Fitting of kinact and KI Values from Endpoint Pre-incubation IC50 Data
Covalent Modifiers
APRIL 7, 2024
Lavleen K. Mader and Jeffrey W. Keillor ACS Medicinal Chemistry Letters 2024 DOI: 10.1021/acsmedchemlett.4c00054 Experiments comprising a “pre-incubation” phase, where enzyme is incubated with inhibitor prior to the addition of assay substrate, are commonly used to evaluate covalent inhibitors, often via discontinuous or “endpoint” IC50 assays. However, due to the lack of mathematical tools to describe its biphasic time-dependent nature, this experiment has thus far been unable to provide kinact
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