Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors

Abstract The initial structure activity relationships around an isoindoline uHTS hit will be described. Information gleaned from ligand co-crystal structures allowed for rapid refinements in both MARK potency and kinase selectivity. These efforts allowed for the identification of a compound with properties suitable for use as an in vitro tool compound for validation studies on MARK as a viable target for Alzheimer’s disease. Download high-res image (27KB) Download full-size image