Q4 · MEDICINE
Article
Author: Batchelor, Joseph D ; Wang, Anlai ; Sun, Frank ; Huang, Shih-Min A ; Erdman, Paul ; Fire, Luke ; Hebert, Andrew ; Maniar, Sachin ; Levit, Mikhail ; Patel, Vinod F ; Czekaj, Mark ; Barberis, Claude ; Liu, Jinyu ; Tserlin, Elina ; Pribish, James
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.