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Muscarinic acetylcholine receptor M1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
PirenzepineIC5019.0 [1]
PirenzepineKi15.0 [1], 23.5 [2]
CarbacholIC504090.0 [1], 10000.0 [2], 124830.0 [3], 150000.0 [4]
CarbacholKi170.0 [1], 3162.28 [2], 501187233627.27 [3]
XanomelineIC500.01 [1]
XanomelineKi158.49 [1], 251188643150958.0 [2]
AtropineKi0.33 [1], 1.2 [2]
ClozapineIC509.4 [1]
ArecolineIC50115.0 [1], 545.0 [2], 65000.0 [3], 115500.0 [4], 145000.0 [5]
ArecolineKi14.0 [1], 29000.0 [2], 29512.09 [3]
OxotremorineIC502.3 [1], 364.0 [2], 9000.0 [3], 27100.0 [4]
OxotremorineKi1.12 [1], 17.0 [2]
MethscopolamineIC501.8 [1]
MethscopolamineKi0.1 [1], 0.17 [2], 0.32 [3]
QuetiapineKi56.0 [1], 100.0 [2], 398.11 [3], 629.8 [4], 1000.0 [5]
Tiotropium bromide monohydrateIC500.03 [1], 0.1 [2], 0.22 [3]
Tiotropium bromide monohydrateKi0.01 [1], 0.12 [2]
HimbacineIC50548.2 [1]
HimbacineKi4.5 [1], 48.0 [2], 107.15 [3], 158.49 [4]
Trimethyl-[[(2R,6S)-6-methyl-1,4-dioxan-2-yl]methyl]azaniumKi8317.64 [1], 12882.5 [2], 30199.52 [3]
3-(4-Imidazol-1-ylbutoxy)-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazoleIC50870.96 [1], 2290.87 [2], 52480.75 [3], 53703.18 [4]
HaloperidolIC505500.0 [1]
HaloperidolKi1600.0 [1]
OlanzapineKi2.1 [1], 4.7 [2], 10.0 [3], 100.0 [4]
ScopolamineIC501.74 [1], 3.31 [2], 4.37 [3]
ScopolamineKi7.5 [1]
N-IsopropylatropineIC502.65 [1], 2.9 [2]
N-IsopropylatropineKi0.43 [1], 1.51 [2]
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chlorideIC504000.0 [1], 7240.0 [2]
(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chlorideKi1949.84 [1]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl esterKi4.6 [1], 21000.0 [2], 21379.62 [3]
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-thiadiazoleKi0.1 [1], 0.12 [2], 1e+16 [3]
1-[3-[4-(5-Hydroxypentyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC5028.84 [1], 10000.0 [2], 26302.68 [3]
1-[3-[4-(5-Hydroxypentyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi467.74 [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-oneIC50645.65 [1], 4265.8 [2], 5370.32 [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-oneKi6.76 [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-oneIC5021.88 [1], 380.19 [2], 741.31 [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-oneKi0.91 [1]
1-[3-[4-(9-Hydroxynonyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC50489.78 [1], 10000.0 [2], 19498.45 [3]
1-[3-[4-(9-Hydroxynonyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi281.84 [1]
AcetylcholineKi5800.0 [1], 13489.63 [2], 23000.0 [3]
RisperidoneKi1000.0 [1], 2800.0 [2], 5000.0 [3]
OxybutyninKi0.85 [1], 1.0 [2], 2.4 [3]
Aclidinium bromideIC500.1 [1], 0.14 [2]
Aclidinium bromideKi0.08 [1]
AprofeneKi2.1 [1], 15.1 [2], 26.5 [3]
1-[3-(4-Butylpiperidino)propyl]-3,4-dihydroquinoline-2(1H)-oneIC50173.78 [1], 1584.89 [2]
1-[3-(4-Butylpiperidino)propyl]-3,4-dihydroquinoline-2(1H)-oneKi316.23 [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-carboxylateIC506558.7 [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-carboxylateKi1318.26 [1], 436515832240167.0 [2]
5-(4-Butoxy-1,2,5-thiadiazol-3-yl)-1-methyl-1,2,3,6-tetrahydropyridineIC503.0 [1], 28.18 [2], 77624.71 [3]
1-Methyl-5-(4-(pentyloxy)-1,2,5-thiadiazol-3-yl)-1,2,3,6-tetrahydropyridineIC500.0 [1], 33.11 [2], 8511.38 [3]
Darotropium bromideIC5010.0 [1]
Darotropium bromideKi0.05 [1]
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-oneIC5014125.38 [1], 147910.84 [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-oneKi1.02 [1]
ChlorpromazineKi20.0 [1], 125.89 [2]
ZiprasidoneKi5100.0 [1], 10000.0 [2]
MuscarineKi56.0 [1], 18197.01 [2]
LinagliptinIC50295.0 [1]
EbastineIC501100.0 [1]
EbastineKi101.2 [1]
OtenzepadKi179.0 [1], 537.0 [2]
MethoctramineKi49.8 [1], 83.18 [2]
GR-127935Ki1000.0 [1], 10000.0 [2]
AF-DX 384Ki12.4 [1], 30.9 [2]
TripitramineKi1.58 [1], 3.55 [2]
N-(3-Oxo-3-(4-(pyridin-4-yl)piperazin-1-yl)propyl)benzo[c][1,2,5]thiadiazole-4-sulfonamideIC50690.0 [1]
SabcomelineIC50170.0 [1]
SabcomelineKi229.09 [1]
2-Chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo(b,e)(1,4)diazepineIC506.0 [1]
4-(4-Butyl-1-piperidinyl)-1-(2-methylphenyl)-1-butanone HydrochlorideKi891.25 [1], 1737.8 [2]
Unii-I98T8BS72CKi1.5 [1]
6-Acetoxy-8-methyl-8-azonia-bicyclo[3.2.1]octaneKi2300.0 [1], 281838.29 [2]
11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-2-olIC5037.0 [1]
N,N-Dimethyl-2-[3-(pyrazin-2-ylmethyl)-1H-inden-2-yl]ethanamineKi19.0 [1], 19000.0 [2]
R-DimethindeneKi2.4 [1], 1862.09 [2]
Ethyl 4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidine-1-carboxylateKi6.49 [1], 6.5 [2]
[6-(4-Methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepin-8-yl] trifluoromethanesulfonateIC501000.0 [1], 1200.0 [2]
1-Methyl-5-[4-(3-phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1,2,3,6-tetrahydro-pyridineIC5037.15 [1], 2137.96 [2]
Benzo[B]thiophene-2-ethanamine, N,N-dimethyl-3-[(1R)-1-(2-pyridinyl)ethyl]-IC505300.0 [1]
Benzo[B]thiophene-2-ethanamine, N,N-dimethyl-3-[(1R)-1-(2-pyridinyl)ethyl]-Ki5.3 [1]
11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-8-olIC5027.0 [1]
4-(4-(1-(4-(4-Methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)-1-(propylsulfonyl)piperidineKi25.7 [1], 25.82 [2]
Antihistamine-1Ki10000.0 [1]
Trimethyl-[[(2S,4R)-2-methyl-1,3-dioxolan-4-yl]methyl]azaniumKi10964.78 [1]
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-carboxylateKi13180.0 [1], 13182.57 [2]
1-[1-[4-(4-Methoxyphenylsulfinyl)phenyl]ethyl]-4-cyclohexylpiperazineKi6.0 [1]
1-[3-[4-(7-Hydroxyheptyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneIC501148.15 [1]
1-[3-[4-(7-Hydroxyheptyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-oneKi354.81 [1]
[6-(4-Methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepin-3-yl] trifluoromethanesulfonateIC5035.0 [1]
3-Methoxy-6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepineIC5019.0 [1]
2-(4-Hydroxy-phenyl)-2-phenyl-propionic acid 2-diethylamino-ethyl esterKi0.88 [1], 44.0 [2]
8-Methoxy-6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepineIC5039.0 [1]
Ethyl 4-[[(2S)-3-(4-hydroxyphenyl)-1-[[1-[(4-hydroxyphenyl)methyl]pyrrolidin-3-yl]amino]-1-oxopropan-2-yl]carbamoylamino]benzoateIC501995.26 [1]
(2R)-1-[(2S,4R)-4-Hydroxy-1-[3,3,3-tris(4-fluorophenyl)propanoyl]pyrrolidine-2-carbonyl]-N-(piperidin-4-ylmethyl)pyrrolidine-2-carboxamideKi170.0 [1]
Ethyl 4-[[(2S)-3-(4-hydroxyphenyl)-1-[[(3S)-1-[(4-hydroxyphenyl)methyl]pyrrolidin-3-yl]amino]-1-oxopropan-2-yl]carbamoylamino]benzoateIC501000.0 [1]
(2R)-N,3-Dimethyl-2-(methylamino)-N-[(1R,2S,5S,6S,9R,12S,13R,16S)-6,7,13-trimethyl-7-azapentacyclo[10.8.0.02,9.05,9.013,18]icos-18-en-16-yl]butanamideKi11.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Muscarinic acetylcholine receptor M1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Dec2024https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 21). Quest Database™ Muscarinic acetylcholine receptor M1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m1-inhibitors-ic50-ki.
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