446856-99-1Relevant academic research and scientific papers
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors
Feng, Yangbo,Yin, Yan,Weiser, Amiee,Griffin, Evelyn,Cameron, Michael D.,Lin, Li,Ruiz, Claudia,Schürer, Stephan C.,Inoue, Toshihiro,Rao, P. Vasanth,Schr?ter, Thomas,LoGrasso, Philip
supporting information; experimental part, p. 6642 - 6645 (2009/10/23)
The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 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. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.
