A Key/Cornerstone Scientific Publication Confirms the Truly Unique Nature of the Public Screening Collection Assembled in the European Lead Factory

Dec 15, 2015, 08:35 ET from Edelris, Mercachem, Sygnature, Syncom, Taros

LYON, France, December 15, 2015 /PRNewswire/ --

A scientific publication released this month in "Drug Discovery Today" (http://authors.elsevier.com/a/1R-An4r9RkJ4rh) details the results of a benchmark study performed on the screening collection being currently designed and synthesised within the European Lead Factory Consortium.

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The European Lead Factory, initiated in 2013, is a €196 million collaborative venture financed by the Innovative Medicines Initiative (IMI) and is aimed at boosting the initial phases of the drug discovery process. Pharmaceutical companies, academic groups and ten small and medium-sized enterprises (SMEs) have formed a pan-European consortium to address the challenge of delivering an innovative, publicly-accessible, screening deck of synthetically-tractable compounds, named the Public Compound Collection (PCC).  As part of the EU Lead Factory, the seven participating pharmaceutical companies have contributed over 300,000 chemical compounds from their corporate chemical collections and the academic groups and five chemistry SME members will deliver ~200,000 compounds from untapped areas of biologically-relevant chemical space (https://www.europeanleadfactory.eu/).

In March 2015 an important milestone was passed, namely the synthesis of the first 50K compounds. To mark this achievement a diversity analysis was performed on this statistically significant number. The results have now been published in "Drug Discovery Today" and a comparison made with three other pertinent and accessible compound collections.  As anticipated, the compounds within the PCC have good Lipinski-like properties.  What is particularly notable, in contrast to other collections, is the high proportion of sp3 centres (Fsp3 character) and the fact that 85% of the compounds are chiral - this has yielded compounds with a high degree of 3D shape. In addition, over half of the molecular frameworks within the PCC are unique, thereby affording real potential to explore new areas of biological space, which it has not been feasible to investigate previously, or to target known disease pathways in a different way. The novel nature of the library scaffolds within the first 50K compounds of the PCC underlines the radical innovation brought to bear on the ELF in only two years by the Discovery SMEs and their academic partners.

More information can be found in "Drug Discovery Today" which details the quality and diversity of the first 50K compounds in a scientifically-driven and unique public collection generated through a collaborative approach.

These compounds are currently being tested against innovative biological drug targets at the eight EU Lead Factory screening centres and have already had an impact on the results, proving their drug discovery potential. Any European researcher from academia or SME with a potential drug target and associated screening assay can apply to access the 40 screening slots still to be granted. Moving forward, we will endeavour to continue to succeed in this collaborative fashion and look for further opportunities for the SMEs to innovate in both library design and production.  The EU Lead Factory project is set to reach 100K compounds end of 2015 and is on-track to achieve its ultimate goal of delivering ~200K compounds by the end of 2017.

Achieving this milestone demonstrates the formidable capabilities of the European Lead Factory consortium chemistry SME's (Edelris, Mercachem, Sygnature Discovery, Syncom and Taros) which have a combined workforce of over 300 experienced medicinal and analytical chemists. Amongst the state-of-the-art equipment dedicated for chemistry, purification, QC and formatting operations are 10 preparative LC/MS, 20 analytical LC/MS, 5 NMR spectrometers and 30 liquid handlers. With this equipment at their disposal the combined chemistry teams have the capacity and capability to synthesize >100,000 innovative and biologically-relevant lead and drug-like molecules per year.

SOURCE Edelris, Mercachem, Sygnature, Syncom, Taros