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Updated: Jan 11, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

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Elucidating biased signaling in class A GPCRs

Ningyang Xu1, Edwin Legall1, Roger H Johnson2

  • 1Cancer Center and Department of Pharmacology and Toxicology, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Trends in Pharmacological Sciences
|November 8, 2025
PubMed

Keywords:
G protein–coupled receptors (GPCRs)NanoLuc Binary Technology (NanoBiT)biased signalingbioluminescence resonance energy transfer (BRET)cryo–electron microscopy (cryo-EM)structure-based drug design (SBDD)

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