3CP9

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

Summary for 3CP9

• Entry DOI: 10.2210/pdb3cp9/pdb
• Related: 3CPB 3CPC
• Descriptor: Vascular endothelial growth factor receptor 2, 3-(2-aminoquinazolin-6-yl)-1-(3,3-dimethylindolin-6-yl)-4-methylpyridin-2(1H)-one (3 entities in total)
• Functional Keywords: receptor tyrosine kinase, angiogenesis, atp-binding, developmental protein, differentiation, glycoprotein, host-virus interaction, immunoglobulin domain, membrane, nucleotide-binding, phosphoprotein, polymorphism, transferase, transmembrane, tyrosine-protein kinase
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 73364.12

Authors

Whittington, D.A.,Long, A.M.,Rose, P.,Gu, Y.,Zhao, H. (deposition date: 2008-03-31, release date: 2008-06-17, Last modification date: 2024-02-21)

• Primary citation: Hu, E.,Tasker, A.,White, R.D.,Kunz, R.K.,Human, J.,Chen, N.,Burli, R.,Hungate, R.,Novak, P.,Itano, A.,Zhang, X.,Yu, V.,Nguyen, Y.,Tudor, Y.,Plant, M.,Flynn, S.,Xu, Y.,Meagher, K.L.,Whittington, D.A.,Ng, G.Y.; Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit.; J.Med.Chem., 51:3065-3068, 2008; PubMed: 18447379; DOI: 10.1021/jm800188g

Experimental method

X-RAY DIFFRACTION (2.5 Å)