Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
EGFR (Tyr) wild-type & oncogenic mutants: exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), Covalent Inhibitors
Tyrosine kinase
Covalent inhibitor kineticsInhibitor discovery & SARSelectivity & kinome profiling
PhosphoSens
