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| Solution Information | help | |
| Enzyme: | Isoform 2 of Nuclear receptor corepressor 2 (TRAC-1) | |
| inhibitor: | BDBM66188 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: The purpose of this biochemical assay is to determine whether compounds identified as active in a previous set of experiments entitled, "TR-FRET-based primary biochemical high throughput screening assay to identify agonists of nuclear receptor subfamily 2, group E, member 3 (NR2E3)" (AID 2300), and that confirmed activity in a previous set of experiments entitled, "TR-FRET-based biochemical high throughput confirmation assay to identify agonists of nuclear receptor subfamily 2, group E, member 3 (NR2E3)" (AID 2379) were nonselective due to activation of the interaction between PPARgamma-NCOR2. This assay determines dose response curves for tested compounds. In this HTRF-format assay GST-PPARg and its interaction partner, a biotinylated corepressor NCOR2 are incubated in the presence of test compounds, Eu(K)-anti GST antibody, and Streptavidin-D2. Interaction between the NCOR2 and PPARg partners brings the fluorophores together, leading to well FRET. As designed, test | |
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