Structure of PDB 3vhe Chain A

Receptor sequence
>3vheA (length=303) Species: 9606 (Homo sapiens) [Search protein sequence]
LPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTA
TCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGG
PLMVIVEFCKFGNLSTYLRSKRNEFVPYKDLYKDFLTLEHLICYSFQVAK
GMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKAR
LPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFC
RRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQA
NAQ
3D structure
PDB3vhe Design, synthesis, and evaluation of 5-methyl-4-phenoxy-5H-pyrrolo[3,2-d]pyrimidine derivatives: novel VEGFR2 kinase inhibitors binding to inactive kinase conformation.
ChainA
Resolution1.55 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 R1032 N1033 D1046 K1055
Catalytic site (residue number reindexed from 1) D164 R168 N169 D182 K191
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 42Q A L840 V848 A866 K868 E885 L889 V916 F918 C919 L1035 C1045 D1046 F1047 L30 V38 A56 K58 E75 L79 V106 F108 C109 L171 C181 D182 F183 MOAD: ic50=6.2nM
PDBbind-CN: -logKd/Ki=8.21,IC50=6.2nM
BindingDB: Ki=4.6nM,Kd=19nM,IC50=4.7nM
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:3vhe, PDBe:3vhe, PDBj:3vhe
PDBsum3vhe
PubMed20833055
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

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