Insights That Move the GPCR Field Forward

Signaling bias is critical for drug discovery as it forms a selection criterion for agonism. Measuring and quantifying signaling bias reveals which candidates emphasize therapeutically beneficial pathways, and which may be falsely characterized as equivalent by single-pathway assays. Drug discovery programs that do not consider investigating for signaling bias often fail to fully understand the distinction and risk candidate molecules from advancing along the pipeline.

GPCRs are one of the most important families of therapeutic targets in the pharmaceutical industry. They are involved in several pathologies, ranging from neurological, oncological, degenerative, metabolic, immunological… around a third of the drugs in clinical use are GPCR ligands

High-content screening (HCS) has become a cornerstone in GPCR and phenotypic drug discovery, enabling researchers to quantify cellular responses with spatial, temporal, and mechanistic depth. For GPCR-focused programs, the ability to visualize receptor localization, internalization kinetics, and ligand interactions in intact cells offers advantages that extend far beyond traditional biochemical or radioligand assays. Yet, despite remarkable progress, HCS workflows rema