Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors

The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC(50) of ~3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacol...

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Main Authors: Feng, Yangbo, Yin, Yan, Weiser, Amiee, Griffin, Evelyn, Cameron, Michael D., Lin, Li, Ruiz, Claudia, Schürer, Stephan C., Inoue, Toshihiro, Rao, P. Vasanth, Schröter, Thomas, LoGrasso, Philip
Format: Artigo
Language:Inglês
Published: 2008
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC3708311/
https://ncbi.nlm.nih.gov/pubmed/18834107
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm800986w
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