890579-74-5Relevant articles and documents
Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase
Morwick, Tina,Büttner, Frank H.,Cywin, Charles L.,Dahmann, Georg,Hickey, Eugene,Jakes, Scott,Kaplita, Paul,Kashem, Mohammed A.,Kerr, Steven,Kugler, Stanley,Mao, Wang,Marshall, Daniel,Paw, Zofia,Shih, Cheng-Kon,Wu, Frank,Young, Erick
experimental part, p. 759 - 777 (2010/07/09)
Ahighly selective series of bisbenzamide inhibitors of Rho-associated coiled-coil forming protein kinase (ROCK) and a related ureidobenzamide series, both identified by high throughput screening (HTS), are described. Details of the hit validation and lead generation process, including structure-activity relationship (SAR) studies, a selectivity assessment, target-independent profiling (TIP) results, and an analysis of functional activity using a rat aortic ring assay are discussed. 2009 American Chemical Society.
