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• W2962123024 abstract "An increased appreciation of the importance of optimizing drug-binding kinetics has lead to the development of various techniques for measuring the kinetics of unlabeled compounds. One approach is the competition-association kinetic binding method first described in the 1980s. The kinetic characteristics of the tracer employed greatly affects the reliability of estimated kinetic parameters, a barrier to successfully introducing these kinetic assays earlier in the drug discovery process. Using a modeling and Monte Carlo simulation approach, we identify the optimal tracer characteristics for determining the kinetics of the range of unlabeled ligands typically encountered during the different stages of a drug discovery program (i.e., rapidly dissociating, e.g., <i>k</i>_off = 10 minute⁻¹ low-affinity “hits” through to slowly dissociating e.g., <i>k</i>_off = 0.01 minute⁻¹ high-affinity “candidates”). For more rapidly dissociating ligands (e.g., <i>k</i>_off = 10 minute⁻¹), the key to obtaining accurate kinetic parameters was to employ a tracer with a relatively fast off-rate (e.g., <i>k</i>_off = 1 minute⁻¹) or, alternatively, to increase the tracer concentration. Reductions in assay start-time ≤1second and read frequency ≤5 seconds significantly improved the reliability of curve fitting. Timing constraints are largely dictated by the method of detection, its inherent sensitivity (e.g., TR-FRET versus radiometric detection), and the ability to inject samples online. Furthermore, we include data from TR-FRET experiments that validate this simulation approach, confirming its practical utility. These insights into the optimal experimental parameters for development of competition-association assays provide a framework for identifying and testing novel tracers necessary for profiling unlabeled competitors, particularly rapidly dissociating low-affinity competitors." @default.
• W2962123024 created "2019-07-23" @default.
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• W2962123024 date "2019-07-10" @default.
• W2962123024 modified "2023-10-17" @default.
• W2962123024 title "Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds" @default.
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• W2962123024 doi "https://doi.org/10.1124/mol.119.116764" @default.
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