Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

TTD Target ID: TTDS00177

Target Information
NameFatty-acid amide hydrolase    
Type of targetSuccessful target    
SynonymsAnandamide amidase    
Anandamide amidohydrolase    
Anandamide synthase    
Arachidonylethanolamide synthase    
FAAH    
Fatty acid amide hydrolase    
Oleamide hydrolase    
DiseaseAnalgesics    [1]
Anesthetic    [1]
Anxiety disorder, unspecified    [2]
Pain    [1]
Sedation    [1]
Drug(s)PropofolApprovedAnesthetic[3][1]
ThiopentalApprovedAnesthetic[1]
SSR411298Phase IIMajor Depressive Disorder,Depression[4]
BioChemical ClassHydrolases acting on carbon-nitrogen bonds    
EC NumberEC 3.5.1.4
UniProt IDO00519
FunctionDegrades 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.    
SequenceMVQYELWAALPGASGVALACCFVAAAVALRWSGRRTARGAVVRARQRQRAGLENMDRAAQ RFRLQNPDLDSEALLALPLPQLVQKLHSRELAPEAVLFTYVGKAWEVNKGTNCVTSYLAD CETQLSQAPRQGLLYGVPVSLKECFTYKGQDSTLGLSLNEGVPAECDSVVVHVLKLQGAV PFVHTNVPQSMFSYDCSNPLFGQTVNPWKSSKSPGGSSGGEGALIGSGGSPLGLGTDIGG SIRFPSSFCGICGLKPTGNRLSKSGLKGCVYGQEAVRLSVGPMARDVESLALCLRALLCE DMFRLDPTVPPLPFREEVYTSSQPLRVGYYETDNYTMPSPAMRRAVLETKQSLEAAGHTL VPFLPSNIPHALETLSTGGLFSDGGHTFLQNFKGDFVDPCLGDLVSILKLPQWLKGLLAF LVKPLLPRLSAFLSNMKSRSAGKLWELQHEIEVYRKTVIAQWRALDLDVVLTPMLAPALD LNAPGRATGAVSYTMLYNCLDFPAGVVPVTTVTAEDEAQMEHYRGYFGDIWDKMLQKGMK KSVGLPVAVQCVALPWQEELCLRFMREVERLMTPEKQSS
Related US Patent6,562,846
6,579,900
Target ValidationClick to Find Target Validation Information.    
Inhibitor1,4-bis (malimido)xylene[5]
1,8-bis-maleimidodiethyleneglycol[5]
1-DODECANOL[6]
2-arachidonoylglycerol[7]
2-fluorophenylboronic acid[8]
2-methoxyphenylboronic acid[8]
3-cyanophenylboronic acid[8]
3-methoxyphenylboronic acid[8]
4-cyanophenylboronic acid[8]
4-fluorophenylboronic acid[8]
4-methoxyphenylboronic acid[8]
4-nitrophenylboronic acid[8]
4-nonylphenylboronic acid[8]
6-fluoropyridin-3-ylboronic acid[8]
AM-404[9]
AMPEROZIDE[10]
AR-C70484XX[11]
ARACHIDONYL TRIFLUOROMETHYLKETONE[11]
BMS-1[12]
BTNP[13]
Benzylcarbamic Acid Biphenyl-3-yl Ester[14]
Biphenyl-3-ylcarbamic Acid Biphenyl-3-yl Ester[14]
Chlorphrifos oxon[15]
HTS-00798[16]
Isopropyl dodecylfluorophosphonate[15]
Isopropylcarbamic Acid Biphenyl-3-yl Ester[14]
JNJ-1661010[17]
LY-2183240[13]
LY-2318912[18]
Methoxy arachidonyl fluorophosphonate[19]
N- (2-hydroxyethyl)linoleoylamide[20]
N- (2-iodethyl)arachidonylamide[20]
N- (2-iodoethyl)linoleoylamide[20]
N-arachidonylmaleimide[5]
NICARBAZIN[10]
OL-135[21]
OL-92[12]
PARAOXON[15]
PF-622[22]
PHENMEDIPHAM[10]
Phenethylcarbamic Acid Biphenyl-3-yl Ester[14]
Phenylcarbamic Acid Biphenyl-3-yl Ester[14]
Propofol[3][1]
SSR411298[4]
Thiopental[1]
VER-156084[23]
VER-24052[23]
benzo[b]thiophen-2-ylboronic acid[8]
benzofuran-2-ylboronic acid[8]
biphenyl-3-ylboronic acid[8]
biphenyl-3-ylcarbamic acid cyclohexyl ester[5]
biphenyl-4-ylboronic acid[8]
isopropyl 4-nitrophenyl dodecylphosphonate[24]
n-Butylcarbamic Acid Biphenyl-3-yl Ester[14]
n-Hexylcarbamic Acid Biphenyl-3-yl Ester[14]
n-Octylcarbamic Acid Biphenyl-3-yl Ester[14]
naphthalen-2-yl cyclohexylcarbamate[13]
nicotinaldehyde O-4-butoxyphenylcarbamoyl oxime[25]
nicotinaldehyde O-4-ethoxyphenylcarbamoyl oxime[25]
nicotinaldehyde O-4-propoxyphenylcarbamoyl oxime[25]
octane-1-sulfonyl fluoride[24]
phenethylboronic acid[8]
phenyl 1- (4-butoxyphenyl)propylcarbamate[25]
phenyl 4- (decyloxy)phenylcarbamate[25]
phenyl 4- (dodecyloxy)phenylcarbamate[25]
phenyl 4- (heptyloxy)phenylcarbamate[25]
phenyl 4- (hexyloxy)phenylcarbamate[25]
phenyl 4- (octyloxy)phenylcarbamate[25]
phenyl 4- (undecyloxy)phenylcarbamate[25]
phenyl-1,4-bismaleimide[5]
phenylboronic acid[8]
pyridin-3-yl 4-butoxybenzylcarbamate[25]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The general anesthetic propofol increases brain N-arachidonylethanolamine (anandamide) content and inhibits fatty acid amide hydrolase. Br J Pharmacol. 2003 Jul;139(5):1005-13. To Reference
Ref 2Anandamide hydrolysis: a new target for anti-anxiety drugs? Trends Mol Med. 2003 Nov;9(11):474-8. To Reference
Ref 3Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17. To Reference
Ref 4Pharma & Vaccines. Product Development Pipeline. April 29 2009. To Reference
Ref 5J Med Chem. 2009 Dec 10;52(23):7410-20.Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors. To Reference
Ref 6Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 7Bioorg Med Chem Lett. 2007 Nov 1;17(21):5959-63. Epub 2007 Aug 21.Conformationally constrained analogues of 2-arachidonoylglycerol. To Reference
Ref 8J Med Chem. 2008 Nov 27;51(22):7057-60.Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase. To Reference
Ref 9J Med Chem. 2008 Dec 25;51(24):7800-5.New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide. To Reference
Ref 10Bioorg Med Chem Lett. 2009 Dec 1;19(23):6793-6. Epub 2009 Sep 30.Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors. To Reference
Ref 11Bioorg Med Chem. 2010 Jan 15;18(2):945-52. Epub 2009 Nov 17.1-Indol-1-yl-propan-2-ones and related heterocyclic compounds as dual inhibitors of cytosolic phospholipase A(2)alpha and fatty acid amide hydrolase. To Reference
Ref 12J Med Chem. 2009 Jan 8;52(1):170-80.Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors. To Reference
Ref 13J Med Chem. 2008 Dec 11;51(23):7327-43.Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors. To Reference
Ref 14J Med Chem. 2008 Jun 26;51(12):3487-98. Epub 2008 May 29.Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates. To Reference
Ref 15Nat Chem Biol. 2008 Jun;4(6):373-8. Epub 2008 Apr 27.Activation of the endocannabinoid system by organophosphorus nerve agents. To Reference
Ref 16J Med Chem. 2006 Jul 27;49(15):4650-6.Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system. To Reference
Ref 17Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. Epub 2008 Jul 25.Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. To Reference
Ref 18Eur J Med Chem. 2008 Jan;43(1):62-72. Epub 2007 Mar 19.Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation. To Reference
Ref 19Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 20Bioorg Med Chem. 2009 Jan 1;17(1):49-56. Epub 2008 Nov 17.Radiosynthesis, in vitro and in vivo evaluation of 123I-labeled anandamide analogues for mapping brain FAAH. To Reference
Ref 21J Med Chem. 2010 Jan 14;53(1):230-40.X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase. To Reference
Ref 22Bioorg Med Chem Lett. 2009 Dec 1;19(23):6806-9. Epub 2009 Oct 20.Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands. To Reference
Ref 23Bioorg Med Chem Lett. 2009 Aug 1;19(15):4241-4. Epub 2009 May 29.Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. To Reference
Ref 24Bioorg Med Chem Lett. 2008 Nov 15;18(22):5875-8. Epub 2008 Aug 6.Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels. To Reference
Ref 25Bioorg Med Chem Lett. 2010 Feb 1;20(3):1272-7. Epub 2009 Nov 24.Oxime carbamate--discovery of a series of novel FAAH inhibitors. To Reference



 

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