Optimal Design and Execution of Pharmacological Experiments in Drug Discovery

April 9, 2013
12:00 p.m. - 1:30 p.m. EDT


Course Description 

Biologically active molecules (drugs), with defined molecular properties, can interact with various physiological systems to produce different behaviors. As a scientific discipline, Pharmacology is unique in that it has the tools and approaches to extract from such system-dependent drug behavior the molecular properties of drugs so that predictions of behaviors in all systems (including the therapeutic one) can be made. This process facilitates the interaction of biologist and medicinal chemists to optimize drug activity. This course on experimental design has four parts:

  • Defining the Experiment: objective is to quantify the pharmacologic properties of the molecule (affinity, efficacy, orthosteric vs allosteric mechanism, real time offset kinetics of binding) –the use of different assay formats to quantify multiple efficacies
  • Conducting the Experiment: use of null methods / identifying drug effect, describing molecular events through models / comparison to quantitative data to pharmacologic models
  • Interpreting the Data: linking observations with molecular properties / determining significant difference / structure-activity relationships
  • Making Predictions (to Therapeutic systems) from the data: projecting organ-based behaviors from drug molecular properties / determination of next step to optimize drug activity


Learning Objectives 

  • Bring non pharmacologist biologists and chemists up to speed on basic pharmacologic principles and then use those to quantify biological activity
  • Constructively apply pharmacologic principles to the design of biological experiments to yield chemical data about new potential drug molecules in drug discovery programs
  • Generate system-independent measure of biological activity that can be used to predict therapeutic behaviors in all systems
  • Master state of the art knowledge of assay technology to obtain insights into biological activity


Who Should Attend 

  • Pharmacologists
  • All Biologists involved in drug discovery
  • Medicinal chemists
  • Scientists involved with screening technology
  • Managers in Discovery, Drug Safety, Drug Metabolism and Project Management


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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