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Principles of Pharmacology in Drug Discovery I

Dr. Terry Kenakin

Start date: September 5, 2024

Course duration: 4 Weeks

Premium Members benefits:

- Subscribe and save 25% on every GPCR Course

- Early-bird access

- Recordings will be available

Dr. Terry Kenakin

Techniques for Effective Lead Optimization of Candidate Molecules

GPCRs have been and arguably still are the most prolific and fertile therapeutic drug targets; this course describes the essential pharmacologic techniques and knowledge required to create a GPCR Target Program aimed at the discovery of new Drugs. The course will focus on the methods used to quantify GPCR ligand activity (agonists, antagonists, modulators) and the process of characterizing the mechanism of action of ligands to enable the prediction of activity in vivo systems. In general, registrants will receive a comprehensive understanding of the unique science of pharmacology and how it can describe drug action in system-independent ways.

Registrants will learn:

  • Essentials of measuring pharmacologic activity of ligands (affinity, efficacy, co-operativity).

  • Application of this knowledge to determine the mechanism of action of new

    GPCR ligands.

  • The required elements of a comprehensive and effective GPCR Discovery.


  • Lecture 1: GPCR Project Initiation and Design for Discovery of New Molecules.

  • Lecture 2: Drug Affinity: Measurement of Antagonism (Binding and Function) /

    Classifying Antagonists.

  • Lecture 3: Agonists and Efficacy: A New World of GPCR Efficacies / Biased


  • Lecture 4: Allosteric Modulators: NAMs, PAMs, Special Properties, Methods to

    quantify the allosteric effect.

Registrations start on Monday, July 15th, 2024.

  • Classes will be live from Zoom on Thursdays from 10 am to 11:30 am EST.

  • Sessions will include a 1-hour live lecture plus 30 minutes of Q&A.

  • Every participant will also get the chance to have a 1:1 meeting with Dr. Kenakin during

    the four weeks, scheduled according to the professor's availability.

  • Participants who complete the course will get an online certification signed by the

    professor and the Dr.GPCR Team.

A splendid time is guaranteed for all.

Early-bird registration is available for Premium Members

Your Instructor

Dr. Terry Kenakin

After obtaining a BS in chemistry and PhD in Pharmacology at the University of Alberta, Edmonton Canada, I did a post doctoral Fellowship with Sir James Black in London U.K. I then worked at Burroughs-Wellcome in Research Triangle Park, NC (7 years) and then GlaxoSmithKline in RTP for 25 years. I then moved to the University of North Carolina School of Medicine where currently I am a Professor of Pharmacology. My interests are in receptor theory, pharmacology applied to drug discovery and allosteric protein function.

Dr. Terry Kenakin