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Radioligands have been used to study GPCRs for decades, but with the advances in the fluorescence field, assays They are ligands labeled with radioactive isotopes which can be used in binding assays to quantify other that offer an alternative to radioligands in binding assays. design for specific targets:  Not all targets have available high-affinity radioligands, but with the development GPCR-radioligand binding assays.

Overcoming them requires careful assay design and strategic use of the right fluorescent probes. For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and trafficking  • Live-cell kinetic measurements  unavailable to endpoint assays  Multiplexed assessment the gold standard for image-based GPCR assays. development expertise.

Imagine running a calcium assay and discovering your compound shows only weak activity. Kenakin dives deep into a widely used, often misunderstood tool in early drug discovery: the calcium assay Revered for its convenience, the FLIPR assay provides rapid insights into receptor activity. with strategic clarity. 📍 Foundational Level | Calcium Assays 📚 Part of Terry Kenakin’s Pharmacology Unlock "Calcium Assays" now

Explore Martin Marro’s impact on GPCR drug discovery, assay innovation, and translational pharmacology bridging academia, pharma, and biotech. << Back to podcast list Strategic Partner(s) GPCR Assay Strategy Marro’s career spans big pharma and biotech, encompassing functional assay development, GPCR internalization How advanced assay design is essential for translating cell-based GPCR signals to therapeutic outcomes development, small molecule and biologics research, and team leadership through high-profile programs

Michelle Halls reveals how organized GPCR signaling drives assay innovation and new therapeutic insights This conversation is especially valuable for scientists developing functional assays, fluorescence-based development and GPCR research. Why It Might Hit Home If you’ve ever: Faced unexpected assay behavior at ultra-low ligand concentrations Get behind-the-scenes conversations, advanced assay development strategies, and practical GPCR tools

taste receptors in cancer and metabolic diseases, and emerging high-throughput methods for functional assay development. generation How computational approaches and wet-lab validation complement each other in functional assay development Who Should Listen If you face complex GPCR questions at the bench or in translational research His current efforts bridge teaching in Toronto and ongoing research, including the development of an