Review: Determination of drug–receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance

29 May 2012

Previously drug–receptor interactions have only been quantified in terms of their affinity and efficacy but recently the residence time has also been recognized to affect the clinical performance.

In this review Georges Vauquelin aims to try and help chemists to better evaluate the relevance of the kinetic data that may be obtained from compounds by discussing, with the aid of simulations, the different approaches to measure drug binding kinetics that are currently used to measure and calculate ligand–receptor dissociation kinetics, as well as covering some of the potential pitfalls associated with these methods.