| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T72841 | ||||
| Target Name | Estrogen-related receptor-alpha (ESRRA) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol | Drug Info | IC50 = 60 nM | [1] | |
| 4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | IC50 = 4.3 nM | [1] | ||
| 4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | IC50 = 4.6 nM | [1] | ||
| 4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | IC50 = 52 nM | [1] | ||
| 4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | IC50 = 75 nM | [1] | ||
| 7-bromo-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | IC50 = 3.6 nM | [1] | ||
| 7-chloro-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | IC50 = 3.3 nM | [1] | ||
| 7-ethyl-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | IC50 = 46 nM | [1] | ||
| 7-ethynyl-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | IC50 = 52 nM | [1] | ||
| 7-vinyl-6H-chromeno[4,3-b]quinoline-3,9-diol | Drug Info | IC50 = 22 nM | [1] | ||
| References | |||||
| REF 1 | ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4053-6. | ||||
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