Muscarinic acetylcholine receptor M2 Inhibitors (IC50, Ki)

Structure ▲ ▼	Compound Name ▲ ▼	Standard Type ▲ ▼	Standard Values (in nM) ▲ ▼
	Carbachol	IC50	12.59 [1], 63.1 [2], 130.0 [3], 3100.0 [4], 3460.0 [5]
	Carbachol	Ki	20.0 [1], 38.0 [2], 100.0 [3]
	Methscopolamine	IC50	4.3 [1], 398.11 [2], 436.52 [3], 501.19 [4]
	Tiotropium bromide monohydrate	IC50	0.03 [1], 0.06 [2], 0.2 [3], 0.21 [4]
	Tiotropium bromide monohydrate	Ki	0.02 [1], 0.06 [2], 0.1 [3], 0.32 [4]
	Xanomeline	IC50	12.59 [1], 316.23 [2]
	Xanomeline	Ki	50.12 [1]
	Oxotremorine	IC50	400.0 [1]
	Oxotremorine	Ki	17.0 [1], 660.0 [2]
	Arecoline	IC50	1800.0 [1], 4500.0 [2]
	Arecoline	Ki	40.0 [1], 2400.0 [2], 2454.71 [3]
	N-Isopropylatropine	IC50	2.0 [1], 2.24 [2]
	N-Isopropylatropine	Ki	0.41 [1], 0.48 [2], 1.02 [3], 1.26 [4]
	Muscarine	IC50	449.0 [1], 3900.0 [2]
	Muscarine	Ki	25.0 [1], 72.0 [2], 75.0 [3], 489.78 [4]
	Methoctramine	IC50	34.0 [1], 37.0 [2]
	Methoctramine	Ki	2.4 [1], 14.3 [2], 27.0 [3], 36.0 [4]
	Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester	IC50	17.0 [1], 120.0 [2]
	Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester	Ki	2.6 [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-ditritiopropanamide	IC50	181.97 [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-ditritiopropanamide	Ki	0.76 [1]
	Pirenzepine	IC50	968.2 [1]
	Pirenzepine	Ki	173.78 [1], 251.0 [2], 270.0 [3], 524.0 [4]
	Hyoscyamine	Ki	2.82 [1], 3.63 [2], 4.57 [3], 5.01 [4], 12.88 [5]
	Himbacine	IC50	17.5 [1]
	Himbacine	Ki	4.5 [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;dibromide	Ki	75.86 [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;bromide	Ki	2.19 [1], 2.51 [2], 8.71 [3], 10.0 [4], 257.04 [5]
	Trimethyl-[[(2R,6S)-6-methyl-1,4-dioxan-2-yl]methyl]azanium	Ki	1258.93 [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-trimethylazanium	Ki	16.22 [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]-dimethylazanium	Ki	5.25 [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]-dimethylazanium	Ki	2.82 [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]-dimethylazanium	Ki	6.92 [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]-dimethylazanium	Ki	3.31 [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-dicarboxamide	IC50	2691.53 [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-dicarboxamide	Ki	0.41 [1]
	4-(4,5-Dihydro-1,2-oxazol-3-yloxy)but-2-ynyl-dimethyl-[6-(trimethylazaniumyl)hexyl]azanium	Ki	61.66 [1], 64.57 [2], 91.2 [3], 275.42 [4], 1288.25 [5]
	Oxybutynin	Ki	8.1 [1], 9.61 [2], 11.75 [3], 16.0 [4]
	Aclidinium bromide	IC50	0.04 [1], 0.13 [2], 0.17 [3]
	Aclidinium bromide	Ki	0.08 [1]
	Hydriodic acid	IC50	776.25 [1]
	Hydriodic acid	Ki	467.74 [1], 711.0 [2], 3715.35 [3]
	Unii-61gsp3D46U	Ki	0.89 [1]
	6-Acetoxy-8-methyl-8-azonia-bicyclo[3.2.1]octane	Ki	2700.0 [1], 2754.23 [2], 4400.0 [3]
	Ethyl 4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidine-1-carboxylate	Ki	0.07 [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;dibromide	Ki	11.48 [1], 14.45 [2], 19.5 [3], 26.92 [4]
	Acetylcholine	Ki	158.49 [1], 380.0 [2], 390.0 [3]
	Methacholine	IC50	380.0 [1], 5200.0 [2]
	Methacholine	Ki	59.0 [1]
	Methoctramine hydrochloride	IC50	29.0 [1], 34.0 [2]
	Methoctramine hydrochloride	Ki	0.6 [1]
	(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride	IC50	12930.0 [1]
	(4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride	Ki	3235.94 [1]
	CID 167962	IC50	478.63 [1]
	CID 167962	Ki	31.62 [1]
	CID 6321299	Ki	0.81 [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]methanone	Ki	456.0 [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-carboxylate	IC50	3440.7 [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-carboxylate	Ki	537.03 [1], 912010839355912.0 [2]
	4-(4-(1-(4-(4-Methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)-1-(propylsulfonyl)piperidine	Ki	0.29 [1]
	Darotropium bromide	IC50	10.0 [1]
	Darotropium bromide	Ki	0.16 [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]propanamide	Ki	0.76 [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 acid	Ki	0.11 [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-carboxamide	Ki	1.74 [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-trimethylazanium	Ki	40.74 [1], 47.86 [2], 309.03 [3]
	Clozapine	Ki	100.0 [1], 169.0 [2]
	Quetiapine	Ki	1000.0 [1], 1189.2 [2]
	Hydroxychloroquine	Ki	1049.0 [1], 5128.61 [2]
	Tolterodine	Ki	2.7 [1], 4.0 [2]
	Darifenacin	Ki	47.0 [1], 50.0 [2]
	Ebastine	IC50	1000.0 [1]
	Ebastine	Ki	279.5 [1]
	Otenzepad	Ki	52.0 [1], 81.0 [2]
	N,N'-Bis[6-[(2-methoxyphenyl)methylamino]hexyl]octane-1,8-diamine;hydrochloride	IC50	22.0 [1]
	GR-127935	Ki	1000.0 [1], 10000.0 [2]
	3-((4-(4-Chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo[2,3-b]pyridine	Ki	10000.0 [1]
	AF-DX 384	Ki	5.28 [1], 6.03 [2]
	Aprofene	Ki	9.3 [1], 107.0 [2]
	4-(4-Butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Ki	980.0 [1], 1000.0 [2]
	Revefenacin	Ki	5.0 [1]
	Tripitramine	Ki	0.27 [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]methanone	Ki	2500.0 [1]
	3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide	Ki	158.49 [1], 3162.28 [2]
	Sabcomeline	IC50	180.0 [1]
	Sabcomeline	Ki	204.17 [1]
	2,6,3,5-Ethanediylidenepentaleno(1,6-bc)pyrrol-2(1H)-ol, octahydro-1-(phenylmethyl)-	Ki	835.0 [1]
	Tbpb	IC50	3500.0 [1]
	Tbpb	Ki	320.0 [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]methanone	Ki	250.0 [1]
	Unii-I98T8BS72C	Ki	530.0 [1]
	N-[1-[3-(3-Oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamide	Ki	1000.0 [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]methanone	Ki	0.51 [1]
	[4-[(3R)-4-[(1S)-1-[4-(1,3-Benzodioxol-5-ylsulfonyl)phenyl]ethyl]-3-methylpiperazin-1-yl]piperidin-1-yl]-(2,6-dimethylphenyl)methanone	Ki	0.8 [1]
	Trimethyl-[[(2S,4R)-2-methyl-1,3-dioxolan-4-yl]methyl]azanium	Ki	1202.26 [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-thiadiazole	IC50	0.63 [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-thiadiazole	Ki	0.13 [1]

Entire TableStructureCompound NameStandard TypeStandard Values (in nM)

Items per page: 510All1 - 10 of 97 ⟨⟩

---

---

References

This online tool may be cited as follows

MLA	"Quest Database™ Muscarinic acetylcholine receptor M2 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m2-inhibitors-ic50-ki.
APA	AAT Bioquest, Inc. (2024, November 21). Quest Database™ Muscarinic acetylcholine receptor M2 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/muscarinic-acetylcholine-receptor-m2-inhibitors-ic50-ki.
BibTeX	EndNote	RefMan