Webinar
The Critical Importance of GPCR Functional Assays in Drug Discovery Projects
24 June 2026
16:00 CEST / 10:00 EDT / 07:00 PDT
About the webinar – The Critical Importance of GPCR Functional Assays in Drug Discovery Projects
Once a molecule has been identified in the drug discovery process, it is imperative that as much information about the properties of that molecule be accumulated for 2 reasons:
- The candidate will be a probe of very complex physiology and pathophysiology and any information attained will be of great value in future prosecution of the drug target
- If the candidate fails, the follow-up should not have the same properties as the failed candidate but rather have new activities of potential value.
This webinar will present a concerted strategy applying data from cellular in vitro experiments to characterize candidate drug activities (i.e. affinity, efficacy, allosteric parameters) that are system independent and thus will predict activity in all systems (as will be encountered in vivo).
In addition, early pitfalls in the discovery process (i.e. safety show-stoppers, ADME limitations) will be discussed in terms of the assays now available to identify these potential hazards.
G protein-coupled receptors (GPCRs) are crucial drug targets because they regulate a wide range of physiological processes, making them central to therapies in cardiovascular, neurological, psychiatric, respiratory, metabolic, gastrointestinal, immune/inflammatory, and oncology fields.
Keywords
Drug discovery; in vitro pharmacodynamics; drug affinity; efficacy; allosteric parameters; drug candidate selection
Meet the speakers
Terry Kenakin – Key Opinion Leader in GPCR pharmacology | Professor of Pharmacology, University of North Carolina
Alberto di Silvio – Head of the Assay Development Group, Axxam
After getting a BS in Chemistry and PhD in Pharmacology from the U of A Edmonton Canada, Dr Kenakin did a post doctoral Fellowship with Sir James Black at University College London UK. From there he entered industry, first at Burroughs-Wellcome (7 years) and then GlaxoSmithKline (25 years). He joined the University of North Carolina School of Medicine in 2011 where he presently works. His interests are in receptor theory, drug discovery, and allosteric protein function.
Alberto di Silvio earned his degree in Biological Sciences in 1998 from the University of Milan. He joined Axxam in 2002, beginning his career in the Cell Biology Group, where he dedicated the first four years to developing cell-based assays. In 2006, he moved to the High Throughput Screening (HTS) group, gaining extensive experience in HTS and compound profiling techniques.
In June 2019, Alberto was promoted to Unit Manager of the Compound Profiling Unit, where he oversees the work of seven Principal Scientists involved in various compound profiling projects. As of January 2023, he has taken on the role of Head of the Compound Profiling Group within Axxam’s Lead Discovery Services department. Most recently, in January 2026, he was appointed as Head of the Assay Development Group.