Structure of PDB 3cp9 Chain A

Receptor sequence
>3cp9A (length=288) Species: 9606 (Homo sapiens) [Search protein sequence]
AERLPYDASKWEFPRDRLKLGKPLQVIEADAFGIDKTATCRTVAVKMLKE
GATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVITEFCKFG
NLSTYLRSKRNEFVPYKVAPEDLYKDFLTLEHLICYSFQVAKGMEFLASR
KCIHRDLAARNILLSEKNVVKICDFGLPLKWMAPETIFDRVYTIQSDVWS
FGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML
DCWHGEPSQRPTFSELVEHLGNLLQANAQQDRHHHHHH
3D structure
PDB3cp9 Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit.
ChainA
Resolution2.5 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
Catalytic site (residue number reindexed from 1) D156 A158 R160 N161 D174
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 C19 A L840 V848 A866 K868 E885 L889 V898 T916 C919 L1035 C1045 D1046 F1047 L24 V26 A44 K46 E63 L67 V76 T94 C97 L163 C173 D174 F175 PDBbind-CN: -logKd/Ki=7.32,IC50=0.048uM
BindingDB: IC50=48nM
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

View graph for
Biological Process
External links
PDB RCSB:3cp9, PDBe:3cp9, PDBj:3cp9
PDBsum3cp9
PubMed18447379
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

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