Target Validation Information
TTD ID	T98933
Target Name	Thyroid hormone receptor beta (THRB)
Type of Target	Successful
Drug Potency against Target	(3,5-Dibromo-4-butoxy-phenyl)-acetic acid	Drug Info	IC50 = 1900 nM	[1]
	(3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid	Drug Info	IC50 = 800 nM	[1]
	(3,5-Dibromo-4-pentyloxy-phenyl)-acetic acid	Drug Info	IC50 = 5700 nM	[1]
	(4-hexylphenyl)(oxiran-2-yl)methanone	Drug Info	IC50 = 19100 nM	[4]
	(E)-1-(4-heptylphenyl)but-2-en-1-one	Drug Info	IC50 = 7600 nM	[4]
	(Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic acid	Drug Info	IC50 = 17900 nM	[4]
	1-(4-(Hexyloxy)phenyl)-3-morpholinopropan-1-one	Drug Info	IC50 = 4100 nM	[6]
	1-(4-heptylphenyl)prop-2-en-1-one	Drug Info	IC50 = 10500 nM	[4]
	1-(4-hexylphenyl)-3-(propylamino)propan-1-one	Drug Info	IC50 = 15200 nM	[4]
	1-(4-hexylphenyl)-3-morpholinopropan-1-one	Drug Info	IC50 = 2700 nM	[4]
	1-(4-octylphenyl)prop-2-en-1-one	Drug Info	IC50 = 11400 nM	[4]
	2-hexylphenyl acrylate	Drug Info	IC50 = 8200 nM	[4]
	3-(3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid	Drug Info	IC50 = 1000 nM	[1]
	3-(4-(benzyloxy)-3,5-dibromophenyl)propanoic acid	Drug Info	IC50 = 230 nM	[3]
	3-(dibutylamino)-1-(4-hexylphenyl)propan-1-one	Drug Info	IC50 = 4200 nM	[4]
	3-(dimethylamino)-1-(4-heptylphenyl)propan-1-one	Drug Info	IC50 = 9600 nM	[6]
	3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one	Drug Info	IC50 = 4300 nM	[4]
	3-bromo-1-(4-hexylphenyl)propan-1-one	Drug Info	IC50 = 3000 nM	[4]
	4-(3-(Dimethylamino)propanoyl)-N-hexylbenzamide	Drug Info	IC50 = 8100 nM	[6]
	4-(4-hexylphenyl)-4-oxobut-2-enoic acid	Drug Info	IC50 = 17700 nM	[4]
	4-hexylphenyl propiolate	Drug Info	IC50 = 6200 nM	[4]
	Detrothyronine	Drug Info	IC50 = 0.26 nM	[2]
	MB-07811	Drug Info	Ki = 2.95 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	Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. J Med Chem. 2009 Jul 9;52(13):3892-901.

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