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Target Report Card

Target Name and Classification

Target ID CHEMBL5872
Preferred Name G-protein coupled estrogen receptor 1
Synonyms CEPR | CMKRL2 | Chemoattractant receptor-like 2 | DRY12 | FEG-1 | Flow-induced endothelial G-protein coupled receptor 1 | G protein-coupled estrogen receptor 1 | G-protein coupled estrogen receptor 1 | G-protein coupled receptor 30 | GPCR-Br | GPER | GPER1 | GPR30 | IL8-related receptor DRY12 | LYGPR | Lymphocyte-derived G-protein coupled receptor | Membrane estrogen receptor | mER
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > small molecule receptor (family a gpcr) > lipid-like ligand receptor (family a gpcr) > steroid-like ligand receptor

Target Components

Component Description Relationship Accession
G-protein coupled estrogen receptor 1 SINGLE PROTEIN Q99527

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000164850
Ensembl ENSG00000164850
GO Cellular Component GO:0000139 (Golgi membrane)
GO:0005622 (intracellular)
GO:0005634 (nucleus)
GO:0005635 (nuclear envelope)
GO:0005737 (cytoplasm)
GO:0005739 (mitochondrion)
GO:0005768 (endosome)
GO:0005769 (early endosome)
GO:0005783 (endoplasmic reticulum)
GO:0005789 (endoplasmic reticulum membrane)
GO:0005794 (Golgi apparatus)
GO:0005802 (trans-Golgi network)
GO:0005829 (cytosol)
GO:0005856 (cytoskeleton)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0014069 (postsynaptic density)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030054 (cell junction)
GO:0030424 (axon)
GO:0030425 (dendrite)
GO:0030659 (cytoplasmic vesicle membrane)
GO:0031410 (cytoplasmic vesicle)
GO:0031966 (mitochondrial membrane)
GO:0032591 (dendritic spine membrane)
GO:0042734 (presynaptic membrane)
GO:0042995 (cell projection)
GO:0043198 (dendritic shaft)
GO:0043679 (axon terminus)
GO:0044327 (dendritic spine head)
GO:0045095 (keratin filament)
GO:0045202 (synapse)
GO:0048471 (perinuclear region of cytoplasm)
GO:0048786 (presynaptic active zone)
GO:0055037 (recycling endosome)
GO Molecular Function GO:0003682 (chromatin binding)
GO:0003707 (steroid hormone receptor activity)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0005496 (steroid binding)
GO:0005515 (protein binding)
GO:0008144 (drug binding)
GO:0017082 (mineralocorticoid receptor activity)
GO:0030284 (estrogen receptor activity)
GO:0042562 (hormone binding)
GO:1990239 (steroid hormone binding)
GO Biological Process GO:0001934 (positive regulation of protein phosphorylation)
GO:0001956 (positive regulation of neurotransmitter secretion)
GO:0002376 (immune system process)
GO:0002695 (negative regulation of leukocyte activation)
GO:0006915 (apoptotic process)
GO:0006954 (inflammatory response)
GO:0007049 (cell cycle)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007399 (nervous system development)
GO:0008284 (positive regulation of cell proliferation)
GO:0008285 (negative regulation of cell proliferation)
GO:0010579 (positive regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway)
GO:0010628 (positive regulation of gene expression)
GO:0010629 (negative regulation of gene expression)
GO:0010948 (negative regulation of cell cycle process)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0019228 (neuronal action potential)
GO:0030154 (cell differentiation)
GO:0030263 (apoptotic chromosome condensation)
GO:0030264 (nuclear fragmentation involved in apoptotic nuclear change)
GO:0030335 (positive regulation of cell migration)
GO:0030518 (intracellular steroid hormone receptor signaling pathway)
GO:0030819 (positive regulation of cAMP biosynthetic process)
GO:0031959 (mineralocorticoid receptor signaling pathway)
GO:0032024 (positive regulation of insulin secretion)
GO:0032962 (positive regulation of inositol trisphosphate biosynthetic process)
GO:0043065 (positive regulation of apoptotic process)
GO:0043280 (positive regulation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0043401 (steroid hormone mediated signaling pathway)
GO:0043410 (positive regulation of MAPK cascade)
GO:0045087 (innate immune response)
GO:0045599 (negative regulation of fat cell differentiation)
GO:0045742 (positive regulation of epidermal growth factor receptor signaling pathway)
GO:0045745 (positive regulation of G-protein coupled receptor protein signaling pathway)
GO:0045909 (positive regulation of vasodilation)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0050728 (negative regulation of inflammatory response)
GO:0050769 (positive regulation of neurogenesis)
GO:0051053 (negative regulation of DNA metabolic process)
GO:0051055 (negative regulation of lipid biosynthetic process)
GO:0051281 (positive regulation of release of sequestered calcium ion into cytosol)
GO:0051480 (regulation of cytosolic calcium ion concentration)
GO:0051898 (negative regulation of protein kinase B signaling)
GO:0070373 (negative regulation of ERK1 and ERK2 cascade)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0070474 (positive regulation of uterine smooth muscle contraction)
GO:0071157 (negative regulation of cell cycle arrest)
GO:0071333 (cellular response to glucose stimulus)
GO:0071356 (cellular response to tumor necrosis factor)
GO:0071375 (cellular response to peptide hormone stimulus)
GO:0071389 (cellular response to mineralocorticoid stimulus)
GO:0071392 (cellular response to estradiol stimulus)
GO:0090004 (positive regulation of establishment of protein localization to plasma membrane)
GO:0090200 (positive regulation of release of cytochrome c from mitochondria)
GO:1904706 (negative regulation of vascular smooth muscle cell proliferation)
GO:2000353 (positive regulation of endothelial cell apoptotic process)
GO:2000724 (positive regulation of cardiac vascular smooth muscle cell differentiation)
GO:2001238 (positive regulation of extrinsic apoptotic signaling pathway)
Wikipedia GPR30

Target Cross References - Protein

canSAR Q99527
Human Protein Atlas ENSG00000164850
IntAct Q99527
Guide to Pharmacology 221
Open Targets ENSG00000164850
PharmGKB PA28873
Pharos Q99527 (Tchem)
Reactome R-HSA-375276 (Peptide ligand-binding receptors.)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt A8K6C5 B5BUJ1 O00143 O43494 Q13631 Q6FHL1 Q96F42 Q99527 Q99981

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)