Affinity and Beyond! Kinetic insights, driving drug discovery foresight.

This video, presented by Peter Tonge, Distinguished Professor & Chair at Stony Brook University and Jeremy Hague, Chief Business Development Officer at Enzymlogic, covers:

  • How sustained target occupancy can be achieved through structural modifications that increase target (re)binding and/or that decrease the rate of drug dissociation.
  • The benefits of the early evaluation of drug binding kinetics, exemplified by the reversible and irreversible inhibitors of Bruton’s tyrosine kinase (BTK), MET kinase and EGFR family.
  • How kinetic selectivity can be used to widen the therapeutic window even in the absence of thermodynamic (affinity) selectivity.
  • The factors that may affect the translation of sustained occupancy to prolonged drug activity such as target vulnerability and the rate of target turnover.
  • The advantages of PK/PD models that integrate the kinetics of drug-target interactions into predictions of drug activity.
  • How to make binding kinetics assessment of reversible and covalent compounds simpler and easier using KINETICfinder® and COVALfinder®.