5EM8: Egfr Kinase Domain With Pyridone Compound 13: 4-[(2-methoxyphenyl) Amino]-~{n}-[4-(4-methylpiperazin-1-yl)phenyl]-2-oxidanylidene-1~{h}- Pyridine-3-carboxamide

The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with high levels of selectivity over wtEGFR and the broader kinome is described herein.
PDB ID: 5EM8Download
MMDB ID: 135208
PDB Deposition Date: 2015/11/5
Updated in MMDB: 2015/12
Experimental Method:
x-ray diffraction
Resolution: 2.8  Å
Source Organism:
Similar Structures:
Biological Unit for 5EM8: monomeric; determined by author and by software (PISA)
Molecular Components in 5EM8
Label Count Molecule
Protein (1 molecule)
Epidermal Growth Factor Receptor(Gene symbol: EGFR)
Molecule annotation
Chemical (1 molecule)
* Click molecule labels to explore molecular sequence information.

Citing MMDB