Reference Module in Chemistry, Molecular Sciences and Chemical Engineering: The European Lead Factory: a Collaborative Approach to Lead Discovery

F.Giordanetto, P.Jones, A.Nelson, J.Benningshof, G.Müller, A.Pannifer, S.van Boeckel, D.Tzalis

Comprehensive Medicinal Chemistry III 2017, pp 505-519;

The European Lead Factory (ELF) provides preclinical researchers in Europe with an integrated hit identification and evaluation platform to seed the lead generation phase of the drug discovery process. It combines a unique compound collection, ultra-high-throughput screening infrastructure, and hit follow-up capabilities to advance research projects from both private companies and publicly funded researchers. Confidentiality and intellectual property protection in such a competitive phase are ensured by an “honest data broker” data management system. The compound collection originates from private pharmaceutical company chemical repositories and is routinely augmented by innovative, high-quality compound libraries via a crowd-sourcing mechanism involving academic and industrial chemistry research groups. This novel compound file is screened against a wide range of biochemical readouts and its output is triaged according to project-specific screening cascades by expert biologists and medicinal chemists of the ELF screening center. As such, the ELF is a unique, collaborative lead generation engine that has so far resulted in the acceptance of 18 qualified hit lists from successfully completed high-throughput screening and hit evaluation campaigns, and the production of more than 100,000 novel, high-quality library compounds to complement the 327,000 compounds contributed by the pharmaceutical companies.

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