The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative: Phenotypic Drug Discovery
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The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative : Phenotypic Drug Discovery. / 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.
In: ChemMedChem, Vol. 16, No. 11, 2021, p. 1737-1740.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - The European Federation for Medicinal Chemistry and Chemical Biology (EFMC) Best Practice Initiative
T2 - Phenotypic Drug Discovery
AU - Quancard, Jean
AU - Bach, Anders
AU - Cox, Brian
AU - Craft, Russell
AU - Finsinger, Dirk
AU - Guéret, Stéphanie M.
AU - Hartung, Ingo V.
AU - Laufer, Stefan
AU - Messinger, Josef
AU - Sbardella, Gianluca
AU - Koolman, Hannes F.
N1 - This article also appears in: EuroMedChem Talents
PY - 2021
Y1 - 2021
N2 - 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.
AB - 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.
U2 - 10.1002/cmdc.202100041
DO - 10.1002/cmdc.202100041
M3 - Journal article
C2 - 33825353
VL - 16
SP - 1737
EP - 1740
JO - Farmaco
JF - Farmaco
SN - 1860-7179
IS - 11
ER -
ID: 272712245