| Solution Information | help | |
| Enzyme: | Sphingosine 1-phosphate receptor 3 | |
| inhibitor: | BDBM37444 | |
| 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 'Primary HTS Assay for S1P3 Antagonists' 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 = 485. As with the primary HTS assay, the same 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 antagonism. When the S1P3 receptor was stimulated by S1P agonist, transcription of the NFAT-BLA gene occurred via a G-alpha-16 protein coupled signaling cascade. The amount of BLA activity was proportional to the concentration of agonist. In this assay, in order to measure antagonist activity, test wells containing cells were treated with the Ec80 of the agonist S1P which was 800nM. BLA activity was measured with a fluorescent BLA substrate. In this exp | |
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