1415484-35-3Relevant articles and documents
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors
Bhattacharya, Samit K.,Aspnes, Gary E.,Bagley, Scott W.,Boehm, Markus,Brosius, Arthur D.,Buckbinder, Leonard,Chang, Jeanne S.,Dibrino, Joseph,Eng, Heather,Frederick, Kosea S.,Griffith, David A.,Griffor, Matthew C.,Guimar?es, Cristiano R.W.,Guzman-Perez, Angel,Han, Seungil,Kalgutkar, Amit S.,Klug-Mcleod, Jacquelyn,Garcia-Irizarry, Carmen,Li, Jianke,Lippa, Blaise,Price, David A.,Southers, James A.,Walker, Daniel P.,Wei, Liuqing,Xiao, Jun,Zawistoski, Michael P.,Zhao, Xumiao
, p. 7523 - 7529 (2013/02/23)
Previous drug discovery efforts identified classical PYK2 kinase inhibitors such as 2 and 3 that possess selectivity for PYK2 over its intra-family isoform FAK. Efforts to identify more kinome-selective chemical matter that stabilize a DFG-out conformation of the enzyme are described herein. Two sub-series of PYK2 inhibitors, an indole carboxamide-urea and a pyrazole-urea have been identified and found to have different binding interactions with the hinge region of PYK2. These leads proved to be more selective than the original classical inhibitors.
