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Sygnature Discovery delivers over 21K novel compounds to the European Lead Factory, one of the top performing SMEs in the consortium

Sygnature Discovery has announced that is has delivered in excess of 21,000 novel chemical compounds to the Public Compound Collection (PCC) of the European Lead Factory (ELF).

The ELF, 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), including Sygnature Discovery, have formed a pan-European consortium to address the challenge of delivering an innovative, publicly-accessible, screening deck of synthetically-tractable compounds, named the PCC.  As part of the ELF, 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, which includes Sygnature Discovery, will deliver 200,000 compounds from untapped areas of biologically-relevant chemical space by the end of 2017.

In November 2015, a scientific publication was released in “Drug Discovery Today” (Vol. 20, Issue 11, pp 1310-1316) which detailed the results of a benchmark study performed on the first 50K compounds in the screening collection that have been designed and synthesised within the ELF consortium, and were delivered by March 2015.  High-throughput screening (HTS) represents a major cornerstone of drug discovery and the availability of an innovative, relevant and high-quality compound collection to be screened often dictates the final fate of a drug discovery campaign.  Given that the chemical space to be sampled in drug research programmes is practically infinite and sparsely populated, significant efforts and resources need to be invested in the generation and maintenance of a competitive compound collection.  The ELF project is addressing this challenge by leveraging the diverse experience and know-how of academic groups and SMEs engaged in synthetic and/or medicinal chemistry by designing and synthesising a compound collection with novelty, diversity, structural complexity, favourable physico-chemical characteristics and overall attractiveness for HTS purposes.

The novel compounds within the PCC have good Lipinski-like properties, a high proportion of sp3 centres (Fsp3 character) and 85% of the compounds are chiral, thus yielding molecules with a high degree of 3D shape.  In addition, over half of the molecular frameworks within the collection 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 chemistry SMEs, such as Sygnature, and their academic partners.

Dr Simon Hirst, Founder and Chief Executive Officer of Sygnature Discovery said: “Sygnature is proud to be one of the most productive chemistry SME partners, having contributed over 21K novel compounds to the ELF collaboration. This consortium of SMEs and academics has delivered nearly 100K compounds, in total, with novel scaffolds which have the potential to accelerate drug discovery activities throughout Europe and beyond.  We look forward to continuing working with all of our partners in the ELF to supply the remaining compounds to the PCC by the end of 2017.”

About the Innovative Medicines Initiative

The Innovative Medicines Initiative (IMI) is the world’s largest public-private partnership in health. IMI is improving the environment for pharmaceutical innovation in Europe by engaging and supporting networks of industrial and academic experts in collaborative research projects. The European Union contributes €1 billion to the IMI research programme, and this is matched by in kind contributions worth at least another €1 billion from the member companies of the European Federation of Pharmaceutical Industries and Associations (EFPIA). The Innovative Medicines Initiative currently supports 40 projects, many of which are already producing impressive results. The projects all address major bottlenecks in drug development, and so will accelerate the development of safer and more effective treatments for patients.

The research leading to these results has received support from the Innovative Medicines Initiative Joint Undertaking under grant agreement n° 115489, resources of which are composed of financial contribution from the European Union’s Seventh Framework Programme (FP7/2007-2013) and EFPIA companies in kind contribution. More information: http://www.imi.europa.eu/content/european-lead-factory

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