3CPC
Crystal structure of the VEGFR2 kinase domain in complex with a pyridone inhibitor
Summary for 3CPC
| Entry DOI | 10.2210/pdb3cpc/pdb |
| Related | 3CP9 3CPB |
| Descriptor | Vascular endothelial growth factor receptor 2, 3-(2-aminoquinazolin-6-yl)-4-methyl-1-[3-(trifluoromethyl)phenyl]pyridin-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, transferase, transmembrane, tyrosine-protein kinase |
| Biological source | Homo sapiens (Human) More |
| Total number of polymer chains | 2 |
| Total formula weight | 73361.90 |
| 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: 2024-11-06) |
| 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 Cited by PubMed Abstract: Inhibition of c-Kit has the potential to treat mast cell associated fibrotic diseases. We report the discovery of several aminoquinazoline pyridones that are potent inhibitors of c-Kit with greater than 200-fold selectivity against KDR, p38, Lck, and Src. In vivo efficacy of pyridone 16 by dose-dependent inhibition of histamine release was demonstrated in a rodent pharmacodynamic model of mast cell activation. PubMed: 18447379DOI: 10.1021/jm800188g PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (2.4 Å) |
Structure validation
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