In this short presentation, Dr Phil Jones, Chief Scientific Officer at BioAscent, discusses an innovative assay that was developed for a G protein-coupled receptor to help hit confirmation for a programme the team worked on with the European Lead Factory (ELF).
The ELF portfolio comprises many target classes. This case study describes a Gi/Gq linked GPCR, indicated in neuropathic pain. A cell line stably expressing the target was used to screen ~400,000 compounds in an intracellular Ca2+ FLIPR assay producing an initial hit list of 87 compounds. To provide strong corroborative orthogonal evidence of target engagement and prioritise the compounds, a Dynamic Mass Redistribution (DMR) assay (figure 1) was developed and validated using a series of pharmacological agents.
To read more and to see the results, the poster can be viewed here.
About the ELF
The ELF is a public-private partnership aiming to identify hit compounds against molecular targets submitted by European academics and SMEs. These are screened against a Joint European Compound Library (JECL), comprising ~500,000 compounds from the participating pharma companies and compounds synthesised specifically for the project. One aim is to provide high-quality hit series for targets provided by SMEs and academic groups. To find out more, visit the website.