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ID: ALA1155525

Journal: Bioorg Med Chem Lett

Title: Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.

Authors: Wu F, Büttner FH, Chen R, Hickey E, Jakes S, Kaplita P, Kashem MA, Kerr S, Kugler S, Paw Z, Prokopowicz A, Shih CK, Snow R, Young E, Cywin CL.

Abstract: Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of potent leads such as 22 which successfully demonstrated an early in vivo proof of concept for anti-hypertensive activity.

CiteXplore: 20462760

DOI: 10.1016/j.bmcl.2010.04.070