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Review
. 2024 Jul;29(5):100170.
doi: 10.1016/j.slasd.2024.100170. Epub 2024 Jul 3.

High-throughput kinetics in drug discovery

Maria Filipa Pinto  1 , Julija Sirina  2 , Nicholas D Holliday  3 , Claire L McWhirter  4
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Free article
Review

High-throughput kinetics in drug discovery

Maria Filipa Pinto et al. SLAS Discov. 2024 Jul.
Free article

Abstract

The importance of a drug's kinetic profile and interplay of structure-kinetic activity with PK/PD has long been appreciated in drug discovery. However, technical challenges have often limited detailed kinetic characterization of compounds to the latter stages of projects. This review highlights the advances that have been made in recent years in techniques, instrumentation, and data analysis to increase the throughput of detailed kinetic and mechanistic characterization, enabling its application earlier in the drug discovery process.

Keywords: Enzyme kinetics; High-throughput; Mechanism of inhibition (MoI).

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Conflict of interest statement

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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