| Assay Method Information | |
| | UGT1A1 Inhibition Assay |
| Description: | KCI838 was incubated at seven increasing concentrations with human UGT1A1-expressed Supersomes (0.25 mg/mL), alamethicin (25 μg/mL) and UDPGA (5 mM) in the presence of the probe substrate estradiol (10 μM) for 30 min at 37 C. The UGT1A1 inhibitor, atazanavir, was screened alongside the test compounds as a positive control. The reactions were terminated by quenching with one volume of methanol containing an analytical internal standard. The samples will be centrifuged at 5000 rpm for 10 min at 4 C. The metabolites were monitored by LC-MS/MS and a decrease in the formation of the metabolite compared to the vehicle control was used to calculate an IC50 value (test compound concentration which produces 50% inhibition). |
| Affinity data for this assay | |
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