Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors

Abstract Using SBDD, a series of 4-amino-7-azaindoles were discovered as a novel class of Alk5 inhibitors that are potent in both Alk5 enzymatic and cellular assays. Subsequently a ring cyclization strategy was utilized to improve ADME properties leading to the discovery of a series of 1 H -imidazo[4,5- c ]pyridin-2(3 H )-one drug like Alk5 inhibitors.