3CPC: Crystal structure of the VEGFR2 kinase domain in complex with a pyridone inhibitor

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.
PDB ID: 3CPCDownload
MMDB ID: 65006
PDB Deposition Date: 2008/3/31
Updated in MMDB: 2011/10
Experimental Method:
x-ray diffraction
Resolution: 2.4  Å
Source Organism:
Similar Structures:
Biological Unit for 3CPC: monomeric; determined by author and by software (PISA)
Molecular Components in 3CPC
Label Count Molecule
Protein (1 molecule)
Vascular Endothelial Growth Factor Receptor 2(Gene symbol: KDR)
Molecule annotation
Chemical (1 molecule)
* Click molecule labels to explore molecular sequence information.

Citing MMDB