Promiscuity and selectivity in covalent enzyme inhibition: a systematic study of electrophilic fragments.

Abstract

Covalent ligand-target interactions offer significant pharmacological advantages. However, off-target reactivity of the reactive groups, which usually have electrophilic properties, must be minimized, and the selectivity of irreversible inhibitors is a crucial requirement. We therefore performed a systematic study to determine the selectivity of several… (More)
DOI: 10.1021/jm5006918

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