It is increasingly appreciated that the rates at which drugs associate with and dissociate from
receptors—the binding kinetics—directly impact drug efficacy and safety. The molecular …

Highlights•A public–private partnership targets drug-binding kinetics in a multilevel
approach.•New experimental approaches for measuring drug residence time are …

A vast number of marketed drugs act on G protein‐coupled receptors (GPCRs), the most
successful category of drug targets to date. These drugs usually possess high target affinity …

The influence of drug-receptor binding kinetics has often been overlooked during the
development of new therapeutics that target G protein-coupled receptors (GPCRs). Over the …

The quest for ever more selective kinase inhibitors as potential future drugs has yielded a
large repertoire of chemical probes that are selective for specific kinase conformations …

Introduction: The study of drug–target interactions is essential for the understanding of
biological processes and for the efforts to develop new therapeutic molecules. Increased …

Target residence time is emerging as an important optimization parameter in drug discovery,
yet target and off-target engagement dynamics have not been clearly linked to the clinical …

Drug development is a long, expensive and multistage process geared to achieving safe
drugs with high efficacy. A crucial prerequisite for completing the medication regimen for oral …

Background and Purpose Chemogenomics focuses on the discovery of new connections
between chemical and biological space leading to the discovery of new protein targets and …

The kinetics of drug binding and drug residence time are recognized to be important in the
clinical effectiveness of drug candidates. In most cases a long residence time of the drug …