Putting the dynamics into compound profiling: using kinetic assays to shape early stage drug discovery

Watch On Demand

In vitro early stage compound profiling often focusses on single timepoint measurements of drug action, for example the affinity of the drug for its target at equilibrium, or the endpoint response in a signalling assay.

However, in vivo, drug action occurs within a highly dynamic system. Drug and competing messenger concentrations at the site of action are continually changing, and the therapeutic effect itself may depend on a particular pattern of downstream cellular signalling over time.

This webinar, presented by Dr Nick Holliday, Chief Scientific Officer, Excellerate Bioscience, and supported by SPT Labtech, will explore how measurement of the kinetics of drug-target interaction can help optimise functional compound properties within this dynamic environment.

Using case studies from the CNS and respiratory disease areas, it will highlight the benefits of optimising binding on and off rates for duration of action and generation of kinetic selectivity, together with improved inhibitor and antagonist effects.

The presentation will also consider the need to map the kinetics of signalling to better predict the desired functional therapeutic outcome in cells or tissues.

What you will learn:

  • How association and dissociation rate constants describe compound binding kinetics
  • Potential clinical benefits of optimising kinetic constants when compound profiling
  • The wider relevance of signalling kinetics in determining therapeutic effects
  • Methods to implement binding and signalling kinetic screening

About the speaker

Dr Nick Holliday, Chief Scientific Officer (CSO) at Excellerate Bioscience, is also part-time Associate Professor in Pharmacology at the University of Nottingham (UK). Following studies in Cambridge (MA) and King’s College London (PhD), Dr Holliday gained over 25 years’ experience in the molecular pharmacology of receptors and other drug targets, leading development of in vitro imaging based assay systems to measure binding and signalling kinetics. He is a Fellow of the British Pharmacological Society.




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