Protein Information

General Information of the Protein

Protein ID	PT01516
Protein Name	Muscarinic acetylcholine receptor M5
Gene Name	CHRM5
Sequence	MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQLKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMNLLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPLDECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAEKRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQLTTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPNYLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNPNPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLGYWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP Show/Hide
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 Pi turnover. Show/Hide
Uniprot ID	Primary ID: P08912 Secondarily ID: Q96RG7 Show/Hide
Ensembl ID	ENSG00000184984
HGNC ID	HGNC:1954
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
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 Show/Hide	C19H29N5O6S2	2
1	EC50 = 630.96 nM Bioactivity Info	TI LI LO TS
2	Ki = 251.19 nM Bioactivity Info	TI LI LO TS
CP0635477 Compound Info	(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride Show/Hide	C6H15ClN2O2	3
1	EC50 = 1000 nM Bioactivity Info	TI LI LO TS
2	EC50 = 6309.57 nM Bioactivity Info	TI LI LO TS
3	Ki = 19952.62 nM Bioactivity Info	TI LI LO TS
CP0862620 Compound Info	Acetic acid 2-[2-(2-{2-[4-(1-methyl-1,2,5,6-tetrahydro-pyridin-3-yl)-[1,2,5]thiadiazol-3-yloxy]-ethoxy}-ethoxy)-ethoxy]-ethyl ester hydrochloride Show/Hide	C18H30ClN3O6S	1
1	EC50 = 1258.93 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 Show/Hide	C14H23N3OS	3
1	EC50 = 2511.89 nM Bioactivity Info	TI LI LO TS
2	EC50 = 12589.25 nM Bioactivity Info	TI LI LO TS
3	Ki = 1584.89 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 Show/Hide	C24H36N6O5S2	1
1	Ki = 63.1 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 Show/Hide	C21H33N5O7S2	1
1	Ki = 100 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 Show/Hide	C19H25N5O5S2	1
1	Ki = 100 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 Show/Hide	C20H36ClN3O2S	1
1	Ki = 125.89 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 Show/Hide	C23H37N5O3S2	1
1	Ki = 158.49 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 Show/Hide	C15H21N5O4S2	1
1	Ki = 251.19 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 Show/Hide	C19H25N5O5S2	1
1	Ki = 251.19 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 Show/Hide	C19H29N5O6S2	1
1	Ki = 398.11 nM Bioactivity Info	TI LI LO TS
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 Show/Hide	C19H30ClN5O6S2	1
1	Ki = 398.11 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 Show/Hide	C17H25N5O5S2	1
1	Ki = 630.96 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 Show/Hide	C22H38ClN3O3S	1
1	Ki = 630.96 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 Show/Hide	C16H27N3O5S	1
1	Ki = 3981.07 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: CL000035 , NIH 3T3

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 Show/Hide	C12H18N2O	1
1	EC50 = 55 nM
CP0240069 Compound Info	N-ethyl-1-(1H-indazol-5-ylsulfonyl)-N-[[2-(trifluoromethyl)phenyl]methyl]piperidine-4-carboxamide Show/Hide	C23H25F3N4O3S	1
1	EC50 = 190 nM
CP0635477 Compound Info	(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride Show/Hide	C6H15ClN2O2	2
1	EC50 = 360 nM
2	Ki = 4300 nM
CP0018455 Compound Info	1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid methyl ester;hydrobromide Show/Hide	C8H13NO2	2
1	EC50 = 600 nM
2	Ki = 56000 nM
CP0059332 Compound Info	1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione Show/Hide	C17H12F3NO4	2
1	EC50 = 1100 nM
2	EC50 = 1200 nM
CP0071482 Compound Info	1-(4-(6-fluoropyridin-2-yloxy)benzyl)-5-(trifluoromethoxy)indoline-2,3-dione Show/Hide	C21H12F4N2O4	1
1	EC50 = 1500 nM
CP0059333 Compound Info	1-(4-phenoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione Show/Hide	C22H14F3NO4	1
1	EC50 = 1900 nM
CP0113928 Compound Info	1-(4-bromobenzyl)indoline-2,3-dione Show/Hide	C15H10BrNO2	1
1	EC50 = 4100 nM
CP0673968 Compound Info	SID50106181 Show/Hide	C21H26INO2	5
1	IC50 = 0.45 nM
2	IC50 = 0.8 nM
3	IC50 = 0.83 nM
4	Ki = 0.22 nM
5	Ki = 0.42 nM
CP0164125 Compound Info	(9bS)-9b-(4-methoxy-3-methylphenyl)-1-(3,4,5-trifluorobenzoyl)-2,3-dihydroimidazo[2,1-a]isoindol-5-one Show/Hide	C25H19F3N2O3	1
1	IC50 = 246 nM
CP0317131 Compound Info	(9bS)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydroimidazo[2,1-a]isoindol-5-one Show/Hide	C23H15ClF2N2O2	1
1	IC50 = 300 nM
CP0047913 Compound Info	ENDO-ATROPINE Show/Hide	C17H23NO3	1
1	Ki = 0.14 nM
CP0109931 Compound Info	ATROPEN Show/Hide	C17H23NO3	1
1	Ki = 0.4 nM
CP0056034 Compound Info	11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one Show/Hide	C19H21N5O2	1
1	Ki = 126 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 Show/Hide	C37H41F3N4O4	1
1	Ki = 3500 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 Show/Hide	C26H30N2O4	1
1	Ki = 11220 nM
CP0026924 Compound Info	N-[1-[3-(3-oxo-1,4-benzoxazin-4-yl)propyl]piperidin-4-yl]-2-phenylacetamide Show/Hide	C24H29N3O3	1
1	Ki >= 1000 nM
CP0029624 Compound Info	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Show/Hide	C20H31NO	1
1	Ki >= 1000 nM

Clinical Information about the Protein

Target 1 ( Muscarinic acetylcholine receptor M5 (CHRM5) )

Target Type	Successful Target
Disease	18 Target-related Diseases				18
1	Glaucoma/ocular hypertension [ICD-11: 9C61]
2	Organophosphate poisoning [ICD-11: NE6Z]
3	Urinary retention [ICD-11: MF50.3]
4	Amnesia [ICD-11: MB21.1]
5	Examination of eyes or vision [ICD-11: QA00.6]
6	Suprapubic pain [ICD-11: MG30-MG3Z]
7	Gastrointestinal disease [ICD-11: DE2Z]
8	Irritable bowel syndrome [ICD-11: DD91.0]
9	Gastritis [ICD-11: DA42]
10	Peptic ulcer [ICD-11: DA61]
11	Parkinson disease [ICD-11: 8A00.0]
12	Psychomotor agitation [ICD-11: MB23.M]
13	Urinary incontinence [ICD-11: MF50.2]
14	Chronic obstructive pulmonary disease [ICD-11: CA22]
15	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
16	Depression [ICD-11: 6A70-6A7Z]
17	Alzheimer disease [ICD-11: 8A20]
18	Attention deficit hyperactivity disorder [ICD-11: 6A05.Z]
Approved Drug(s)	16 Approved Drugs				16
1	ACECLIDINE	Drug Info	Approved	Glaucoma/ocular hypertension
2	Atropine	Drug Info	Approved	Organophosphate poisoning
3	Bethanechol	Drug Info	Approved	Urinary retention
4	Choline alfoscerate	Drug Info	Approved	Amnesia
5	Cyclopentolate	Drug Info	Approved	Examination of eyes or vision
6	Flavoxate	Drug Info	Approved	Suprapubic pain
7	Hyoscyamine	Drug Info	Approved	Gastrointestinal disease
8	Mebeverine	Drug Info	Approved	Irritable bowel syndrome
9	Mepenzolate	Drug Info	Approved	Gastrointestinal disease
10	Methantheline	Drug Info	Approved	Gastritis
11	Oxyphencyclimine	Drug Info	Approved	Peptic ulcer
12	Pilocarpine	Drug Info	Approved	Glaucoma/ocular hypertension
13	Procyclidine	Drug Info	Approved	Parkinson disease
14	Promazine	Drug Info	Approved	Psychomotor agitation
15	Propiverine	Drug Info	Approved	Urinary incontinence
16	Umeclidinium	Drug Info	Approved	Chronic obstructive pulmonary disease
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	L-651582	Drug Info	Phase 3	Solid tumour/cancer
Discontinued Drug(s)	2 Discontinued Drugs				2
1	Benactyzine	Drug Info	Withdrawn from market	Depression
2	RS 86	Drug Info	Terminated	Alzheimer disease
Investigative Drug(s)	1 Investigative Drug				1
1	PF-3409409	Drug Info	Investigative	Attention deficit hyperactivity disorder

Similar Protein(s) and Bioactivity Statistics

50% Identity

Protein ID	Protein Name	Protein Organism
PT03292	Muscarinic acetylcholine receptor M5	Rattus norvegicus, Rat	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han