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Target Report Card

Target Name and Classification

Target ID CHEMBL206
Target Type SINGLE PROTEIN
Preferred Name Estrogen receptor alpha
Synonyms ER | ER-alpha | ESR | ESR1 | Estradiol receptor | Estrogen receptor | NR3A1 | Nuclear receptor subfamily 3 group A member 1
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transcription factor > nuclear receptor > nuclear hormone receptor subfamily 3 > nuclear hormone receptor subfamily 3 group a > nuclear hormone receptor subfamily 3 group a member 1

Target Components

Component Description Relationship Accession
Estrogen receptor SINGLE PROTEIN P03372

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2093866 Estrogen receptor PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL411 DIETHYLSTILBESTROL Estrogen receptor alpha agonist 4 PubMed
CHEMBL135 ESTRADIOL Estrogen receptor alpha agonist 4 DailyMed
CHEMBL691 ETHINYL ESTRADIOL Estrogen receptor alpha agonist 4 ISBN
CHEMBL786 TAMOXIFEN CITRATE Estrogen receptor alpha modulator 4 DailyMed PubMed
CHEMBL1018 DIENESTROL Estrogen receptor alpha agonist 4 ISBN PubMed
CHEMBL1405 ESTRONE Estrogen receptor alpha agonist 4 PubMed
CHEMBL1511 ESTRADIOL VALERATE Estrogen receptor alpha agonist 4 DailyMed
CHEMBL1200430 ESTRADIOL ACETATE Estrogen receptor alpha agonist 4 DailyMed
CHEMBL1200973 ESTRADIOL CYPIONATE Estrogen receptor alpha agonist 4 DailyMed
CHEMBL1200980 ESTROPIPATE Estrogen receptor alpha agonist 4 FDA
CHEMBL1201151 MESTRANOL Estrogen receptor alpha agonist 4 ISBN PubMed
CHEMBL1201477 POLYESTRADIOL PHOSPHATE Estrogen receptor alpha agonist 4 PubMed
CHEMBL3185958 CLOMIPHENE CITRATE Estrogen receptor alpha modulator 4 DailyMed FDA
CHEMBL3545015 RAD1901 Estrogen receptor alpha degrader 2 Other Other PubMed
CHEMBL3545017 GTx-758 Estrogen receptor alpha agonist 2 Other PubMed PubMed PubMed
CHEMBL3545210 SR16234 Estrogen receptor alpha antagonist 2 Other PubMed
CHEMBL3545390 GDC-0810 Estrogen receptor alpha antagonist 2 Other
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000091831
Ensembl ENSG00000091831
GO Cellular Component GO:0000790 (nuclear chromatin)
GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005794 (Golgi apparatus)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030315 (T-tubule)
GO:0035327 (transcriptionally active chromatin)
GO:0043005 (neuron projection)
GO:0043195 (terminal bouton)
GO:0043204 (perikaryon)
GO:0043234 (protein complex)
GO:0048471 (perinuclear region of cytoplasm)
GO Molecular Function GO:0000978 (RNA polymerase II core promoter proximal region sequence-specific DNA binding)
GO:0001046 (core promoter sequence-specific DNA binding)
GO:0001077 (transcriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific binding)
GO:0001223 (transcription coactivator binding)
GO:0003677 (DNA binding)
GO:0003682 (chromatin binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0003707 (steroid hormone receptor activity)
GO:0004879 (RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding)
GO:0005496 (steroid binding)
GO:0005515 (protein binding)
GO:0008013 (beta-catenin binding)
GO:0008134 (transcription factor binding)
GO:0008270 (zinc ion binding)
GO:0008289 (lipid binding)
GO:0019899 (enzyme binding)
GO:0030235 (nitric-oxide synthase regulator activity)
GO:0030284 (estrogen receptor activity)
GO:0031798 (type 1 metabotropic glutamate receptor binding)
GO:0032403 (protein complex binding)
GO:0034056 (estrogen response element binding)
GO:0036312 (phosphatidylinositol 3-kinase regulatory subunit binding)
GO:0038052 (RNA polymerase II transcription factor activity, estrogen-activated sequence-specific DNA binding)
GO:0042562 (hormone binding)
GO:0042802 (identical protein binding)
GO:0043565 (sequence-specific DNA binding)
GO:0046872 (metal ion binding)
GO:0051117 (ATPase binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0001547 (antral ovarian follicle growth)
GO:0002064 (epithelial cell development)
GO:0002076 (osteoblast development)
GO:0006338 (chromatin remodeling)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006366 (transcription from RNA polymerase II promoter)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0007165 (signal transduction)
GO:0007200 (phospholipase C-activating G-protein coupled receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0008209 (androgen metabolic process)
GO:0008584 (male gonad development)
GO:0010629 (negative regulation of gene expression)
GO:0010863 (positive regulation of phospholipase C activity)
GO:0030518 (intracellular steroid hormone receptor signaling pathway)
GO:0030520 (intracellular estrogen receptor signaling pathway)
GO:0032355 (response to estradiol)
GO:0042981 (regulation of apoptotic process)
GO:0043124 (negative regulation of I-kappaB kinase/NF-kappaB signaling)
GO:0043401 (steroid hormone mediated signaling pathway)
GO:0043433 (negative regulation of sequence-specific DNA binding transcription factor activity)
GO:0043523 (regulation of neuron apoptotic process)
GO:0043627 (response to estrogen)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045742 (positive regulation of epidermal growth factor receptor signaling pathway)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046325 (negative regulation of glucose import)
GO:0046697 (decidualization)
GO:0048146 (positive regulation of fibroblast proliferation)
GO:0048662 (negative regulation of smooth muscle cell proliferation)
GO:0050679 (positive regulation of epithelial cell proliferation)
GO:0051000 (positive regulation of nitric-oxide synthase activity)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0060009 (Sertoli cell development)
GO:0060011 (Sertoli cell proliferation)
GO:0060065 (uterus development)
GO:0060068 (vagina development)
GO:0060523 (prostate epithelial cord elongation)
GO:0060527 (prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis)
GO:0060687 (regulation of branching involved in prostate gland morphogenesis)
GO:0060745 (mammary gland branching involved in pregnancy)
GO:0060749 (mammary gland alveolus development)
GO:0060750 (epithelial cell proliferation involved in mammary gland duct elongation)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071168 (protein localization to chromatin)
GO:0071391 (cellular response to estrogen stimulus)
GO:0071392 (cellular response to estradiol stimulus)
GO:0090209 (negative regulation of triglyceride metabolic process)
GO:1901215 (negative regulation of neuron death)
GO:1903799 (negative regulation of production of miRNAs involved in gene silencing by miRNA)
GO:1990375 (baculum development)
Wikipedia Estrogen_receptor_alpha

Target Cross References - Protein

canSAR P03372
CGD Estrogen resistance
Human Protein Atlas ENSG00000091831
IntAct P03372
Guide to Pharmacology 620
Open Targets ENSG00000091831
PharmGKB PA156
Pharos P03372 (Tclin)
Reactome R-HSA-1251985 (Nuclear signaling by ERBB4.)
R-HSA-383280 (Nuclear Receptor transcription pathway.)
R-HSA-5689896 (Ovarian tumor domain proteases.)
R-HSA-8866910 (TFAP2 (AP-2) family regulates transcription of growth factors and their receptors.)
UniProt P03372 Q13511 Q14276 Q5T5H7 Q6MZQ9 Q9NU51 Q9UDZ7 Q9UIS7

Target Cross References - Domain

InterPro IPR000536 (Nucl_hrmn_rcpt_lig-bd.)
IPR001292 (Oestr_rcpt.)
IPR001628 (Znf_hrmn_rcpt.)
IPR001723 (Nuclear_hrmn_rcpt.)
IPR013088 (Znf_NHR/GATA.)
IPR024178 (Oest_rcpt/oest-rel_rcp.)
IPR024736 (Oestrogen-typ_rcpt_final_C_dom.)
Pfam PF00104 (Hormone_recep)
PF00105 (zf-C4)
PF02159 (Oest_recep)
PF12743 (ESR1_C)

Target Cross References - Structure

PDBe 1A52 1ERE 1ERR 1G50 1GWQ 1GWR 1HCQ 1L2I 1PCG 1QKT 1QKU 1R5K 1SJ0 1UOM 1X7E 1X7R 1XP1 1XP6 1XP9 1XPC 1XQC 1YIM 1YIN 1ZKY More...
CREDO 1A52 1ERE 1ERR 1G50 1GWQ 1GWR 1HCQ 1L2I 1PCG 1QKT 1QKU 1R5K 1SJ0 1UOM 1X7E 1X7R 1XP1 1XP6 1XP9 1XPC 1XQC 1YIM 1YIN 1ZKY More...
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