Target Validation Information
TTD ID	T75440
Target Name	Translocator protein (TSPO)
Type of Target	Successful
Drug Potency against Target	Dextofisopam	Drug Info	IC50 < 100 nM	[6]
		Drug Info	Ki = 100 nM	[5]
	(R)PK-11195	Drug Info	IC50 = 8.26 nM	[1]
	4-Methoxy-5-phenyl-6-thia-10b-aza-benzo[e]azulene	Drug Info	Ki = 7000 nM	[3]
	5-Phenyl-6-thia-10b-aza-benzo[e]azulen-4-one	Drug Info	IC50 = 1220 nM	[4]
	5-Phenyl-6-thia-10b-aza-benzo[e]azulene	Drug Info	Ki = 3150 nM	[3]
	6-Thia-10b-aza-benzo[e]azulen-4-one	Drug Info	IC50 = 14000 nM	[4]
	Alpidem	Drug Info	Ki = 0.5 nM	[2]
	N,N-Diethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	Drug Info	Ki = 156 nM	[5]
	N,N-Dihexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	Drug Info	Ki = 9.7 nM	[5]
	N,N-Dimethyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	Drug Info	Ki = 170 nM	[5]
	N-Hexyl-2-(2-phenyl-1H-indol-3-yl)-acetamide	Drug Info	Ki = 96 nM	[5]
References
REF 1	[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). Bioorg Med Chem Lett. 2003 Jan 20;13(2):201-4.
REF 2	Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis. J Med Chem. 2008 Sep 25;51(18):5798-806.
REF 3	A concerted study using binding measurements, X-ray structural data, and molecular modeling on the stereochemical features responsible for the affi... J Med Chem. 1995 Nov 10;38(23):4730-8.
REF 4	Novel ligands specific for mitochondrial benzodiazepine receptors: 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives. Synthesis, structure-activ... J Med Chem. 1994 May 13;37(10):1427-38.
REF 5	Chemistry, binding affinities, and behavioral properties of a new class of "antineophobic" mitochondrial DBI receptor complex (mDRC) ligands. J Med Chem. 1993 Oct 1;36(20):2908-20.
REF 6	Tofizopam affects binding of [3H]muscimol to gamma-amino-butyric acid receptors in rat and mouse brains. Pharmacol Res Commun. 1982 Sep;14(8):745-57.

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