Structure of PDB 3vo3 Chain A

Receptor sequence
>3vo3A (length=303) Species: 9606 (Homo sapiens) [Search protein sequence]
PLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTAT
CRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGP
LMVIVEFCKFGNLSTYLRSKRNEFVPYKDLYKDFLTLEHLICYSFQVAKG
MEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDA
RLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEF
CRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQ
ANA
3D structure
PDB3vo3 Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor
ChainA
Resolution1.52 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1028 A1030 R1032 N1033 D1046 K1055
Catalytic site (residue number reindexed from 1) D163 A165 R167 N168 D181 K190
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine kinase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 0KF A L840 V848 A866 K868 E885 L889 V916 F918 C919 G922 L1035 C1045 D1046 F1047 L29 V37 A55 K57 E74 L78 V105 F107 C108 G111 L170 C180 D181 F182 MOAD: ic50=1.4nM
PDBbind-CN: -logKd/Ki=8.85,IC50=1.4nM
BindingDB: IC50=1.8nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0004714 transmembrane receptor protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway

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Molecular Function
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Biological Process
External links
PDB RCSB:3vo3, PDBe:3vo3, PDBj:3vo3
PDBsum3vo3
PubMed23498918
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

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