双环分子
化学
效力
内酰胺
立体化学
药理学
生物化学
体外
生物
作者
Michael R. Witten,Liangxing Wu,Cheng Tsung Lai,Kanishk Kapilashrami,Michelle Pusey,Karen Gallagher,Yaoyu Chen,Wenqing Yao
标识
DOI:10.1016/j.bmcl.2021.128452
摘要
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.
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