The Design of Screening Assays for New Drug Discovery

October 9, 2012


Course Description 

This session will outline the new knowledge available to enable pharmacologists and medicinal chemists to design optimal assays for the discovery of synthetic molecules for therapeutic benefit. Specifically, concepts related to (1) the differential importance of assay sensitivity on ligand detection vs characterization, (2) the special requirements for assays designed for detection of allosteric molecules (antagonists and PAMs), (3) new knowledge related to the optimization of ligand libraries for screening, (4) Comparison of functional screening vs binding assays, (5) how biased signaling has impacted new drug screening, will be discussed.

Learning Objectives 

  • The design of screening libraries.
  • Criteria for the design of functional screens
  • Special considerations for Allosteric screens.
  • Consideration and accommodation of Biased signaling.


Who Should Attend 

  • Pharmacologists
  • All Biologists involved in drug discovery
  • Medicinal chemists
  • Scientists involved with screening technology


Instructor Information: Terry KenakinTerry Kenakin Ph.D.
Professor, Department of Pharmacology
University of North Carolina School of Medicine
Chapel Hill NC (formerly of GlaxoSmithKline Research and Development)

Instructor Biography:Beginning his career as a synthetic chemist, Terry Kenakin received a Ph.D. in Pharmacology at the University of Alberta, Edmonton Canada. After a post-doctoral Fellowship at University College London, U.K., he joined Burrough-Wellcome as an associate Scientist. From there he continued working in drug discovery at Glaxo Inc, GlaxoWellcome. and GlaxoSmithKline Research and Development laboratories at Research Triangle Park, N.C. USA. He currently is a Professor in the Dept. of Pharmacology, University of North Carolina School of Medicine , Chapel Hill N.C.

Dr Kenakin has been involved in drug discovery for over 30 years. Currently he is engaged in studies aimed at the optimal design of drug activity assays systems as well as the discovery and testing of. allosteric molecules for the treatment of diabetes. He is a member of numerous editorial boards as well as Editor-in-Chief of the Journal of Receptors and Signal Transduction and co-Editor in Chief of Current Opinion in Pharmacology. In addition, he has authored numerous articles and has written 9 books on Pharmacology.

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