Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors
Hu Liu1, Cyrille Kuhn, Frederic Feru
1Department of Chemistry, Cambridge South Laboratories, Pfizer Inc., 620 Memorial Drive, Cambridge, MA 02139, USA. hu.liu@pfizer.com
Abstract:
By targeting an extended region of the conventional 'DFG-out' pocket of p38alpha, 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 p38alpha inhibitors with good potencies, and excellent selectivity.
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