🤝 Webinar in collaboration with: Eurofins DiscoverX
Receptor Signaling Bias: A Valuable and Accessible Property of New Drug Candidates
Turning functional selectivity into a practical decision-making tool in GPCR drug discovery
Beyond Potency: What Ligand-Dependent Signaling Reveals About Drug Candidates
G protein-coupled receptors 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.
The Biology Behind Bias
Ligands produce differential pathway engagement at a single receptor because they stabilize distinct receptor conformations. These conformations determine which downstream pathways are favored and which are muted. Due to this potential inherent bias, it is best practice to evaluate multiple pathways using different GPCR assays to obtain a better understanding of the ligand effects on the GPCR system.
Speaker
Dr. Terry Kenakin
Professor of Pharmacology & Pharmacology Course Coordinator Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill.
Dr. Kenakin trained in chemistry and pharmacology at the University of Alberta and completed postdoctoral work at University College London in the laboratory of Sir James Black. He spent 25 years in drug discovery at Glaxo (now GlaxoSmithKline) before joining UNC Chapel Hill, where he teaches and leads research in receptor pharmacology.
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.
Within the Dr. GPCR ecosystem, Terry hosts Terry's Corner, a live room where GPCR scientists get direct access to him. It's where the mechanistic questions that usually sit beneath the data get asked out loud, and where receptor theory, biased signaling, and the pharmacology of real drug discovery decisions are worked through together.
Organizers
Eurofins DiscoverX
Eurofins DiscoverX is a one-stop-shop for GPCR drug discovery and development, with 25+ years of expertise and validated cell-based assays spanning basic research through therapeutic discovery, optimization, and regulatory submission. Their assays are industry-standard, accepted for regulatory potency testing, and backed by thousands of peer-reviewed publications and partnerships with leading pharma and biotech companies.
1,500 human GPCR products covering ~90% of the GPCR-ome, including orphan receptors and ortholog variants
Multiple mechanisms of action: cAMP accumulation, β-arrestin recruitment, receptor internalization, ligand binding, calcium flux, and pharmaco-chaperone discovery
Flexible formats: cell line assay kits, ready-to-use eXpress kits, qualified bioassays, membrane preps, detection kits, and custom products
Applications across target identification, HTS, lead optimization, ligand bias and allostery evaluation, safety assessment, and regulatory potency testing
Dedicated portfolio for obesity and diabetes GPCR targets (GLP-1R, GIPR, GCGR, MC4R, AMY receptors, and more)
Dr. GPCR
Dr. GPCR is a membership-based nonprofit ecosystem dedicated to advancing GPCR-targeted drug discovery. It provides curated industry intelligence, expert-led masterclasses, and structured engagement opportunities for scientists and biotech leaders working across pharmacology, translational research, and therapeutic development.
Curated intelligence on GPCR drug discovery trends and developments
Expert-led webinars and masterclasses with leading researchers
Structured networking for scientists and biotech professionals
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Free membership tier available