| Solution Information | help | |
| Enzyme: | Sphingosine 1-phosphate receptor 2 | |
| inhibitor: | BDBM41664 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: A cell line expressing the beta-lactamase (BLA) reporter-gene under control of the cAMP Response Element (CRE) promoter was used to measure activation of the CRE pathway. Under normal conditions, the cells have low CRE basal activity and therefore cells express low BLA levels. Stimulation of the CRE pathway by an agonist induces transcription of the BLA gene in proportion to agonist concentration, resulting in increased BLA activity. This increase is monitored by measuring fluorescence resonance energy transfer (FRET) of a cleavable fluorogenic cell permeable BLA substrate. Protocol Summary: In this assay 63 available out of 64 compounds that had greater than 50 percent activity and passed hit selection criteria from a previous set of experiments entitled, "Primary Cell-Based High-Throughput Screening to Identify Agonists of the Sphingosine 1-Phosphate Receptor 2" (PubChem AID = 729) were assayed for their ability to activate the CRE-BLA reporter in the parental c | |
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