Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET07YRL)
Name
GPCR19 receptor (GPBAR1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
G-protein coupled bile acid receptor 1; BG37; G-protein coupled receptor GPCR19; M-BAR; Membrane-type receptor for bile acids; TGR5; hBG37; hGPCR19
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name GPBAR1 Gene ID
151306
UniProt ID GPBAR_HUMAN (click to find more protein-related data of this DBT)
TTD ID T86273 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN
Function
Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids. Receptor for bile acid.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Sodium desoxycholate 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; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 4390 nM (estimated based on the structural similarity with CHEMBL3391714 ) [1]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID GPBAR_HUMAN
References
1 Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. J Med Chem. 2008 Mar 27; 51(6):1831-41.

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