| Assay Method Information | |
| | In Vitro Cav3.1 Single Point and IC50 (VDB) Data |
| Description: | The compound plate was created at 2× concentrated in the extracellular solution. The compound was diluted to 1:2 when added to the recording well. The amount of DMSO in the extracellular solution was held constant at the level used for the highest tested concentration. For the voltage clamp experiments on Cav3.1, data were sampled at 10 KHz. After establishment of the seal and the passage in the whole cell configuration, the cells were held at −120 mV. Cav3.1 current was evoked using a 100 ms step to −20 mV (to measure resting state block), followed by a 1600 ms step to −65 mV and a second 100 ms step to −20 mV (to measure voltage dependent block). The voltage protocol was applied every 15 seconds in the absence and in the presence of the compounds under investigation. 2.5 mM Nickel was used to completely inhibit Cav3.1 current to allow for offline subtraction of non-Cav3.1 current. Current amplitude (pA) was measured in the peak 1 and 2. The average of last 3 sweeps of each liquid period (vehicle, compound under investigation, full block) was calculated. Nickel-sensitive current was used to calculate the % of inhibition in the presence of the compound under investigation. |
| Affinity data for this assay | |
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