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

Yangbo Feng, Yan Yin, Amiee Weiser, Evelyn Griffin, Michael D Cameron, Li Lin, Claudia Ruiz, Stephan C Schürer, Toshihiro Inoue, P Vasanth Rao, Thomas Schröter, Philip Lograsso

J Med Chem. 2008 Nov 13;51(21):6642-5.

PMID: 18834107

Abstract:

The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC 50 of approximately 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. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP1072959671 SR 3677 SR 3677 1072959-67-1 Price
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