Insights That Move the GPCR Field Forward

Live-cell high-content screening (HCS) offers an increasingly valuable alternative. By quantifying ligand–receptor interactions directly in intact cells, HCS allows researchers to observe binding events under near-physiological conditions while simultaneously generating image-based evidence to support numerical affinity estimates. For targets such as CB2, where nuanced shifts in receptor conformation affect signaling outcomes, a whole-cell environment can strengthen early-sta

Most GPCR programs don’t fail because of weak molecules—they fail because biology behaves differently than the assay implied. This week’s feature goes straight to the foundation: how system-level GPCR thinking protects discovery teams from the costly misinterpretations that derail programs. If your work touches GPCR pharmacology, these insights aren’t optional—they’re essential.

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