Page last updated: 2024-08-07 15:48:27

Muscarinic acetylcholine receptor M5

A muscarinic acetylcholine receptor M5 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08912]

Synonyms

Research

Bioassay Publications (89)

TimeframeStudies on this Protein(%)All Drugs %
pre-19907 (7.87)18.7374
1990's12 (13.48)18.2507
2000's31 (34.83)29.6817
2010's37 (41.57)24.3611
2020's2 (2.25)2.80

Compounds (143)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
quinacrineHomo sapiens (human)IC503.736010
quinacrineHomo sapiens (human)Ki2.684010
amiodaroneHomo sapiens (human)IC501.499010
amiodaroneHomo sapiens (human)Ki1.077010
amitriptylineHomo sapiens (human)IC500.008010
amitriptylineHomo sapiens (human)Ki0.005810
amoxapineHomo sapiens (human)IC500.856010
amoxapineHomo sapiens (human)Ki0.615010
1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl esterHomo sapiens (human)Ki0.933211
arecolineHomo sapiens (human)IC5062.500011
arecolineHomo sapiens (human)Ki56.117022
astemizoleHomo sapiens (human)IC500.703010
astemizoleHomo sapiens (human)Ki0.505010
bethanecholHomo sapiens (human)Ki0.097011
carbamylcholineHomo sapiens (human)Ki0.005011
chloroquineHomo sapiens (human)Ki21.877611
chlorpromazineHomo sapiens (human)IC500.025010
chlorpromazineHomo sapiens (human)Ki0.018010
clomipramineHomo sapiens (human)IC500.053010
clomipramineHomo sapiens (human)Ki0.038010
cyproheptadineHomo sapiens (human)IC500.003810
cyproheptadineHomo sapiens (human)Ki0.003421
dicyclomineHomo sapiens (human)IC500.002410
dicyclomineHomo sapiens (human)Ki0.001710
diphenidolHomo sapiens (human)IC501.191010
diphenidolHomo sapiens (human)Ki0.855010
diphenhydramineHomo sapiens (human)IC500.162010
diphenhydramineHomo sapiens (human)Ki0.116010
doxepinHomo sapiens (human)IC500.026010
doxepinHomo sapiens (human)Ki0.019010
droperidolHomo sapiens (human)IC502.298010
droperidolHomo sapiens (human)Ki1.651010
ebastineHomo sapiens (human)IC500.337810
ebastineHomo sapiens (human)Ki0.242710
fluoxetineHomo sapiens (human)IC501.358010
fluoxetineHomo sapiens (human)Ki0.976010
haloperidolHomo sapiens (human)IC503.890010
haloperidolHomo sapiens (human)Ki3.732521
hydroxychloroquineHomo sapiens (human)Ki19.952611
ketotifenHomo sapiens (human)IC500.374010
ketotifenHomo sapiens (human)Ki0.269010
maprotilineHomo sapiens (human)IC500.160010
maprotilineHomo sapiens (human)Ki0.115010
methapyrileneHomo sapiens (human)IC503.265010
methapyrileneHomo sapiens (human)Ki2.346010
methoctramineHomo sapiens (human)Ki0.431322
n-methylcarbamylcholineHomo sapiens (human)Ki0.150011
5-methylfurtrethoniumHomo sapiens (human)Ki6.918311
mianserinHomo sapiens (human)IC500.320010
mianserinHomo sapiens (human)Ki0.230010
nortriptylineHomo sapiens (human)IC500.027010
nortriptylineHomo sapiens (human)Ki0.020010
orphenadrineHomo sapiens (human)IC500.028010
orphenadrineHomo sapiens (human)Ki0.020010
oxotremorineHomo sapiens (human)IC508.000011
oxybutyninHomo sapiens (human)IC500.003210
oxybutyninHomo sapiens (human)Ki0.008221
oxymetazolineHomo sapiens (human)IC501.332010
oxymetazolineHomo sapiens (human)Ki0.957010
pentamidineHomo sapiens (human)IC502.885010
pentamidineHomo sapiens (human)Ki2.073010
perhexilineHomo sapiens (human)IC501.093210
perhexilineHomo sapiens (human)Ki0.785410
pirenzepineHomo sapiens (human)IC500.340611
pirenzepineHomo sapiens (human)Ki0.230533
prochlorperazineHomo sapiens (human)IC500.220010
prochlorperazineHomo sapiens (human)Ki0.158010
promazineHomo sapiens (human)IC500.064010
promazineHomo sapiens (human)Ki0.046010
promethazineHomo sapiens (human)IC500.004610
promethazineHomo sapiens (human)Ki0.003310
pyridostigmineHomo sapiens (human)Ki100.000011
quetiapineHomo sapiens (human)IC503.000710
quetiapineHomo sapiens (human)Ki1.588021
risperidoneHomo sapiens (human)Ki5.000011
spiperoneHomo sapiens (human)Ki49.600011
sulconazoleHomo sapiens (human)IC502.607010
sulconazoleHomo sapiens (human)Ki1.873010
thioridazineHomo sapiens (human)IC500.009210
thioridazineHomo sapiens (human)Ki0.006610
trihexyphenidylHomo sapiens (human)IC500.012010
trihexyphenidylHomo sapiens (human)Ki0.008710
tropicamideHomo sapiens (human)IC500.089010
tropicamideHomo sapiens (human)Ki0.064010
carbacholHomo sapiens (human)IC5025.200011
carbacholHomo sapiens (human)Ki37.69481313
pilocarpineHomo sapiens (human)Ki10.232911
(4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chlorideHomo sapiens (human)Ki3.801922
mepazineHomo sapiens (human)IC500.040010
mepazineHomo sapiens (human)Ki0.028010
cyclizineHomo sapiens (human)IC500.633010
cyclizineHomo sapiens (human)Ki0.455010
benzethonium chlorideHomo sapiens (human)IC500.134010
benzethonium chlorideHomo sapiens (human)Ki0.096010
sterogenolHomo sapiens (human)IC500.010010
sterogenolHomo sapiens (human)Ki0.007310
indopanHomo sapiens (human)Ki10.000011
dimenhydrinateHomo sapiens (human)IC500.316010
dimenhydrinateHomo sapiens (human)Ki0.227010
gentian violetHomo sapiens (human)IC500.535010
gentian violetHomo sapiens (human)Ki0.384010
glycopyrrolateHomo sapiens (human)IC500.000211
4-octylphenolHomo sapiens (human)IC5030.764010
4-octylphenolHomo sapiens (human)Ki22.102010
dimethindeneHomo sapiens (human)Ki0.794311
quinuclidinyl benzilateHomo sapiens (human)Ki0.000246
clemastineHomo sapiens (human)IC500.008410
clemastineHomo sapiens (human)Ki0.016821
dexchlorpheniramineHomo sapiens (human)IC501.043010
dexchlorpheniramineHomo sapiens (human)Ki0.749010
butaclamolHomo sapiens (human)Ki5.200011
paroxetineHomo sapiens (human)IC500.123010
paroxetineHomo sapiens (human)Ki0.089010
n-methyl-n-(1-methyl-4-pyrrolidino-2-butynyl)acetamideHomo sapiens (human)Ki0.330011
sertindoleHomo sapiens (human)Ki5.000011
xanomelineHomo sapiens (human)Ki0.708288
ziprasidoneHomo sapiens (human)Ki5.000011
nelfinavirHomo sapiens (human)IC5086.074010
nelfinavirHomo sapiens (human)Ki61.840010
trihexyphenidyl hydrochlorideHomo sapiens (human)IC500.010311
diphenidol hydrochlorideHomo sapiens (human)Ki1.288211
sertralineHomo sapiens (human)IC500.507310
sertralineHomo sapiens (human)Ki0.364510
esaprazoleHomo sapiens (human)IC5071.000011
aprofenHomo sapiens (human)Ki0.037022
n-methylscopolamineHomo sapiens (human)IC500.002311
n-methylscopolamineHomo sapiens (human)Ki0.000444
gr 127935Homo sapiens (human)Ki5.500022
afdx 384Homo sapiens (human)Ki0.537022
desloratadineHomo sapiens (human)IC500.292010
desloratadineHomo sapiens (human)Ki0.210010
l 670548Homo sapiens (human)Ki0.000211
azaprophenHomo sapiens (human)Ki0.000311
aq-ra 741Homo sapiens (human)Ki1.045322
bibn 99Homo sapiens (human)Ki1.445411
tripitramineHomo sapiens (human)Ki0.033911
solifenacinHomo sapiens (human)Ki0.043611
hyoscyamineHomo sapiens (human)Ki0.001034
harmalanHomo sapiens (human)Ki10.000011
atropineHomo sapiens (human)IC500.000910
atropineHomo sapiens (human)Ki0.00101213
dizocilpineHomo sapiens (human)IC500.002011
1-methyl-6-methoxy-dihydro-beta-carbolineHomo sapiens (human)Ki10.000011
terconazoleHomo sapiens (human)IC504.362010
terconazoleHomo sapiens (human)Ki3.134010
tolterodineHomo sapiens (human)Ki0.002211
darifenacinHomo sapiens (human)Ki0.002311
tropisetronHomo sapiens (human)IC503.450010
tropisetronHomo sapiens (human)Ki2.479010
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanolHomo sapiens (human)IC504.486810
(1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanolHomo sapiens (human)Ki3.223510
ipratropium bromide anhydrousHomo sapiens (human)Ki0.001011
methamilane methiodideHomo sapiens (human)Ki21.877611
flunarizineHomo sapiens (human)IC501.107010
flunarizineHomo sapiens (human)Ki0.795010
benztropineHomo sapiens (human)IC500.002010
benztropineHomo sapiens (human)Ki0.001510
cinnarizineHomo sapiens (human)IC500.759010
cinnarizineHomo sapiens (human)Ki0.545010
enclomipheneHomo sapiens (human)IC501.771010
enclomipheneHomo sapiens (human)Ki1.272010
tamoxifenHomo sapiens (human)IC502.585010
tamoxifenHomo sapiens (human)Ki1.857010
4-diphenylacetoxy-n-methylpiperidine methiodideHomo sapiens (human)IC500.000555
4-diphenylacetoxy-n-methylpiperidine methiodideHomo sapiens (human)Ki0.000433
harmineHomo sapiens (human)Ki10.000011
trospium chlorideHomo sapiens (human)Ki0.006011
l 745870Homo sapiens (human)Ki10.000011
homatropine hydrobromide, (endo-(+-)-isomer)Homo sapiens (human)IC500.055010
homatropine hydrobromide, (endo-(+-)-isomer)Homo sapiens (human)Ki0.039010
himbacineHomo sapiens (human)IC501.016011
himbacineHomo sapiens (human)Ki0.489811
fm1 43Homo sapiens (human)Ki0.083011
milamelineHomo sapiens (human)Ki3.162311
pd 144418Homo sapiens (human)Ki28.183811
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chlorideHomo sapiens (human)Ki2.750022
tert-butyl peroxybenzoateHomo sapiens (human)IC504.898912
tert-butyl peroxybenzoateHomo sapiens (human)Ki0.940011
77-lh-28-1Homo sapiens (human)Ki5.370311
meridianin aHomo sapiens (human)Ki10.000011
PB28Homo sapiens (human)Ki3.548111
amd 070Homo sapiens (human)IC5017.000011
naluzotanHomo sapiens (human)Ki2.000011
tiotropium bromideHomo sapiens (human)IC500.000111
tiotropium bromideHomo sapiens (human)Ki0.000011
aclidinium bromideHomo sapiens (human)IC500.000211
scopolamine hydrobromideHomo sapiens (human)Ki0.009422
a 803467Homo sapiens (human)IC5010.000011
sp 203Homo sapiens (human)Ki10.000011
pf 3246799Homo sapiens (human)IC500.300011
1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dioneHomo sapiens (human)Ki0.884522
n,n-diallyl-5-methoxytryptamineHomo sapiens (human)Ki10.000011
clozapineHomo sapiens (human)IC500.013010
clozapineHomo sapiens (human)Ki0.021821
olanzapineHomo sapiens (human)IC500.040010
olanzapineHomo sapiens (human)Ki0.027521
norclozapineHomo sapiens (human)Ki0.051011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
arecolineHomo sapiens (human)EC500.600011
oxotremorineHomo sapiens (human)EC500.055011
oxotremorineHomo sapiens (human)Kd0.930011
carbacholHomo sapiens (human)EC509,120,110,011.04221010
carbacholHomo sapiens (human)Kd17.000012
acetylcholine chlorideHomo sapiens (human)EC500.790011
muscarineHomo sapiens (human)EC501.300011
xanomelineHomo sapiens (human)EC503.234377
methoctramineHomo sapiens (human)Kd0.007411
atropineHomo sapiens (human)Kd0.001423
dinitrofluorobenzeneHomo sapiens (human)EC502.600011
sabcomelineHomo sapiens (human)EC500.123011
ac 260584Homo sapiens (human)EC501.000011
tert-butyl peroxybenzoateHomo sapiens (human)EC5043.333333
1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dioneHomo sapiens (human)EC501.140044
ml 137Homo sapiens (human)EC500.600011
ml253Homo sapiens (human)EC5030.000011
vu0364572Homo sapiens (human)EC5030.000011
vu0467154Homo sapiens (human)EC5030.000011
norclozapineHomo sapiens (human)EC500.170011

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
nifedipineHomo sapiens (human)ID50700,000.005022
carbacholHomo sapiens (human)ED502.050022
1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl esterHomo sapiens (human)ID504,000,000.000011
1,4-dihydro-2,6-dimethyl-4-(4-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl esterHomo sapiens (human)ID503,200,000.000011
atropineHomo sapiens (human)ED500.000122
atropineHomo sapiens (human)ID500.000111

Enables

This protein enables 4 target(s):

TargetCategoryDefinition
phosphatidylinositol phospholipase C activitymolecular functionCatalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate + H2O = 1,2-diacylglycerol + 1D-myo-inositol 1,4,5-trisphosphate + H+. [EC:3.1.4.11, RHEA:33179]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
G protein-coupled acetylcholine receptor activitymolecular functionCombining with acetylcholine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:fj, GOC:mah]
G protein-coupled serotonin receptor activitymolecular functionCombining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai]

Located In

This protein is located in 2 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
postsynaptic membranecellular componentA specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732]

Active In

This protein is active in 3 target(s):

TargetCategoryDefinition
dendritecellular componentA neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
synapsecellular componentThe junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]

Involved In

This protein is involved in 9 target(s):

TargetCategoryDefinition
gastric acid secretionbiological processThe regulated release of gastric acid (hydrochloric acid) by parietal or oxyntic cells during digestion. [GOC:hjd]
G protein-coupled acetylcholine receptor signaling pathwaybiological processA G protein-coupled receptor signaling pathway initiated by a ligand binding to an acetylcholine receptor on the surface of a target cell, and ends with regulation of a downstream cellular process, e.g. transcription. [GOC:mah, ISBN:0815316194]
dopamine transportbiological processThe directed movement of dopamine into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Dopamine is a catecholamine neurotransmitter and a metabolic precursor of noradrenaline and adrenaline. [GOC:ai]
transmission of nerve impulsebiological processThe neurological system process in which a signal is transmitted through the nervous system by a combination of action potential propagation and synaptic transmission. [GOC:curators, ISBN:0815316194]
regulation of phosphatidylinositol dephosphorylationbiological processAny process that modulates the frequency, rate or extent of the chemical reaction involving the removal of one or more phosphate groups from a phosphatidylinositol. [GOC:dph, GOC:tb]
G protein-coupled serotonin receptor signaling pathwaybiological processThe series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah]
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerbiological processA G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194]
chemical synaptic transmissionbiological processThe vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435]
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwaybiological processAn adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb]