2. Academic Validation
  3. Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase

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

  • J Med Chem. 2010 Jan 28;53(2):759-77. doi: 10.1021/jm9014263.
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

Affiliation

  • 1 Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, Connecticut 06801-0368, USA. tmorwick@rdg.boehringer-ingelheim.com
PMID: 20000469 DOI: 10.1021/jm9014263
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.

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