European Lead Factory reaches milestone of 200,000 novel compounds

News
07 June 2018

Within a period of five years, the European Lead Factory (ELF) has reached one of its goals by completing the Public Compound Collection (PCC), comprising a commendable total of 200,000 novel compounds. The library production partners collaborated closely with the academic groups within ELF to reach this goal. The pan-European Public Chemistry Consortium is duly celebrating the achievement of this challenging objective.

Generating 200,000 innovative compounds from scratch

The European Lead Factory, a public-private partnership initiated by the Innovative Medicines Initiative (IMI), was established in 2013 to discover valuable lead candidates that were previously inaccessible – compounds that can result in the development of novel treatment options for patients. For the new biological space addressed, new chemical space needed to be explored. To achieve this, one key objective of ELF was to generate a library of 200,000 innovative compounds from scratch, through ELF’s own synthetic chemistry programme, which was supported by 7 SMEs and 11 academic partners - the Public Compound Collection.

Over thousand library design ideas were crowdsourced from academic and industrial chemists across Europe and were subjected to a rigorous selection process to end up in this unique compound collection. Library proposals were carefully evaluated by an experienced Library Selection Committee, for novelty, drug-like properties, diversity and synthetic tractability (detailed criteria). After this vigorous selection process, the production of the library compounds was initiated. Dimitrios Tzalis, Head of Chemistry at the European Lead Factory and CEO of Taros Chemicals, does not weary of emphasizing the merits and achievements of this joint pan-European effort: “All partners of the Public Chemistry Consortium made considerable collaborative efforts to reach this goal. It was a huge challenge to collate and translate those innovative library ideas into physical compounds. We all hope to have served and to further serve the wider European scientific community on their drug discovery research programmes to ultimately benefit the many patients in need worldwide.”

EFPIA and Public compound collection together form the unique 500,000-strong JECL

The PCC complements the 326,486 proprietary compounds of the partners from the European Federation of Pharmaceutical Industries and Associations (EFPIA), in order to build up the Joint European Compound Library (JECL) - a world-class chemistry asset and one of the core pillars of ELF. JECL has been screened and delivered more than 7,500 hits so far against 200 innovative targets, many of which were proven too challenging for in-house screening campaigns. In line with these impressive results, Prof Reuven Stein from University of Tel Aviv commented enthusiastically on the ELF compounds: “The results of the ELF screen exceeded all expectations. Our hit list included several compound classes of unprecedented potency, with low nanomolar activities not only on the target itself, but also in the cell-based assay”. His colleague Professor Micha Fridman added: “The compounds have the inhibition levels and physicochemical properties you would expect from an Active Pharmaceutical Ingredient.”

Library collection forms strong basis for outstanding results

So far, ELF’s successes include more than 70 publications, six notable patent applications, numerous new breakthroughs in a variety of therapeutic areas, and the foundation of two promising biotech start-ups specializing in neurodegeneration and metabolic diseases. During its short operational time frame, ELF has become instrumental in boosting early drug discovery in Europe. Its continuing goal is to offer unrivalled opportunities for the discovery of chemical starting points for new drug candidates – to public and private organisations – in order to address unmet medical needs.

Looking towards a bright future

Ton Rijnders, Head of Screening at the European Lead Factory and Scientific Leadership at Lygature looks ahead: “The future for ELF is bright. In the past five years, we’ve proved to our stakeholders that this setup works and is the way forward. We are actively pursuing continued funding, both from public sources such as EU funding, as well as from charities and other organizations, which may have active projects that could benefit from screening campaigns using ELF.” This compound collection is tailor-made for screening against innovative drug targets and we aim to continue offering this opportunity to the wider scientific drug discovery community. ELF aims to resume enrolment of new programmes by the end of 2018. This is a loud call for participation from scientists interested in screening their drug targets, by submitting their Intent to Apply.