Enhanced selectivity profile of pyrazole-urea based DFG-out p38α inhibitors
2010
Abstract 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.
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