552332-08-8Relevant articles and documents
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity
Lin, Hong,Yamashita, Dennis S.,Zeng, Jin,Xie, Ren,Wang, Wenyong,Nidarmarthy, Sirishkumar,Luengo, Juan I.,Rhodes, Nelson,Knick, Victoria B.,Choudhry, Anthony E.,Lai, Zhihong,Minthorn, Elisabeth A.,Strum, Susan L.,Wood, Edgar R.,Elkins, Patricia A.,Concha, Nestor O.,Heerding, Dirk A.
scheme or table, p. 673 - 678 (2010/07/05)
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.
Kinase inhibitors
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, (2008/06/13)
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.