The development of benzimidazoles as selective rho kinase inhibitors.
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).
Sessions
E Hampton
EH
Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA.
Smolinski
Michael
M
Wang
Bo
B
Frackowiak
Bozena
B
Chowdhury
Sarwat
S
Yin
Yan
Y
Chen
Yen Ting
YT
Ruiz
Claudia
C
Lin
Li
L
Pocas
Jennifer
J
Schröter
Thomas
T
Cameron
Michael D
MD
LoGrasso
Philip
P
Feng
Yangbo
Y
Bannister
Thomas D
TD
D001562:Benzimidazoles / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D054460:rho-Associated Kinases