Inhibition of ALK2 with bicyclic pyridyllactams.
Basic Information
ID: ALA5131405
Journal: Bioorg Med Chem Lett
Title: Inhibition of ALK2 with bicyclic pyridyllactams.
Authors: Witten MR, Wu L, Lai CT, Kapilashrami K, Pusey M, Gallagher K, Chen Y, Yao W.
Abstract: Activin receptor-like kinase 2 (ALK2) has been implicated as a key target in multiple rare diseases. Herein, we describe the design of a novel bicyclic lactam series of potent and selective ALK2 inhibitors. This manuscript details an improvement in potency of two orders of magnitude from the initial bicyclic structure as well as a two-fold improvement in cellular potency from the original monocyclic inhibitor. Furthermore, we provide a detailed strategy for progressing this project in the future.
CiteXplore: 34780900
DOI: 10.1016/j.bmcl.2021.128452
Patent ID: ┄