DGIdb - ESR2 Gene Record

ESR2 2100 Druggable Genome

Alternate Names:

ESR2
2100
ESTROGEN RECEPTOR 2
ER-BETA
ESR-BETA
ESRB
ESTRB
Erb
NR3A2
601663
3468
ENSG00000140009
OTTHUMG00000141306
Q92731
ESTROGEN RECEPTOR BETA (ER-BETA). [SOURCE:UNIPROT/SWISSPROT;ACC:Q92731]
BE0000792
ESTROGEN RECEPTOR BETA
ESR2_HUMAN
PA27886
621
NP_001428
NM_001040276
Estrogen receptor-β
Nuclear receptor subfamily 3 group A member 2
T80896

Gene Info:

Target Class	Receptors
Target Subclass	Nuclear receptor
Human Readable Name	DRUGGABLE GENOME
Initial Gene Query	NR3A2
Counted Citations from 1950-2000	3987
Interpro Name	Nuclear hormone receptor, ligand-binding, core
Human Readable Name	NUCLEAR HORMONE RECEPTOR
Interpro Type	Domain
Uniprot Status	Swiss-Prot
Interpro Acc	IPR000536
Interpro Short Name	Nucl_hrmn_rcpt_lig-bd_core
Uniprot Evidence	1: Evidence at protein level
GuideToPharmacology Gene Category Name	3A. Estrogen receptors
GuideToPharmacology Gene Category ID	96
Target Main Class	Receptors
Gene Biotype	PROTEIN_CODING

(13 More Sources)

Gene Categories: Category Details

NUCLEAR HORMONE RECEPTOR
DRUGGABLE GENOME
TRANSCRIPTION FACTOR

Publications:

Mc Ilroy et al., 2006, Tamoxifen-induced ER-alpha-SRC-3 interaction in HER2 positive human breast cancer; a possible mechanism for ER isoform specific recurrence., Endocr. Relat. Cancer
Hayes et al., 2010, Estrogen receptor genotypes, menopausal status, and the effects of tamoxifen on lipid levels: revised and updated results., Clin. Pharmacol. Ther.
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
Chen et al., 2005, Potential of endogenous estrogen receptor beta to influence the selective ER modulator ERbeta complex., Int. J. Oncol.
Sasson, 1991, Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor., Pathol. Biol.
Horner-Glister et al., 2005, Influence of oestradiol and tamoxifen on oestrogen receptors-alpha and -beta protein degradation and non-genomic signalling pathways in uterine and breast carcinoma cells., J. Mol. Endocrinol.
Gruvberger-Saal et al., 2007, Estrogen receptor beta expression is associated with tamoxifen response in ERalpha-negative breast carcinoma., Clin. Cancer Res.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Girault et al., 2006, Role of estrogen receptor alpha transcriptional coregulators in tamoxifen resistance in breast cancer., Maturitas
Ntukidem NI et al., 2008, Estrogen receptor genotypes, menopausal status, and the lipid effects of tamoxifen., Clin Pharmacol Ther
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Min J et al., 2013, Thiophene-core estrogen receptor ligands having superagonist activity., J Med Chem
Komm BS et al., 2005, Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity., Endocrinology
Bryant et al., An estrogen receptor basis for raloxifene action in bone., J. Steroid Biochem. Mol. Biol.
Zhou et al., 2002, Selective estrogen receptor modulator effects in the rat brain., Neuroendocrinology
Kim et al., 2002, Raloxifene, a selective estrogen receptor modulator, induces apoptosis in androgen-responsive human prostate cancer cell line LNCaP through an androgen-independent pathway., Cancer Res.
Iannone et al., 2001, Multiplexed molecular interactions of nuclear receptors using fluorescent microspheres., Cytometry
Sun et al., 2002, Antagonists selective for estrogen receptor alpha., Endocrinology
Jiang Y et al., 2013, Mechanisms enforcing the estrogen receptor β selectivity of botanical estrogens., FASEB J
Vijayanathan et al., 2007, Effects of estradiol and 4-hydroxytamoxifen on the conformation, thermal stability, and DNA recognition of estrogen receptor beta., Biochem. Cell Biol.
Bologa et al., 2006, Virtual and biomolecular screening converge on a selective agonist for GPR30., Nat. Chem. Biol.
Paterni I et al., 2014, Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential., Steroids
Renner S et al., 2009, Bioactivity-guided mapping and navigation of chemical space., Nat Chem Biol
Mishra et al., 2006, Metabolite ligands of estrogen receptor-beta reduce primate coronary hyperreactivity., Am. J. Physiol. Heart Circ. Physiol.
Calogeropoulou T et al., 2009, Novel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activity., J Med Chem
Peng J et al., 2009, Potential of selective estrogen receptor modulators as treatments and preventives of breast cancer., Anticancer Agents Med Chem
Barker et al., 2006, Comparison of effects of 4-hydroxy tamoxifen and trilostane on oestrogen-regulated gene expression in MCF-7 cells: up-regulation of oestrogen receptor beta., J. Steroid Biochem. Mol. Biol.
Puddefoot et al., 2006, Trilostane in advanced breast cancer., Expert Opin Pharmacother
Puddefoot et al., 2002, Non-competitive steroid inhibition of oestrogen receptor functions., Int. J. Cancer
Woo HI et al., 2012, Effect of genetic polymorphisms on therapeutic response and clinical outcomes in pancreatic cancer patients treated with gemcitabine., Pharmacogenomics
Setchell KD et al., 2005, S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora., Am J Clin Nutr
Mueller SO et al., 2004, Phytoestrogens and their human metabolites show distinct agonistic and antagonistic properties on estrogen receptor alpha (ERalpha) and ERbeta in human cells., Toxicol Sci
Ho, 2004, Estrogens and anti-estrogens: key mediators of prostate carcinogenesis and new therapeutic candidates., J. Cell. Biochem.
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
2008, Final amended report on the safety assessment of Methylparaben, Ethylparaben, Propylparaben, Isopropylparaben, Butylparaben, Isobutylparaben, and Benzylparaben as used in cosmetic products., Int. J. Toxicol.
Geistlinger et al., 2004, Ligand-selective inhibition of the interaction of steroid receptor coactivators and estrogen receptor isoforms., Chem. Biol.
Kuiper GG et al., 1998, Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor beta., Endocrinology
Chen et al., 2005, Direct agonist/antagonist functions of dehydroepiandrosterone., Endocrinology
Gutendorf B et al., 2001, Comparison of an array of in vitro assays for the assessment of the estrogenic potential of natural and synthetic estrogens, phytoestrogens and xenoestrogens., Toxicology
Dang Z, 2010, Comparison of relative binding affinities to fish and mammalian estrogen receptors: the regulatory implications., Toxicol Lett
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
van der Woude H et al., 2005, The stimulation of cell proliferation by quercetin is mediated by the estrogen receptor., Mol Nutr Food Res
Leung LK et al., 2004, Effect of dietary flavonols on oestrogen receptor transactivation and cell death induction., Br J Nutr
Maggiolini M et al., 2001, Estrogen receptor alpha mediates the proliferative but not the cytotoxic dose-dependent effects of two major phytoestrogens on human breast cancer cells., Mol Pharmacol
Howes MJ et al., 2002, Assessment of estrogenic activity in some common essential oil constituents., J Pharm Pharmacol
Jayaraman A et al., 2009, Progesterone attenuates oestrogen neuroprotection via downregulation of oestrogen receptor expression in cultured neurones., J Neuroendocrinol
Aguirre C et al., 2010, Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β., J Neurochem
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.
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
Matsumoto H et al., 2005, [Estrogenic activity of ultraviolet absorbers and the related compounds]., Yakugaku Zasshi
Naoum F et al., 2007, Synthesis of novel nitro-substituted triaryl pyrazole derivatives as potential estrogen receptor ligands., Molecules
Norata et al., 2010, The androgen derivative 5alpha-androstane-3beta,17beta-diol inhibits tumor necrosis factor alpha and lipopolysaccharide induced inflammatory response in human endothelial cells and in mice aorta., Atherosclerosis
Takeuchi S et al., 2005, Differential effects of phthalate esters on transcriptional activities via human estrogen receptors alpha and beta, and androgen receptor., Toxicology

MF101 ESR2

Interaction Score: 2.27

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name MF101 ,Menerba

Novel drug target Established target

Mechanism of Interaction Estrogen receptor beta agonist

PMIDs:
None found

Sources:
TdgClinicalTrial TTD DrugBank ChemblInteractions
CHEMBL346455 ESR2

Interaction Score: 1.7

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17139284 17016423

Sources:
DrugBank
AUS-131 ESR2

Interaction Score: 1.7

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor beta agonist

Trial Name AUS-131

PMIDs:
15883431 15084758

Sources:
TdgClinicalTrial TTD DrugBank ChemblInteractions
CHEMBL1222035 ESR2

Interaction Score: 1.7

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20659801 10592235 17139284 17016423

Sources:
DTC DrugBank
CHEMBL211614 ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL360410 ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL367588 ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL236720 ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
ANDROSTANEDIOL ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
20557886

Sources:
DrugBank
ERTEBEREL ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor beta agonist

Direct Interaction yes

PMIDs:
10592235

Sources:
TTD DrugBank ChemblInteractions
CHEMBL2332580 ESR2

Interaction Score: 1.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23586645

Sources:
DTC
PRINABEREL ESR2

Interaction Score: 0.95

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor beta agonist

Specific Action of the Ligand Agonist

PMIDs:
10592235

Sources:
TTD DrugBank GuideToPharmacology ChemblInteractions
CHEMBL185918 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL395308 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL187105 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL236718 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL364092 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL1232445 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL192154 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL190467 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL236086 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL363498 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
MK-6913 ESR2

Interaction Score: 0.57

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
ARZOXIFENE ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD DrugBank
SR16234 ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name TAS-108

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial DrugBank
ESTROGEN ESR2

Interaction Score: 0.57

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
LASOFOXIFENE ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Partial agonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
19519291

Sources:
DrugBank GuideToPharmacology
FISPEMIFENE ESR2

Interaction Score: 0.57

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
BAZEDOXIFENE ESR2

Interaction Score: 0.57

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

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

Specific Action of the Ligand Antagonist

PMIDs:
15961563

Sources:
TdgClinicalTrial DrugBank GuideToPharmacology
ESTROPIPATE ESR2

Interaction Score: 0.43

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
2011412 17464340

Sources:
DrugBank
ESTRIOL ESR2

Interaction Score: 0.43

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
16199482

Sources:
DrugBank GuideToPharmacology
TRILOSTANE ESR2

Interaction Score: 0.41

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

PMIDs:
16806905 17109615 12209583

Sources:
TTD DrugBank
CHEMBL184151 ESR2

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10592235

Sources:
DrugBank
CHEMBL3559901 ESR2

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16199482

Sources:
DrugBank
OCTOCRYLENE ESR2

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16079615

Sources:
DrugBank
BENZOPHENONE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16079615

Sources:
DrugBank
ENZACAMENE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16079615

Sources:
DrugBank
RALOXIFEN ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name Evista

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ACOLBIFENE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

modulator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor modulator

PMIDs:
None found

Sources:
ChemblInteractions
CHF4227 ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESTROGENS, CONJUGATED SYNTHETIC A ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DIETHYLSTILBESTROL DIPHOSPHATE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SYNTHETIC CONJUGATED ESTROGENS, B ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LY2245461 ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESTROGENS, CONJUGATED ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SIVIFENE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name A-007

PMIDs:
None found

Sources:
TdgClinicalTrial
LIQUIRTIGENIN ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Details of the Assay for Interaction Measuring activation of the ERE tk-Luc reporter by ER&bets; in transfected U2OS cells.

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
ESTRAMUSTINE PHOSPHATE SODIUM ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

modulator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor beta

PMIDs:
None found

Sources:
ChemblInteractions
ESTROGENS, ESTERIFIED ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor agonist

PMIDs:
None found

Sources:
ChemblInteractions
DIARYLPROPIONITRILE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Direct Interaction? True

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
CR 1447 ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor beta agonist

PMIDs:
None found

Sources:
ChemblInteractions
OSPEMIFENE ESR2

Interaction Score: 0.28

Interaction Types & Directionality:

modulator

Interaction Info:

Trial Name ospemifene,Ophena

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
FULVESTRANT ESR2

Interaction Score: 0.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Notes

Mechanism of Interaction Estrogen receptor antagonist

Direct Interaction yes

PMIDs:
19845386

Sources:
DTC PharmGKB TALC GuideToPharmacology ChemblInteractions
RALOXIFENE ESR2

Interaction Score: 0.23

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Specific Action of the Ligand Antagonist

PMIDs:
20659801 10418979 11810032 12097269 11752352 11500849 11861516

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
ESTRONE ESR2

Interaction Score: 0.21

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? True

PMIDs:
11518614 19913605

Sources:
DrugBank GuideToPharmacology
EUGENOL ESR2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12495555

Sources:
DrugBank
BAZEDOXIFENE ACETATE ESR2

Interaction Score: 0.19

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESTRADIOL ESR2

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name Bio-E-Gel, estradiol,Elestrin

Novel drug target Established target

Trial Name drospirenone plus estradiol,Angeliq

PMIDs:
20659801 23882126 2011412 17464340 16520733 24971815 19561619

Sources:
TEND DTC TdgClinicalTrial DrugBank
PYRAZOLE ESR2

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17909483

Sources:
DrugBank
OXYBENZONE ESR2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16079615

Sources:
DrugBank
AFIMOXIFENE ESR2

Interaction Score: 0.14

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
NARINGENIN ESR2

Interaction Score: 0.14

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

PMIDs:
9751507

Sources:
TTD DrugBank
TOREMIFENE ESR2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name atamestane-plus-toremifene

PMIDs:
None found

Sources:
PharmGKB TdgClinicalTrial
IDOXIFENE ESR2

Interaction Score: 0.14

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TAMOXIFEN ESR2

Interaction Score: 0.14

Interaction Types & Directionality:

agonist (activating)

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
17158759 20827267 20659801 16010412 2011412 16326830 17404078 11752352 16822624 17713466

Sources:
TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
ESTRADIOL BENZOATE ESR2

Interaction Score: 0.13

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
2011412 17464340

Sources:
DrugBank
PHTHALIC ACID ESR2

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15840436

Sources:
DrugBank
QUINESTROL ESR2

Interaction Score: 0.11

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHLOROTRIANISENE ESR2

Interaction Score: 0.11

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor beta modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
AFIMOXIFENE ESR2

Interaction Score: 0.1

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
15846122

Sources:
DrugBank ChemblInteractions
DROLOXIFENE ESR2

Interaction Score: 0.09

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TOREMIFENE CITRATE ESR2

Interaction Score: 0.08

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GOSERELIN ESR2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
LETROZOLE ESR2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26536870

Sources:
PharmGKB
ESTRAMUSTINE ESR2

Interaction Score: 0.08

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
14755680

Sources:
DrugBank
PERTUZUMAB ESR2

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DIETHYLSTILBESTROL ESR2

Interaction Score: 0.07

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
19101832 15123288

Sources:
DrugBank GuideToPharmacology
ERIBULIN ESR2

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
GENISTEIN ESR2

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Specific Action of the Ligand Agonist

Endogenous Drug? False

PMIDs:
10592235 17139284 17016423

Sources:
TTD DrugBank GuideToPharmacology
NERATINIB ESR2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
CHEMBL600336 ESR2

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PRASTERONE ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

activator (activating)

Interaction Info:

PMIDs:
15994348

Sources:
DrugBank
ETHINYL ESTRADIOL ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Agonist

PMIDs:
None found

Sources:
GuideToPharmacology
ANASTROZOLE ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
EXEMESTANE ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ABEMACICLIB ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PROGESTERONE ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

negative modulator (inhibitory)

agonist (activating)

Interaction Info:

PMIDs:
19094096 20977477 17341305 11014241

Sources:
DrugBank
RIBOCICLIB ESR2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
QUERCETIN ESR2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15937998 15182386 11502892 9751507

Sources:
DrugBank
IXABEPILONE ESR2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
RALOXIFENE HYDROCHLORIDE ESR2

Interaction Score: 0.03

Interaction Types & Directionality:

modulator

Interaction Info:

Mechanism of Interaction Estrogen receptor beta modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BITHIONOL ESR2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TRASTUZUMAB ESR2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
LAPATINIB ESR2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
OLAPARIB ESR2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ALPELISIB ESR2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
GEMCITABINE ESR2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22838950

Sources:
PharmGKB
EVEROLIMUS ESR2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PALBOCICLIB ESR2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DOCETAXEL ESR2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

Ensembl: ENSG00000140009
- Version: 101_38
Alternate Names:

ESR2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
BaderLabGenes: ESR2
- Version: February-2014
Alternate Names:

2100 Entrez Gene ID

Gene Info:

Initial Gene Query NR3A2

Counted Citations from 1950-2000 3987

Gene Categories:

NUCLEAR HORMONE RECEPTOR

Publications:
RussLampel: ENSG00000140009
- Version: 26-July-2011
Alternate Names:

ESR2 Display Id

ESTROGEN RECEPTOR BETA (ER-BETA). [SOURCE:UNIPROT/SWISSPROT;ACC:Q92731] Description

ENSG00000140009 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
HopkinsGroom: Q92731
- Version: 11-September-2012
Alternate Names:

ESR2 Uniprot Gene Name

ENSG00000140009 Ensembl Gene Id

2100 Entrez Gene Id

Gene Info:

Interpro Name Nuclear hormone receptor, ligand-binding, core

Human Readable Name DRUGGABLE GENOME

Human Readable Name NUCLEAR HORMONE RECEPTOR

Gene Categories:

NUCLEAR HORMONE RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: Q92731
- Version: 01-August-2011
Alternate Names:

ENSG00000140009 Ensembl Gene Id

Q92731 Uniprot Accession

2100 Entrez Gene Id

Gene Info:

Target Subclass Nuclear receptor

Target Main Class Receptors

Publications:
TdgClinicalTrial: Q92731
- Version: January-2014
Alternate Names:

ESR2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass Nuclear receptor

Publications:
GuideToPharmacology: 2100
- Version: 29-September-2020
Alternate Names:

3468 HUGO Gene ID

3468 HUGO Gene Symbol

estrogen receptor 2 HUGO Gene Name

Gene Info:

GuideToPharmacology Gene Category Name 3A. Estrogen receptors

GuideToPharmacology Gene Category ID 96

Gene Categories:

NUCLEAR HORMONE RECEPTOR

Publications:

PharmGKB: ESR2

Version: 18-August-2020

Alternate Names:

PA27886 PharmGKB ID

Gene Info:

Publications:

Ntukidem NI et al., 2008, Estrogen receptor genotypes, menopausal status, and the lipid effects of tamoxifen., Clin Pharmacol Ther

Woo HI et al., 2012, Effect of genetic polymorphisms on therapeutic response and clinical outcomes in pancreatic cancer patients treated with gemcitabine., Pharmacogenomics

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

DrugBank: BE0000792

Version: 5.1.7

Alternate Names:

ESR2 DrugBank Gene Name

Q92731 UniProt Accession

2100 Entrez Gene Id

Gene Info:

Publications:

Cada DJ et al., 2014, Conjugated estrogens and bazedoxifene., Hosp Pharm

Ropero et al., 2006, Heart estrogen receptor alpha: distinct membrane and nuclear distribution patterns and regulation by estrogen., J. Mol. Cell. Cardiol.

Stroud et al., 2006, Concentrations of isoflavones in macaques consuming standard laboratory monkey diet., J. Am. Assoc. Lab. Anim. Sci.

TTD: Estrogen receptor beta
- Version: 2020.06.01
Alternate Names:

ESR2 TTD Gene Abbreviation

T80896 TTD Target ID

Gene Info:

Publications:

Chollet JA, 2011, Update on alternative therapies for vulvovaginal atrophy., Patient Prefer Adherence

DTC: ESR2

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Calogeropoulou T et al., 2009, Novel dehydroepiandrosterone derivatives with antiapoptotic, neuroprotective activity., 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

Bologa et al., 2006, Virtual and biomolecular screening converge on a selective agonist for GPR30., Nat. Chem. Biol.

HingoraniCasas: ENSG00000140009
- Version: 31-May-2017
Alternate Names:

ENSG00000140009 Gene Symbol

ESR2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
TALC: ESR2
- Version: 12-May-2016
Alternate Names:

ESR2 Gene Symbol

Gene Info:

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

NR3A2 GENE_SYMBOL

ESR2 GENE_SYMBOL

Estrogen receptor beta UNIPROT

Gene Info:

Publications:
Pharos: ESR2
- Version: 03-September-2020
Alternate Names:

Estrogen receptor beta Gene Name

Q92731 UniProt ID

Gene Info:

Gene Categories:

NUCLEAR HORMONE RECEPTOR, TRANSCRIPTION FACTOR

Publications:
GO: ESR2
- Version: 05-September-2020
Alternate Names:

ESTRB GO Gene Synonym

NR3A2 GO Gene Synonym

Gene Info:

Gene Categories:

NUCLEAR HORMONE RECEPTOR

Publications:
dGene: ESR2
- Version: 27-Jun-2013
Alternate Names:

2100 Gene ID

ER-BETA dGene Synonym

ESR-BETA dGene Synonym

Gene Info:

Gene Categories:

NUCLEAR HORMONE RECEPTOR

Publications:

Trial Name	MF101 ,Menerba
Novel drug target	Established target
Mechanism of Interaction	Estrogen receptor beta agonist

Direct Interaction	yes
Mechanism of Interaction	Estrogen receptor beta agonist
Trial Name	AUS-131

Mechanism of Interaction	Estrogen receptor agonist
Direct Interaction	yes
Trial Name	MK-6913

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

Specific Action of the Ligand	Partial agonist
Endogenous Drug?	False
Direct Interaction?	False

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

Details of the Assay for Interaction	Measuring activation of the ERE tk-Luc reporter by ER&bets; in transfected U2OS cells.
Specific Action of the Ligand	Agonist
Endogenous Drug?	False

Trial Name	ospemifene,Ophena
Novel drug target	Established target
Direct Interaction	yes

Notes
Mechanism of Interaction	Estrogen receptor antagonist
Direct Interaction	yes

Trial Name	Bio-E-Gel, estradiol,Elestrin
Novel drug target	Established target
Trial Name	drospirenone plus estradiol,Angeliq

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

Mechanism of Interaction	Estrogen receptor beta modulator
Direct Interaction	yes

ESR2	Display Id
ESTROGEN RECEPTOR BETA (ER-BETA). [SOURCE:UNIPROT/SWISSPROT;ACC:Q92731]	Description
ENSG00000140009	Ensembl Gene Id

ESR2	Uniprot Gene Name
ENSG00000140009	Ensembl Gene Id
2100	Entrez Gene Id

3468	HUGO Gene ID
3468	HUGO Gene Symbol
estrogen receptor 2	HUGO Gene Name

ESR2	DrugBank Gene Name
Q92731	UniProt Accession
2100	Entrez Gene Id

NR3A2	GENE_SYMBOL
ESR2	GENE_SYMBOL
Estrogen receptor beta	UNIPROT

ESR2 Gene Record

ESR2 2100 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name MF101 ,Menerba Novel drug target Established target Mechanism of Interaction Estrogen receptor beta agonist

PMIDs: None found

Sources: TdgClinicalTrial TTD DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17139284 17016423

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Estrogen receptor beta agonist Trial Name AUS-131

PMIDs: 15883431 15084758

Sources: TdgClinicalTrial TTD DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20659801 10592235 17139284 17016423

Sources: DTC DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 20557886

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 10592235

Sources: TTD DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23586645

Sources: DTC

Interaction Types & Directionality: agonist (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Estrogen receptor beta agonist Specific Action of the Ligand Agonist

PMIDs: 10592235

Sources: TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10592235

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name MF101 ,Menerba

Novel drug target Established target

Mechanism of Interaction Estrogen receptor beta agonist

PMIDs:
None found

Sources:
TdgClinicalTrial TTD DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
17139284 17016423

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor beta agonist

Trial Name AUS-131

PMIDs:
15883431 15084758

Sources:
TdgClinicalTrial TTD DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
20659801 10592235 17139284 17016423

Sources:
DTC DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

PMIDs:
20557886

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Estrogen receptor beta agonist

Direct Interaction yes

PMIDs:
10592235

Sources:
TTD DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
23586645

Sources:
DTC

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Estrogen receptor beta agonist

Specific Action of the Ligand Agonist

PMIDs:
10592235

Sources:
TTD DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10592235

Sources:
DrugBank

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

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD DrugBank

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name TAS-108

Novel drug target Established target

PMIDs:
None found