| Solution Information | help | |
| Enzyme: | Sphingosine 1-phosphate receptor 3 | |
| inhibitor: | BDBM37335 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: Compounds identified from a previously described set of experiments entitled "S1P3 Agonist Primary HTS and Confirmation Assays" were selected for testing in this assay. Further information on the previous set of experiments can be found by searching on this website for PubChem AID = 373. A cell line containing the human S1P3 receptor as well as the beta-lactamase (BLA) reporter-gene under control of the nuclear factor of activated T-cells (NFAT) promoter was used to measure S1P3 agonism. If the S1P3 receptor was stimulated by agonist, transcription of the NFAT-BLA gene occurred via a G-alpha16 protein coupled signaling cascade. The amount of BLA activity was proportional to the concentration of agonist. BLA activity was measured with a fluorescent BLA substrate. In this experiment, 69 compounds that passed hit selection criteria were tested to determine individual EC50 values. The compounds were "hit-picked" at a 10 millimolar in DMSO and further serially diluted | |
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