Discovery of SARxxxx92, a pan-PIM kinase Inhibitor, efficacious in a KG1 tumor model.

Abstract N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chemical properties allowed us to solve inherent hERG and permeability liabilities, and provided compound 27, which subsequently impacted KG-1 tumor growth in a mouse model.