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ID: ALA4425174

Journal: Bioorg Med Chem Lett

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

Authors: Wang H, Lawson JD, Scorah N, Kamran R, Hixon MS, Atienza J, Dougan DR, Sabat M.

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 1H-imidazo[4,5-c]pyridin-2(3H)-one drug like Alk5 inhibitors.

CiteXplore: 27460209

DOI: 10.1016/j.bmcl.2016.07.030