Target Validation Information
TTD ID	T70967
Target Name	Neuronal acetylcholine receptor alpha-4 (CHRNA4)
Type of Target	Successful
Drug Potency against Target	Pentolinium	Drug Info	IC50 = 3400 nM	[10]
	Trimethaphan	Drug Info	IC50 = 12500 nM	[10]
	Varenicline	Drug Info	EC50 = 2300 nM	[9]
	Sofinicline	Drug Info	EC50 = 40 nM	[6]
	(2S,3S)-2-(m-Tolyl)-3,5,5-trimethylmorpholin-2-ol	Drug Info	IC50 = 6000 nM	[7]
	(2S,3S)-2-Phenyl-3,5,5-trimethylmorpholin-2-ol	Drug Info	IC50 = 6400 nM	[7]
	3-[2-(N,N,N-trimethylammonium)ethoxy]pyridine	Drug Info	Ki = 0.5 nM	[2]
	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Drug Info	Ki < 1000 nM	[8]
	6'-methylepibatidine	Drug Info	Ki = 256 nM	[5]
	BOLDINE	Drug Info	Ki = 3000 nM	[4]
	CYTISINE	Drug Info	Ki = 2.59 nM	[3]
	HOMOEPIBATIDINE	Drug Info	Ki = 0.127 nM	[3]
	N,N-dimethyl(pyridin-3-yl)methanamine	Drug Info	Ki = 540 nM	[1]
	N,N-dimethyl-2-(pyridin-3-yloxy)ethanamine	Drug Info	Ki = 21 nM	[1]
	N,N-dimethyl-4-(pyridin-3-yl)but-3-yn-1-amine	Drug Info	Ki = 510 nM	[1]
	N-ethyl-N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine	Drug Info	Ki = 1770 nM	[1]
	N-methyl-2-(pyridin-3-yloxy)ethanamine	Drug Info	Ki = 35 nM	[1]
	N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine	Drug Info	Ki = 113 nM	[1]
	N-methyl-N-(pyridin-3-ylmethyl)ethanamine	Drug Info	Ki = 28 nM	[1]
	Predicentrine methiodide	Drug Info	Ki = 970 nM	[4]
References
REF 1	Synthesis and analgesic activity of secondary amine analogues of pyridylmethylamine and positional isomeric analogues of ABT-594. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2013-6.
REF 2	Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4283-6.
REF 3	Epibatidine isomers and analogues: structure-activity relationships. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5493-7.
REF 4	Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. Bioorg Med Chem. 2007 May 15;15(10):3368-72.
REF 5	Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine. J Med Chem. 2007 Dec 13;50(25):6383-91.
REF 6	In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methy... J Pharmacol Exp Ther. 2009 Jul;330(1):257-67.
REF 7	Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation. J Med Chem. 2010 Jun 24;53(12):4731-48.
REF 8	Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 9	Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5.
REF 10	Beta-subunits co-determine the sensitivity of rat neuronal nicotinic receptors to antagonists. Pflugers Arch. 1995 Jan;429(3):449-51.

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