Target Validation Information
TTD ID	T55815
Target Name	Neuronal acetylcholine receptor alpha-2 (CHRNA2)
Type of Target	Successful
Drug Potency against Target	Carbachol	Drug Info	Ki = 728 nM	[6]
	Tubocurarine	Drug Info	Ki = 7770 nM	[6]
	(S)-3-(azetidin-2-ylmethoxy)-2-fluoropyridine	Drug Info	Ki = 180 nM	[5]
	1,1-Dimethyl-4-phenyl-piperazin-1-ium iodide	Drug Info	Ki = 1300 nM	[1]
	1-(piperidin-3-ylmethyl)pyridin-2(1H)-one	Drug Info	Ki = 4630 nM	[4]
	1-(piperidin-4-ylmethyl)pyridin-2(1H)-one	Drug Info	Ki = 3600 nM	[4]
	2-Pyridin-3-yl-7-aza-bicyclo[2.2.1]heptane	Drug Info	Ki = 3.3 nM	[2]
	3-((S)-Azetidin-2-yloxy)-5-iodo-pyridine	Drug Info	Ki = 47 nM	[1]
	5-(1-Methyl-pyrrolidin-2-yl)-2-phenethyl-pyridine	Drug Info	Ki = 1200 nM	[3]
	CHOLINE	Drug Info	Ki = 18000 nM	[1]
	CYTISINE	Drug Info	Ki = 5.41 nM	[4]
References
REF 1	Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1845-8.
REF 2	Epibatidine structure-activity relationships. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1889-96.
REF 3	6-(2-Phenylethyl)nicotine: a novel nicotinic cholinergic receptor ligand. Bioorg Med Chem Lett. 2005 Jul 1;15(13):3237-40.
REF 4	Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity. J Med Chem. 2006 May 4;49(9):2673-6.
REF 5	Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acety... Bioorg Med Chem. 2009 Jul 1;17(13):4367-77.
REF 6	Receptor binding thermodynamics at the neuronal nicotinic receptor. Curr Top Med Chem. 2004;4(3):361-8.

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