Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0SE3Y)
Name
Cannabinoid CB2 receptor (CNR2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Cannabinoid receptor 2; CB-2; CB2; CB2A; CB2B; CX5; hCB2; mCB2
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name CNR2 Gene ID
1269
UniProt ID CNR2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T37693 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MEECWVTEIANGSKDGLDSNPMKDYMILSGPQKTAVAVLCTLLGLLSALENVAVLYLILS
SHQLRRKPSYLFIGSLAGADFLASVVFACSFVNFHVFHGVDSKAVFLLKIGSVTMTFTAS
VGSLLLTAIDRYLCLRYPPSYKALLTRGRALVTLGIMWVLSALVSYLPLMGWTCCPRPCS
ELFPLIPNDYLLSWLLFIAFLFSGIIYTYGHVLWKAHQHVASLSGHQDRQVPGMARMRLD
VRLAKTLGLVLAVLLICWFPVLALMAHSLATTLSDQVKKAFAFCSMLCLINSMVNPVIYA
LRSGEIRSSAHHCLAHWKKCVRGLGSEAKEEAPRSSVTETEADGKITPWPDSRDLDLSDC
Function
May function in inflammatory response, nociceptive transmission and bone homeostasis. Heterotrimeric G protein-coupled receptor for endocannabinoid 2-arachidonoylglycerol mediating inhibition of adenylate cyclase.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Caryophyllene 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 Ki = 150 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CNR2_HUMAN
          DIG Name: FD&C blue no. 1 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 = 608.6 nM (estimated based on the structural similarity with CHEMBL2326294 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.805970149
                   Tested Species Homo sapiens (Human)
                   UniProt ID CNR2_HUMAN
          DIG Name: Light green CF yellowish 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 Ki = 4.3 nM (estimated based on the structural similarity with CHEMBL2326300 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.837037037
                   Tested Species Homo sapiens (Human)
                   UniProt ID CNR2_HUMAN
          DIG Name: Tricaprilin 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; Lubricant; Penetration agent; Plasticizing agent; Solubilizing agent; Solvent; Surfactant
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki > 1000 nM (estimated based on the structural similarity with CHEMBL26440 ) [3]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Homo sapiens (Human)
                   UniProt ID CNR2_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki > 1000 nM (estimated based on the structural similarity with CHEMBL26440 ) [3]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Mus musculus (Mouse)
                   UniProt ID CNR2_MOUSE
References
1 Medicinal properties of terpenes found in Cannabis sativa and Humulus lupulus. Eur J Med Chem. 2018 Sep 5; 157:198-228.
2 Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation. J Med Chem. 2013 Mar 14; 56(5):2045-58.
3 Assay and inhibition of diacylglycerol lipase activity. Bioorg Med Chem Lett. 2012 Jul 15; 22(14):4585-92.

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