| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T98933 | ||||
| Target Name | Thyroid hormone receptor beta-1 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | 1-(4-hexylphenyl)-3-(propylamino)propan-1-one | Drug Info | IC50 = 15200 nM | [529081] | |
| 4-(4-hexylphenyl)-4-oxobut-2-enoic acid | Drug Info | IC50 = 17700 nM | [529081] | ||
| Detrothyronine | Drug Info | IC50 = 0.26 nM | [527923] | ||
| MB-07811 | Drug Info | Ki = 2.95 nM | [529784] | ||
| (4-hexylphenyl)(oxiran-2-yl)methanone | Drug Info | IC50 = 19100 nM | [529081] | ||
| (Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic acid | Drug Info | IC50 = 17900 nM | [529081] | ||
| (E)-1-(4-heptylphenyl)but-2-en-1-one | Drug Info | IC50 = 7600 nM | [529081] | ||
| 4-hexylphenyl propiolate | Drug Info | IC50 = 6200 nM | [529081] | ||
| 3-(3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid | Drug Info | IC50 = 1000 nM | [527532] | ||
| 2-hexylphenyl acrylate | Drug Info | IC50 = 8200 nM | [529081] | ||
| 3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | IC50 = 4300 nM | [529081] | ||
| 4-(3-(Dimethylamino)propanoyl)-N-hexylbenzamide | Drug Info | IC50 = 8100 nM | [530166] | ||
| 3-(dimethylamino)-1-(4-heptylphenyl)propan-1-one | Drug Info | IC50 = 9600 nM | [530166] | ||
| 1-(4-(Hexyloxy)phenyl)-3-morpholinopropan-1-one | Drug Info | IC50 = 4100 nM | [530166] | ||
| (3,5-Dibromo-4-butoxy-phenyl)-acetic acid | Drug Info | IC50 = 1900 nM | [527532] | ||
| 3-(dibutylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | IC50 = 4200 nM | [529081] | ||
| 1-(4-octylphenyl)prop-2-en-1-one | Drug Info | IC50 = 11400 nM | [529081] | ||
| 1-(4-heptylphenyl)prop-2-en-1-one | Drug Info | IC50 = 10500 nM | [529081] | ||
| 1-(4-hexylphenyl)-3-morpholinopropan-1-one | Drug Info | IC50 = 2700 nM | [529081] | ||
| (3,5-Dibromo-4-pentyloxy-phenyl)-acetic acid | Drug Info | IC50 = 5700 nM | [527532] | ||
| 3-bromo-1-(4-hexylphenyl)propan-1-one | Drug Info | IC50 = 3000 nM | [529081] | ||
| (3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid | Drug Info | IC50 = 800 nM | [527532] | ||
| 3-(4-(benzyloxy)-3,5-dibromophenyl)propanoic acid | Drug Info | IC50 = 230 nM | [528640] | ||
| References | |||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 527923 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1240-4. Epub 2005 Dec 9.Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta. | ||||
| Ref 529784 | J Med Chem. 2008 Nov 27;51(22):7075-93.Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 527532 | J Med Chem. 2005 May 5;48(9):3114-7.Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 530166 | J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. | ||||
| Ref 530166 | J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. | ||||
| Ref 530166 | J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. | ||||
| Ref 527532 | J Med Chem. 2005 May 5;48(9):3114-7.Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 527532 | J Med Chem. 2005 May 5;48(9):3114-7.Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. | ||||
| Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
| Ref 527532 | J Med Chem. 2005 May 5;48(9):3114-7.Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. | ||||
| Ref 528640 | Bioorg Med Chem Lett. 2007 Apr 1;17(7):2018-21. Epub 2007 Jan 13.Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. | ||||
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