Target Validation Information
TTD ID	T46828
Target Name	Dopamine D5 receptor (D5R)
Type of Target	Successful
Drug Potency against Target	(+/-)-nantenine	Drug Info	Ki = 2397 nM	[4]
	1-(4-(4-phenyl-1-piperazinyl)butyl)indolin-2-one	Drug Info	Ki = 330 nM	[2]
	1-Dibenzo[b,f]oxepin-10-yl-4-methyl-piperazine	Drug Info	IC50 = 1500 nM	[7]
	1-[2-(2-Benzyl-phenoxy)-ethyl]-piperidine	Drug Info	Ki = 43 nM	[1]
	1-[2-(2-Benzyl-phenoxy)-ethyl]-pyrrolidine	Drug Info	Ki = 951 nM	[1]
	1-[3-(2-Benzyl-phenoxy)-propyl]-pyrrolidine	Drug Info	Ki = 113 nM	[1]
	4-[2-(2-Benzyl-phenoxy)-ethyl]-morpholine	Drug Info	Ki = 366 nM	[1]
	FLUMEZAPINE	Drug Info	IC50 = 20 nM	[6]
	FLUTROLINE	Drug Info	IC50 = 14 nM	[5]
	ISOCLOZAPINE	Drug Info	IC50 = 758 nM	[7]
	ISOLOXAPINE	Drug Info	IC50 = 2480 nM	[8]
	Phenyltoloxamine	Drug Info	Ki = 414 nM	[1]
	STEPHOLIDINE	Drug Info	Ki = 4.4 nM	[3]
References
REF 1	Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 ... J Med Chem. 2004 Aug 12;47(17):4155-8.
REF 2	Synthesis of novel lactam derivatives and their evaluation as ligands for the dopamine receptors, leading to a D(4)-selective ligand. Bioorg Med Chem. 2007 Sep 1;15(17):5811-8.
REF 3	Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities Bioorg Med Chem. 2009 Oct 1;17(19):6898-907.
REF 4	Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 5	Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines. J Med Chem. 1980 Jun;23(6):635-43.
REF 6	Effects of conformationally restricted 4-piperazinyl-10H-thienobenzodiazepine neuroleptics on central dopaminergic and cholinergic systems. J Med Chem. 1982 Oct;25(10):1133-40.
REF 7	Affinity of 10-(4-methylpiperazino)dibenz[b,f]oxepins for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1982 Jul;25(7):855-8.
REF 8	Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6.

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