General Information of the Protein
Protein ID
PT01156
Protein Name
Muscarinic acetylcholine receptor M4
Gene Name
CHRM4
Sequence
MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGSATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIVPATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
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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 inhibition of adenylate cyclase.
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Uniprot ID
Primary ID:
P08173

Secondarily ID:
B2RPP4
Q0VD60
Q4VBK7
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Ensembl ID
ENSG00000180720
HGNC ID
HGNC:1953
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0847519
 Compound Info 
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 = 15.85 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
Ki = 2.512 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0371787
 Compound Info 
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 = 25.12 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
Ki = 39.81 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0635477
 Compound Info 
(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride
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C6H15ClN2O2
  2
1
IC50 = 1000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
Ki = 398.11 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0376259
 Compound Info 
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
  1
1
Ki = 1.995 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0179471
 Compound Info 
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 = 2.512 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0739672
 Compound Info 
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 = 12.59 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0846924
 Compound Info 
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 = 19.95 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0781215
 Compound Info 
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 = 25.12 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0853783
 Compound Info 
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 = 31.62 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0847850
 Compound Info 
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 = 63.1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0847854
 Compound Info 
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 = 79.43 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0849748
 Compound Info 
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 = 79.43 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0847851
 Compound Info 
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 = 158.49 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0847853
 Compound Info 
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
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0847381
 Compound Info 
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 = 794.33 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000051 , BHK-21
 Cell Line Info 
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000845 , CHO-K9
 Cell Line Info 
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000035 , NIH 3T3
 Cell Line Info 
Cell Line ID: CL000278 , RBL-2H3
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0037621
 Compound Info 
(oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyrrolidin-2-one
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C12H18N2O
  1
1 EC50 = 33 nM
CP0635477
 Compound Info 
(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride
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C6H15ClN2O2
  3
1 EC50 = 75 nM
2 IC50 = 7200 nM
3 Ki = 7600 nM
CP0224773
 Compound Info 
3-amino-N-(2,3-difluorobenzyl)-4-methyl-6-(4-pyridylmethoxy)thieno[2,3-b]pyridine-2-carboxamide
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C22H18F2N4O2S
  1
1 EC50 = 95 nM
CP0018455
 Compound Info 
1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid methyl ester;hydrobromide
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C8H13NO2
  3
1 EC50 = 130 nM
2 IC50 = 13500 nM
3 Ki = 60000 nM
CP0180462
 Compound Info 
3-amino-4,6-dimethyl-N-p-anisyl-thieno[2,3-b]pyridine-2-carboxamide
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C18H19N3O2S
  2
1 EC50 = 520 nM
2 EC50 = 680 nM
CP0673968
 Compound Info 
SID50106181
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C21H26INO2
  6
1 IC50 = 0.61 nM
2 IC50 = 0.83 nM
3 IC50 = 1.1 nM
4 IC50 = 1.9 nM
5 Ki = 0.37 nM
6 Ki = 0.66 nM
CP0049755
 Compound Info 
(R)-1-Aza-bicyclo[2.2.2]oct-3-yl-[(Z)-methoxyimino]-acetonitrile
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C10H15N3O
  1
1 IC50 = 90 nM
CP0317131
 Compound Info 
(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
CP0067390
 Compound Info 
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 = 1 nM
CP0164673
 Compound Info 
2,2-Diphenyl-propionic acid 2-diethylamino-ethyl ester
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C21H27NO2
  1
1 Ki = 7.4 nM
CP0067391
 Compound Info 
(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 = 42 nM
CP0025667
 Compound Info 
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
CP0056034
 Compound Info 
11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
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C19H21N5O2
  1
1 Ki = 105 nM
CP0040250
 Compound Info 
2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol
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C21H25N3O2S
  1
1 Ki = 1000 nM
CP0045063
 Compound Info 
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine
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C17H20N4S
  1
1 Ki = 1000 nM
CP0026924
 Compound Info 
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
 Compound Info 
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 M4 (CHRM4) )
Target Type Successful Target
Disease 5 Target-related Diseases  5
1 Glaucoma/ocular hypertension [ICD-11: 9C61]
2 Nausea [ICD-11: MD90]
3 bronchial hyperreactivity [ICD-11: CB40]
4 Mydriasis [ICD-11: LA11.62]
5 Attention deficit hyperactivity disorder [ICD-11: 6A05.Z]
Approved Drug(s) 4 Approved Drugs  4
1 ACECLIDINE
 Drug Info 
Approved
Glaucoma/ocular hypertension
2 Diphenidol
 Drug Info 
Approved
Nausea
3 Methacholine Chloride
 Drug Info 
Approved
bronchial hyperreactivity
4 Tropicamide
 Drug Info 
Approved
Mydriasis
Investigative Drug(s) 1 Investigative Drug  1
1 PF-3409409
 Drug Info 
Investigative
Attention deficit hyperactivity disorder
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01736 Muscarinic acetylcholine receptor M4 Rattus norvegicus, Rat
 Protein Info