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ELF

European Lead Factory

Summary

The European Lead Factory is a pan-European platform for drug discovery supported by the Innovative Medicines Initiative (IMI) that is set to give a major boost to drug discovery in Europe. Comprising a collection of half a million compounds (derived from new public and existing private company collections) and a screening centre, the European Lead Factory will offer researchers in academia, small and medium-sized enterprises (SMEs) and patient organisations an unprecedented opportunity to advance medical research and develop new medicines.

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A key tool in the earlier stages of drug development is a technique called High Throughput Screening (HTS), in which researchers screen large collections of chemical compounds in the hunt for molecules that could be potential drugs or be used in drug development in other ways. Although pharmaceutical companies have built up large libraries of compounds over the years, access to these collections has been tightly restricted to in-house use by the owners.

Meanwhile, the academic community is becoming increasingly interested in HTS, but public compound collections tend to be rather small and expertise in the area is scattered across many institutions. As a result, few public drug targets have been screened against large, high-quality compound libraries. This has hampered efforts to generate promising leads for the development of innovative drugs.

A unique resource

Enter the European Lead Factory, which will provide a select group of researchers in universities, small business and patient organisations with access to an industry-like platform for the identification of ‘hits’. Hits are compounds that could potentially be developed into new medicines. The pharmaceutical companies in the consortium will contribute a total of over 300 000 compounds to the project to create a joint compound collection.

To this will be added an estimated additional 200 000 novel compounds generated by public partner contributions during the project, resulting in a unique Joint European Compound Collection with some 500 000 compounds. Proposals for novel compounds from the public partners will be submitted to a transparent selection and validation process addressing several criteria such as novelty, diversity potential, innovative design and synthetic tractability. Once approved, the SMEs together with the academic institutions will seamlessly translate the most compelling ideas into high quality compound libraries to be shipped to the consortium’s HTS facilities.

The project will also establish a screening centre providing HTS services for projects for the selected public projects from academia and SMEs. It will also handle all logistics for the Joint European Compound Collection, acting as a neutral, ‘honest’ broker in the transfer, handling and analysis of confidential data.

The project in practice

Once up and running, the European Lead Factory will provide the compounds and support for 48 HTS screens per year. Of these, 24 will come from the industry partners, who will run their own screens. The other 24 HTS projects will be selected from the public sector following competitive Calls for proposals.

Public programmes selected by the project will be further advanced by the European Lead Factory. It will provide guidance in the design of the experiments, support on medicinal chemistry, and help setting up partnerships with others if needed. Once the HTS has been run, the ‘target owner’ (i.e. the organisation that submitted the target for inclusion in the project) will receive a list of a maximum of 50 compounds that have been identified. The project hopes to attract public screening proposals in a variety of therapeutic areas.

Strength in diversity

The European Lead Factory combines the power of the pharmaceutical industry’s previously inaccessible compound libraries with the innovation of the academic communities in designing novel compounds and the expertise of many SMEs in HTS and library generation. Importantly, it will provide a screening platform of industrial quality focused on value generation. Looking to the future, the European Lead Factory is set to become a centre of excellence in Europe for small molecule drug discovery programmes in the public sector. A key output of the project is a comprehensive business plan that will ensure the viability of the initiative once the initial IMI project has ended.

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Achievements & News

European Lead Factory successfully creates ‘drug-like’ hit compounds

Just a few months after it was included in drug target screening programmesone of the first compounds synthesised within the European Lead Factory was identified as a ‘drug-like’ hit. The compounds were synthesised by the Public Chemistry Consortiumbased on library proposals from academic groups and small- and medium-sized enterprises (SMEs) in Europe. ###The EU Lead Factory carefully selects library proposals for novelty, drug-like properties, diversity and synthetic tractability. The hit compound was among the first compounds to be synthesised within the EU Lead Factory, and was added to the Joint European Compound Library (JECL) along with 28 000 other compounds in January 2015. In addition to the hit compound, another 130 compounds have already been identified as ‘preliminary hits’ over multiple drug-target screening programmes in only 5 months, highlighting the potential of the EU Lead Factory compounds. Together with 326 000 high-quality compounds that were already contributed by 7 large pharmaceutical companies, the JECL now holds over 350 000 compounds. The collection is available for screening against novel drug targets and will continue to grow. Want to learn more about the EU Lead Factory? Visit www.europeanleadfactory.eu or meet them in person at MipTec 2015 in Basel, Switzerland in September 2015 where the team will be at stand D25 in the exhibition. (June 2015)

European Lead Factory launches new animations
IMI’s European Lead Factory has published four short videos to help SMEs and academics understand how the programme works. The videos explain ###the programme’s aims and give an overview of how target assays are introduced and handled, as well as how to test chemical scaffold ideas using the European Lead Factory’s online compound tool. Programme owners' rights & obligations are also covered in this light-hearted series of animations.  
- Watch the videos
- Find out more about the European Lead Factory
- Read the latest European Lead Factory newsletter 
(May 2015)

European Lead Factory scoops Bio-IT World best practice prize
The European Lead Factory has won a prestigious Bio-IT World Best Practices prize in the knowledge management category for its Honest Data Broker (HDB) implementation of the ScienceCloud platform from BIOVIA. ScienceCloud HDB is a core technology ### providing an innovative solution to the particular challenges of this open innovation platform in drug discovery: providing access to ELF’s extensive library with compounds from the pharmaceutical industry and public partners, as well as to details on the screening data, the HDB also provides reassurance to compound and target owners that their intellectual property is protected. The HDB therefore combines fine-grained permissions with efficient access to the vast range of chemistry and biology data it stores, which allows good science to be carried out while safeguarding IP interests. For the Bio-IT judges, the HDB is ‘the only platform in its class’. This peer recognition coincides with a number of high-impact scientific publications from the ELF chemistry partners in a special issue of Bioorganic & Medicinal Chemistry on ‘Emerging Approaches for the Design and Synthesis of Innovative Small Molecule Libraries’. This is the second time an IMI project has received a Bio-IT World Best Practice award; in 2014, severe asthma project U-BIOPRED won in the research and drug discovery category.
- Announcement  of the Bio IT Winners
- Read the press release 
Bioorganic & Medicinal Chemistry Journal 
(May 2015)


Find out how the European Lead Factory can help you
IMI’s European Lead Factory project will demonstrate how its services can help to boost the drug discovery programmes of diverse organisations at a free workshop on 25 March at the SLAS Conference on Compound Management in Dortmund, Germany. The event will spotlight the extensive drug target screening and compound synthesis resources now available through the European Lead Factory. ###As such, it offers attendees an excellent opportunity to think about their target assay development and compound library design plans. Meanwhile the panel will be able to answer questions on the wider role of crowdsourced innovation and on working within extended public-private partnerships. The European Lead Factory currently comprises a 350 000-compound screening collection originating from private partners or synthesised by public partners, as well as a screening centre that is accepting proposals for screening programmes. The first screens have already been completed and feedback from users is highly positive.
- Register to attend the workshop
- Find out how to submit a proposal for a target or scaffold
- Learn more about the European Lead Factory’s successes in its latest newsletter

European Lead Factory proves potential with first results
IMI’s European Lead Factory project has proven its potential for drug discovery with the delivery of its first results in the form of four ‘qualified hit lists’ – lists of up to 50 compounds identified as showing activity against a drug target submitted to ###the European Lead Factory’s screening programme. One of the beneficiaries of these results is the Netherlands Cancer Institute, which stated that access to the European Lead Factory had fast-forwarded its oncology drug discovery work ‘by several years’. Another list went to pharmaceutical company UCB, which noted that access to the 300 000-strong Joint European Compound Collection had provided it with a list of ‘highly interesting’ compounds that would allow it to take a fresh look at a particularly challenging drug target.
Organisations wishing to take advantage of the project’s extensive compound collection can submit target proposals via the project website. The project is also accepting proposals for external compound libraries via its website. If proposals result in the addition of over 50 compounds to the library, the proposer receives a payment.
   -   Read the project’s press release on the results
   -   Find out how to submit compounds to the library
   -   Find out how to submit target programmes to the project
(June 2014)

European Lead Factory open for proposals
The European Lead Factory project is now accepting proposals for both compounds and target programmes from project partners as well as external academics and small and medium-sized enterprises (SMEs). Compound ideas will be ###assessed by a selection committee made up of respected chemists from the pharmaceutical industry, SMEs, and academia. The committee, which is bound by a confidentiality agreement, will assess proposals on the basis of their molecular properties, structural features, novelty, and innovation, among other things. Compounds that make the grade will be added to the Joint European Compound Collection; the selection committee will decide the financial reward due to the proposers.
Meanwhile, the project’s biology target programme is open to submissions for all disease areas, including oncology, cardiovascular, central nervous system (CNS), respiratory, and neglected diseases. Target screening programmes should be novel, of high quality, and ready for high throughput screening (HTS).
Details of how to apply, plus information on the project's intellectual property policy, can be found on the project website.
(December 2013)

European Lead Factory runs first screen
This summer, IMI’s European Lead Factory project successfully completed its first miniaturised screening programme, highlighting the capabilities of the project’s Screening Centre at Pivot Park in Oss, the Netherlands. Where a traditional lab would test ###tens to hundreds of compounds per day, the robot in Oss completed testing of 300 000 compounds in under 3 days. The European Lead Factory has two main components – the Screening Centre in the Netherlands, and the Compound Collection, which is based in Scotland and currently comprises the 300 000 compounds contributed to the project by the pharmaceutical companies. A further 200 000 compounds will be added to the Compound Collection throughout the project by the public partners. Looking to the future, the project hopes to open Calls for further public screens in the near future.
(September 2013)

Participants

EFPIA companies

  • Bayer Pharma AG, Germany
  • AstraZeneca AB, Sweden
  • H. Lundbeck A/S, Denmark
  • Janssen Pharmaceutica NV, a Pharmaceutical Company of Johnson & Johnson, Belgium
  • Merck KGaA, Germany
  • Sanofi, France
  • UCB Pharma SA, Belgium

Universities, research organisations, public bodies, non-profit groups

  • Foundation Top Institute Pharma (Stichting Top Instituut Pharma), The Netherlands
  • Leiden University, The Netherlands
  • Max Planck Gesellschaft zur Förderung der Wissenschaften E.V., Germany
  • Radboud University Nijmegen, The Netherlands
  • Stichting Het Nederlands Kanker Instituut, The Netherlands
  • Technical University of Denmark, Denmark
  • Universität Duisburg-Essen, Germany
  • University of Dundee, UK
  • University of Groningen, The Netherlands
  • University of Leeds, UK
  • University of Nottingham, UK
  • University of Oxford, UK
  • VU-University Amsterdam, The Netherlands

SMEs

  • BioCity Scotland Ltd, UK
  • ChemAxon, Hungary
  • Edelris S.A.S, France
  • Gabo:Mi Gesellschaft fur Ablauforganisation:Milliarium Mbh & Co Kg, Germany
  • Lead Discovery Center GmbH, Germany
  • Mercachem B.V., The Netherlands
  • Pivot Park Screening Centre B.V, The Netherlands
  • Sygnature Discovery Limited, UK
  • Syncom, The Netherlands
  • Taros Chemicals GmbH & Co KG, Germany

 

Facts & Figures

Start Date 01/01/2013
End Date 31/12/2017  
   
Contributions       € 
IMI Funding 79 999 157
EFPIA in kind 91 337 070
Other 24 967 255
Total cost 196 303 482

Contact

Project Coordinator
Eckhard Ottow
Bayer
Tel: +49 30 468 15522
E-mail: eckhard.ottow[AT]bayer.com

Head Chemistry Consortium
Dimitrios Tzalis

Taros Chemicals
Tel: +49 231 97 427211
E-mail: dtzalis[AT]taros-chemicals.de

Head Screening Consortium
Ton Rijnders

TI Pharma
Tel: +31 71 332 2035
E-mail: ton.rijnders[AT]tipharma.com