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The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Phenotypic Drug Discovery
Author(s) -
Quancard Jean,
Bach Anders,
Cox Brian,
Craft Russell,
Finsinger Dirk,
Guéret Stéphanie M.,
Hartung Ingo V.,
Laufer Stefan,
Messinger Josef,
Sbardella Gianluca,
Koolman Hannes F.
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100041
Subject(s) - drug discovery , phenotypic screening , chemical biology , computational biology , drug , chemistry , phenotype , biology , pharmacology , biochemistry , gene
Phenotypic drug discovery has a long track record of delivering innovative drugs and has received renewed attention in the last few years. The promise of this approach, however, comes with several challenges that should be addressed to avoid wasting time and resources on drugs with undesired modes of action or, worse, false‐positive hits. In this set of best practices, we go over the essential steps of phenotypic drug discovery and provide guidance on how to increase the chance of success in identifying validated and relevant chemical starting points for optimization: selecting the right assay, selecting the right compound screening library and developing appropriate hit validation assays. Then, we highlight the importance of initiating studies to determine the mode of action of the identified hits early and present the current state of the art.