The drug-target residence time model was first introduced in 2006 and has been broadly adopted across the chemical biology, biotechnology and pharmaceutical communities. While traditional in vitro methods view drug-target interactions exclusively in terms of equilibrium affinity, the residence time model takes into account the conformational dynamics of target macromolecules that affect drug binding and dissociation. The key tenet of this model is that the lifetime, or residence time, of the binary drug-target complex and not the binding affinity per se, dictates much of in vivo pharmacological activity. Here, we revisit this model and highlight key applications over the past ten years.

Drug-target residence time model: A 10-year retrospective

253rd National Meeting (2017)

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