Sponsored by Eurofins DiscoverX
G protein-coupled receptors (GPCRs) can signal through multiple intracellular pathways, and ligands do not necessarily engage those pathways to the same extent. This phenomenon, receptor signaling bias or functional selectivity, is now recognized as a meaningful property of many drug candidates and a potential route to improved efficacy, better tolerability, and new opportunities in challenging targets. Bias is not an anomaly. It is a consequence of ligand-dependent receptor conformations and allosteric probe dependence, and it can be revealed with the right combination of functional assays.
This webinar explains the biological basis of signaling bias, shows how to detect and quantify it using reliable functional assays, and discusses how these data can guide lead selection and optimization. Practical assay strategies, interpretation pitfalls, and the value of comparing pathway outputs quantitatively, rather than relying on potency alone, sit at the center of the session.
Learning Objectives:
• Discover what GPCR ligand-dependent signaling reveals about drug candidates
• Learn how to detect and quantify GPCR signaling bias using reliable functional assays
• Turn functional selectivity into a practical decision-making tool in GPCR drug discovery
Privacy Policy
His work is central to the quantitative framework used today to describe receptor signaling bias, allosteric function, and agonism. He proposed one of the first mechanistic explanations of biased signaling and co-authored the widely-applied simple method for quantifying functional selectivity. He is the author of A Pharmacology Primer, Editor-in-Chief of the Journal of Receptors and Signal Transduction, and a Fellow of the British Pharmacological Society, recognized with the Goodman and Gilman Award from ASPET and the Gaddum Memorial Award.
