General Information of the Protein
Protein ID
PT01913
Protein Name
Muscarinic acetylcholine receptor M1
Gene Name
CHRM1
Secondarily
Gene Name
Chrm-1
Sequence
MNTSVPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVNNYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLISFDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYIQFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSSSERSQPGAEGSPESPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEVVIKMPMVDSEAQAPTKQPPKSSPNTVKRPTKKGRDRGGKGQKPRGKEQLAKRKTFSLVKEKKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTVNPMCYALCNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
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Organism
Rattus norvegicus, Rat
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.
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Uniprot ID
P08482
Ensembl ID
ENSG00000168539
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
CP0055122
CAS_80880-90-6
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C19H22N4O2S
 1
1
Ki = 1.8 nM
   TI
   LI
   LO
   TS
CP0453946
11-{2-[4-(10-Diethylamino-decyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
   Show/Hide
C32H48N6O2
 1
1
Ki = 3 nM
   TI
   LI
   LO
   TS
CP0409457
11-(2-{4-[10-(2-Methoxy-benzylamino)-decyl]-piperazin-1-yl}-acetyl)-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C36H48N6O3
 1
1
Ki = 3.3 nM
   TI
   LI
   LO
   TS
CP0408848
11-{2-[4-(10-Amino-decyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C28H40N6O2
 1
1
Ki = 15.8 nM
   TI
   LI
   LO
   TS
CP0471999
2-(6-{4-[2-Oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-hexyl)-isoindole-1,3-dione
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C32H34N6O4
 1
1
Ki = 18 nM
   TI
   LI
   LO
   TS
CP0453431
11-{2-[4-(8-Amino-octyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C26H36N6O2
 1
1
Ki = 20 nM
   TI
   LI
   LO
   TS
CP0437473
11-{2-[4-(9-Amino-nonyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C27H38N6O2
 1
1
Ki = 24 nM
   TI
   LI
   LO
   TS
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
 1
1
Ki = 29 nM
   TI
   LI
   LO
   TS
CP0384751
(6-{4-[2-Oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-hexyl)-carbamic acid tert-butyl ester
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C29H40N6O4
 1
1
Ki = 37.1 nM
   TI
   LI
   LO
   TS
CP0402507
N-[9-[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]nonyl]acetamide
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C29H40N6O3
 1
1
Ki = 52 nM
   TI
   LI
   LO
   TS
CP0406343
11-{2-[4-(2-Chloro-ethyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C20H22ClN5O2
 1
1
Ki = 52 nM
   TI
   LI
   LO
   TS
CP0430186
2-(5-{4-[2-Oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-pentyl)-isoindole-1,3-dione
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C31H32N6O4
 1
1
Ki = 60 nM
   TI
   LI
   LO
   TS
CP0427214
11-{2-[4-(7-Amino-heptyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C25H34N6O2
 1
1
Ki = 66 nM
   TI
   LI
   LO
   TS
CP0409620
N-[10-[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]decyl]acetamide
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C30H42N6O3
 1
1
Ki = 75 nM
   TI
   LI
   LO
   TS
CP0508633
2-(4-{4-[2-Oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-butyl)-isoindole-1,3-dione
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C30H30N6O4
 1
1
Ki = 170 nM
   TI
   LI
   LO
   TS
CP0440213
11-[2-(4-Benzyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C25H25N5O2
 1
1
Ki = 330 nM
   TI
   LI
   LO
   TS
CP0406182
2-(2-piperazin-1-ylacetyl)-2,4,9,15-tetrazatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-10-one
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C17H18N6O2
 1
1
Ki = 370 nM
   TI
   LI
   LO
   TS
CP0402515
N-[2-[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]ethyl]acetamide
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C22H26N6O3
 1
1
Ki = 670 nM
   TI
   LI
   LO
   TS
CP0457427
11-{2-[4-(5-Amino-pentyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C23H30N6O2
 1
1
Ki = 1170 nM
   TI
   LI
   LO
   TS
CP0457434
11-{2-[4-(2-Amino-ethyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C20H24N6O2
 1
1
Ki = 1190 nM
   TI
   LI
   LO
   TS
CP0430187
11-{2-[4-(6-Amino-hexyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C24H32N6O2
 1
1
Ki = 1310 nM
   TI
   LI
   LO
   TS
CP0402503
N-(2-aminoethyl)-4-[[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]methyl]benzamide
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C28H31N7O3
 1
1
Ki = 1390 nM
   TI
   LI
   LO
   TS
CP0441785
11-[2-(4-Prop-2-ynyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C21H21N5O2
 1
1
Ki = 1670 nM
   TI
   LI
   LO
   TS
CP0403862
tert-butyl N-[4-[[4-[[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]methyl]benzoyl]amino]butyl]carbamate
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C35H43N7O5
 1
1
Ki = 1680 nM
   TI
   LI
   LO
   TS
CP0384753
2-(3-{4-[2-Oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-propyl)-isoindole-1,3-dione
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C29H28N6O4
 1
1
Ki = 1810 nM
   TI
   LI
   LO
   TS
CP0403763
N-methyl-4-[[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]methyl]benzamide
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C27H28N6O3
 1
1
Ki = 2840 nM
   TI
   LI
   LO
   TS
CP0437410
11-{2-[4-(4-Amino-butyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C22H28N6O2
 1
1
Ki = 3080 nM
   TI
   LI
   LO
   TS
CP0453207
11-{2-[4-(3-Amino-propyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C21H26N6O2
 1
1
Ki = 3870 nM
   TI
   LI
   LO
   TS
CP0427347
3-Amino-N-(2-{4-[2-oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-ethyl)-propionamide
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C23H29N7O3
 1
1
Ki = 4340 nM
   TI
   LI
   LO
   TS
CP0453131
9-Hydroxymethyl-11-[2-(4-methyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C20H23N5O3
 1
1
Ki = 4400 nM
   TI
   LI
   LO
   TS
CP0455134
11-[2-(4-Methyl-piperazin-1-yl)-acetyl]-8-methylsulfanyl-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C20H23N5O2S
 1
1
Ki = 4660 nM
   TI
   LI
   LO
   TS
CP0493507
tert-butyl N-[4-oxo-4-[2-[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]ethylamino]butyl]carbamate
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C29H39N7O5
 1
1
Ki = 4800 nM
   TI
   LI
   LO
   TS
CP0402490
11-{2-[4-(2-Hydroxy-ethyl)-piperazin-1-yl]-acetyl}-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C20H23N5O3
 1
1
Ki = 5800 nM
   TI
   LI
   LO
   TS
CP0453230
5-Ethyl-11-[2-(4-methyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
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C21H25N5O2
 1
1
Ki = 7700 nM
   TI
   LI
   LO
   TS
CP0448531
7-{11-[2-(4-Methyl-piperazin-1-yl)-acetyl]-6-oxo-6,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-5-yl}-heptanenitrile
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C26H32N6O2
 1
1
Ki = 8900 nM
   TI
   LI
   LO
   TS
CP0399996
4-Amino-N-(2-{4-[2-oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-ethyl)-butyramide
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C24H31N7O3
 1
1
Ki = 9530 nM
   TI
   LI
   LO
   TS
CP0391379
4-Acetylamino-N-(2-{4-[2-oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-ethyl)-butyramide
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C26H33N7O4
 1
1
Ki = 9650 nM
   TI
   LI
   LO
   TS
CP0504150
tert-butyl N-[3-oxo-3-[2-[4-[2-oxo-2-(6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]piperazin-1-yl]ethylamino]propyl]carbamate
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C28H37N7O5
 1
1
Ki = 13300 nM
   TI
   LI
   LO
   TS
CP0416042
(2-{11-[2-(4-Methyl-piperazin-1-yl)-acetyl]-6-oxo-6,11-dihydro-5H-benzo[e]pyrido[3,2-b][1,4]diazepine-8-sulfonylamino}-ethyl)-carbamic acid tert-butyl ester
   Show/Hide
C26H35N7O6S
 1
1
Ki > 30000 nM
   TI
   LI
   LO
   TS
CP0453537
11-[2-(4-Methyl-piperazin-1-yl)-acetyl]-6-oxo-6,11-dihydro-5H-benzo[e]pyrido[3,2-b][1,4]diazepine-8-sulfonic acid (2-amino-ethyl)-amide
   Show/Hide
C21H27N7O4S
 1
1
Ki > 30000 nM
   TI
   LI
   LO
   TS
CP0462831
N-[2-[[11-[2-(4-methylpiperazin-1-yl)acetyl]-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepin-8-yl]sulfonylamino]ethyl]acetamide
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C23H29N7O5S
 1
1
Ki > 30000 nM
   TI
   LI
   LO
   TS
CP0524164
11-[2-(4-Methyl-piperazin-1-yl)-acetyl]-6-oxo-6,11-dihydro-5H-benzo[e]pyrido[3,2-b][1,4]diazepine-8-sulfonic acid amide
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C19H22N6O4S
 1
1
Ki > 30000 nM
   TI
   LI
   LO
   TS
CP0472255
9-(tert-Butyl-dimethyl-silanyloxymethyl)-11-[2-(4-methyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
   Show/Hide
C26H37N5O3Si
 1
1
Ki > 30000 nM
   TI
   LI
   LO
   TS
CP0403855
3-Acetylamino-N-(2-{4-[2-oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazin-1-yl}-ethyl)-propionamide
   Show/Hide
C25H31N7O4
 1
1
Ki = 39400 nM
   TI
   LI
   LO
   TS
CP0427351
4-[2-Oxo-2-(6-oxo-5,6-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-11-yl)-ethyl]-piperazine-1-carbothioic acid phenylamide
   Show/Hide
C25H24N6O2S
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0436010
11-[2-(4-Acetyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
   Show/Hide
C20H21N5O3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0490155
11-[2-(4-Benzoyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
   Show/Hide
C25H23N5O3
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
CP0497274
11-[2-(4-Methanesulfonyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
   Show/Hide
C19H21N5O4S
 1
1
Ki > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0020189
6-acetoxy-8-azonia-bicyclo[3.2.1]octane
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C9H15NO2
 2
1 Ki = 5.6 nM
2 Ki = 22000 nM
CP0056034
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 = 6.457 nM
CP0054630
((2S,4R,5S)-4-Hydroxy-5-methyl-tetrahydro-furan-2-ylmethyl)-trimethyl-ammonium
   Show/Hide
C9H20NO2+
 1
1 Ki = 27 nM
CP0635477
(2-Carbamoyloxy-ethyl)-trimethyl-ammonium chloride
   Show/Hide
C6H15ClN2O2
 1
1 Ki = 31 nM
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01310 Muscarinic acetylcholine receptor M1 Homo sapiens, Human
PT03415 Muscarinic acetylcholine receptor M1 Mus musculus, Mouse