| Solution Information | help | |
| Enzyme: | Isoform 2 of Nuclear receptor ROR-alpha (Alpha-2) | |
| inhibitor: | BDBM39529 | |
| substrate: | n/a | |
| Solution Type: | Aqueous | |
| pH at Preparation: | n/a | |
| Temp. Prep.: | n/a | |
| Comments: | Assay Overview: Nine hundred and seventy nine compounds have been identified as hits during a previously described set of experiments entitled "Primary Cell-based High Throughput Screening assay for activators of the Retinoic Acid Receptor-related orphan receptor A (RORA)". Further information on the primary screen can be found by searching on this website for PubChem AID=560. Among those hits, a subset of compounds showing selectivity towards RORA was selected by applying the following criteria: (1) RORA% >70% AND S/A>4 OR (2) 70>RORA % >50 AND S/A>6 OR(3) RORA% >50 AND SF1% <0 where "RORA%" represents the percentage of activation measured in the RORA primary screening (AID=560), "SF1%" the percentage of activation measured in the SF1 primary screening (AID=522) and "S/A" the ratio RORA% / SF1%. Sixty three compounds selected using criteria stated above were assessed in dose-response experiments in 10 point, 1:3 serial dilutions starting at a nominal test concentration of 100 m | |
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