General Information of the Protein
Protein ID
PT01198
Protein Name
Muscarinic acetylcholine receptor M2
Gene Name
CHRM2
Sequence
MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNYFLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQFFSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRIVKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDEITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNIVARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNTVWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Acetylcholine receptor
Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then triggers calcium ion release into the cytosol.
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Uniprot ID
Primary ID:
P08172

Secondarily ID:
Q4VBK6
Q9P1X9
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Ensembl ID
ENSG00000181072
HGNC ID
HGNC:1951
Subcellular Location
Cell membrane
Postsynaptic cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000398 , A-9
Compound ID Compound Name Compound Formula
CP0847519
5-{4-[2-(2-{2-[2-(4-Methoxy-[1,2,5]thiadiazol-3-yloxy)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-[1,2,5]thiadiazol-3-yl}-1-methyl-1,2,3,6-tetrahydro-pyridine hydrochloride
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C19H30ClN5O6S2
 2
1
IC50 = 0.5012 nM
   TI
   LI
   LO
   TS
2
Ki = 7.943 nM
   TI
   LI
   LO
   TS
CP0376259
1-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]-2-[2-(2-{2-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]ethoxy}ethoxy)ethoxy]ethane
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C24H36N6O5S2
 2
1
IC50 = 0.631 nM
   TI
   LI
   LO
   TS
2
Ki = 0.1259 nM
   TI
   LI
   LO
   TS
CP0371787
5-(4-Hexyloxy-[1,2,5]thiadiazol-3-yl)-1-methyl-1,2,3,6-tetrahydro-pyridine; oxalic acid
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C14H23N3OS
 2
1
IC50 = 12.59 nM
   TI
   LI
   LO
   TS
2
Ki = 50.12 nM
   TI
   LI
   LO
   TS
CP0635477
(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride
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C6H15ClN2O2
 2
1
IC50 = 12.59 nM
   TI
   LI
   LO
   TS
2
Ki = 100 nM
   TI
   LI
   LO
   TS
CP0739672
penta(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether
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C21H33N5O7S2
 1
1
Ki = 2.512 nM
   TI
   LI
   LO
   TS
CP0179471
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
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C19H29N5O6S2
 1
1
Ki = 7.943 nM
   TI
   LI
   LO
   TS
CP0846924
5-{4-[12-(4-Methoxy-[1,2,5]thiadiazol-3-yloxy)-dodecyloxy]-[1,2,5]thiadiazol-3-yl}-1-methyl-1,2,3,6-tetrahydro-pyridine
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C23H37N5O3S2
 1
1
Ki = 15.85 nM
   TI
   LI
   LO
   TS
CP0849748
Acetic acid 12-[4-(1-methyl-1,2,5,6-tetrahydro-pyridin-3-yl)-[1,2,5]thiadiazol-3-yloxy]-dodecyl ester hydrochloride
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C22H38ClN3O3S
 1
1
Ki = 15.85 nM
   TI
   LI
   LO
   TS
CP0853783
12-[4-(1-Methyl-1,2,5,6-tetrahydro-pyridin-3-yl)-[1,2,5]thiadiazol-3-yloxy]-dodecan-1-ol hydrochloride
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C20H36ClN3O2S
 1
1
Ki = 15.85 nM
   TI
   LI
   LO
   TS
CP0781215
tetra(ethylene glycol)(3-methoxy-1,2,4-thiadiazol-5-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether
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C19H29N5O6S2
 1
1
Ki = 39.81 nM
   TI
   LI
   LO
   TS
CP0847850
di(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether
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C15H21N5O4S2
 1
1
Ki = 39.81 nM
   TI
   LI
   LO
   TS
CP0847854
tri(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether
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C17H25N5O5S2
 1
1
Ki = 39.81 nM
   TI
   LI
   LO
   TS
CP0847851
tri(propylene glycol)(3-methoxy-1,2,4-thiadiazol-5-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether
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C19H25N5O5S2
 1
1
Ki = 63.1 nM
   TI
   LI
   LO
   TS
CP0847853
tri(propylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether
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C19H25N5O5S2
 1
1
Ki = 158.49 nM
   TI
   LI
   LO
   TS
CP0847381
2-(2-(2-(2-(4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazol-3-yloxy)ethoxy)ethoxy)ethoxy)ethanol
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C16H27N3O5S
 1
1
Ki = 316.23 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037621
(oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyrrolidin-2-one
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C12H18N2O
 2
1 EC50 = 19 nM
2 Ki = 10000 nM
CP0018455
1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid methyl ester;hydrobromide
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C8H13NO2
 3
1 EC50 = 25 nM
2 IC50 = 1800 nM
3 Ki = 2400 nM
CP0635477
(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride
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C6H15ClN2O2
 5
1 EC50 = 74 nM
2 IC50 = 130 nM
3 IC50 = 1400 nM
4 IC50 = 3100 nM
5 Ki = 1300 nM
CP0020189
6-acetoxy-8-azonia-bicyclo[3.2.1]octane
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C9H15NO2
 2
1 IC50 = 17 nM
2 IC50 = 120 nM
CP0010104
N,N'-bis[6-[(2-methoxyphenyl)methylamino]hexyl]octane-1,8-diamine
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C36H62N4O2
 5
1 IC50 = 34 nM
2 IC50 = 37 nM
3 IC50 = 51 nM
4 Ki = 26 nM
5 Ki = 36 nM
CP0049755
(R)-1-Aza-bicyclo[2.2.2]oct-3-yl-[(Z)-methoxyimino]-acetonitrile
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C10H15N3O
 1
1 IC50 = 180 nM
CP0167696
2-acetoxypropyl(trimethyl)ammonium;chloride
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C8H18NO2+
 2
1 IC50 = 380 nM
2 IC50 = 5200 nM
CP0054630
((2S,4R,5S)-4-Hydroxy-5-methyl-tetrahydro-furan-2-ylmethyl)-trimethyl-ammonium
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C9H20NO2+
 2
1 IC50 = 449 nM
2 IC50 = 3900 nM
CP0317131
(9bS)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydroimidazo[2,1-a]isoindol-5-one
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C23H15ClF2N2O2
 1
1 IC50 > 30000 nM
CP0666404
Tiotropium bromide
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C19H24BrNO5S2
 2
1 Ki = 0.01995 nM
2 Ki = 0.1 nM
CP0705209
(3R)-3-{[(2S)-2-Cyclopentyl-2-hydroxy-2-(2-thienyl)acetyl]-oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide
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C27H36BrNO4S
 1
1 Ki = 0.06 nM
CP0666488
(3R)-3-{[Hydroxy(di-2-thienyl)acetyl]oxy}-1-(2-phenylethyl)-1-azoniabicyclo[2.2.2]octane bromide
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C25H28BrNO3S2
 1
1 Ki = 0.08 nM
CP0696953
Aclidinium bromide
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C26H30BrNO4S2
 1
1 Ki = 0.08 nM
CP0167280
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid ethyl ester
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C28H36N2O5S
 1
1 Ki = 0.1099 nM
CP0366483
1-(isopropylsulfonyl)-4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidine
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C28H38N2O5S2
 1
1 Ki = 0.16 nM
CP0080609
1-Cyclohexyl-4-{1-[4-(4-methoxy-benzenesulfonyl)-phenyl]-vinyl}-piperidine
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C26H33NO3S
 1
1 Ki = 0.17 nM
CP0274359
cyclopropyl-[4-[4-[1-[4-(4-methoxyphenyl)sulfonylphenyl]ethenyl]piperidin-1-yl]piperidin-1-yl]methanone
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C29H36N2O4S
 1
1 Ki = 0.26 nM
CP0209448
4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)-1-(propylsulfonyl)piperidine
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C28H38N2O5S2
 1
1 Ki = 0.2897 nM
CP0203331
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid isobutyl ester
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C30H40N2O5S
 1
1 Ki = 0.2999 nM
CP0109931
ATROPEN
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C17H23NO3
 2
1 Ki = 0.344 nM
2 Ki = 1 nM
CP0177376
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid butyl ester
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C30H40N2O5S
 1
1 Ki = 0.3499 nM
CP0177381
1'-Benzenesulfonyl-4-{1-[4-(4-methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl
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C31H36N2O5S2
 1
1 Ki = 0.3597 nM
CP0212797
1'-(Butane-1-sulfonyl)-4-{1-[4-(4-methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl
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C29H40N2O5S2
 1
1 Ki = 0.3802 nM
CP0220544
1-(4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidin-1-yl)butan-1-one
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C29H38N2O4S
 1
1 Ki = 0.3802 nM
CP0177380
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid isopropyl ester
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C29H38N2O5S
 1
1 Ki = 0.4102 nM
CP0167279
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid benzyl ester
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C33H38N2O5S
 1
1 Ki = 0.4498 nM
CP0287765
1'-Ethanesulfonyl-4-{1-[4-(4-methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl
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C27H36N2O5S2
 1
1 Ki = 0.4603 nM
CP0203327
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid propyl ester
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C29H38N2O5S
 1
1 Ki = 0.5902 nM
CP0036569
(R)-3-(3-methoxyquinuclidin-3-yl)-1,1-diphenylprop-2-yn-1-ol
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C23H25NO2
 1
1 Ki = 0.79 nM
CP0245329
(2-Amino-3-methyl-phenyl)-{4-[4-(3-chloro-benzenesulfonyl)-benzyl]-[1,4']bipiperidinyl-1'-yl}-methanone
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C31H36ClN3O3S
 1
1 Ki = 0.89 nM
CP0406733
naphthalen-1-yl-[4-[4-[(4-propan-2-ylsulfanylphenyl)methyl]piperidin-1-yl]piperidin-1-yl]methanone
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C31H38N2OS
 1
1 Ki = 0.9 nM
CP0177377
4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid methyl ester
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C27H34N2O5S
 1
1 Ki = 0.9908 nM
CP0070586
Ipratropium Bromide
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C20H30BrNO3
 1
1 Ki = 1.02 nM
CP0203329
4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)-1-(piperidin-4-yl)piperidine
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C25H32N2O3S
 1
1 Ki = 1.14 nM
CP0212795
1-(benzylsulfonyl)-4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidine
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C32H38N2O5S2
 1
1 Ki = 1.449 nM
CP0203332
1-(4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidin-1-yl)-2-methylpropan-1-one
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C29H38N2O4S
 1
1 Ki = 2.198 nM
CP0177378
1-(4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidin-1-yl)-2-phenylethanone
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C33H38N2O4S
 1
1 Ki = 2.992 nM
CP0177379
1-(4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidin-1-yl)propan-1-one
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C28H36N2O4S
 1
1 Ki = 3.802 nM
CP0007317
(+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol
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C22H31NO
 1
1 Ki = 4 nM
CP0296594
(3S,3aR,4R,4aS,8aR,9aS)-4-[2-((2R,6S)-1,6-Dimethyl-piperidin-2-yl)-ethyl]-3-methyl-decahydro-naphtho[2,3-c]furan-1-one
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C22H37NO2
 1
1 Ki = 4.3 nM
CP0054849
(3S,3aR,4R,4aS,8aR,9aS)-3-Methyl-4-[2-((R)-1-methyl-6-(S)-methyl-piperidin-2-yl)-vinyl]-decahydro-naphtho[2,3-c]furan-1-one
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C22H35NO2
 1
1 Ki = 4.5 nM
CP0164673
2,2-Diphenyl-propionic acid 2-diethylamino-ethyl ester
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C21H27NO2
 1
1 Ki = 9.3 nM
CP0062485
4-(Diethylamino)-2-butynyl alpha-phenylcyclohexaneglycolic acid ester
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C22H31NO3
 1
1 Ki = 16 nM
CP0172665
(S)-1-cyclohexyl-3-((R)-3-methoxyquinuclidin-3-yl)-1-phenylprop-2-yn-1-ol
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C23H31NO2
 1
1 Ki = 20 nM
CP0010653
2-{1-[2-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-pyrrolidin-3-yl}-2,2-diphenyl-acetamide (Darifenacin)
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C28H30N2O2
 1
1 Ki = 50 nM
CP0037535
(AF-DX 116) 11-[2-(2-Diethylaminomethyl-piperidin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C24H31N5O2
 1
1 Ki = 81 nM
CP0025667
2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone
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C18H19ClN4
 1
1 Ki = 100 nM
CP0459246
(2-Amino-3-methyl-phenyl)-{4-[4-(propane-2-sulfonyl)-benzyl]-[1,4']bipiperidinyl-1'-yl}-methanone
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C28H39N3O3S
 1
1 Ki = 104 nM
CP0056034
11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
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C19H21N5O2
 2
1 Ki = 270 nM
2 Ki = 524 nM
CP0067390
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-carboxylate
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C26H30N2O4
 1
1 Ki = 339 nM
CP0067391
(2R)-1-((2S,4R)-4-hydroxy-1-[3,3,3-tris(4-fluorophenyl)propanoyl]pyrrolidine-2-yl)carbonyl-N-(4-piperidinylmethyl)pyrrolidine-2-carboxamide
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C37H41F3N4O4
 1
1 Ki = 490 nM
CP0026924
N-[1-[3-(3-oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamide
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C24H29N3O3
 1
1 Ki >= 1000 nM
CP0029624
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one
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C20H31NO
 1
1 Ki >= 1000 nM
Clinical Information about the Protein
Target 1 ( Muscarinic acetylcholine receptor M2 (CHRM2) )
Target Type Successful Target
Disease 8 Target-related Diseases  8
1 Glaucoma/ocular hypertension [ICD-11: 9C61]
2 Stabilize muscle contraction [ICD-11: FB3Z]
3 bronchial hyperreactivity [ICD-11: CB40]
4 Peptic ulcer [ICD-11: DA61]
5 Heart failure [ICD-11: BD10-BD13]
6 Parkinson disease [ICD-11: 8A00.0]
7 Alzheimer disease [ICD-11: 8A20]
8 Cardiovascular disease [ICD-11: BA00-BE2Z]
Approved Drug(s) 4 Approved Drugs  4
1 ACECLIDINE Approved
Glaucoma/ocular hypertension
2 Gallamine Triethiodide Approved
Stabilize muscle contraction
3 Methacholine Chloride Approved
bronchial hyperreactivity
4 Methylscopolamine Approved
Peptic ulcer
Discontinued Drug(s) 7 Discontinued Drugs  7
1 Otenzepad Discontinued in Phase 2
Heart failure
2 SCH-211803 Discontinued in Phase 1
Parkinson disease
3 Alvameline Terminated
Alzheimer disease
4 AQ-RA-741 Terminated
Cardiovascular disease
5 BIBN-140 Terminated
Alzheimer disease
6 BIBN-99 Terminated
Alzheimer disease
7 Sch-57790 Terminated
Alzheimer disease
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01470 Muscarinic acetylcholine receptor M2 Rattus norvegicus, Rat
PT04553 Muscarinic acetylcholine receptor M2 Mus musculus, Mouse