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Muscarinic acetylcholine receptor M2 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
CarbacholIC5012.59 [1], 63.1 [2], 130.0 [3], 3100.0 [4], 3460.0 [5]
CarbacholKi20.0 [1], 38.0 [2], 100.0 [3]
MethscopolamineIC504.3 [1], 398.11 [2], 436.52 [3], 501.19 [4]
Tiotropium bromide monohydrateIC500.03 [1], 0.06 [2], 0.2 [3], 0.21 [4]
Tiotropium bromide monohydrateKi0.02 [1], 0.06 [2], 0.1 [3], 0.32 [4]
XanomelineIC5012.59 [1], 316.23 [2]
XanomelineKi50.12 [1]
OxotremorineIC50400.0 [1]
OxotremorineKi17.0 [1], 660.0 [2]
ArecolineIC501800.0 [1], 4500.0 [2]
ArecolineKi40.0 [1], 2400.0 [2], 2454.71 [3]
N-IsopropylatropineIC502.0 [1], 2.24 [2]
N-IsopropylatropineKi0.41 [1], 0.48 [2], 1.02 [3], 1.26 [4]
MuscarineIC50449.0 [1], 3900.0 [2]
MuscarineKi25.0 [1], 72.0 [2], 75.0 [3], 489.78 [4]
MethoctramineIC5034.0 [1], 37.0 [2]
MethoctramineKi2.4 [1], 14.3 [2], 27.0 [3], 36.0 [4]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterIC5017.0 [1], 120.0 [2]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi2.6 [1], 2.63 [2], 7.0 [3]
N-[2-[3-[1-[4-[1-[2-Oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]imidazol-4-yl]propanoylamino]ethyl]-2,3-ditritiopropanamideIC50181.97 [1], 281.84 [2], 630.96 [3], 1348.96 [4], 2089.3 [5]
N-[2-[3-[1-[4-[1-[2-Oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]imidazol-4-yl]propanoylamino]ethyl]-2,3-ditritiopropanamideKi0.76 [1]
PirenzepineIC50968.2 [1]
PirenzepineKi173.78 [1], 251.0 [2], 270.0 [3], 524.0 [4]
HyoscyamineKi2.82 [1], 3.63 [2], 4.57 [3], 5.01 [4], 12.88 [5]
HimbacineIC5017.5 [1]
HimbacineKi4.5 [1], 4.68 [2], 10.0 [3], 48.4 [4]
4-(4,5-Dihydro-1,2-oxazol-3-yloxy)but-2-ynyl-[6-[3-(1,3-dioxoisoindol-2-yl)propyl-dimethylazaniumyl]hexyl]-dimethylazanium;dibromideKi75.86 [1], 91.2 [2], 199.53 [3], 204.17 [4], 275.42 [5]
4-(4,5-Dihydro-1,2-oxazol-3-yloxy)but-2-ynyl-trimethylazanium;bromideKi2.19 [1], 2.51 [2], 8.71 [3], 10.0 [4], 257.04 [5]
Trimethyl-[[(2R,6S)-6-methyl-1,4-dioxan-2-yl]methyl]azaniumKi1258.93 [1], 1584.89 [2], 2089.3 [3], 37153.52 [4]
6-[(1R,5R)-3-(3-Hydroxy-2-phenylpropanoyl)oxy-8-methyl-8-azoniabicyclo[3.2.1]octan-8-yl]hexyl-trimethylazaniumKi16.22 [1], 18.2 [2], 18.62 [3], 54.95 [4], 151.36 [5]
[3-(1,3-Dioxoisoindol-2-yl)-2,2-dimethylpropyl]-[6-[(1R,5R)-3-(3-hydroxy-2-phenylpropanoyl)oxy-8-methyl-8-azoniabicyclo[3.2.1]octan-8-yl]hexyl]-dimethylazaniumKi5.25 [1], 5.37 [2], 9.77 [3], 16.6 [4]
[3-(1,3-Dioxobenzo[de]isoquinolin-2-yl)-2,2-dimethylpropyl]-[6-[(1R,5R)-3-(3-hydroxy-2-phenylpropanoyl)oxy-8-methyl-8-azoniabicyclo[3.2.1]octan-8-yl]hexyl]-dimethylazaniumKi2.82 [1], 8.51 [2], 21.38 [3], 61.66 [4]
3-(1,3-Dioxoisoindol-2-yl)propyl-[6-[(1S,2S,4R,5R)-7-[(2S)-3-hydroxy-2-phenylpropanoyl]oxy-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-9-yl]hexyl]-dimethylazaniumKi6.92 [1], 7.08 [2], 8.13 [3], 50.12 [4]
[3-(1,3-Dioxobenzo[de]isoquinolin-2-yl)-2,2-dimethylpropyl]-[6-[(1S,2S,4R,5R)-7-[(2S)-3-hydroxy-2-phenylpropanoyl]oxy-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-9-yl]hexyl]-dimethylazaniumKi3.31 [1], 6.17 [2], 6.46 [3], 8.91 [4], 131.83 [5]
5-[(2,3-Ditritiopropanoylamino)methyl]-1-N,3-N-bis[2-[3-[1-[4-[1-[2-oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]imidazol-4-yl]propanoylamino]ethyl]benzene-1,3-dicarboxamideIC502691.53 [1], 6606.93 [2], 10471.29 [3], 18620.87 [4]
5-[(2,3-Ditritiopropanoylamino)methyl]-1-N,3-N-bis[2-[3-[1-[4-[1-[2-oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]imidazol-4-yl]propanoylamino]ethyl]benzene-1,3-dicarboxamideKi0.41 [1]
4-(4,5-Dihydro-1,2-oxazol-3-yloxy)but-2-ynyl-dimethyl-[6-(trimethylazaniumyl)hexyl]azaniumKi61.66 [1], 64.57 [2], 91.2 [3], 275.42 [4], 1288.25 [5]
OxybutyninKi8.1 [1], 9.61 [2], 11.75 [3], 16.0 [4]
Aclidinium bromideIC500.04 [1], 0.13 [2], 0.17 [3]
Aclidinium bromideKi0.08 [1]
Hydriodic acidIC50776.25 [1]
Hydriodic acidKi467.74 [1], 711.0 [2], 3715.35 [3]
Unii-61gsp3D46UKi0.89 [1]
6-Acetoxy-8-methyl-8-azonia-bicyclo[3.2.1]octaneKi2700.0 [1], 2754.23 [2], 4400.0 [3]
Ethyl 4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidine-1-carboxylateKi0.07 [1], 0.11 [2]
4-(4,5-Dihydro-1,2-oxazol-3-yloxy)but-2-ynyl-[6-[[3-(1,3-dioxobenzo[de]isoquinolin-2-yl)-2,2-dimethylpropyl]-dimethylazaniumyl]hexyl]-dimethylazanium;dibromideKi11.48 [1], 14.45 [2], 19.5 [3], 26.92 [4]
AcetylcholineKi158.49 [1], 380.0 [2], 390.0 [3]
MethacholineIC50380.0 [1], 5200.0 [2]
MethacholineKi59.0 [1]
Methoctramine hydrochlorideIC5029.0 [1], 34.0 [2]
Methoctramine hydrochlorideKi0.6 [1]
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chlorideIC5012930.0 [1]
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chlorideKi3235.94 [1]
CID 167962IC50478.63 [1]
CID 167962Ki31.62 [1]
CID 6321299Ki0.81 [1], 15.85 [2], 16.98 [3]
(4,6-Dimethylpyrimidin-5-yl)-[4-methyl-4-[(3S)-3-methyl-4-[(1S)-1-[4-(trifluoromethyl)phenyl]ethyl]piperazin-1-yl]piperidin-1-yl]methanoneKi456.0 [1], 575.0 [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-carboxylateIC503440.7 [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-carboxylateKi537.03 [1], 912010839355912.0 [2]
4-(4-(1-(4-(4-Methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)-1-(propylsulfonyl)piperidineKi0.29 [1]
Darotropium bromideIC5010.0 [1]
Darotropium bromideKi0.16 [1], 0.17 [2]
3-[1-[4-[1-[2-Oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]imidazol-4-yl]-N-[2-(propanoylamino)ethyl]propanamideKi0.76 [1], 1.1 [2], 10.23 [3]
1-N,3-N-Bis[2-[3-[1-[4-[1-[2-oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]imidazol-4-yl]propanoylamino]ethyl]-5-[(propanoylamino)methyl]benzene-1,3-dicarboxamide;2,2,2-trifluoroacetic acidKi0.11 [1], 0.41 [2], 1.05 [3]
N-[2-[2-[(Dipropylamino)methyl]piperidin-1-yl]ethyl]-5-oxo-6H-pyrido[3,2-c][1,5]benzodiazepine-11-carboxamideKi1.74 [1], 6.31 [2], 23.44 [3]
6-[(1S,2S,4R,5R)-7-[(2S)-3-Hydroxy-2-phenylpropanoyl]oxy-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonan-9-yl]hexyl-trimethylazaniumKi40.74 [1], 47.86 [2], 309.03 [3]
ClozapineKi100.0 [1], 169.0 [2]
QuetiapineKi1000.0 [1], 1189.2 [2]
HydroxychloroquineKi1049.0 [1], 5128.61 [2]
TolterodineKi2.7 [1], 4.0 [2]
DarifenacinKi47.0 [1], 50.0 [2]
EbastineIC501000.0 [1]
EbastineKi279.5 [1]
OtenzepadKi52.0 [1], 81.0 [2]
N,N'-Bis[6-[(2-methoxyphenyl)methylamino]hexyl]octane-1,8-diamine;hydrochlorideIC5022.0 [1]
GR-127935Ki1000.0 [1], 10000.0 [2]
3-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridineKi10000.0 [1]
AF-DX 384Ki5.28 [1], 6.03 [2]
AprofeneKi9.3 [1], 107.0 [2]
4-(4-Butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi980.0 [1], 1000.0 [2]
RevefenacinKi5.0 [1]
TripitramineKi0.27 [1], 0.3 [2]
(2,4-Dimethylpyridin-3-yl)-[4-methyl-4-[(3S)-3-methyl-4-[(1S)-1-[4-(trifluoromethyl)phenyl]ethyl]piperazin-1-yl]piperidin-1-yl]methanoneKi2500.0 [1]
3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamideKi158.49 [1], 3162.28 [2]
SabcomelineIC50180.0 [1]
SabcomelineKi204.17 [1]
2,6,3,5-Ethanediylidenepentaleno(1,6-bc)pyrrol-2(1H)-ol, octahydro-1-(phenylmethyl)-Ki835.0 [1]
TbpbIC503500.0 [1]
TbpbKi320.0 [1]
(2,4-Dimethyl-1-oxidopyridin-1-ium-3-yl)-[4-methyl-4-[(3S)-3-methyl-4-[(1S)-1-[4-(trifluoromethyl)phenyl]ethyl]piperazin-1-yl]piperidin-1-yl]methanoneKi250.0 [1]
Unii-I98T8BS72CKi530.0 [1]
N-[1-[3-(3-Oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamideKi1000.0 [1], 2200.0 [2]
(4-Fluoronaphthalen-1-yl)-[4-[4-[2-[4-(4-methoxyphenyl)sulfonylphenyl]-1,3-dioxolan-2-yl]piperidin-1-yl]piperidin-1-yl]methanoneKi0.51 [1]
[4-[(3R)-4-[(1S)-1-[4-(1,3-Benzodioxol-5-ylsulfonyl)phenyl]ethyl]-3-methylpiperazin-1-yl]piperidin-1-yl]-(2,6-dimethylphenyl)methanoneKi0.8 [1]
Trimethyl-[[(2S,4R)-2-methyl-1,3-dioxolan-4-yl]methyl]azaniumKi1202.26 [1]
3-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-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-thiadiazoleIC500.63 [1]
3-(1-Methyl-3,6-dihydro-2H-pyridin-5-yl)-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-thiadiazoleKi0.13 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Muscarinic acetylcholine receptor M2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.9 May2024https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m2-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 9). Quest Database™ Muscarinic acetylcholine receptor M2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m2-inhibitors-ic50-ki.
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