Protein Information

General Information of the Protein

Protein ID	PT01310
Protein Name	Muscarinic acetylcholine receptor M1
Gene Name	CHRM1
Sequence	MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVNNYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLISFDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYIQFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSSSERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEVVIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKEKKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYALCNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC 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: P11229 Secondarily ID: Q96RH1 Show/Hide
Ensembl ID	ENSG00000168539
HGNC ID	HGNC:1950
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
CP0375816 Compound Info	(1R,5R,6R)-6-[4-(3-Phenyl-prop-2-ynylsulfanyl)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[3.2.1]octane Show/Hide	C18H19N3S2	1
1	EC50 = 0.2 nM Bioactivity Info	TI LI LO TS
CP0375500 Compound Info	(1R,5R,6R)-6-[4-(3-Phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[3.2.1]octane Show/Hide	C18H19N3OS	1
1	EC50 = 0.5 nM Bioactivity Info	TI LI LO TS
CP0405062 Compound Info	(R)-3-[4-(3-Phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[2.2.1]heptane Show/Hide	C17H17N3OS	1
1	EC50 = 0.99 nM Bioactivity Info	TI LI LO TS
CP0403809 Compound Info	6-(4-Propylsulfanyl-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[3.2.1]octane Show/Hide	C12H19N3OS2	1
1	EC50 = 1 nM Bioactivity Info	TI LI LO TS
CP0416658 Compound Info	(1R,5R,6S)-6-[4-(3-Phenyl-prop-2-ynylsulfanyl)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[3.2.1]octane Show/Hide	C18H19N3S2	1
1	EC50 = 1 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	7
1	EC50 = 7.943 nM Bioactivity Info	TI LI LO TS
2	EC50 = 8.5 nM Bioactivity Info	TI LI LO TS
3	EC50 = 10 nM Bioactivity Info	TI LI LO TS
4	EC50 = 50.12 nM Bioactivity Info	TI LI LO TS
5	Ki = 0.1 nM Bioactivity Info	TI LI LO TS
6	Ki = 0.12 nM Bioactivity Info	TI LI LO TS
7	Ki = 100 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	8
1	EC50 = 10 nM Bioactivity Info	TI LI LO TS
2	EC50 = 57 nM Bioactivity Info	TI LI LO TS
3	EC50 = 158.49 nM Bioactivity Info	TI LI LO TS
4	EC50 = 200 nM Bioactivity Info	TI LI LO TS
5	EC50 = 316.23 nM Bioactivity Info	TI LI LO TS
6	Ki = 82 nM Bioactivity Info	TI LI LO TS
7	Ki = 158.49 nM Bioactivity Info	TI LI LO TS
8	Ki = 3981.07 nM Bioactivity Info	TI LI LO TS
CP0403949 Compound Info	3-[4-(3-Phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[2.2.2]octane Show/Hide	C18H19N3OS	1
1	EC50 = 15.7 nM Bioactivity Info	TI LI LO TS
CP0500904 Compound Info	3-(4-Butylsulfanyl-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[2.2.2]octane Show/Hide	C13H21N3OS2	1
1	EC50 = 22.3 nM Bioactivity Info	TI LI LO TS
CP0375675 Compound Info	(1R,5R,6S)-6-[4-(3-Phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[3.2.1]octane Show/Hide	C18H19N3OS	1
1	EC50 = 28.3 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	4
1	EC50 = 63.1 nM Bioactivity Info	TI LI LO TS
2	EC50 = 251.19 nM Bioactivity Info	TI LI LO TS
3	EC50 = 1995.26 nM Bioactivity Info	TI LI LO TS
4	Ki = 50.12 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	2
1	EC50 = 63.1 nM Bioactivity Info	TI LI LO TS
2	Ki = 25.12 nM Bioactivity Info	TI LI LO TS
CP0441169 Compound Info	3-[4-(3-Phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[2.2.1]heptane Show/Hide	C17H17N3OS	1
1	EC50 = 67.3 nM Bioactivity Info	TI LI LO TS
CP0403933 Compound Info	1-[4-(3-Phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-4-aza-tricyclo[2.2.1.02,6]heptane Show/Hide	C17H15N3OS	1
1	EC50 = 70.5 nM Bioactivity Info	TI LI LO TS
CP0476699 Compound Info	1,5-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]pentane Show/Hide	C21H30N6S4	2
1	EC50 = 79 nM Bioactivity Info	TI LI LO TS
2	Ki = 14 nM Bioactivity Info	TI LI LO TS
CP0457009 Compound Info	3-(4-Butoxy-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[2.2.2]octane Show/Hide	C13H21N3O2S	1
1	EC50 = 102 nM Bioactivity Info	TI LI LO TS
CP0403635 Compound Info	1-Methyl-5-[4-(3-phenyl-prop-2-ynyloxy)-[1,2,5]thiadiazol-3-yl]-1,2,3,6-tetrahydro-pyridine Show/Hide	C17H17N3OS	1
1	EC50 = 110 nM Bioactivity Info	TI LI LO TS
CP0441212 Compound Info	1,9-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]nonane Show/Hide	C25H38N6S4	2
1	EC50 = 120 nM Bioactivity Info	TI LI LO TS
2	Ki = 17 nM Bioactivity Info	TI LI LO TS
CP0409441 Compound Info	3-[(3R,4S)-1-azabicyclo[2.2.1]heptan-3-yl]-4-(3-phenylprop-2-ynoxy)-1,2,5-thiadiazole Show/Hide	C17H17N3OS	1
1	EC50 = 159 nM Bioactivity Info	TI LI LO TS
CP0448660 Compound Info	3-(4-Pentyloxy-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[2.2.2]octane Show/Hide	C14H23N3O2S	1
1	EC50 = 164.8 nM Bioactivity Info	TI LI LO TS
CP0460763 Compound Info	1,7-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]heptane Show/Hide	C23H34N6S4	2
1	EC50 = 180 nM Bioactivity Info	TI LI LO TS
2	Ki = 7.6 nM Bioactivity Info	TI LI LO TS
CP0374676 Compound Info	3-(4-Hexylsulfanyl-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[2.2.2]octane Show/Hide	C15H25N3OS2	1
1	EC50 = 225 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	2
1	EC50 = 251.19 nM Bioactivity Info	TI LI LO TS
2	Ki = 398.11 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 Show/Hide	C19H29N5O6S2	2
1	EC50 = 251.19 nM Bioactivity Info	TI LI LO TS
2	Ki = 199.53 nM Bioactivity Info	TI LI LO TS
CP0409501 Compound Info	3-(4-Hexyloxy-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[2.2.2]octane Show/Hide	C15H25N3O2S	1
1	EC50 = 258.9 nM Bioactivity Info	TI LI LO TS
CP0460884 Compound Info	1,12-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]dodecane Show/Hide	C28H44N6O2S2	2
1	EC50 = 340 nM Bioactivity Info	TI LI LO TS
2	Ki = 1.6 nM Bioactivity Info	TI LI LO TS
CP0406497 Compound Info	1,3-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]propane Show/Hide	C19H26N6S4	2
1	EC50 = 350 nM Bioactivity Info	TI LI LO TS
2	Ki = 1.2 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	2
1	EC50 = 398.11 nM Bioactivity Info	TI LI LO TS
2	Ki = 1995.26 nM Bioactivity Info	TI LI LO TS
CP0395501 Compound Info	3-(4-Propylsulfanyl-[1,2,5]thiadiazol-3-yloxy)-1-aza-bicyclo[2.2.2]octane Show/Hide	C12H19N3OS2	1
1	EC50 = 430.9 nM Bioactivity Info	TI LI LO TS
CP0468061 Compound Info	1,2-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]ethane Show/Hide	C18H24N6S4	2
1	EC50 = 440 nM Bioactivity Info	TI LI LO TS
2	Ki = 20 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	2
1	EC50 = 501.19 nM Bioactivity Info	TI LI LO TS
2	Ki = 63.1 nM Bioactivity Info	TI LI LO TS
CP0380108 Compound Info	1,4-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]butane Show/Hide	C20H28N6S4	2
1	EC50 = 570 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.93 nM Bioactivity Info	TI LI LO TS
CP0407175 Compound Info	1,6-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]hexane Show/Hide	C22H32N6S4	2
1	EC50 = 590 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.87 nM Bioactivity Info	TI LI LO TS
CP0853788 Compound Info	2-[2-(2-{2-[4-(1-Methyl-1,2,5,6-tetrahydro-pyridin-3-yl)-[1,2,5]thiadiazol-3-yloxy]-ethoxy}-ethoxy)-ethoxy]-ethanol hydrochloride Show/Hide	C16H28ClN3O5S	2
1	EC50 = 630.96 nM Bioactivity Info	TI LI LO TS
2	Ki = 79.43 nM Bioactivity Info	TI LI LO TS
CP0399528 Compound Info	1,9-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]nonane Show/Hide	C25H38N6O2S2	2
1	EC50 = 720 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.84 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	2
1	EC50 = 794.33 nM Bioactivity Info	TI LI LO TS
2	Ki = 1000 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	2
1	EC50 = 794.33 nM Bioactivity Info	TI LI LO TS
2	Ki = 316.23 nM Bioactivity Info	TI LI LO TS
CP0463033 Compound Info	1,8-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]octane Show/Hide	C24H36N6S4	2
1	EC50 = 920 nM Bioactivity Info	TI LI LO TS
2	Ki = 5 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	2
1	EC50 = 1000 nM Bioactivity Info	TI LI LO TS
2	Ki = 794.33 nM Bioactivity Info	TI LI LO TS
CP0449083 Compound Info	1,11-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]undecane Show/Hide	C27H42N6S4	2
1	EC50 = 1500 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.57 nM Bioactivity Info	TI LI LO TS
CP0476680 Compound Info	1,10-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]decane Show/Hide	C26H40N6S4	2
1	EC50 = 2100 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.32 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	2
1	EC50 = 2511.89 nM Bioactivity Info	TI LI LO TS
2	Ki = 3.981 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	2
1	EC50 = 3162.28 nM Bioactivity Info	TI LI LO TS
2	Ki = 100 nM Bioactivity Info	TI LI LO TS
CP0635477 Compound Info	(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride Show/Hide	C6H15ClN2O2	7
1	EC50 = 3162.28 nM Bioactivity Info	TI LI LO TS
2	EC50 = 3811 nM Bioactivity Info	TI LI LO TS
3	EC50 = 5011.87 nM Bioactivity Info	TI LI LO TS
4	EC50 = 13000 nM Bioactivity Info	TI LI LO TS
5	EC50 = 15848.93 nM Bioactivity Info	TI LI LO TS
6	Ki = 3162.28 nM Bioactivity Info	TI LI LO TS
7	Ki = 20000 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	2
1	EC50 = 3162.28 nM Bioactivity Info	TI LI LO TS
2	Ki = 50.12 nM Bioactivity Info	TI LI LO TS
CP0210785 Compound Info	Aceclidine Show/Hide	C9H15NO2	1
1	EC50 = 4466 nM Bioactivity Info	TI LI LO TS
CP0449112 Compound Info	3-Butoxy-4-(pyrrolidin-3-yloxy)-[1,2,5]thiadiazole Show/Hide	C10H17N3O2S	1
1	EC50 = 4867 nM Bioactivity Info	TI LI LO TS
CP0018455 Compound Info	1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid methyl ester;hydrobromide Show/Hide	C8H13NO2	1
1	EC50 = 5603 nM Bioactivity Info	TI LI LO TS
CP0445380 Compound Info	3-(Azetidin-3-yloxy)-4-butoxy-[1,2,5]thiadiazole Show/Hide	C9H15N3O2S	1
1	EC50 = 6202 nM Bioactivity Info	TI LI LO TS
CP0900174 Compound Info	5-[4-(2-{2-[2-(2-Ethoxy-ethoxy)-ethoxy]-ethoxy}-ethoxy)-[1,2,5]thiadiazol-3-yl]-1-methyl-1,2,3,6-tetrahydro-pyridine hydrochloride Show/Hide	C18H32ClN3O5S	2
1	EC50 = 6309.57 nM Bioactivity Info	TI LI LO TS
2	Ki = 398.11 nM Bioactivity Info	TI LI LO TS
CP0089021 Compound Info	(+)-pilocarpine Show/Hide	C11H16N2O2	1
1	EC50 = 8792 nM Bioactivity Info	TI LI LO TS
CP0383357 Compound Info	1,12-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-ylsulfanyl]dodecane Show/Hide	C28H44N6S4	2
1	EC50 = 13000 nM Bioactivity Info	TI LI LO TS
2	Ki = 0.69 nM Bioactivity Info	TI LI LO TS
CP0397762 Compound Info	(1R,3S,4R)-3-[4-(3-Phenyl-prop-2-ynylsulfanyl)-[1,2,5]thiadiazol-3-yl]-1-aza-bicyclo[2.2.1]heptane Show/Hide	C17H17N3S2	1
1	EC50 > 100 nM Bioactivity Info	TI LI LO TS
CP0382879 Compound Info	1-Aza-bicyclo[2.2.1]heptan-3-one O-[3-(3-methoxy-phenyl)-prop-2-ynyl]-oxime Show/Hide	C16H18N2O2	1
1	EC50 > 1000 nM Bioactivity Info	TI LI LO TS
CP0376490 Compound Info	1,8-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]octane Show/Hide	C24H36N6O2S2	1
1	Ki = 0.19 nM Bioactivity Info	TI LI LO TS
CP0471023 Compound Info	1,10-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]decane Show/Hide	C26H40N6O2S2	1
1	Ki = 0.23 nM Bioactivity Info	TI LI LO TS
CP0401666 Compound Info	1,6-di[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]hexane Show/Hide	C22H32N6O2S2	1
1	Ki = 0.61 nM Bioactivity Info	TI LI LO TS
CP0377637 Compound Info	1-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]-2-{2-[2-(2-{2-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]ethoxy}ethoxy)ethoxy]ethoxy}ethane Show/Hide	C26H40N6O6S2	1
1	Ki = 1.5 nM Bioactivity Info	TI LI LO TS
CP0511621 Compound Info	1-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]-2-(2-{2-[2-(2-{2-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]ethoxy}ethoxy)ethoxy]ethoxy}ethoxy)ethane Show/Hide	C28H44N6O7S2	1
1	Ki = 1.9 nM Bioactivity Info	TI LI LO TS
CP0176132 Compound Info	11-[2-[4-[4-(diethylamino)butyl]piperidin-1-yl]acetyl]-5H-benzo[b][1,4]benzodiazepin-6-one Show/Hide	C28H38N4O2	1
1	Ki = 3.981 nM Bioactivity Info	TI LI LO TS
CP0477109 Compound Info	1-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]-2-{2-[4-(1-methyl-1,2,3,6-tetrahydro-5-pyridinyl)-1,2,5-thiadiazol-3-yloxy]ethoxy}ethane Show/Hide	C20H28N6O3S2	1
1	Ki = 4.9 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	Ki = 199.53 nM Bioactivity Info	TI LI LO TS
CP0895259 Compound Info	5-(4-{2-[2-(2-Ethoxy-ethoxy)-ethoxy]-ethoxy}-[1,2,5]thiadiazol-3-yl)-1-methyl-1,2,3,6-tetrahydro-pyridine hydrochloride Show/Hide	C16H28ClN3O4S	1
1	Ki = 630.96 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000051 , BHK-21

Cell Line Info

Cell Line ID: CL000943 , CellSensor NFAT-bla CHO-K1

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: CL000386 , Flp-In-CHO

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: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0379273 Compound Info	2-[4,6-difluoro-1-[[6-(1-methylpyrazol-4-yl)pyridin-3-yl]methyl]indol-3-yl]sulfonyl-N-(5-methyl-1,2-oxazol-3-yl)acetamide Show/Hide	C24H20F2N6O4S	1
1	EC50 = 310 nM
CP0037621 Compound Info	(oxotremorine)1-(4-Pyrrolidin-1-yl-but-2-ynyl)-pyrrolidin-2-one Show/Hide	C12H18N2O	1
1	EC50 = 390 nM
CP0314375 Compound Info	1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid Show/Hide	C18H15NO4	1
1	EC50 = 820 nM
CP0055373 Compound Info	1-(2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)benzyl)indoline-2,3-dione Show/Hide	C19H14FN3O2	2
1	EC50 = 830 nM
2	EC50 > 30000 nM
CP0191257 Compound Info	3-[[2,6-difluoro-4-(2-methylindazol-4-yl)phenyl]methyl]pyrido[3,4-d]pyrimidin-4-one Show/Hide	C22H15F2N5O	2
1	EC50 = 980 nM
2	EC50 > 10000 nM
CP0123721 Compound Info	6-[[2-fluoro-4-(1-methylpyrazol-4-yl)phenyl]methyl]-7H-pyrrolo[3,4-b]pyridin-5-one Show/Hide	C18H15FN4O	2
1	EC50 = 2600 nM
2	EC50 > 10000 nM
CP0018455 Compound Info	1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid methyl ester;hydrobromide Show/Hide	C8H13NO2	3
1	EC50 = 3200 nM
2	IC50 = 65000 nM
3	Ki = 29000 nM
CP0635477 Compound Info	(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride Show/Hide	C6H15ClN2O2	2
1	EC50 = 4600 nM
2	Ki = 12000 nM
CP0113928 Compound Info	1-(4-bromobenzyl)indoline-2,3-dione Show/Hide	C15H10BrNO2	1
1	EC50 = 6000 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	11
1	IC50 = 12 nM
2	IC50 = 19 nM
3	IC50 = 22 nM
4	IC50 = 27 nM
5	IC50 = 29 nM
6	Kd = 20 nM
7	Ki = 9.1 nM
8	Ki = 10 nM
9	Ki = 15 nM
10	Ki = 23.5 nM
11	Ki = 25 nM
CP0059084 Compound Info	8-((S)-3-amino-piperidin-1-yl)-3-methyl-7-(3-methyl-but-2-enyl)-1-(2-oxo-2-phenyl-ethyl)-3,7-dihydro-purine-2,6-dione Show/Hide	C24H30N6O3	1
1	IC50 = 50 nM
CP0049755 Compound Info	(R)-1-Aza-bicyclo[2.2.2]oct-3-yl-[(Z)-methoxyimino]-acetonitrile Show/Hide	C10H15N3O	1
1	IC50 = 170 nM
CP0079344 Compound Info	(R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione Show/Hide	C25H28N8O2	2
1	IC50 = 295 nM
2	IC50 = 300 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 > 30000 nM
CP0282150 Compound Info	1-N-[2-[4-[4-(2-oxo-3H-benzimidazol-1-yl)piperidin-1-yl]piperidin-1-yl]ethyl]-3-N-[2-[4-[4-[1-[2-oxo-2-(6-oxo-5H-benzo[b][1,4]benzodiazepin-11-yl)ethyl]piperidin-4-yl]butyl]piperazin-1-yl]ethyl]-5-[(propanoylamino)methyl]benzene-1,3-dicarboxamide Show/Hide	C61H80N12O6	1
1	Kd = 0.8128 nM
CP0381998 Compound Info	2-[3-(diethylamino)-6-diethylazaniumylidenexanthen-9-yl]-5-[5-[1-[4-(2-methylphenyl)-4-oxobutyl]piperidin-4-yl]pentylsulfamoyl]benzenesulfonate Show/Hide	C48H62N4O7S2	1
1	Kd = 794.33 nM
CP0089021 Compound Info	(+)-pilocarpine Show/Hide	C11H16N2O2	2
1	Kd = 2691.53 nM
2	Ki = 7943.28 nM
CP0207650 Compound Info	(4R,5S)-5-Methyl-4-[(E)-3-((R)-1-methyl-piperidin-2-yl)-allyl]-dihydro-furan-2-one Show/Hide	C14H23NO2	1
1	Kd = 9700 nM
CP0000324 Compound Info	2-acetoxyethyl(trimethyl)ammonium;bromide Show/Hide	C7H16NO2+	2
1	Kd = 17378.01 nM
2	Ki = 12589.25 nM
CP0666488 Compound Info	(3R)-3-{[Hydroxy(di-2-thienyl)acetyl]oxy}-1-(2-phenylethyl)-1-azoniabicyclo[2.2.2]octane bromide Show/Hide	C25H28BrNO3S2	1
1	Ki = 0.08 nM
CP0696953 Compound Info	Aclidinium bromide Show/Hide	C26H30BrNO4S2	1
1	Ki = 0.08 nM
CP0705209 Compound Info	(3R)-3-{[(2S)-2-Cyclopentyl-2-hydroxy-2-(2-thienyl)acetyl]-oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide Show/Hide	C27H36BrNO4S	1
1	Ki = 0.09 nM
CP0666404 Compound Info	Tiotropium bromide Show/Hide	C19H24BrNO5S2	1
1	Ki = 0.12 nM
CP0109931 Compound Info	ATROPEN Show/Hide	C17H23NO3	2
1	Ki = 0.3 nM
2	Ki = 2 nM
CP0025667 Compound Info	2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone Show/Hide	C18H19ClN4	3
1	Ki = 0.98 nM
2	Ki = 1.8 nM
3	Ki = 100 nM
CP0070586 Compound Info	Ipratropium Bromide Show/Hide	C20H30BrNO3	1
1	Ki = 1.51 nM
CP0164673 Compound Info	2,2-Diphenyl-propionic acid 2-diethylamino-ethyl ester Show/Hide	C21H27NO2	2
1	Ki = 2.1 nM
2	Ki = 26.5 nM
CP0045063 Compound Info	2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine Show/Hide	C17H20N4S	3
1	Ki = 2.1 nM
2	Ki = 4.7 nM
3	Ki = 100 nM
CP0080609 Compound Info	1-Cyclohexyl-4-{1-[4-(4-methoxy-benzenesulfonyl)-phenyl]-vinyl}-piperidine Show/Hide	C26H33NO3S	1
1	Ki = 2.8 nM
CP0167280 Compound Info	4-{1-[4-(4-Methoxy-benzenesulfonyl)-phenyl]-vinyl}-[1,4']bipiperidinyl-1'-carboxylic acid ethyl ester Show/Hide	C28H36N2O5S	1
1	Ki = 6.486 nM
CP0203329 Compound Info	4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)-1-(piperidin-4-yl)piperidine Show/Hide	C25H32N2O3S	1
1	Ki = 9.099 nM
CP0209448 Compound Info	4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)-1-(propylsulfonyl)piperidine Show/Hide	C28H38N2O5S2	1
1	Ki = 25.82 nM
CP0296594 Compound Info	(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 Show/Hide	C22H37NO2	1
1	Ki = 32 nM
CP0220544 Compound Info	1-(4-(4-(1-(4-(4-methoxyphenylsulfonyl)phenyl)vinyl)piperidin-1-yl)piperidin-1-yl)butan-1-one Show/Hide	C29H38N2O4S	1
1	Ki = 42.17 nM
CP0101233 Compound Info	2-(4-Hydroxy-phenyl)-2-phenyl-propionic acid 2-diethylamino-ethyl ester Show/Hide	C21H27NO3	1
1	Ki = 44 nM
CP0054849 Compound Info	(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 Show/Hide	C22H35NO2	1
1	Ki = 48 nM
CP0040250 Compound Info	2-[2-(4-Dibenzo[b,f][1,4]thiazepin-11-yl-1-piperazinyl)ethoxy]ethanol Show/Hide	C21H25N3O2S	3
1	Ki = 56 nM
2	Ki = 100 nM
3	Ki = 1000 nM
CP0673820 Compound Info	2-(2,2-diphenylacetoxy)-N,N,N-triethylethanaminiumiodide Show/Hide	C22H30INO2	1
1	Ki = 65.5 nM
CP0042567 Compound Info	[3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone Show/Hide	C32H43N5O2	1
1	Ki = 97 nM
CP0822547 Compound Info	2-(2,2-diphenylacetoxy)-N,N-diethyl-Nmethylethanaminiumbromide Show/Hide	C21H28BrNO2	1
1	Ki = 164 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 = 170 nM
CP0842192 Compound Info	2-(2,2-diphenylacetoxy)-N,N,Ntrimethylethanaminiumbromide Show/Hide	C19H24BrNO2	1
1	Ki = 254 nM
CP0220610 Compound Info	Bietamiverine Show/Hide	C19H30N2O2	1
1	Ki = 517 nM
CP0037535 Compound Info	(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 Show/Hide	C24H31N5O2	1
1	Ki = 537 nM
CP0008601 Compound Info	4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl) Show/Hide	C21H23ClFNO2	1
1	Ki = 1600 nM
CP0156301 Compound Info	2-(diethylamino)ethyl 2-(4-chlorophenyl)sulfanylbenzoate Show/Hide	C19H22ClNO2S	1
1	Ki = 2670 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 = 13180 nM
CP0056536 Compound Info	N,N-dimethyl-2-[3-(pyrazin-2-ylmethyl)-1H-inden-2-yl]ethanamine Show/Hide	C18H21N3	1
1	Ki = 19000 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
CP0040489 Compound Info	1-(4-fluorobenzyl)-2-(4-(4-methyl-1H-pyrazol-1-yl)piperidin-1-yl)-1H-benzo[d]imidazole Show/Hide	C23H24FN5	1
1	Ki > 10000 nM

Clinical Information about the Protein

Target 1 ( Muscarinic acetylcholine receptor M1 (CHRM1) )

Target Type	Successful Target
Disease	18 Target-related Diseases				18
1	Glaucoma/ocular hypertension [ICD-11: 9C61]
2	Parkinson disease [ICD-11: 8A00.0]
3	Functional bowel syndrome [ICD-11: DD91.0]
4	Peptic ulcer [ICD-11: DA61]
5	Overactive bladder [ICD-11: GC50.0]
6	Anaesthesia [ICD-11: 9A78.6]
7	Visceral spasms [ICD-11: MD81.4]
8	Stomach ulcer [ICD-11: DA60.Z]
9	Dystonia [ICD-11: 8A02]
10	Urinary incontinence [ICD-11: MF50.2]
11	Schizoaffective disorder [ICD-11: 6A21]
12	Dementia [ICD-11: 6D80-6D86]
13	Chronic obstructive pulmonary disease [ICD-11: CA22]
14	Inflammatory bowel disease [ICD-11: DD72]
15	Cognitive impairment [ICD-11: 6D71]
16	Schizophrenia [ICD-11: 6A20]
17	Alzheimer disease [ICD-11: 8A20]
18	Neurological disorder [ICD-11: 6B60]
Approved Drug(s)	12 Approved Drugs				12
1	ACECLIDINE	Drug Info	Approved	Glaucoma/ocular hypertension
2	Benztropine	Drug Info	Approved	Parkinson disease
3	Biperiden	Drug Info	Approved	Parkinson disease
4	Dicyclomine	Drug Info	Approved	Functional bowel syndrome
5	Diphemanil Methylsulfate	Drug Info	Approved	Peptic ulcer
6	Fesoterodine fumarate	Drug Info	Approved	Overactive bladder
7	Glycopyrrolate	Drug Info	Approved	Anaesthesia
8	Metixene	Drug Info	Approved	Parkinson disease
9	Oxyphenonium	Drug Info	Approved	Visceral spasms
10	Pirenzepine	Drug Info	Approved	Peptic ulcer
11	Propantheline	Drug Info	Approved	Stomach ulcer
12	Trihexyphenidyl	Drug Info	Approved	Dystonia
Clinical Trial Drug(s)	4 Clinical Trial Drugs				4
1	(S)-oxybutynin	Drug Info	Phase 2	Urinary incontinence
2	N-DESMETHYLCLOZAPINE	Drug Info	Phase 2	Schizoaffective disorder
3	Arecoline	Drug Info	Phase 1	Parkinson disease
4	B7-2/GM-CSF	Drug Info	Phase 1	Dementia
Discontinued Drug(s)	8 Discontinued Drugs				8
1	Telenzepine	Drug Info	Discontinued in Preregistration	Chronic obstructive pulmonary disease
2	Declopramide	Drug Info	Discontinued in Phase 2	Inflammatory bowel disease
3	YM-796	Drug Info	Discontinued in Phase 2	Cognitive impairment
4	PD-151832	Drug Info	Discontinued in Phase 1/2	Parkinson disease
5	SDZ-210-086	Drug Info	Discontinued in Phase 1	Cognitive impairment
6	TAZOMELINE	Drug Info	Discontinued in Phase 1	Cognitive impairment
7	AC-260584	Drug Info	Terminated	Schizophrenia
8	Alvameline	Drug Info	Terminated	Alzheimer disease
Investigative Drug(s)	1 Investigative Drug				1
1	BQCA	Drug Info	Investigative	Neurological disorder

Similar Protein(s) and Bioactivity Statistics

90% Identity

Protein ID	Protein Name	Protein Organism
PT01913	Muscarinic acetylcholine receptor M1	Rattus norvegicus, Rat	Protein Info
PT03415	Muscarinic acetylcholine receptor M1	Mus musculus, Mouse	Protein Info

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han