Phenotypic Drug Discovery

Recent years have seen a renaissance of Phenotypic drug discovery (PPD) with novel screening technologies and a track record that is thought to match or surpass that of target-centric approaches. We present a view on best practices to consider when running phenotypic drug discovery campaigns to increase the chance of success of these black box approachs.

Successful phenotypic drug discovery relies on high-quality hits, which are best generated following our Hit Generation guidelines, and refined using Hit-to-Lead Optimization principles. To ensure the validity of assay outcomes, it’s essential to work with well-characterized compounds as outlined in our Best Practices for Validating Chemical Probes.

Please cite the EFMC Best Practices in Medicinal Chemistry WG work as following (please include both):

1. J. Quancard, A. Bach, B. Cox, R. Craft, D. Finsinger, S. M. Guéret, I. V. Hartung, S. Laufer, J. Messinger, G. Sbardella, H. F. Koolman, ChemMedChem2021, 16, 1737. https://doi.org/10.1002/cmdc.202100041;
2. The material (webinars, slide decks and case studies) is freely accessible for personal use or for use in further training or teaching material from the EFMC website https://www.efmc.info/phenotypic-drug-discovery