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ACS Med Chem Lett. 2015 Dec 17;7(1):100-4. doi: 10.1021/acsmedchemlett.5b00428. eCollection 2016 Jan 14.

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

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Genentech , South San Francisco, California 94080, United States.
Argenta, Early Discovery Charles River , 7/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, United Kingdom.


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.


Mutant EGFR; T790M; noncovalent; pyridone

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