Structure of PDB 3b8q Chain A

Receptor sequence
>3b8qA (length=292) Species: 9606 (Homo sapiens) [Search protein sequence]
ERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAV
KMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVITE
FCKFGNLSTYLRSKRNEFVPYKVAPEDLYKDFLTLEHLICYSFQVAKGME
FLASRKCIHRDLAARNILLSEKNVVKICDFLPLKWMAPETIFDRVYTIQS
DVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMY
QTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDRHHHHHH
3D structure
PDB3b8q Naphthamides as Novel and Potent Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitors: Design, Synthesis and Evaluation
ChainA
Resolution2.75 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) D161 A163 R165 N166 D179
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 900 A L840 V848 A866 K868 E885 L889 T916 C919 L1035 C1045 D1046 F1047 L23 V31 A49 K51 E68 L72 T99 C102 L168 C178 D179 F180 PDBbind-CN: -logKd/Ki=9.30,IC50=0.5nM
BindingDB: IC50=0.480000nM
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:3b8q, PDBe:3b8q, PDBj:3b8q
PDBsum3b8q
PubMed18324761
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

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