van Vlijmen H, Pannifer AD, Cochrane P, Basting D, Li VM, Engkvist O, Ortholand JY, Wagener M, Duffy J, Finsinger D, Davis J, van Helden SP, de Vlieger JSB; European Lead Factory Consortium. The European Lead Factory: Results from a decade of collaborative, public-private, drug discovery programs. Drug Discov Today. 2024 Mar;29(3):103886. doi: 10.1016/j.drudis.2024.103886. Epub 2024 Jan 18. PMID: 38244673.
The highlights
- More than 250 high throughput screens on a wide variety of targets have been completed by academic groups, small biotech companies, non-profits, and large pharma companies on a shared collection of half a million compounds.
- An effective mechanism was set up for sharing proprietary screening compounds with full enablement of intellectual property creation.
- Screening hits from the European Lead Factory consortium have led to multiple active compound optimization programs at the participating academic and industry organizations, and two companies have been created on the basis of hits from the ELF.
- Analysis of the screening results indicates that compound promiscuity is correlated with lipophilicity and anti-correlated with three-dimensionality of compounds.
- There is no indication of the existence of dark chemical matter in this collection, as we continuously observed previously inactive compounds to be active in new screens.
