| Solution Information | help | |
| Enzyme: | Galanin receptor type 2 | |
| inhibitor: | BDBM42057 | |
| 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 for test compounds from the MLSCN library that were active in a previous screen entitled, "Confirmatory cell-based high-throughput screening assay to identify antagonists of galanin receptor 2 (GALR2)," (PubChem AID 866). Compounds were assessed in triplicate in a 10-point, 1:3 dilution series starting at a nominal test concentration of 42 uM. In this assay GALR2 antagonism was measured using a cell line stably expressing human GALR2 and beta-lactamase (BLA) genes under control of the Nuclear Factor of Activated T-cells (NFAT) promoter. Stimulation of GALR2 and coupling to Gq induces release of cytoplasmic Ca2+ and nuclear translocation of NFAT where it activates transcription of the BLA reporter gene. In the presence of antagonist GALR2 exhibits low basal activity and cells express low BLA levels. Thus, BLA expression is inversely proportional to antagonist concentration. Changes in BLA expression a | |
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