Two Qualified Hit Lists have been delivered
Early confirmation of the drug-discovery potential of the European Lead Factory has emerged with delivery of the first two Qualified Hit Lists (QHLs).
Launched in January 2013, the five-year, €196m Innovative Medicines Initiative (IMI)-funded project gives the European research community access to a unique, high quality and extensive lead-like compound library, the Joint European Compound Library (JECL).
The European Lead Factory, managed by an international consortium of 30 partners, has been designed to offer unrivalled opportunities to non-contractual public and private parties for the discovery of new drug lead molecules. It offers the infrastructure and expertise needed to screen against novel biological targets, summarised in a Qualified Hit List (QHL), for use either as pharmacological tools or as the starting points for drug discovery projects.
In addition to programmes taking place within participating EFPIA members, the European Lead Factory has already accepted 26 biology target programmes from universities and small and medium-sized enterprises (SMEs) across Europe, culminating in the delivery of the first two QHLs to the Netherlands Cancer Institute (NKI) and to UCB, one of the corporate partners in the project.
'Access to the European Lead Factory has fast-forwarded our drug discovery programme in the field of oncology by several years,' said Huib Ovaa, professor and group leader in chemical biology at NKI.
Access to the European Lead Factory has fast-forwarded our drug discovery programme in the field of oncology by several years
'The lead-like nature of JECL compounds and the expertise and facilities provided by the European Lead Factory mean that our results are of very high quality. This QHL goes far beyond a simple list of primary hits and I’m looking forward to further exploring the outcomes of this programme.'
Alongside the public target programme, industrial partners are also screening their own targets against the JECL.
Jeremy Davis, Director of Medicinal Chemistry at UCB, said this early hit list shows how important the European Lead Factory will be over the next few years. 'Access to the JECL has provided us with a list of highly interesting hit compounds and a second chance to develop lead molecules,' he said.
Targets submitted to and accepted by the European Lead Factory are screened against the JECL, which contains over 300,000 compounds from the proprietary collections of seven major pharmaceutical companies.
As part of the project, the JECL will be expanded until it contains up to 500,000 compounds through crowdsourcing of chemical library ideas.
From January this year, a web portal has enabled the submission of both biology targets and external compound library proposals to the European Lead Factory. Chemical library proposals benefit from fixed monetary rewards if they lead to the addition of more than 50 compounds to the JECL. To date, 214 chemistry proposals have been submitted by public chemistry partners, and 52 libraries have been successfully validated, resulting in more than 12,000 compounds synthesised and ready for screening.
Biological target programme owners receive QHLs of up to 50 compounds that show activity against their target and also fulfil additional (de)selection criteria as set out in the screening programme.
The UCB and NKI programmes will now progress to follow-up work, designed ultimately to generate drug candidates. UCB will conduct research in-house, while NKI will be using the facilities provided by the European Lead Factory that are able to deliver an Improved Hit List (IHL).
The European Lead Factory aims to accept and execute another 100 public programmes over the next four years.