Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2010 Jan 28;53(2):759-77.
doi: 10.1021/jm9014263.

Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase

Tina Morwick  1 , Frank H Büttner, Charles L Cywin, Georg Dahmann, Eugene Hickey, Scott Jakes, Paul Kaplita, Mohammed A Kashem, Steven Kerr, Stanley Kugler, Wang Mao, Daniel Marshall, Zofia Paw, Cheng-Kon Shih, Frank Wu, Erick Young
Affiliations

Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase

Tina Morwick et al. J Med Chem. .

Abstract

A highly 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.

PubMed Disclaimer

MeSH terms

LinkOut - more resources