Affiliation: Johnson and Johnson Pharmaceutical Research and Development
Kuo G, Prouty C, Deangelis A, Shen L, O Neill D, Shah C, et al. Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. J Med Chem. 2003;46:4021-31 pubmed
..Both 28 and 29 displayed good potency in GS cell-based assay. Molecular docking studies were conducted in an attempt to rationalize the GSK-3beta selectivity of azaindolylmaleimides. ..
Kuo G, Wang A, Emanuel S, Deangelis A, Zhang R, Connolly P, et al. Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. J Med Chem. 2005;48:1886-900 pubmed
..Molecular docking studies were conducted in an attempt to rationalize the unexpected high VEGFR-2 selectivity of 15. ..