| Solution Information | help | |
| Enzyme: | Sphingosine 1-phosphate receptor 2 | |
| inhibitor: | BDBM62228 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: A Chinese Hamster Ovary (CHO) cell line stably transfected with the human S1P2 receptor and a cAMP Response Element-beta lactamase (CRE-BLA) reporter construct was used to measure S1P2 antagonism. Under normal conditions, S1P2 has low basal activity and therefore cells express low BLA levels. In this assay, cells have been stimulated with the S1P agonist, which stimulates the S1P2 receptor, hence increasing BLA gene transcription. An antagonist is identified as a compound that prevents activation by exogenously added S1P. Therefore, in the presence of a potential S1P2 antagonist, transcription of the BLA gene will decrease. This decrease is monitored by measuring fluorescence resonance energy transfer (FRET) of a cleavable fluorogenic cell permeable BLA substrate. As designed, test compounds that act as S1P2 antagonists will inhibit BLA transcription and cleavage of the fluorogenic substrate, leading to no increase in well FRET. Compounds were tested in triplicate us | |
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