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| Solution Information | help | |
| Enzyme: | Isoform 2 of Nuclear receptor ROR-alpha (Alpha-2) | |
| inhibitor: | BDBM38917 | |
| 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 Cell-based High Throughput Screening assay for inhibitors of the Retinoic Acid Receptor-related orphan receptor A (RORA)" were selected for testing in this assay. Further information on the primary screen can be found by searching on this website for PubChem AID=561. Among 278 compounds selected during the primary screening, 273 compounds were assessed in dose-response experiments in 10 point, 1:3 serial dilutions starting at a nominal test concentration of 100 micromolar. As with the primary screen, the dose-response assay utilizes a fusion of the DNA-binding domain of the yeast transcriptional factor Gal4 with the ligand-binding domain of target receptor RORA (encoded by the pFA-hRORA plasmid, Orphagen Pharmaceuticals) to regulate a luciferase reporter containing 5xGal4 response elements at its promoter region (pG5-luc, Stratagene). Both pFA-hRORA and pG5-luc plasmids are transient | |
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