Insights That Move the GPCR Field Forward

The A₂A adenosine receptor NanoBRET® competitive binding assay enables real-time quantification of ligand–receptor interactions in living cells. By combining NanoLuc-tagged receptors with fluorescent tracers, this approach allows direct measurement of binding displacement, delivering robust pIC₅₀ and pKᵢ values that align with established pharmacology. In this article, we examine the assay principle, validation strategy, and performance across reference antagonists and agonis