Ontology highlight
ABSTRACT:
SUBMITTER: Bachovchin DA
PROVIDER: S-EPMC5953424 | biostudies-literature | 2014 Aug
REPOSITORIES: biostudies-literature
Bachovchin Daniel A DA Koblan Luke W LW Wu Wengen W Liu Yuxin Y Li Youhua Y Zhao Peng P Woznica Iwona I Shu Ying Y Lai Jack H JH Poplawski Sarah E SE Kiritsy Christopher P CP Healey Sarah E SE DiMare Matthew M Sanford David G DG Munford Robert S RS Bachovchin William W WW Golub Todd R TR
Nature chemical biology 20140706 8
The selectivity of an enzyme inhibitor is a key determinant of its usefulness as a tool compound or its safety as a drug. Yet selectivity is never assessed comprehensively in the early stages of the drug discovery process, and only rarely in the later stages, because technical limitations prohibit doing otherwise. Here, we report EnPlex, an efficient, high-throughput method for simultaneously assessing inhibitor potency and specificity, and pilot its application to 96 serine hydrolases. EnPlex a ...[more]