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Identifying Compound Efficacy Targets in Phenotypic Drug Discovery

Jenkins, Jeremy and Schirle, Markus (2016) Identifying Compound Efficacy Targets in Phenotypic Drug Discovery. Drug Discovery Today.


The identification of the efficacy target(s) for hits from phenotypic compound screens remains a key step to progress compounds into drug development. In addition to efficacy targets, the characterization of epistatic nodes influencing compound activity often facilitates the elucidation of the underlying mechanism of action, and, further, early determination of off-targets that cause potentially unwanted secondary phenotypes helps in assessing potential liabilities of a scaffold. This short review discusses the most important technologies currently available for characterizing the direct and indirect target space of bioactive compounds following phenotypic screening. We present a comprehensive strategy leveraging complementary approaches to balance individual strengths and weaknesses.

Item Type: Article
Date Deposited: 26 Apr 2016 23:45
Last Modified: 26 Apr 2016 23:45


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