3rd EFMC Short Course on Medicinal Chemistry
Principles and Applications of in vitro Pharmacology in Drug Discovery for Medicinal Chemists
Castle “Oud Poelgeest”, Oegstgeest, The Netherlands - April 10-13, 2011

In the initial phases of drug discovery where compound potency and selectivity are major considerations, data derived by biologists is of prime importance to the chemists.

This short course will be a mixture of talks, tutorials and case histories involving GPCRs (G protein coupled receptors), enzymes and ion channels.

The course will discuss:

• The techniques and data that biologists use to assess potency and selectivity of agonists, antagonists and enzyme inhibitors.
• The ‘rules’ under which such data is collected – and what happens if these rules are not obeyed.
• Distinguishing between potency and affinity.
• Equilibrium and kinetic assays.
• How kinetic assays can seriously improve your project.
• Translating in vitro data to the in vivo environment.