| Assay Method Information | |
| | Biochemical hERG Inhibition Assay |
| Description: | 1. Test System: Kit: Predictor hERG fluorescence polarization detection kit (ThermoFisher), the kit contained the following components: positive control compound hERG potassium channel blocker E4031; hERG cell membrane; affinity tracer Tracer; and hERG buffer. 2. Test Parameters: hERG concentration: 1 ; Tracer concentration: 1 nM; incubation time: 2 h; BMG PHERAstar FS FP. 3. Test Method: The test was carried out according to the kit instructions, and the steps were as follows: Test group: 10 μM and 1 μM of the test compound were added to the microplate containing hERG cell membrane, the Tracer (a tracer with high hERG affinity) was added to each well, the microplate was incubated at room temperature for 2 hours, and a multi-plate reader was used to detect changes of fluorescence polarization values (excitation wavelength: 540 nm; emission wavelength: 590 nm). Positive control group: 30 μM positive control compound E4031 was used to replace the test compound, and the experimental method was the same as that of the test group. Blank control group: hERG buffer was used to replace the test compound without the addition of hERG cell membrane, and the experimental method was the same as that of the test group. 4. Data Processing: According to the data ratio, the percent inhibition rates (%) of the compounds of the present invention to hERG at different concentrations were calculated, and the ranges of the half inhibitory concentration (IC50) of the compounds were determined. |
| Affinity data for this assay | |
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