1232836-35-9Relevant articles and documents
Discovery of type II inhibitors of tgfβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)
Tan, Li,Nomanbhoy, Tyzoon,Gurbani, Deepak,Patricelli, Matthew,Hunter, John,Geng, Jiefei,Herhaus, Lina,Zhang, Jianming,Pauls, Eduardo,Ham, Youngjin,Choi, Hwan Geun,Xie, Ting,Deng, Xianming,Buhrlage, Sara J.,Sim, Taebo,Cohen, Philip,Sapkota, Gopal,Westover, Kenneth D.,Gray, Nathanael S.
, p. 183 - 196 (2015/03/04)
We developed a pharmacophore model for type II inhibitors that was used to guide the construction of a library of kinase inhibitors. Kinome-wide selectivity profiling of the library resulted in the identification of a series of 4-substituted 1H-pyrrolo[2,
Broad spectrum alkynyl inhibitors of T315I Bcr-Abl
Deng, Xianming,Lim, Sang Min,Zhang, Jianming,Gray, Nathanael S.
scheme or table, p. 4196 - 4200 (2010/08/22)
A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC50 of less than 1 nM against wild-type Bcr-Abl and an EC50 of 10 nM again
