Target Validation Information
TTD ID	T11211
Target Name	Androgen receptor (AR)
Type of Target	Successful
Drug Potency against Target	1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane	Drug Info	IC50 = 163 nM	[5]
	11-methyl-6,11-dihydro-5H-benzo[a]carbazol-9-ol	Drug Info	IC50 = 30 nM	[4]
	6,11-dihydrothiochromeno[4,3-b]indol-8-ol	Drug Info	IC50 = 4500 nM	[4]
	RU-59063	Drug Info	Ki = 2.23 nM	[1]
	ZANOTERONE	Drug Info	Ki = 2200 nM	[2]
	ZANOTERONE	Drug Info	Ki = 2000 nM	[3]
	[3H]mibolerone	Drug Info	Ki = 0.75 nM	[1]
References
REF 1	Design, synthesis, and pharmacological characterization of 4-[4, 4-dimethyl-3-(4-hydroxybutyl)-5-oxo-2-thioxo-1-imidazolidinyl]- 2-iodobenzonitrile... J Med Chem. 2000 Aug 24;43(17):3344-7.
REF 2	Chiral derivatives of 2-cyclohexylideneperhydro-4,7-methanoindenes, a novel class of nonsteroidal androgen receptor ligand: synthesis, X-ray analys... J Med Chem. 2000 Nov 30;43(24):4629-35.
REF 3	Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. J Med Chem. 1992 May 15;35(10):1663-70.
REF 4	Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3233-7.
REF 5	Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist. J Med Chem. 2006 Dec 14;49(25):7366-72.

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