Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0T2VY)
Name
Oleamide hydrolase 1 (FAAH)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Anandamide amidohydrolase 1; Fatty-acid amide hydrolase 1; FAAH; FAAH1; Fatty acid ester hydrolase
Family Hydrolase (HDase)  >>  Ester bond hydrolase (EC 3.1)
Organism
Homo sapiens (Human)
Gene Name FAAH1 Gene ID
2166
UniProt ID FAAH1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T34389 (click to find more therapeutic target data of this DBT)
INTEDE ID DME0208 (click to find more drug-metabolizing enzyme data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MVQYELWAALPGASGVALACCFVAAAVALRWSGRRTARGAVVRARQRQRAGLENMDRAAQ
RFRLQNPDLDSEALLALPLPQLVQKLHSRELAPEAVLFTYVGKAWEVNKGTNCVTSYLAD
CETQLSQAPRQGLLYGVPVSLKECFTYKGQDSTLGLSLNEGVPAECDSVVVHVLKLQGAV
PFVHTNVPQSMFSYDCSNPLFGQTVNPWKSSKSPGGSSGGEGALIGSGGSPLGLGTDIGG
SIRFPSSFCGICGLKPTGNRLSKSGLKGCVYGQEAVRLSVGPMARDVESLALCLRALLCE
DMFRLDPTVPPLPFREEVYTSSQPLRVGYYETDNYTMPSPAMRRAVLETKQSLEAAGHTL
VPFLPSNIPHALETLSTGGLFSDGGHTFLQNFKGDFVDPCLGDLVSILKLPQWLKGLLAF
LVKPLLPRLSAFLSNMKSRSAGKLWELQHEIEVYRKTVIAQWRALDLDVVLTPMLAPALD
LNAPGRATGAVSYTMLYNCLDFPAGVVPVTTVTAEDEAQMEHYRGYFGDIWDKMLQKGMK
KSVGLPVAVQCVALPWQEELCLRFMREVERLMTPEKQSS
Function
Hydrolyzes polyunsaturated substrate anandamide preferentially as compared to monounsaturated substrates. Degrades bioactive fatty acid amides like oleamide, the endogenous cannabinoid, anandamide and myristic amide to their corresponding acids, thereby serving to terminate the signaling functions of these molecules.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Entsufon 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
Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 256 nM (estimated based on the structural similarity with CHEMBL3683959 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.867768595
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID FAAH1_RAT
          DIG Name: Niacinamide 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; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 3300 nM (tested by experiment) [2]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID FAAH1_RAT
          DIG Name: Stearamidoethyl diethylamine 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 = 3548.13 nM (estimated based on the structural similarity with CHEMBL32886 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.923076923
                   Tested Species Homo sapiens (Human)
                   UniProt ID FAAH1_HUMAN
          DIG Name: Triolein 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
Complexing agent; Microencapsulating agent; Modified-release agent; Solubilizing agent; Tonicity agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 11000 nM (estimated based on the structural similarity with CHEMBL230967 ) [4]
                   Structural Similarity Tanimoto coefficient = 0.93442623
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID FAAH1_RAT
References
1 US patent application no. 9102622B2, FATTY ACID AMIDE HYDROLASE INHIBITORS.
2 Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system. J Med Chem. 2006 Jul 27; 49(15):4650-6.
3 Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors. J Med Chem. 2008 Dec 11; 51(23):7327-43.
4 Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase. J Med Chem. 2007 Oct 4; 50(20):5012-23.

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