

PMIDs:
2011412 17138652 17125913 11752352

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor alpha antagonist

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name RAD1901

Novel drug target Established target

Mechanism of Interaction Estrogen receptor alpha degrader

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD OncoKB

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
14670645 2175153 14672731 25970022

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
20334372

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
22647217

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
20430632

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
23214428

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor alpha agonist

Direct Interaction yes

Novel drug target Established target

PMIDs:
3622377 3334987 9558716 11752352 9048584 15276617 18976723

Sources:
DTC TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

agonist (activating)

modulator

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
21075131 17016423 17139284 11752352

Sources:
TdgClinicalTrial ChemblInteractions TEND TTD

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2307235 6872937 11752352 17236558

Sources:
DTC TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

agonist (activating)