Neuronal acetylcholine receptor; alpha4/beta2 Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Nicotine	IC50	427.0 [1]
	Nicotine	Ki	1.05 [1]
	Varenicline	IC50	39.0 [1], 70.0 [2], 94.0 [3], 50000.0 [4]
	Epibatidine	IC50	1.06 [1]
	Epibatidine	Ki	0.07 [1]
	Sazetidine A	IC50	4.8 [1], 7.5 [2], 11.0 [3]
	Sazetidine A	Ki	0.06 [1]
	Cytisine	IC50	50.0 [1], 28000.0 [2]
	Cytisine	Ki	0.23 [1], 2.0 [2], 2.59 [3]
	(S)-3-(Azetidin-2-ylmethoxy)pyridine	IC50	1.51 [1]
	(S)-3-(Azetidin-2-ylmethoxy)pyridine	Ki	0.04 [1], 0.05 [2]
	Bupropion	IC50	12.0 [1], 12000.0 [2]
	Dihydro-beta-erythroidine	IC50	20.0 [1], 410.0 [2]
	Dihydro-beta-erythroidine	Ki	98.0 [1]
	N,N-Dimethyl-2-(pyridin-3-yloxy)ethanamine	Ki	21.0 [1], 300.0 [2]
	Dimethyl-pyridin-3-ylmethyl-amine	Ki	540.0 [1]
	N-Methyl-4-(pyridin-3-yl)but-3-yn-1-amine	Ki	58.0 [1], 113.0 [2]
	3-[(2s)-Azetidin-2-Ylmethoxy]-5-[(1s,2r)-2-(2-Methoxyethyl)cyclopropyl]pyridine	IC50	5.6 [1]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-hex-1-ynyl-2-methylpyridine	IC50	18.0 [1], 260.0 [2]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-hex-1-ynyl-2-methylpyridine	Ki	12.0 [1]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-fluorohex-1-ynyl)-2-methylpyridine	IC50	130.0 [1], 140.0 [2]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-fluorohex-1-ynyl)-2-methylpyridine	Ki	4.2 [1]
	6-[5-[[(2S)-Azetidin-2-yl]methoxy]-6-methylpyridin-3-yl]hex-5-yn-1-ol	IC50	42.0 [1], 51.0 [2]
	6-[5-[[(2S)-Azetidin-2-yl]methoxy]-6-methylpyridin-3-yl]hex-5-yn-1-ol	Ki	4.3 [1]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-chlorohex-1-ynyl)-2-methylpyridine	IC50	260.0 [1], 270.0 [2]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-chlorohex-1-ynyl)-2-methylpyridine	Ki	4.7 [1]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-cyclopropylethynyl)-2-methylpyridine	IC50	11.0 [1], 110.0 [2]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-cyclopropylethynyl)-2-methylpyridine	Ki	9.6 [1]
	5-Hex-1-ynyl-2-methyl-3-[[(2S)-pyrrolidin-2-yl]methoxy]pyridine	IC50	1600.0 [1]
	5-Hex-1-ynyl-2-methyl-3-[[(2S)-pyrrolidin-2-yl]methoxy]pyridine	Ki	73.0 [1]
	[1-[(3-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazanium	IC50	14700.0 [1]
	[1-[(3-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazanium	Ki	1600.0 [1], 112000.0 [2]
	Ondansetron	IC50	66000.0 [1]
	Ondansetron	Ki	46000.0 [1]
	7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine	IC50	94.0 [1]
	7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine	Ki	0.12 [1]
	Tropisetron	IC50	170000.0 [1]
	Tropisetron	Ki	55000.0 [1]
	(+)-Epibatidine	Ki	0.03 [1], 0.04 [2]
	Lobelin	Ki	4.0 [1], 5.01 [2]
	alpha-Methyltryptamine	Ki	10000.0 [1]
	Rivanicline	Ki	25.0 [1], 26.0 [2]
	Radafaxine	IC50	20000.0 [1], 31000.0 [2]
	N,N-Diallyl-5-methoxytryptamine	Ki	10000.0 [1]
	5-(6-Chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-ene	Ki	0.04 [1], 0.27 [2]
	N-(2-Fluorophenyl)-2-{4-[(4-fluorophenyl)sulfonyl]piperazin-1-yl}acetamide	IC50	9300.0 [1], 9800.0 [2]
	2-(3-Pyridyl)-1,4-ethanopiperidine	Ki	1.0 [1], 2.9 [2]
	3-(5-Chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octane	Ki	30.0 [1]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-phenylethynyl)pyridine	IC50	16.0 [1]
	3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-phenylethynyl)pyridine	Ki	0.05 [1]
	N-Methyl-1-(pyridin-3-yl)methanamine	Ki	10000.0 [1]
	(1R,2R,4S)-2-(6-Chloropyridin-3-yl)-7-methyl-7-azabicyclo[2.2.1]heptane	Ki	0.04 [1], 0.26 [2]
	Erysotrine	Ki	600.0 [1]
	3-(N-Ethyl-N-methylaminomethyl)pyridine	Ki	28.0 [1]
	N-Methyl-2-(pyridin-3-yloxy)ethanamine	Ki	35.0 [1]
	3-[(Z)-(3-Pyridyl)methylene]-1-azabicyclo[2.2.2]octane	Ki	2.0 [1], 6.0 [2]
	Trimethyl(2-pyridin-3-yloxyethyl)azanium	Ki	0.5 [1]
	3-(3-Pyridinyl)-3,7-diazabicyclo[3.3.1]nonane	Ki	0.1 [1], 0.2 [2]
	Cyclopropyl(3,7-diazabicyclo[3.3.1]nonan-3-yl)methanone	Ki	1.0 [1]
	2,3,3a,4,6,6a-Hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl(cyclopropyl)methanone	Ki	4.0 [1]
	N-[(2R,3R)-2-(Pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]octan-3-yl]-1-benzofuran-2-carboxamide	Ki	157.0 [1], 10000.0 [2]
	N,N-Dimethyl-4-(pyridin-3-yl)but-3-yn-1-amine	Ki	510.0 [1]
	N-Ethyl-N-methyl-4-(pyridin-3-yl)but-3-yn-1-amine	Ki	1770.0 [1]
	(2S,3S)-2-(3-Fluorophenyl)-3,5,5-trimethylmorpholin-2-ol	IC50	1300.0 [1], 23000.0 [2]
	(2S,3S)-2-(3-Bromophenyl)-3,5,5-trimethylmorpholin-2-ol	IC50	550.0 [1], 12000.0 [2]
	(2S,3S)-2-(3-Chlorophenyl)-3-ethyl-5,5-dimethylmorpholin-2-ol	IC50	2900.0 [1], 14000.0 [2]
	(2S,3S)-2-(3-Chlorophenyl)-5,5-dimethyl-3-propyl-morpholin-2-ol	IC50	7500.0 [1], 9500.0 [2]
	(2S,3S)-2-(3-Chlorophenyl)-3,4,5,5-tetramethylmorpholin-2-ol	IC50	7100.0 [1], 16000.0 [2]
	(R,R)-Hydroxy Bupropion	IC50	3300.0 [1], 17000.0 [2]
	3-Butyl-5-((S)-1-methyl-pyrrolidin-2-ylmethoxy)-pyridine	IC50	640.0 [1], 5000.0 [2]
	3-((S)-1-Methyl-pyrrolidin-2-ylmethoxy)-5-propyl-pyridine	IC50	2400.0 [1], 3200.0 [2]
	5-[(1R,2S,4R)-7-Azabicyclo[2.2.1]heptan-2-yl]-3-methyl-1,2-oxazole	Ki	0.46 [1], 1.33 [2]
	[(1r,5s)-8-Phenethyl-8-Azabicyclo[3.2.1]octan-3-Yl] Benzoate	Ki	31622.78 [1]
	[(1S,5R)-8-[2-(3,5-Dihydroxyphenyl)-2-hydroxyethyl]-8-azabicyclo[3.2.1]octan-3-yl] benzoate	Ki	31622.78 [1]
	2,3,3a,4,6,6a-Hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl-(4-phenoxyphenyl)methanone	IC50	7800.0 [1]
	2,3,3a,4,6,6a-Hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl-(4-phenoxyphenyl)methanone	Ki	19.0 [1]
	4-Chlorobenzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl ester	IC50	3600.0 [1], 95000.0 [2]
	4-(Benzyloxy)benzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl ester	IC50	3600.0 [1], 25800.0 [2]
	Benzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl ester	IC50	2500.0 [1], 313000.0 [2]
	3-Aminobenzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl ester	IC50	1020.0 [1], 4300.0 [2]
	1-Decyl-3-((S)-1-methyl-pyrrolidin-2-yl)-pyridinium; iodide	IC50	200.0 [1]
	1-Decyl-3-((S)-1-methyl-pyrrolidin-2-yl)-pyridinium; iodide	Ki	0.09 [1]
	[1-[(4-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazanium	IC50	24900.0 [1]
	[1-[(4-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazanium	Ki	600.0 [1]
	Carbastat	Ki	750.0 [1]
	Tubocurarine chloride	IC50	9200.0 [1]
	Mecamylamine	IC50	600.0 [1]
	Imidacloprid	Ki	720.0 [1]
	Granisetron	Ki	38000.0 [1]
	Tetramethylammonium	Ki	24.0 [1]
	1-(9-Azabicyclo[4.2.1]non-4-en-5-yl)ethanone	Ki	1.1 [1]
	Lobeline	Ki	5.01 [1]
	3-(Piperidin-2-yl)pyridine	Ki	92.0 [1]
	Anatoxin A	Ki	0.34 [1]
	Methyllycaconitine	Ki	10000.0 [1]
	Boldine	Ki	3000.0 [1]
	Nornicotine	Ki	29.0 [1]
	3-(2,4-Dimethoxybenzylidene)anabaseine	Ki	51.0 [1]
	Polygodial	IC50	62500.0 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 10 of 99 ⟨⟩

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References

This online tool may be cited as follows

MLA	"Quest Database™ Neuronal acetylcholine receptor; alpha4/beta2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 22 Feb. 2025, https://www.aatbio.com/data-sets/neuronal-acetylcholine-receptor-alpha4-beta2-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2025, February 22). Quest Database™ Neuronal acetylcholine receptor; alpha4/beta2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/neuronal-acetylcholine-receptor-alpha4-beta2-inhibitors-ic50-ki.
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