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Muscarinic acetylcholine receptor M4 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
CarbacholIC500.4 [1], 50.12 [2], 1000.0 [3], 7200.0 [4]
CarbacholKi24.0 [1], 398.11 [2], 2600.0 [3]
4-Damp methiodideIC501.9 [1]
4-Damp methiodideKi0.51 [1], 0.88 [2]
PirenzepineIC501.15 [1], 246.8 [2], 1047.13 [3]
PirenzepineKi13.8 [1], 34.67 [2], 105.0 [3]
ArecolineIC5013500.0 [1], 47500.0 [2]
ArecolineKi26.0 [1], 2400.0 [2], 60000.0 [3]
XanomelineIC5025.12 [1]
XanomelineKi11.22 [1], 39.81 [2], 72.0 [3]
1-[3-(4-Butylpiperidino)propyl]-3,4-dihydroquinoline-2(1H)-oneIC50177.83 [1], 2238.72 [2], 7585.78 [3], 47863.01 [4], 120226.44 [5]
1-[3-(4-Butylpiperidino)propyl]-3,4-dihydroquinoline-2(1H)-oneKi208.93 [1]
AtropineKi0.1 [1], 0.34 [2], 1.39 [3], 3.0 [4]
ScopolamineIC501.29 [1], 3.8 [2]
ScopolamineKi36.9 [1]
MethscopolamineIC502.3 [1]
MethscopolamineKi0.14 [1]
Ethyl 17-methoxy-6-methyl-12-oxa-1,7-diazapentacyclo[11.8.0.03,11.04,8.014,19]henicosa-3(11),4(8),5,9,14(19),15,17-heptaene-5-carboxylateIC5090.7 [1], 1000.0 [2]
Ethyl 17-methoxy-6-methyl-12-oxa-1,7-diazapentacyclo[11.8.0.03,11.04,8.014,19]henicosa-3(11),4(8),5,9,14(19),15,17-heptaene-5-carboxylateKi6.46 [1], 7.08 [2]
1-[3-[4-(5-Hydroxypentyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC501621.81 [1], 3311.31 [2], 12302.69 [3]
1-[3-[4-(5-Hydroxypentyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi446.68 [1]
1-[3-[4-(7-Hydroxyheptyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC50588.84 [1], 794.33 [2], 1479.11 [3]
1-[3-[4-(7-Hydroxyheptyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi389.05 [1]
1-[3-[4-[5-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]pentyl]piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC50354.81 [1], 446.68 [2], 630.96 [3]
1-[3-[4-[5-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]pentyl]piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi7.94 [1]
1-[3-[4-[7-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]heptyl]piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC50144.54 [1], 407.38 [2], 1862.09 [3]
1-[3-[4-[7-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]heptyl]piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi0.89 [1]
1-[3-[4-(9-Hydroxynonyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC50588.84 [1], 812.83 [2], 3630.78 [3]
1-[3-[4-(9-Hydroxynonyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi154.88 [1]
Trimethyl-[[(2R,6S)-6-methyl-1,4-dioxan-2-yl]methyl]azaniumKi9772.37 [1], 11481.54 [2]
ClozapineKi6.3 [1], 12.59 [2], 100.0 [3]
OlanzapineKi12.59 [1], 22.0 [2], 1000.0 [3]
QuetiapineKi125.89 [1], 220.2 [2], 1000.0 [3]
OxotremorineIC505000.0 [1]
OxotremorineKi1.5 [1], 160.0 [2]
MuscarineKi23.0 [1], 1400.0 [2], 28000.0 [3]
HimbacineIC50114.4 [1]
HimbacineKi8.71 [1], 10.96 [2]
6-Acetoxy-8-methyl-8-azonia-bicyclo[3.2.1]octaneKi900.0 [1], 8300.0 [2]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi4.0 [1], 33.0 [2]
1-[3-[4-[9-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]nonyl]piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC502454.71 [1], 95499.26 [2]
1-[3-[4-[9-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]nonyl]piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi1.07 [1]
ChlorpromazineKi21.0 [1], 158.49 [2]
OxybutyninKi0.28 [1], 3.63 [2]
Tiotropium bromide monohydrateIC500.04 [1]
Tiotropium bromide monohydrateKi0.01 [1]
ClemastineKi2.77 [1], 53.7 [2]
MethoctramineKi38.0 [1], 107.15 [2]
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chlorideKi9120.11 [1]
AprofeneKi7.4 [1], 628.0 [2]
4-(4-Butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi1000.0 [1], 1400.0 [2]
TripitramineKi6.46 [1], 11.48 [2]
2,6,3,5-Ethanediylidenepentaleno(1,6-bc)pyrrol-2(1H)-ol, octahydro-1-(phenylmethyl)-Ki1415.0 [1]
CID 6321299Ki0.64 [1], 1.6 [2]
TbpbIC50734.0 [1]
TbpbKi130.0 [1]
2-Benzyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepineIC50300.0 [1], 6800.0 [2]
N-[1-[3-(3-Oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamideKi1000.0 [1], 6900.0 [2]
Ethyl 6-butyl-17-methoxy-12-oxa-1,7-diazapentacyclo[11.8.0.03,11.04,8.014,19]henicosa-3(11),4(8),5,9,14(19),15,17-heptaene-5-carboxylateKi1.0 [1]
(2R)-1-[(2S,4R)-4-Hydroxy-1-[3,3,3-tris(4-fluorophenyl)propanoyl]pyrrolidine-2-carbonyl]-N-(piperidin-4-ylmethyl)pyrrolidine-2-carboxamideKi42.0 [1]
(8S)-N-[2-(3-Fluorophenyl)ethyl]pentacyclo[5.4.0.02,6.03,10.05,9]undecan-8-amineKi705.0 [1]
5-(2-Pyridin-2-ylethyl)-5-azahexacyclo[5.4.1.02,6.03,10.04,8.09,12]dodecan-4-olKi2961.0 [1]
5-(1,3-Benzodioxol-5-ylmethyl)-5-azahexacyclo[5.4.1.02,6.03,10.04,8.09,12]dodecan-4-olKi1302.0 [1]
5-[(3,4-Dimethoxyphenyl)methyl]-5-azahexacyclo[5.4.1.02,6.03,10.04,8.09,12]dodecan-4-olKi1233.0 [1]
Unii-9JE7tat31DIC5012.59 [1]
Unii-9JE7tat31DKi2.51 [1]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi190.0 [1], 500.0 [2]
2-[2-[2-[2-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethanolIC5025118.86 [1]
2-[2-[2-[2-[[4-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethanolKi794.33 [1]
3-Methoxy-4-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazole;hydrochlorideIC5015.85 [1]
3-Methoxy-4-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazole;hydrochlorideKi2.51 [1]
Benzoic acid 8-methyl-8-aza-bicyclo[3.2.1]oct-6-yl esterKi410.0 [1], 910.0 [2]
2-(4-Methoxyphenyl)ethyl 1-ethyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylateIC5042313.0 [1]
2-(4-Methoxyphenyl)ethyl 1-ethyl-4-phenyl-3,6-dihydro-2H-pyridine-5-carboxylateKi1730.0 [1]
[1-[6-(2,4-Difluorophenoxy)pyrimidin-4-yl]piperidin-4-yl]-(3,4-dihydro-1H-isoquinolin-2-yl)methanoneIC50100.0 [1]
[1-[6-(2,4-Difluorophenoxy)pyrimidin-4-yl]piperidin-4-yl]-(3,4-dihydro-1H-isoquinolin-2-yl)methanoneKi10.3 [1]
4-[4-[6-(3,3-Dimethylpiperidin-1-yl)pyridazin-3-yl]piperazin-1-yl]sulfonyl-3,5-dimethyl-1,2-oxazoleIC50109.65 [1]
4-[4-[6-(3,3-Dimethylpiperidin-1-yl)pyridazin-3-yl]piperazin-1-yl]sulfonyl-3,5-dimethyl-1,2-oxazoleKi7.78 [1]
3-Methoxy-4-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]-1,2,5-thiadiazoleIC507943.28 [1]
3-Methoxy-4-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]-1,2,5-thiadiazoleKi63.1 [1]
3-Methoxy-4-[2-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazoleIC50398.11 [1]
3-Methoxy-4-[2-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazoleKi12.59 [1]
3-Methoxy-4-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazoleIC507943.28 [1]
3-Methoxy-4-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]-1,2,5-thiadiazoleKi79.43 [1]
3-Methoxy-5-[3-[3-[3-[(4-pyridin-3-yl-1,2,5-thiadiazol-3-yl)oxy]propoxy]propoxy]propoxy]-1,2,4-thiadiazoleIC506309.57 [1]
3-Methoxy-5-[3-[3-[3-[(4-pyridin-3-yl-1,2,5-thiadiazol-3-yl)oxy]propoxy]propoxy]propoxy]-1,2,4-thiadiazoleKi158.49 [1]
4-Nitro-benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi48.0 [1], 450.0 [2]
Cyclohexanecarboxylic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi840.0 [1], 2200.0 [2]
Propionic acid 8-methyl-8-aza-bicyclo[3.2.1]oct-6-yl esterKi960.0 [1], 1400.0 [2]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi85.0 [1], 660.0 [2]
(8-Methyl-8-azabicyclo[3.2.1]octan-6-yl) 2,2,2-trichloroethyl carbonateKi42.0 [1], 2300.0 [2]
Cyclohexanecarboxylic acid 8-methyl-8-aza-bicyclo[3.2.1]oct-6-yl esterKi300.0 [1], 700.0 [2]
3-Methoxy-5-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-6-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,4-thiadiazoleIC501258.93 [1]
3-Methoxy-5-[2-[2-[2-[2-[[4-(1-methyl-3,6-dihydro-2H-pyridin-6-yl)-1,2,5-thiadiazol-3-yl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]-1,2,4-thiadiazoleKi25.12 [1]
4-[4-[1-(4-Hydroxy-4,4-diphenylbutyl)-1-methylpiperidin-1-ium-4-yl]-1-methylpiperidin-1-ium-1-yl]-1,1-diphenylbutan-1-ol;diiodideIC501000.0 [1]
4-[4-[1-(4-Hydroxy-4,4-diphenylbutyl)-1-methylpiperidin-1-ium-4-yl]-1-methylpiperidin-1-ium-1-yl]-1,1-diphenylbutan-1-ol;diiodideKi12.59 [1]
3-(4-((2-Chlorophenyl)sulfonyl)piperazin-1-yl)-6-(2-methylpiperidin-1-yl)pyridazineIC50524.81 [1], 1000.0 [2]
Trimethyl-[[(2R,6R)-6-methyl-1,4-dioxan-2-yl]methyl]azaniumKi87096.36 [1], 100000.0 [2]
AcetylcholineKi8511.38 [1]
TamoxifenKi672.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Muscarinic acetylcholine receptor M4 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m4-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Muscarinic acetylcholine receptor M4 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m4-inhibitors-ic50-ki.
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