Objective

G-protein coupled receptors (GPCRs) are a superfamily of transmembrane signalling proteins. With their involvement in a wide variety of pathologies, GPCRs represent more than 50% of drug targets in the clinic. However the pharmaceutical industry faces a problem of a narrowing pipeline in GPCR ligand discovery. Peptides found in snake and spider venom can activate GPCRs which highlights the potential of natural products as a novel source of tool compounds or hit-to-lead chemistry in drug discovery. Using high throughput techniques, this work profiled Venomtech’s GPCR targeted venom discovery array against GPCR targets that previously failed to generate meaningful hits. Multiple hits were found in single concentration testing, with one hit validated against GPR120 in concentration responses. Confirmation of further hits is required.