High-throughput kinetics in drug discovery

被引：1

作者：

Pinto, Maria Filipa ^{[1
]}

Sirina, Julija ^{[2
]}

Holliday, Nicholas D. ^{[2
,3
]}

Mcwhirter, Claire L. ^{[1
]}

机构：

[1] Artios Pharma Ltd, B940,Babraham Res Campus, Cambridge CB22 3FH, England

[2] Excellerate Biosci Ltd, 21 Triangle,NG2 Business Pk, Nottingham NG2 1AE, England

[3] Univ Nottingham, Sch Life Sci, Med Sch, Nottingham NG7 2UH, England

来源：

SLAS DISCOVERY | 2024年 / 29卷 / 05期

关键词：

Mechanism of inhibition (MoI); High; -throughput; Enzyme kinetics; TARGET RESIDENCE TIME; BINDING-KINETICS; PHARMACOLOGICAL CHARACTERIZATION; CLINICAL PHARMACOKINETICS; ENZYME-KINETICS; LIGAND-BINDING; INHIBITORS; COVALENT; ASSAY; MECHANISMS;

D O I：

10.1016/j.slasd.2024.100170

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页数：14

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