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

Structure
Compound Name
Standard Type
Standard Values (in nM)
NicotineIC50427.0 [1]
NicotineKi1.05 [1]
VareniclineIC5039.0 [1], 70.0 [2], 94.0 [3], 50000.0 [4]
EpibatidineIC501.06 [1]
EpibatidineKi0.07 [1]
Sazetidine AIC504.8 [1], 7.5 [2], 11.0 [3]
Sazetidine AKi0.06 [1]
CytisineIC5050.0 [1], 28000.0 [2]
CytisineKi0.23 [1], 2.0 [2], 2.59 [3]
(S)-3-(Azetidin-2-ylmethoxy)pyridineIC501.51 [1]
(S)-3-(Azetidin-2-ylmethoxy)pyridineKi0.04 [1], 0.05 [2]
BupropionIC5012.0 [1], 12000.0 [2]
Dihydro-beta-erythroidineIC5020.0 [1], 410.0 [2]
Dihydro-beta-erythroidineKi98.0 [1]
N,N-Dimethyl-2-(pyridin-3-yloxy)ethanamineKi21.0 [1], 300.0 [2]
Dimethyl-pyridin-3-ylmethyl-amineKi540.0 [1]
N-Methyl-4-(pyridin-3-yl)but-3-yn-1-amineKi58.0 [1], 113.0 [2]
3-[(2s)-Azetidin-2-Ylmethoxy]-5-[(1s,2r)-2-(2-Methoxyethyl)cyclopropyl]pyridineIC505.6 [1]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-hex-1-ynyl-2-methylpyridineIC5018.0 [1], 260.0 [2]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-hex-1-ynyl-2-methylpyridineKi12.0 [1]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-fluorohex-1-ynyl)-2-methylpyridineIC50130.0 [1], 140.0 [2]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-fluorohex-1-ynyl)-2-methylpyridineKi4.2 [1]
6-[5-[[(2S)-Azetidin-2-yl]methoxy]-6-methylpyridin-3-yl]hex-5-yn-1-olIC5042.0 [1], 51.0 [2]
6-[5-[[(2S)-Azetidin-2-yl]methoxy]-6-methylpyridin-3-yl]hex-5-yn-1-olKi4.3 [1]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-chlorohex-1-ynyl)-2-methylpyridineIC50260.0 [1], 270.0 [2]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(6-chlorohex-1-ynyl)-2-methylpyridineKi4.7 [1]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-cyclopropylethynyl)-2-methylpyridineIC5011.0 [1], 110.0 [2]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-cyclopropylethynyl)-2-methylpyridineKi9.6 [1]
5-Hex-1-ynyl-2-methyl-3-[[(2S)-pyrrolidin-2-yl]methoxy]pyridineIC501600.0 [1]
5-Hex-1-ynyl-2-methyl-3-[[(2S)-pyrrolidin-2-yl]methoxy]pyridineKi73.0 [1]
[1-[(3-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazaniumIC5014700.0 [1]
[1-[(3-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazaniumKi1600.0 [1], 112000.0 [2]
OndansetronIC5066000.0 [1]
OndansetronKi46000.0 [1]
7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepineIC5094.0 [1]
7,8,9,10-Tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepineKi0.12 [1]
TropisetronIC50170000.0 [1]
TropisetronKi55000.0 [1]
(+)-EpibatidineKi0.03 [1], 0.04 [2]
LobelinKi4.0 [1], 5.01 [2]
alpha-MethyltryptamineKi10000.0 [1]
RivaniclineKi25.0 [1], 26.0 [2]
RadafaxineIC5020000.0 [1], 31000.0 [2]
N,N-Diallyl-5-methoxytryptamineKi10000.0 [1]
5-(6-Chloro-3-pyridinyl)-9-azabicyclo[4.2.1]non-4-eneKi0.04 [1], 0.27 [2]
N-(2-Fluorophenyl)-2-{4-[(4-fluorophenyl)sulfonyl]piperazin-1-yl}acetamideIC509300.0 [1], 9800.0 [2]
2-(3-Pyridyl)-1,4-ethanopiperidineKi1.0 [1], 2.9 [2]
3-(5-Chloro-2-furoyl)-3,7-diazabicyclo[3.3.0]octaneKi30.0 [1]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-phenylethynyl)pyridineIC5016.0 [1]
3-[[(2S)-Azetidin-2-yl]methoxy]-5-(2-phenylethynyl)pyridineKi0.05 [1]
N-Methyl-1-(pyridin-3-yl)methanamineKi10000.0 [1]
(1R,2R,4S)-2-(6-Chloropyridin-3-yl)-7-methyl-7-azabicyclo[2.2.1]heptaneKi0.04 [1], 0.26 [2]
ErysotrineKi600.0 [1]
3-(N-Ethyl-N-methylaminomethyl)pyridineKi28.0 [1]
N-Methyl-2-(pyridin-3-yloxy)ethanamineKi35.0 [1]
3-[(Z)-(3-Pyridyl)methylene]-1-azabicyclo[2.2.2]octaneKi2.0 [1], 6.0 [2]
Trimethyl(2-pyridin-3-yloxyethyl)azaniumKi0.5 [1]
3-(3-Pyridinyl)-3,7-diazabicyclo[3.3.1]nonaneKi0.1 [1], 0.2 [2]
Cyclopropyl(3,7-diazabicyclo[3.3.1]nonan-3-yl)methanoneKi1.0 [1]
2,3,3a,4,6,6a-Hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl(cyclopropyl)methanoneKi4.0 [1]
N-[(2R,3R)-2-(Pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]octan-3-yl]-1-benzofuran-2-carboxamideKi157.0 [1], 10000.0 [2]
N,N-Dimethyl-4-(pyridin-3-yl)but-3-yn-1-amineKi510.0 [1]
N-Ethyl-N-methyl-4-(pyridin-3-yl)but-3-yn-1-amineKi1770.0 [1]
(2S,3S)-2-(3-Fluorophenyl)-3,5,5-trimethylmorpholin-2-olIC501300.0 [1], 23000.0 [2]
(2S,3S)-2-(3-Bromophenyl)-3,5,5-trimethylmorpholin-2-olIC50550.0 [1], 12000.0 [2]
(2S,3S)-2-(3-Chlorophenyl)-3-ethyl-5,5-dimethylmorpholin-2-olIC502900.0 [1], 14000.0 [2]
(2S,3S)-2-(3-Chlorophenyl)-5,5-dimethyl-3-propyl-morpholin-2-olIC507500.0 [1], 9500.0 [2]
(2S,3S)-2-(3-Chlorophenyl)-3,4,5,5-tetramethylmorpholin-2-olIC507100.0 [1], 16000.0 [2]
(R,R)-Hydroxy BupropionIC503300.0 [1], 17000.0 [2]
3-Butyl-5-((S)-1-methyl-pyrrolidin-2-ylmethoxy)-pyridineIC50640.0 [1], 5000.0 [2]
3-((S)-1-Methyl-pyrrolidin-2-ylmethoxy)-5-propyl-pyridineIC502400.0 [1], 3200.0 [2]
5-[(1R,2S,4R)-7-Azabicyclo[2.2.1]heptan-2-yl]-3-methyl-1,2-oxazoleKi0.46 [1], 1.33 [2]
[(1r,5s)-8-Phenethyl-8-Azabicyclo[3.2.1]octan-3-Yl] BenzoateKi31622.78 [1]
[(1S,5R)-8-[2-(3,5-Dihydroxyphenyl)-2-hydroxyethyl]-8-azabicyclo[3.2.1]octan-3-yl] benzoateKi31622.78 [1]
2,3,3a,4,6,6a-Hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl-(4-phenoxyphenyl)methanoneIC507800.0 [1]
2,3,3a,4,6,6a-Hexahydro-1H-pyrrolo[3,4-c]pyrrol-5-yl-(4-phenoxyphenyl)methanoneKi19.0 [1]
4-Chlorobenzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl esterIC503600.0 [1], 95000.0 [2]
4-(Benzyloxy)benzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl esterIC503600.0 [1], 25800.0 [2]
Benzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl esterIC502500.0 [1], 313000.0 [2]
3-Aminobenzoic acid [(2S)-1-methylpyrrolidine-2-yl]methyl esterIC501020.0 [1], 4300.0 [2]
1-Decyl-3-((S)-1-methyl-pyrrolidin-2-yl)-pyridinium; iodideIC50200.0 [1]
1-Decyl-3-((S)-1-methyl-pyrrolidin-2-yl)-pyridinium; iodideKi0.09 [1]
[1-[(4-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazaniumIC5024900.0 [1]
[1-[(4-Hydroxyphenyl)methyl]indol-3-yl]methyl-trimethylazaniumKi600.0 [1]
CarbastatKi750.0 [1]
Tubocurarine chlorideIC509200.0 [1]
MecamylamineIC50600.0 [1]
ImidaclopridKi720.0 [1]
GranisetronKi38000.0 [1]
TetramethylammoniumKi24.0 [1]
1-(9-Azabicyclo[4.2.1]non-4-en-5-yl)ethanoneKi1.1 [1]
LobelineKi5.01 [1]
3-(Piperidin-2-yl)pyridineKi92.0 [1]
Anatoxin AKi0.34 [1]
MethyllycaconitineKi10000.0 [1]
BoldineKi3000.0 [1]
NornicotineKi29.0 [1]
3-(2,4-Dimethoxybenzylidene)anabaseineKi51.0 [1]
PolygodialIC5062500.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Neuronal acetylcholine receptor; alpha4/beta2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/neuronal-acetylcholine-receptor-alpha4-beta2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). 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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