Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0B6AO)
Name
Muscarinic receptor M1 (ACM1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Muscarinic acetylcholine receptor M1; Cholinergic receptor, muscarinic 1; M1R; M1 receptor; CHRM1; Chrm1; Cholinergic/acetylcholine receptor M1
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name CHRM1 Gene ID
1128
UniProt ID ACM1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T28893 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MNTSAPPAVSPNITVLAPGKGPWQVAFIGITTGLLSLATVTGNLLVLISFKVNTELKTVN
NYFLLSLACADLIIGTFSMNLYTTYLLMGHWALGTLACDLWLALDYVASNASVMNLLLIS
FDRYFSVTRPLSYRAKRTPRRAALMIGLAWLVSFVLWAPAILFWQYLVGERTVLAGQCYI
QFLSQPIITFGTAMAAFYLPVTVMCTLYWRIYRETENRARELAALQGSETPGKGGGSSSS
SERSQPGAEGSPETPPGRCCRCCRAPRLLQAYSWKEEEEEDEGSMESLTSSEGEEPGSEV
VIKMPMVDPEAQAPTKQPPRSSPNTVKRPTKKGRDRAGKGQKPRGKEQLAKRKTFSLVKE
KKAARTLSAILLAFILTWTPYNIMVLVSTFCKDCVPETLWELGYWLCYVNSTINPMCYAL
CNKAFRDTFRLLLLCRWDKRRWRKIPKRPGSVHRTPSRQC
Function
Primary transducing effect is Pi turnover. 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.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Butylparaben Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 12 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Cetylpyridinium chloride Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative; Penetration agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 18 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: D&C red no. 28 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 > 1 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Oleic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 13 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Propyl 4-hydroxybenzoate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 23 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Sodium lauryl sulfate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 29 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Benzethonium chloride Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 > 10 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1.8 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Chloroxylenol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 9.9 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Methylene blue Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 6.3 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Methylpyrrolidone Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Penetration agent; Solubilizing agent; Solvent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 7400 nM (estimated based on the structural similarity with CHEMBL23957 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.87804878
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 700 nM (estimated based on the structural similarity with CHEMBL23957 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.87804878
                   Tested Species Mus musculus (Mouse)
                   UniProt ID ACM1_MOUSE
          DIG Name: Phenylmercuric acetate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 8.1 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Thimerosal Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 30 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Thymol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antioxidant; Flavoring agent; Penetration agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 14 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Butylhydroxyanisole Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative; Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 19 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: FD&C red no. 3 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Colorant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 > 0.3 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 > 0.1 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Polysorbate 80 Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 2.6 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
          DIG Name: Cocomonoethanolamide Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Other agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 18 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM1_HUMAN
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors. Bioorg Med Chem. 2011 Feb 1; 19(3):1048-54.
3 Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists. J Med Chem. 1997 Apr 11; 40(8):1230-46.

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