Quantifying GPCR Activation with NanoBiT Assay for Ligand Screening

A versatile NanoBiT assay for ligand screening

GPCRs remain key therapeutic targets, yet many – including receptors with complex G-protein coupling, such as those linked to Gα12/13- are difficult to study using conventional functional assays.

Sygnature Discovery has developed a NanoBiT-based biosensor platform that quantifies GPCR activation through Gβγ-GRK interactions, providing a proximal, live-cell readout of receptor engagement.

The assay delivers robust, high-throughput performance, compatible with automation and orthogonal validation using chimeric G-protein calcium flux assays, enabling confident discrimination between agonists, partial agonists and antagonists, and is adaptable to a wide range of GPCR families.