title: The development of benzimidazoles as selective rho kinase inhibitors.
abstract: Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC(50)<10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
authors.affiliation: Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA.
authors.forename: E Hampton
authors.initials: EH
authors.lastname: Sessions
authors.forename: Michael
authors.initials: M
authors.lastname: Smolinski
authors.forename: Bo
authors.initials: B
authors.lastname: Wang
authors.forename: Bozena
authors.initials: B
authors.lastname: Frackowiak
authors.forename: Sarwat
authors.initials: S
authors.lastname: Chowdhury
authors.forename: Yan
authors.initials: Y
authors.lastname: Yin
authors.forename: Yen Ting
authors.initials: YT
authors.lastname: Chen
authors.forename: Claudia
authors.initials: C
authors.lastname: Ruiz
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.forename: Jennifer
authors.initials: J
authors.lastname: Pocas
authors.forename: Thomas
authors.initials: T
authors.lastname: Schröter
authors.forename: Michael D
authors.initials: MD
authors.lastname: Cameron
authors.forename: Philip
authors.initials: P
authors.lastname: LoGrasso
authors.forename: Yangbo
authors.initials: Y
authors.lastname: Feng
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Bannister
mesh_terms: D001562:Benzimidazoles / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
chemical_list: D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D054460:rho-Associated Kinases