Abstract
Glutathione trapping enables the detection and characterization of reactive metabolites which result from enzymatic bioactivation of compounds. Data obtained from this assay is used to estimate any potential bioactivation liabilities associated with drugs. This is useful in terms of guidance for design and safety assessment of discovery compounds. There are several reported variations of GSH trapping assays, each with their own unique advantages and disadvantages. Here, we describe a simplified reactive metabolite screening assay optimized for semi-high throughput analysis of drug discovery candidates.
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Johnson, K.M. (2021). Cytochrome P450-Mediated Drug Bioactivation Assay: An Untargeted High Resolution Accurate Mass LC/MS Assay. In: Yan, Z., Caldwell, G.W. (eds) Cytochrome P450. Methods in Pharmacology and Toxicology. Humana, New York, NY. https://doi.org/10.1007/978-1-0716-1542-3_19
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DOI: https://doi.org/10.1007/978-1-0716-1542-3_19
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