Structure of PDB 3cpb Chain A

Receptor sequence
>3cpbA (length=285) Species: 9606 (Homo sapiens) [Search protein sequence]
RLPYDASKWEFPRDRLKLGKPLQVIEADAFGIDKTATCRTVAVKMLKEGA
THSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVITEFCKFGNL
STYLRSKRNEFVPYKVAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKC
IHRDLAARNILLSEKNVVKICDFLPLKWMAPETIFDRVYTIQSDVWSFGV
LLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCW
HGEPSQRPTFSELVEHLGNLLQANAQQDRHHHHHH
3D structure
PDB3cpb Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit.
ChainA
Resolution2.7 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) D154 A156 R158 N159 D172
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 C92 A A866 K868 E885 V914 T916 F918 C919 L1035 C1045 D1046 F1047 A42 K44 E61 V90 T92 F94 C95 L161 C171 D172 F173 PDBbind-CN: -logKd/Ki=4.60,IC50=25uM
BindingDB: IC50=>25000nM
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

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:3cpb, PDBe:3cpb, PDBj:3cpb
PDBsum3cpb
PubMed18447379
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

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