Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET06MMQ)
Name
Free fatty acid receptor 3 (FFAR3)
Synonyms    Click to Show/Hide the Synonyms of This DBT
G-protein coupled receptor 41; GPR41
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name FFAR3 Gene ID
2865
UniProt ID FFAR3_HUMAN (click to find more protein-related data of this DBT)
TTD ID T80513 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MDTGPDQSYFSGNHWFVFSVYLLTFLVGLPLNLLALVVFVGKLQRRPVAVDVLLLNLTAS
DLLLLLFLPFRMVEAANGMHWPLPFILCPLSGFIFFTTIYLTALFLAAVSIERFLSVAHP
LWYKTRPRLGQAGLVSVACWLLASAHCSVVYVIEFSGDISHSQGTNGTCYLEFRKDQLAI
LLPVRLEMAVVLFVVPLIITSYCYSRLVWILGRGGSHRRQRRVAGLLAATLLNFLVCFGP
YNVSHVVGYICGESPAWRIYVTLLSTLNSCVDPFVYYFSSSGFQADFHELLRRLCGLWGQ
WQQESSMELKEQKGGEEQRADRPAERKTSEHSQGCGTGGQVACAES
Function
G protein-coupled receptor that is activated by a major product of dietary fiber digestion, the short chain fatty acids (SCFAs), and that plays a role in the regulation of whole-body energy homeostasis and in intestinal immunity. In omnivorous mammals, the short chain fatty acids acetate, propionate and butyrate are produced primarily by the gut microbiome that metabolizes dietary fibers. SCFAs serve as a source of energy but also act as signaling molecules.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Acetic 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
Acidulant; Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 12000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR3_HUMAN
          DIG Name: Ethyl butyrate 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
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 10100 nM (estimated based on the structural similarity with CHEMBL62381 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.807692308
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR3_HUMAN
          DIG Name: Potassium 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
Film/membrane-forming agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 5000 nM (estimated based on the structural similarity with CHEMBL500826 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.789473684
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID FFAR3_RAT
          DIG Name: Sodium stearate 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; Gelling agent; Glidant; Modified-release agent; Stiffening agent; lubricant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 100000 nM (estimated based on the structural similarity with CHEMBL3925414 ) [3]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID FFAR3_RAT
          DIG Name: Acetic anhydride 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
Acidulant; Buffering agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 12000 nM (estimated based on the structural similarity with CHEMBL539 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.761904762
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR3_HUMAN
          DIG Name: Propionic 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
Acidulant; Antimicrobial preservative; Antioxidant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 10715.19 nM (tested by experiment) [4]
                   Tested Species Homo sapiens (Human)
                   UniProt ID FFAR3_HUMAN
References
1 Microbiota-Host Transgenomic Metabolism, Bioactive Molecules from the Inside. J Med Chem. 2018 Jan 11; 61(1):47-61.
2 Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists. ACS Med Chem Lett. 2016 Mar 30; 7(6):579-83.
3 WO patent application no. 2001061359A2, NOVEL ASSAY.
4 Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators. J Med Chem. 2020 Apr 9; 63(7):3577-3595.

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