Thursday, October 29th, 2026
8am PDT / 11am EDT / 3pm GMT / 4pm CET

The pharmacological behaviour of drugs is determined not only by their intrinsic properties but also by the sensitivity of the biological systems in which they are evaluated. Variations in receptor density and signal transduction efficiency can significantly influence observed drug responses, complicating the translation of in vitro findings to in vivo contexts. Consequently, methods that systematically account for these variations are essential for accurate characterisation of drug candidates.

In this webinar hosted by DDW and supported by Eurofins DiscoverX, Dr Terry Kenakin (North Carolina School of Medicine, Chapel Hill), will examine the concept of functional “volume control” as a strategy to modulate system sensitivity and thereby elucidate the true pharmacological properties of ligands acting at GPCRs. By experimentally tuning receptor density and cellular responsiveness, it is possible to quantitatively assess ligand affinity and efficacy within a unified operational framework.
 
Applications of this approach will be discussed; specifically, reducing system sensitivity can enable the estimation of intrinsic efficacy and affinity through partial agonism, while further modulation may convert low-efficacy agonists into measurable antagonists. Conversely, increasing system sensitivity can reveal latent efficacies, including partial agonism or inverse agonism in compounds previously classified as neutral antagonists.
 
The webinar will also highlight how functional volume control facilitates mechanistic differentiation of allosteric modulators by distinguishing effects on affinity versus efficacy.
 
Overall, these approaches provide a framework for improving the quantitative interpretation of pharmacological data and enhancing the predictive value of in vitro assays for in vivo drug activity.

 

Q&A with the speakers follows the presentations.

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