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Target Report Card

Target Name and Classification

Target ID CHEMBL2007
Preferred Name Platelet-derived growth factor receptor alpha
Synonyms Alpha platelet-derived growth factor receptor | Alpha-type platelet-derived growth factor receptor | CD140 antigen-like family member A | CD140a antigen | CD_antigen=CD140a | PDGF-R-alpha | PDGFR-2 | PDGFR-alpha | PDGFR2 | PDGFRA | Platelet-derived growth factor alpha receptor | Platelet-derived growth factor receptor 2 | Platelet-derived growth factor receptor alpha | RHEPDGFRA
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase pdgfr family

Target Components

Component Description Relationship Accession
Platelet-derived growth factor receptor alpha SINGLE PROTEIN P16234

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2095189 Platelet-derived growth factor receptor PROTEIN COMPLEX

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1743049 OLARATUMAB Platelet-derived growth factor receptor alpha antagonist 4 PubMed PubMed
CHEMBL2103851 AMUVATINIB Platelet-derived growth factor receptor alpha inhibitor 2 Other PubMed PubMed
CHEMBL2364651 TOVETUMAB Platelet-derived growth factor receptor alpha inhibitor 2 Other PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000134853
Ensembl ENSG00000134853
GO Cellular Component GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0005902 (microvillus)
GO:0009897 (external side of plasma membrane)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030054 (cell junction)
GO:0031226 (intrinsic component of plasma membrane)
GO:0032991 (macromolecular complex)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0004672 (protein kinase activity)
GO:0004713 (protein tyrosine kinase activity)
GO:0004714 (transmembrane receptor protein tyrosine kinase activity)
GO:0005018 (platelet-derived growth factor alpha-receptor activity)
GO:0005021 (vascular endothelial growth factor-activated receptor activity)
GO:0005088 (Ras guanyl-nucleotide exchange factor activity)
GO:0005161 (platelet-derived growth factor receptor binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0038085 (vascular endothelial growth factor binding)
GO:0042803 (protein homodimerization activity)
GO:0044877 (macromolecular complex binding)
GO:0046934 (phosphatidylinositol-4,5-bisphosphate 3-kinase activity)
GO:0048407 (platelet-derived growth factor binding)
GO Biological Process GO:0000165 (MAPK cascade)
GO:0001553 (luteinization)
GO:0001701 (in utero embryonic development)
GO:0001775 (cell activation)
GO:0002244 (hematopoietic progenitor cell differentiation)
GO:0006468 (protein phosphorylation)
GO:0006935 (chemotaxis)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007275 (multicellular organism development)
GO:0008210 (estrogen metabolic process)
GO:0008284 (positive regulation of cell proliferation)
GO:0008585 (female gonad development)
GO:0009653 (anatomical structure morphogenesis)
GO:0009887 (organ morphogenesis)
GO:0010544 (negative regulation of platelet activation)
GO:0010863 (positive regulation of phospholipase C activity)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016032 (viral process)
GO:0016310 (phosphorylation)
GO:0016477 (cell migration)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0023019 (signal transduction involved in regulation of gene expression)
GO:0030198 (extracellular matrix organization)
GO:0030324 (lung development)
GO:0030325 (adrenal gland development)
GO:0030335 (positive regulation of cell migration)
GO:0030539 (male genitalia development)
GO:0033327 (Leydig cell differentiation)
GO:0034614 (cellular response to reactive oxygen species)
GO:0035790 (platelet-derived growth factor receptor-alpha signaling pathway)
GO:0038091 (positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathway)
GO:0042060 (wound healing)
GO:0042475 (odontogenesis of dentin-containing tooth)
GO:0043552 (positive regulation of phosphatidylinositol 3-kinase activity)
GO:0046777 (protein autophosphorylation)
GO:0046854 (phosphatidylinositol phosphorylation)
GO:0048008 (platelet-derived growth factor receptor signaling pathway)
GO:0048015 (phosphatidylinositol-mediated signaling)
GO:0048146 (positive regulation of fibroblast proliferation)
GO:0048557 (embryonic digestive tract morphogenesis)
GO:0048701 (embryonic cranial skeleton morphogenesis)
GO:0048704 (embryonic skeletal system morphogenesis)
GO:0048705 (skeletal system morphogenesis)
GO:0050920 (regulation of chemotaxis)
GO:0051897 (positive regulation of protein kinase B signaling)
GO:0055003 (cardiac myofibril assembly)
GO:0060021 (palate development)
GO:0060325 (face morphogenesis)
GO:0060326 (cell chemotaxis)
GO:0061298 (retina vasculature development in camera-type eye)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0070527 (platelet aggregation)
GO:0071230 (cellular response to amino acid stimulus)
GO:0072277 (metanephric glomerular capillary formation)
GO:2000249 (regulation of actin cytoskeleton reorganization)
GO:2000587 (negative regulation of platelet-derived growth factor receptor-beta signaling pathway)
GO:2000739 (regulation of mesenchymal stem cell differentiation)
Wikipedia PDGFRA

Target Cross References - Protein

canSAR P16234
CGD Gastrointestinal stromal tumor
Human Protein Atlas ENSG00000134853
IntAct P16234
Guide to Pharmacology 1803
Open Targets ENSG00000134853
PharmGKB PA33147
Pharos P16234 (Tclin)
Reactome R-HSA-1257604 (PIP3 activates AKT signaling.)
R-HSA-186763 (Downstream signal transduction.)
R-HSA-186797 (Signaling by PDGF.)
R-HSA-2219530 (Constitutive Signaling by Aberrant PI3K in Cancer.)
R-HSA-5673001 (RAF/MAP kinase cascade.)
R-HSA-6811558 (PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling.)
UniProt B2RE69 E9PBH0 P16234 Q6P4H5 Q96KZ7 Q9UD28

Target Cross References - Domain

InterPro IPR000719 (Prot_kinase_dom.)
IPR001245 (Ser-Thr/Tyr_kinase_cat_dom.)
IPR001824 (Tyr_kinase_rcpt_3_CS.)
IPR003598 (Ig_sub2.)
IPR003599 (Ig_sub.)
IPR007110 (Ig-like_dom.)
IPR008266 (Tyr_kinase_AS.)
IPR011009 (Kinase-like_dom_sf.)
IPR013098 (Ig_I-set.)
IPR013783 (Ig-like_fold.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
IPR027290 (PDGFRA.)
IPR036179 (Ig-like_dom_sf.)
Pfam PF07679 (I-set)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure