ChEMBL logo

ChEMBL

spacer
ChEMBL Statistics
  Loading Statistics...
spacer

Target Report Card

Target Name and Classification

Target ID CHEMBL206
Target Type SINGLE PROTEIN
Preferred Name Estrogen receptor alpha
Synonyms 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
CHEMBL3885521 Baculoviral IAP repeat-containing protein 2/Estrogen receptor PROTEIN COMPLEX
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 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
CHEMBL3581693 BRILANESTRANT 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:0005794 (Golgi apparatus)
GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0032991 (macromolecular complex)
GO:0035327 (transcriptionally active chromatin)
GO:0097550 (transcriptional preinitiation complex)
GO Molecular Function GO:0000978 (RNA polymerase II core promoter proximal region sequence-specific DNA binding)
GO:0000981 (RNA polymerase II transcription factor activity, 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:0001093 (TFIIB-class transcription factor 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:0017025 (TBP-class protein binding)
GO:0019899 (enzyme binding)
GO:0019901 (protein kinase binding)
GO:0030235 (nitric-oxide synthase regulator activity)
GO:0030284 (estrogen receptor activity)
GO:0030331 (estrogen receptor binding)
GO:0034056 (estrogen response element binding)
GO:0038052 (RNA polymerase II transcription factor activity, estrogen-activated sequence-specific DNA binding)
GO:0042802 (identical protein binding)
GO:0043565 (sequence-specific DNA binding)
GO:0046872 (metal ion binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
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:0006338 (chromatin remodeling)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006357 (regulation of transcription from RNA polymerase II promoter)
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:0016579 (protein deubiquitination)
GO:0030111 (regulation of Wnt signaling pathway)
GO:0030518 (intracellular steroid hormone receptor signaling pathway)
GO:0030520 (intracellular estrogen receptor signaling pathway)
GO:0032355 (response to estradiol)
GO:0033146 (regulation of intracellular estrogen receptor signaling pathway)
GO:0034121 (regulation of toll-like receptor signaling pathway)
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:0043627 (response to estrogen)
GO:0045429 (positive regulation of nitric oxide biosynthetic process)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045899 (positive regulation of RNA polymerase II transcriptional preinitiation complex assembly)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048146 (positive regulation of fibroblast proliferation)
GO:0048863 (stem cell differentiation)
GO:0050727 (regulation of inflammatory response)
GO:0051000 (positive regulation of nitric-oxide synthase activity)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0051897 (positive regulation of protein kinase B signaling)
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:0071168 (protein localization to chromatin)
GO:0071391 (cellular response to estrogen stimulus)
GO:0071392 (cellular response to estradiol stimulus)
GO:1903799 (negative regulation of production of miRNAs involved in gene silencing by miRNA)
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-1257604 (PIP3 activates AKT signaling.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-383280 (Nuclear Receptor transcription pathway.)
R-HSA-5689896 (Ovarian tumor domain proteases.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
R-HSA-8866910 (TFAP2 (AP-2) family regulates transcription of growth factors and their receptors.)
R-HSA-8931987 (RUNX1 regulates estrogen receptor mediated transcription.)
R-HSA-8939256 (RUNX1 regulates transcription of genes involved in WNT signaling.)
R-HSA-8939902 (Regulation of RUNX2 expression and activity.)
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.)
IPR035500 (NHR_like_dom_sf.)
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...
spacer
spacer