Het-PDB Navi2 (PDB: 3CPC)

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Ligands
Code	Name		Style	Show	Link
C52	3-(2-aminoquinazolin-6-yl)-4-methyl-1-[3-(trifluoromethyl)phenyl]pyridin-2(1h)-one				PoSSuM

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Download interaction data: 3CPC

Code :

3CPC PDBj RCSB PDB PDBe

Header :

TRANSFERASE

Title :

Crystal structure of the VEGFR2 kinase domain in complex with a pyridone inhibitor

Release Data :

2008-06-17

Compound :

mol_id	molecule	chains	synonym
1	Vascular endothelial growth factor receptor 2	A,B	VEGFR-2, Kinase insert domain receptor, Protein-tyrosine kinase receptor Flk-1, CD309 antigen
	ec: 2.7.10.1 fragment: PROTEIN KINASE DOMAIN, RESIDUES 940-989 DELETED mutation: C817A, V916T, E990V

Source :

mol_id	organism_scientific	organism_common	expression_system
1	Homo sapiens (taxid:9606)	Human	Trichoplusia ni (taxid:7111)
	gene: KDR, FLK1 expression_system_vector_type: baculovirus

Authors :

Whittington, D.A., Long, A.M., Rose, P., Gu, Y., Zhao, H.

Keywords :

receptor tyrosine kinase, angiogenesis, ATP-binding, Developmental protein, Differentiation, Glycoprotein, Host-virus interaction, Immunoglobulin domain, Membrane, Nucleotide-binding, Phosphoprotein, Transferase, Transmembrane, Tyrosine-protein kinase

Exp. method :

X-RAY DIFFRACTION ( 2.40 Å )

Citation :

Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit.

Hu, E.,Tasker, A.,White, R.D. et al.
(2008) J.Med.Chem. 51 : 3065 - 3068

PubMed: 18447379
DOI: 10.1021/jm800188g

Chain :

A, B

UniProt :

P35968 (VGFR2_HUMAN)

Reaction:	EC:	Evidence:
Reaction:	Physiological Direction:	Evidence:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein]	2.7.10.1	PROSITE-ProRule:PRU10028, PubMed:10037737, PubMed:10102632
	-	PROSITE-ProRule:PRU10028, PubMed:10037737, PubMed:10102632

PDB ID: 3CPC

Hetero Atom Contents

Structure summary

Reaction