Enhanced selectivity profile of pyrazole-urea based DFG-out p38α inhibitors

By targeting an extended region of the conventional ‘DFG-out’ pocket of p38α, while minimizing interactions with the specificity pocket and eliminating interactions with the adenine binding site, we are able to design and synthesize a number of pyrazole-urea based DFG-out p38α inhibitors with good potencies, and excellent selectivity.

The development of potent and selective p38 inhibitor 11 is reported.Figure optionsDownload as PowerPoint slide