Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET04FGC)
Name
Opioid receptor mu (OPRM1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Mu opiate receptor; Mu opioid receptor; Mu-type opioid receptor; M-OR-1; MOP; MOR-1; MOR1; MOR1A; hMOP
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name OPRM1 Gene ID
4988
UniProt ID OPRM_HUMAN (click to find more protein-related data of this DBT)
TTD ID T47768 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MDSSAAPTNASNCTDALAYSSCSPAPSPGSWVNLSHLDGNLSDPCGPNRTDLGGRDSLCP
PTGSPSMITAITIMALYSIVCVVGLFGNFLVMYVIVRYTKMKTATNIYIFNLALADALAT
STLPFQSVNYLMGTWPFGTILCKIVISIDYYNMFTSIFTLCTMSVDRYIAVCHPVKALDF
RTPRNAKIINVCNWILSSAIGLPVMFMATTKYRQGSIDCTLTFSHPTWYWENLLKICVFI
FAFIMPVLIITVCYGLMILRLKSVRMLSGSKEKDRNLRRITRMVLVVVAVFIVCWTPIHI
YVIIKALVTIPETTFQTVSWHFCIALGYTNSCLNPVLYAFLDENFKRCFREFCIPTSSNI
EQQNSTRIRQNTRDHPSTANTVDRTNHQLENLEAETAPLP
Function
Receptor for natural and synthetic opioids including morphine, heroin, DAMGO, fentanyl, etorphine, buprenorphin and methadone. Agonist binding to the receptor induces coupling to an inactive GDP-bound heterotrimeric G-protein complex and subsequent exchange of GDP for GTP in the G-protein alpha subunit leading to dissociation of the G-protein complex with the free GTP-bound G-protein alpha and the G-protein beta-gamma dimer activating downstream cellular effectors.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          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 IC50 = 5.1 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_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 IC50 = 0.8 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_HUMAN
          DIG Name: Hydrazine yellow 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 = 16 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_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 for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 6 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_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 = 6.2 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_HUMAN
          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 IC50 = 3.8 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_HUMAN
          DIG Name: Simethicone 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
Antifoaming agent; Diluent; Water-repelling agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1.5 nM (estimated based on the structural similarity with CHEMBL1707 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.942028986
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_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 IC50 = 27 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_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 for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.6 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID OPRM_HUMAN
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J Med Chem. 2001 Oct 11; 44(21):3378-90.

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