Measuring and Interpreting Efficacy versus Affinity in Modern GPCR Ligands |
Автор: Dr. GPCR
Загружено: 2026-02-25
Просмотров: 4
Описание:
Designing drugs for GPCRs is never just about potency. The challenge is knowing how efficacy and pathway bias shape the real cellular outcomes that matter for drug action. Distinguishing between simple binding and actual signal transduction drives more rational drug discovery.
This session breaks down how to separate efficacy from affinity, measure pathway bias, and read dynamic ligand behaviors. You’ll see the operational models in action, make sense of ensemble theory, and learn to interpret bias using practical visualization tools, from bias plots to webs of efficacy.
Dr. Terry Kenakin walks through each principle step by step, showing how log(max/EC50) and pluridimensional efficacy connect to decision-making in the lab. The approach gives you a toolkit for rationalizing ligand responses and predicting therapeutic profiles.
Learning Outcomes
Distinguish efficacy from affinity in GPCR ligand analysis
Quantify and visualize pathway bias using operational models
Interpret log(max/EC50) and multidimensional efficacy data in context
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