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Assessing reversible and irreversible binding effects of kinase covalent inhibitors through ADP-Glo assays

Typical enzymatic inhibition assays often demonstrate improved potency for kinase covalent inhibitors compared to reversible inhibitors. This can primarily be attributed to the irreversible mode of action and could affect the evaluations of the ATP-competitive nature of covalent inhibitors, hinderin...

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Detalles Bibliográficos
Autores principales: Schröder, Martin, Chaikuad, Apirat
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8353353/
https://www.ncbi.nlm.nih.gov/pubmed/34401783
http://dx.doi.org/10.1016/j.xpro.2021.100717