Phil Jones, European Screening Centre, Newhouse
The IMI funded European Lead Factory[i] has assembled a high quality screening collection (Joint European Compound Library or JECL) and established facilities to allow the high throughput screening of this collection and follow up of hits. Both resulting hit lists and follow-up activities are provided free to academic groups and SMEs[ii]. This creates a unique opportunity for groups who want to access lead chemical matter for innovative therapeutic targets.
The JECL brings together 300,000 compounds from the seven participating pharma company’s compound collections.[iii] These are being supplemented with bespoke compounds prepared specifically for the JECL from crowd-sourced ideas. These ideas will be prioritized, validated and then the compounds prepared and added to the JECL. The goal is to ultimately provide a collection of up to 500,000 compounds.
Screening and follow-up of hits is carried out at the European Screening Centre based in Newhouse, Scotland and Oss, The Netherlands. Selected target owners will provide assays which will be optimized for screening. Once screening is complete the resulting hits are triaged using a selection of in vitro and biophysical techniques in order to characterize the nature of the target modulation and selectivity. The triaging is guided by in-silico assessments to assist the selection of optimal compounds. A selection of hits will be further characterized by carrying out initial medicinal chemistry optimization and collecting biostructural, biophysical and/or in vitro DMPK data.
The first hit lists have already emerged from the European Lead Factory for academic and industry partners.[iv] If you would like to submit your own target or ideas for compounds please go to www.europeanleadfactory.eu.
[ii] The submitting target owner will be subject to some terms and conditions.
[iii] For further details see J. Besnard, A Pannifer, publication in preparation