Insights That Move the GPCR Field Forward

Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi

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