2,3,5-Trisubstituted pyridines have been designed as potent AKT inhibitors that are selective against ROCK1 based on the comparison between AKT and ROCK1 structures. Substitution at the 2-position of the core pyridine is the key element to provide selectivity against ROCK1. An X-ray co-crystal structure of 9p in PKA supports the proposed rationale of ROCK1 selectivity.
Susan L Strum合作论文数1Ren Xie合作论文数1Ds Yamashita合作论文数1Heerding Dirk A合作论文数1Jin Zeng合作论文数1Hong Lin合作论文数1
Juan I. Luengo合作论文数Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals1Elisabeth Minthorn合作论文数1Nelson Rhodes合作论文数1Patricia A. Elkins合作论文数1
Wenyong Wang合作论文数United Research Laboratories, LLC1Anthony E. Choudhry合作论文数1Victoria B. Knick合作论文数1Nestor O. Concha合作论文数1Zhihong Lai合作论文数1
Edgar Wood合作论文数GlaxoSmithKline1
