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Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

Cheng H, Nair SK, Murray BW, … Kath JC · J Med Chem 2016 · J Med Chem 59(5):2005-24

EGFR & Mutants (Tyr), Covalent Inhibitors Tyrosine kinase Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling PhosphoSens

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