| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T79591 | ||||
| Target Name | Thyroid hormone receptor alpha (THRA) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Liothyronine | Drug Info | IC50 = 0.3 nM | [6] | |
| (3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid | Drug Info | IC50 = 700 nM | [1] | ||
| (E)-1-(4-heptylphenyl)but-2-en-1-one | Drug Info | IC50 = 18900 nM | [4] | ||
| (Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic acid | Drug Info | IC50 = 17500 nM | [4] | ||
| 1-(4-hexylphenyl)-3-morpholinopropan-1-one | Drug Info | IC50 = 4100 nM | [4] | ||
| 3-(3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid | Drug Info | IC50 = 600 nM | [1] | ||
| 3-(4-(benzyloxy)-3,5-dibromophenyl)propanoic acid | Drug Info | IC50 = 680 nM | [3] | ||
| 3-(dibutylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | IC50 = 6900 nM | [4] | ||
| 3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | IC50 = 10600 nM | [4] | ||
| 3-bromo-1-(4-hexylphenyl)propan-1-one | Drug Info | IC50 = 4200 nM | [4] | ||
| 4-(4-hexylphenyl)-4-oxobut-2-enoic acid | Drug Info | IC50 = 19200 nM | [4] | ||
| 4-hexylphenyl propiolate | Drug Info | IC50 = 16700 nM | [4] | ||
| Detrothyronine | Drug Info | IC50 = 0.24 nM | [2] | ||
| MB-07811 | Drug Info | Ki = 35.2 nM | [5] | ||
| References | |||||
| REF 1 | Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. J Med Chem. 2005 May 5;48(9):3114-7. | ||||
| REF 2 | Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1240-4. | ||||
| REF 3 | Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. Bioorg Med Chem Lett. 2007 Apr 1;17(7):2018-21. | ||||
| REF 4 | Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. J Med Chem. 2007 Nov 1;50(22):5269-80. | ||||
| REF 5 | Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. J Med Chem. 2008 Nov 27;51(22):7075-93. | ||||
| REF 6 | Recent advances in the development of agonists selective for beta1-type thyroid hormone receptor. Mini Rev Med Chem. 2007 Jan;7(1):79-86. | ||||
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