| Assay Method Information | |
| | Cytochrome P450 Inhibition of VNN1 Inhibitors |
| Description: | Table 3 and 4: The cocktail was incubated in human liver microsome with NADPH regenerating system (NRS) in a shaking bath at 37±2° C. The formation of specific metabolites was monitored by LC/MS/MS. Test compound was added to the cocktail-liver microsome mixture at varying concentrations and its effect on cytochrome P450 activity was determined by analyzing the rate of specific metabolite formation. The percent inhibition was calculated and plotted with reference to the concentration, and the IC50 value for inhibition was derived by fitting the data with a standard sigmoidal dose-response equation via MLA “Quest Graph™ ED50 Calculator.” AAT Bioquest, Inc, 17 Sep. 2020, aatbio.com/tools/ed50-calculator. IC50 values were obtained only when the data fit in the curve, and if the % inhibition was less than 50% at 100 μM, then IC50 will be >100 μM. The reliability of the inhibition assay was established by confirming the inhibition of known inhibitors on different P450 enzymes. |
| Affinity data for this assay | |
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