Target Validation Information
Target ID T79591
Target Name Thyroid hormone receptor alpha
Target Type
Successful
Drug Potency against Target Detrothyronine Drug Info IC50 = 0.24 nM [527923]
(Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic acid Drug Info IC50 = 17500 nM [529081]
3-(dibutylamino)-1-(4-hexylphenyl)propan-1-one Drug Info IC50 = 6900 nM [529081]
3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one Drug Info IC50 = 10600 nM [529081]
(E)-1-(4-heptylphenyl)but-2-en-1-one Drug Info IC50 = 18900 nM [529081]
4-hexylphenyl propiolate Drug Info IC50 = 16700 nM [529081]
Liothyronine Drug Info IC50 = 0.3 nM [552674]
3-(3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid Drug Info IC50 = 600 nM [527532]
3-bromo-1-(4-hexylphenyl)propan-1-one Drug Info IC50 = 4200 nM [529081]
MB-07811 Drug Info Ki = 35.2 nM [529784]
1-(4-hexylphenyl)-3-morpholinopropan-1-one Drug Info IC50 = 4100 nM [529081]
4-(4-hexylphenyl)-4-oxobut-2-enoic acid Drug Info IC50 = 19200 nM [529081]
(3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid Drug Info IC50 = 700 nM [527532]
3-(4-(benzyloxy)-3,5-dibromophenyl)propanoic acid Drug Info IC50 = 680 nM [528640]
References
Ref 527923Bioorg 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 529081J 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 529081J 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 529081J 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 529081J 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 529081J 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 552674Recent advances in the development of agonists selective for beta1-type thyroid hormone receptor. Mini Rev Med Chem. 2007 Jan;7(1):79-86.
Ref 527532J 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 529081J 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 529784J 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 529081J 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 529081J 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 527532J 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 528640Bioorg 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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