GSK brings scientific and technical expertise to the Challenge.
Winners of the Discovery Fast Track Challenge will be given access to our world-class knowledge in drug discovery and our highly diverse compound collections. Using our expertise in drug discovery, we will design the best screening plans and we may provide¹ the chemical structures of high-quality chemical tools from successful screens according to the four possible research outcomes.
Reagents and Assays
Reagents and assays are customized to identify quality chemical tools. A wide range of biochemical, biophysical, cellular and phenotypic assays can be exploited and scaled to meet lead discovery needs.
High Throughput Screening (HTS)
HTS enables the testing of millions of pure compounds using a diverse set of technologies in biochemical and cellular assays of different complexity. Our HTS chemical library consists of approximately 2 million compounds selected to enhance the success in finding high-quality molecules for lead optimization programs. The infrastructure in miniaturization, robotics and data analysis together with years of experience make HTS a fast and high-quality process. HTS scientists analyze the results with sophisticated chemical probe selection algorithms that include robust statistics, chemical clustering, data mining and physiochemical properties.
DNA-Encoded Compound Library Technology (ELT)
ELT is an affinity-based selection methodology for hit identification. This technology is based on the synthesis and screening of a highly diverse collection of DNA-encoded small molecules. In a simple affinity selection experiment, libraries containing billions of compounds are exposed to the target. Bound molecules are then recovered and de-convoluted using next-generation sequencing. This technology has minimal target requirements and has been successfully applied to a range of enzyme, protein-protein and receptor targets.
Hit Qualification Support
Selecting the optimal tool compound(s) from the hundreds or thousands of raw screening hits typically requires the use of a range of assays (e.g. biochemical, biophysical, cell-based), along with computational chemistry approaches to identify emergent structure-activity-relationships. To accomplish this, GSK operates a fully integrated environment, and takes a holistic computational and experimental approach. We provide both the relevant measurements and the interpretational guidance, ensuring the selected compounds possess the best chemical properties and interact with the target via a desired modality.