| Solution Information | help | |
| Enzyme: | Galanin receptor type 2 | |
| inhibitor: | BDBM41947 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this assay is to determine dose response curves of compounds that were identified as active in a previous set of experiments entitled, "Confirmatory cell-based high-throughput screening assay to identify agonists of galanin receptor 2 (GALR2)" (PubChem AID 864). Test compounds were assayed in triplicate in a 10-point, 1:3 dilution series starting at a nominal test concentration of approximately 56 micromolar. This assay also serves to determine whether these compounds were assay artifact due to non-specific activation of the beta-lactamase reporter gene or interference with the assay readout. In this assay a cell line stably expressing the beta-lactamase (BLA) reporter under control of the Nuclear Factor of Activated T-cells (NFAT) promoter was used. Changes in BLA expression are monitored by measuring fluorescence resonance energy transfer (FRET) of a cleavable fluorogenic cell permeable BLA substrate. As designed, a compound that increases FRE | |
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