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Target Report Card

Target Name and Classification

Target ID CHEMBL252
Preferred Name Endothelin receptor ET-A
Synonyms EDNRA | ET-A | ETA | ETA-R | ETRA | Endothelin A receptor | Endothelin-1 receptor | hET-AR
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > peptide receptor (family a gpcr) > short peptide receptor (family a gpcr) > endothelin receptor

Target Components

Component Description Relationship Accession
Endothelin-1 receptor SINGLE PROTEIN P25101

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2096678 Endothelin receptor, ET-A/ET-B PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL23261 DARUSENTAN Endothelin receptor ET-A antagonist 3 PubMed
CHEMBL61780 TEZOSENTAN Endothelin receptor ET-A antagonist 3 PubMed PubMed PubMed
CHEMBL109648 CLAZOSENTAN Endothelin receptor ET-A antagonist 3 PubMed
CHEMBL1628688 ZIBOTENTAN Endothelin receptor ET-A antagonist 3 PubMed
CHEMBL2106068 ATRASENTAN HYDROCHLORIDE Endothelin receptor ET-A antagonist 3 PubMed
CHEMBL2107803 AVOSENTAN Endothelin receptor ET-A antagonist 3 Other PubMed
CHEMBL431651 ENRASENTAN Endothelin receptor ET-A antagonist 2 PubMed
CHEMBL539423 SPARSENTAN Endothelin receptor ET-A antagonist 2 Other Other PubMed
CHEMBL2107760 NEBENTAN Endothelin receptor ET-A antagonist 2 PubMed PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000151617
Ensembl ENSG00000151617
GO Cellular Component GO:0005829 (cytosol)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030315 (T-tubule)
GO:0031965 (nuclear membrane)
GO:0045121 (membrane raft)
GO Molecular Function GO:0004435 (phosphatidylinositol phospholipase C activity)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004962 (endothelin receptor activity)
GO:0005515 (protein binding)
GO Biological Process GO:0001569 (patterning of blood vessels)
GO:0001666 (response to hypoxia)
GO:0001701 (in utero embryonic development)
GO:0001821 (histamine secretion)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0003094 (glomerular filtration)
GO:0006939 (smooth muscle contraction)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007190 (activation of adenylate cyclase activity)
GO:0007202 (activation of phospholipase C activity)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007205 (protein kinase C-activating G-protein coupled receptor signaling pathway)
GO:0007266 (Rho protein signal transduction)
GO:0007507 (heart development)
GO:0007568 (aging)
GO:0007585 (respiratory gaseous exchange)
GO:0008217 (regulation of blood pressure)
GO:0008283 (cell proliferation)
GO:0008284 (positive regulation of cell proliferation)
GO:0014032 (neural crest cell development)
GO:0014070 (response to organic cyclic compound)
GO:0014824 (artery smooth muscle contraction)
GO:0015758 (glucose transport)
GO:0019233 (sensory perception of pain)
GO:0030818 (negative regulation of cAMP biosynthetic process)
GO:0032496 (response to lipopolysaccharide)
GO:0042310 (vasoconstriction)
GO:0042482 (positive regulation of odontogenesis)
GO:0043066 (negative regulation of apoptotic process)
GO:0043084 (penile erection)
GO:0043278 (response to morphine)
GO:0048144 (fibroblast proliferation)
GO:0048484 (enteric nervous system development)
GO:0048659 (smooth muscle cell proliferation)
GO:0050678 (regulation of epithelial cell proliferation)
GO:0050729 (positive regulation of inflammatory response)
GO:0051281 (positive regulation of release of sequestered calcium ion into cytosol)
GO:0051482 (positive regulation of cytosolic calcium ion concentration involved in phospholipase C-activating G-protein coupled signaling pathway)
GO:0051928 (positive regulation of calcium ion transport)
GO:0060137 (maternal process involved in parturition)
GO:0060322 (head development)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0071260 (cellular response to mechanical stimulus)
GO:0086100 (endothelin receptor signaling pathway)
GO:0090023 (positive regulation of neutrophil chemotaxis)
GO:0090184 (positive regulation of kidney development)
Wikipedia Endothelin_receptor_type_A

Target Cross References - Protein

canSAR P25101
Human Protein Atlas ENSG00000151617
IntAct P25101
Guide to Pharmacology 219
Open Targets ENSG00000151617
PharmGKB PA27617
Pharos P25101 (Tclin)
Reactome R-HSA-375276 (Peptide ligand-binding receptors.)
R-HSA-416476 (G alpha (q) signalling events.)
UniProt B2R723 B4E2V6 B7Z9G6 D3DP03 E7ER36 O43441 P25101 Q16432 Q16433 Q8TBH2

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000499 (Endthln_rcpt.)
IPR002175 (ETA_rcpt.)
IPR017452 (GPCR_Rhodpsn_7TM.)
Pfam PF00001 (7tm_1)