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Target Report Card

Target Name and Classification

Target ID CHEMBL279
Target Type SINGLE PROTEIN
Preferred Name Vascular endothelial growth factor receptor 2
Synonyms CD_antigen=CD309 | FLK-1 | FLK1 | Fetal liver kinase 1 | KDR | KDR | Kinase insert domain receptor | Protein-tyrosine kinase receptor flk-1 | VEGFR-2 | VEGFR2 | Vascular endothelial growth factor receptor 2
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > kinase > protein kinase > tk protein kinase group > tyrosine protein kinase vegfr family

Target Components

Component Description Relationship Accession
Vascular endothelial growth factor receptor 2 SINGLE PROTEIN P35968

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2111434 VEGF-receptor 2 and Fibroblast growth factor receptor 2 SELECTIVITY GROUP
CHEMBL2095227 Vascular endothelial growth factor receptor PROTEIN FAMILY
CHEMBL2111375 Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2) SELECTIVITY GROUP
CHEMBL2111336 VEGF-receptor 2 and tyrosine-protein kinase SRC SELECTIVITY GROUP
CHEMBL2111409 Vascular endothelial growth factor receptor 2 and 3 (KDR and Flt-4) SELECTIVITY GROUP
CHEMBL2111440 VEGF-receptor 2 and PDGF-receptor beta (KDR and PDGFR beta) SELECTIVITY GROUP
CHEMBL2111480 Vascular endothelial growth factor receptor 1 and 2 (Flt-1 and KDR) SELECTIVITY GROUP
CHEMBL2111428 VEGF-receptor 2 and stem cell growth factor receptor (KDR and KIT) SELECTIVITY GROUP
CHEMBL2111439 VEGF-receptor 2 and Fibroblast growth factor receptor 1 PROTEIN FAMILY

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL1743062 RAMUCIRUMAB Vascular endothelial growth factor receptor 2 inhibitor 4 FDA
CHEMBL2103868 CABOZANTINIB S-MALATE Vascular endothelial growth factor receptor 2 inhibitor 4 DailyMed PubMed PubMed
CHEMBL274654 ORANTINIB Vascular endothelial growth factor receptor 2 inhibitor 3 PubMed
CHEMBL608533 MIDOSTAURIN Vascular endothelial growth factor receptor 2 inhibitor 3 PubMed PubMed
CHEMBL3545414 Apatinib Vascular endothelial growth factor receptor 2 inhibitor 3 Other PubMed PubMed
CHEMBL52885 ENMD-981693 Vascular endothelial growth factor receptor 2 inhibitor 2 Other
CHEMBL253969 OSI-632 Vascular endothelial growth factor receptor 2 inhibitor 2 PubMed PubMed
CHEMBL403989 TG100-801 Vascular endothelial growth factor receptor 2 inhibitor 2 PubMed PubMed PubMed
CHEMBL482968 ENMD-2076 Vascular endothelial growth factor receptor 2 inhibitor 2 Other PubMed PubMed
CHEMBL558752 CHIR-265 Vascular endothelial growth factor receptor 2 inhibitor 2 PubMed PubMed
CHEMBL587723 AEE-788 Vascular endothelial growth factor receptor 2 inhibitor 2 PubMed
CHEMBL2079588 TELATINIB Vascular endothelial growth factor receptor 2 inhibitor 2 PubMed PubMed
CHEMBL3039525 GOLVATINIB Vascular endothelial growth factor receptor 2 inhibitor 2 PubMed PubMed
CHEMBL3545021 Anlotinib Vascular endothelial growth factor receptor 2 inhibitor 2 ClinicalTrials Other
CHEMBL3545026 Famitinib Vascular endothelial growth factor receptor 2 inhibitor 2 ClinicalTrials DOI PubMed
CHEMBL3545155 JI-101 Vascular endothelial growth factor receptor 2 inhibitor 2 DOI PubMed
CHEMBL482967 CYC-116 Vascular endothelial growth factor receptor 2 inhibitor 1 PubMed PubMed
CHEMBL3544937 ZD-4190 Vascular endothelial growth factor receptor 2 inhibitor 1 PubMed
CHEMBL3545050 BMS-817378 Vascular endothelial growth factor receptor 2 inhibitor 1 DOI
CHEMBL3545088 Puquitinib Vascular endothelial growth factor receptor 2 inhibitor 1 DOI PubMed PubMed
CHEMBL3545119 BMS-794833 Vascular endothelial growth factor receptor 2 inhibitor 1 Other
CHEMBL3545136 PF-00337210 Vascular endothelial growth factor receptor 2 inhibitor 1 Other PubMed
CHEMBL3545144 TAS-115 Vascular endothelial growth factor receptor 2 inhibitor 1 Other PubMed
CHEMBL3545365 ALTIRATINIB Vascular endothelial growth factor receptor 2 inhibitor 1 Other PubMed
CHEMBL3545416 Henatinib Vascular endothelial growth factor receptor 2 inhibitor 1 DOI Other
CHEMBL3545427 CM-082 Vascular endothelial growth factor receptor 2 inhibitor 1 Other
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000128052
Ensembl ENSG00000128052
GO Cellular Component GO:0005576 (extracellular region)
GO:0005634 (nucleus)
GO:0005737 (cytoplasm)
GO:0005768 (endosome)
GO:0005769 (early endosome)
GO:0005783 (endoplasmic reticulum)
GO:0005794 (Golgi apparatus)
GO:0005886 (plasma membrane)
GO:0005887 (integral component of plasma membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0016023 (cytoplasmic, membrane-bounded vesicle)
GO:0030054 (cell junction)
GO:0031410 (cytoplasmic vesicle)
GO:0045121 (membrane raft)
GO:0097443 (sorting endosome)
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:0004716 (receptor signaling protein tyrosine kinase activity)
GO:0005021 (vascular endothelial growth factor-activated receptor activity)
GO:0005178 (integrin binding)
GO:0005515 (protein binding)
GO:0005524 (ATP binding)
GO:0016301 (kinase activity)
GO:0016740 (transferase activity)
GO:0019838 (growth factor binding)
GO:0038085 (vascular endothelial growth factor binding)
GO:0051879 (Hsp90 protein binding)
GO Biological Process GO:0001525 (angiogenesis)
GO:0001570 (vasculogenesis)
GO:0001934 (positive regulation of protein phosphorylation)
GO:0001938 (positive regulation of endothelial cell proliferation)
GO:0002042 (cell migration involved in sprouting angiogenesis)
GO:0003158 (endothelium development)
GO:0006468 (protein phosphorylation)
GO:0007169 (transmembrane receptor protein tyrosine kinase signaling pathway)
GO:0007275 (multicellular organism development)
GO:0008284 (positive regulation of cell proliferation)
GO:0008360 (regulation of cell shape)
GO:0010595 (positive regulation of endothelial cell migration)
GO:0014068 (positive regulation of phosphatidylinositol 3-kinase signaling)
GO:0016032 (viral process)
GO:0016239 (positive regulation of macroautophagy)
GO:0016310 (phosphorylation)
GO:0018108 (peptidyl-tyrosine phosphorylation)
GO:0023014 (signal transduction by protein phosphorylation)
GO:0030154 (cell differentiation)
GO:0030198 (extracellular matrix organization)
GO:0030335 (positive regulation of cell migration)
GO:0035162 (embryonic hemopoiesis)
GO:0035584 (calcium-mediated signaling using intracellular calcium source)
GO:0035924 (cellular response to vascular endothelial growth factor stimulus)
GO:0038033 (positive regulation of endothelial cell chemotaxis by VEGF-activated vascular endothelial growth factor receptor signaling pathway)
GO:0038083 (peptidyl-tyrosine autophosphorylation)
GO:0043066 (negative regulation of apoptotic process)
GO:0043410 (positive regulation of MAPK cascade)
GO:0045766 (positive regulation of angiogenesis)
GO:0046777 (protein autophosphorylation)
GO:0048010 (vascular endothelial growth factor receptor signaling pathway)
GO:0050927 (positive regulation of positive chemotaxis)
GO:0051770 (positive regulation of nitric-oxide synthase biosynthetic process)
GO:0051894 (positive regulation of focal adhesion assembly)
GO:0051901 (positive regulation of mitochondrial depolarization)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
GO:0090141 (positive regulation of mitochondrial fission)
GO:2000352 (negative regulation of endothelial cell apoptotic process)
GO:2001214 (positive regulation of vasculogenesis)
Wikipedia Kinase_insert_domain_receptor

Target Cross References - Protein

canSAR P35968
Human Protein Atlas ENSG00000128052
IntAct P35968
Guide to Pharmacology 1813
Open Targets ENSG00000128052
PharmGKB PA30086
Pharos P35968 (Tclin)
Reactome R-HSA-194306 (Neurophilin interactions with VEGF and VEGFR.)
R-HSA-195399 (VEGF binds to VEGFR leading to receptor dimerization.)
R-HSA-216083 (Integrin cell surface interactions.)
R-HSA-3928663 (EPHA-mediated growth cone collapse.)
R-HSA-4420097 (VEGFA-VEGFR2 Pathway.)
R-HSA-5218921 (VEGFR2 mediated cell proliferation.)
UniProt A2RRS0 B5A925 C5IFA0 O60723 P35968 Q14178

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.)
IPR009136 (VEGFR2_rcpt.)
IPR011009 (Kinase-like_dom.)
IPR013098 (Ig_I-set.)
IPR013151 (Immunoglobulin.)
IPR013783 (Ig-like_fold.)
IPR017441 (Protein_kinase_ATP_BS.)
IPR020635 (Tyr_kinase_cat_dom.)
Pfam PF00047 (ig)
PF07679 (I-set)
PF07714 (Pkinase_Tyr)

Target Cross References - Structure

PDBe 1VR2 1Y6A 1Y6B 1YWN 2OH4 2P2H 2P2I 2QU5 2QU6 2RL5 2X1W 2X1X 2XIR 3B8Q 3B8R 3BE2 3C7Q 3CJF 3CJG 3CP9 3CPB 3CPC 3DTW 3EFL More...
CREDO 1VR2 1Y6A 1Y6B 1YWN 2OH4 2P2H 2P2I 2QU5 2QU6 2RL5 2X1W 2X1X 2XIR 3B8Q 3B8R 3BE2 3C7Q 3CJF 3CJG 3CP9 3CPB 3CPC 3DTW 3EFL More...
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