| Solution Information | help | |
| Enzyme: | Melanin-concentrating hormone receptor 1 | |
| inhibitor: | BDBM75927 | |
| 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 for a set of synthesized compounds in a 384-well format counterscreen assay for antagonism of the melanin-concentrating hormone receptor 1 (MCHR1). MCHR1 (GPR24) is the receptor for MCH, a cyclic hypothalamic neuropeptide that promotes food intake (14), increases leptin and insulin release (15), and modulates energy metabolism (16). This assay employs HEK cells stably co-transfected with human MCHR1 and a chimeric Gaqi3. Cells are treated with test compounds followed by measurement of intracellular calcium as monitored by the FLUO-8 fluorescent, cell permeable calcium indicator dye. As designed, compounds that act as human MCHR1 antagonists will decrease calcium mobilization, resulting in decreased relative fluorescence of the indicator dye, and thus decreased well fluorescence. Test compounds were assayed in triplicate in an 8-point 1:3 dilution series starting at a nominal test concentration of 20 uM. Protocol | |
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