| Solution Information | help | |
| Enzyme: | Sphingosine 1-phosphate receptor 3 | |
| inhibitor: | BDBM31372 | |
| 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 compounds identified as active in a previous set of experiments entitled, "Primary HTS Assay for S1P3 Antagonists," (PubChem AID 485) and that confirmed activity in a subsequent set of experiments entitled, "Confirmation cell-based high throughput screening assay to identify S1P3 antagonists," (PubChem AID 1429). In this assay, a CHO cell line containing human S1P3 and the beta-lactamase (BLA) reporter-gene under the control of the nuclear factor of activated T-cells (NFAT) promoter was used to measure S1P3 antagonism by test compound. Stimulation of S1P3 by S1P induces transcription of NFAT-BLA via a G-alpha16 protein coupled signaling cascade, and an increase in BLA activity. BLA activity is measured using a BLA FRET substrate. As designed, a compound that acts as a S1P3 antagonist will decrease well FRET. Compounds were tested in triplicate using a 10-point 1:3 dilution series, starting at a nominal | |
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