Structure of PDB 3cjf Chain A

Receptor sequence
>3cjfA (length=281) Species: 9606 (Homo sapiens) [Search protein sequence]
CERLPYDASKWEFPRDRLNLGKPLGRGAFGQVIEADAFGIDKTATCRTVA
VKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIV
EFCKFGNLSTYLRSKRNEFVPYKKDFLTLEHLICYSFQVAKGMEFLASRK
CIHRDLAARNILLSEKNVVKICDLARDIYKPLKWMAPETIFDRVYTIQSD
VWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQ
TMLDCWHGEPSQRPTFSELVEHLGNLLQANA
3D structure
PDB3cjf Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
ChainA
Resolution2.15 Å
3D
structure
Catalytic site residues are labeled in the structure
[Spin on]
[Spin off]
[Reset orientation]

[High quality]
[Low quality]

[White background]
[Black background]

[Download]
[Download structure with residue number starting from 1]
Enzymatic activity
Catalytic site (original residue number in PDB) D1026 A1028 R1030 N1031 D1044 K1053
Catalytic site (residue number reindexed from 1) D155 A157 R159 N160 D173 K180
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 SAV A L838 A864 F916 C917 K918 G920 L1033 L24 A50 F102 C103 K104 G106 L162 MOAD: ic50=6.3nM
PDBbind-CN: -logKd/Ki=8.20,IC50=6.3nM
BindingDB: IC50=6.3nM
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:3cjf, PDBe:3cjf, PDBj:3cjf
PDBsum3cjf
PubMed18620382
UniProtP35968|VGFR2_HUMAN Vascular endothelial growth factor receptor 2 (Gene Name=KDR)

[Back to BioLiP]