Structure of PDB 3b8r Chain A

Receptor sequence
>3b8rA (length=289) Species: 9606 (Homo sapiens) [Search protein sequence]
ERLPYDASKWEFPRDRLKLGKPLGQVIEADAFGIDKTATCRTVAVKMLKE
GATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVITEFCKFG
NLSTYLRSKRNEFVPYKVAPEDLYKDFLTLEHLICYSFQVAKGMEFLASR
KCIHRDLAARNILLSEKNVVKICDFGLLPLKWMAPETIFDRVYTIQSDVW
SFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTM
LDCWHGEPSQRPTFSELVEHLGNLLQANAQQDRHHHHHH
3D structure
PDB3b8r Evaluation of a Series of Naphthamides as Potent, Orally Active Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitors
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) 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 887 A L840 V848 A866 K868 E885 L889 T916 C919 L1035 C1045 D1046 F1047 L23 V26 A44 K46 E63 L67 T94 C97 L163 C173 D174 F175 PDBbind-CN: -logKd/Ki=9.22,IC50=0.6nM
BindingDB: IC50=0.600000nM
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:3b8r, PDBe:3b8r, PDBj:3b8r
PDBsum3b8r
PubMed18324759
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

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