Target Information

Target General Infomation
Target ID
T11754
Former ID
TTDS00177
Target Name
Fatty-acid amide hydrolase
Gene Name
FAAH
Synonyms
Anandamide amidase; Anandamide amidohydrolase; Anandamide synthase; Arachidonylethanolamide synthase; Fatty acid amide hydrolase; Oleamidehydrolase; FAAH
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Anesthesia [ICD9: 338; ICD10: R20.0]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Liver disease [ICD9: 570-574; ICD10: K70-K77]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Neuropathic pain [ICD9: 356.0, 356.8; ICD10: G64, G90.0]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Unspecified [ICD code not available]
Function
Degradesbioactive 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. Hydrolyzes polyunsaturated substrate anandamide preferentially as compared to monounsaturated substrates.
BioChemical Class
Carbon-nitrogen hydrolase
Target Validation
T11754
UniProt ID
O00519
EC Number
EC 3.5.1.99
Sequence
MVQYELWAALPGASGVALACCFVAAAVALRWSGRRTARGAVVRARQRQRAGLENMDRAAQ
RFRLQNPDLDSEALLALPLPQLVQKLHSRELAPEAVLFTYVGKAWEVNKGTNCVTSYLAD
CETQLSQAPRQGLLYGVPVSLKECFTYKGQDSTLGLSLNEGVPAECDSVVVHVLKLQGAV
PFVHTNVPQSMFSYDCSNPLFGQTVNPWKSSKSPGGSSGGEGALIGSGGSPLGLGTDIGG
SIRFPSSFCGICGLKPTGNRLSKSGLKGCVYGQEAVRLSVGPMARDVESLALCLRALLCE
DMFRLDPTVPPLPFREEVYTSSQPLRVGYYETDNYTMPSPAMRRAVLETKQSLEAAGHTL
VPFLPSNIPHALETLSTGGLFSDGGHTFLQNFKGDFVDPCLGDLVSILKLPQWLKGLLAF
LVKPLLPRLSAFLSNMKSRSAGKLWELQHEIEVYRKTVIAQWRALDLDVVLTPMLAPALD
LNAPGRATGAVSYTMLYNCLDFPAGVVPVTTVTAEDEAQMEHYRGYFGDIWDKMLQKGMK
KSVGLPVAVQCVALPWQEELCLRFMREVERLMTPEKQSS
Drugs and Mode of Action
Drug(s) Propofol Drug Info Approved Anesthesia [1], [2]
Thiopental Drug Info Approved Anesthesia [3], [4]
IW-6118 Drug Info Phase 2 Inflammatory disease [5]
PF-04457845 Drug Info Phase 2 Liver disease [6]
SSR411298 Drug Info Phase 2 Major depressive disorder [7]
IPI-940 Drug Info Phase 1 Pain [8]
Propofol Drug Info Investigative Unspecified [9], [10]
Inhibitor (+/-)-3-(but-3-enyl)-1-pent-4-enoylazetidin-2-one Drug Info [11]
(+/-)-3-(pent-4-enyl)azetidin-2-one Drug Info [11]
(+/-)-3-allyl-1-pent-4-enoylazetidin-2-one Drug Info [11]
(+/-)-3-allylazetidin-2-one Drug Info [11]
(+/-)-oxiran-2-ylmethyl (9Z)-hexadec-9-enoate Drug Info [12]
(+/-)-oxiran-2-ylmethyl (9Z)-octadec-9-enoate Drug Info [12]
(Z)-1,1,1-Trifluoro-nonadec-10-en-2-one Drug Info [13]
(Z)-1-(4-phenyloxazol-2-yl)octadec-9-en-1-one Drug Info [14]
(Z)-1-(benzo[d]oxazol-2-yl)octadec-9-en-1-one Drug Info [14]
(Z)-1-(pyridazin-3-yl)octadec-9-en-1-one Drug Info [14]
(Z)-2,2-Dimethyl-1-oxazol-2-yl-octadec-9-en-1-one Drug Info [15]
(Z)-2-Methyl-1-oxazol-2-yl-octadec-9-en-1-one Drug Info [15]
1,1,1-trifluoro-3-(hexylthio)propan-2-one Drug Info [16]
1,1,1-trifluoro-3-(octylsulfinyl)propan-2-one Drug Info [16]
1,1,1-trifluoro-3-(octylsulfonyl)propan-2-one Drug Info [16]
1,1,1-trifluoro-3-(octylthio)propan-2-one Drug Info [16]
1,1,1-Trifluoro-7-phenylheptan-2-one Drug Info [13]
1,1,1-Trifluoro-8-phenyl-octan-2-one Drug Info [13]
1,1,1-Trifluoro-9-phenyl-nonan-2-one Drug Info [13]
1,1,1-Trifluoro-nonadecan-2-one Drug Info [13]
1,1,1-Trifluoro-tridecan-2-one Drug Info [13]
1,1,1-Trifluoro-undecan-2-one Drug Info [13]
1,1,1-trifluorododecan-2-one Drug Info [16]
1,10-(methylenedi-4,1-phenylene)bismaleimide Drug Info [17]
1,4-bis(malimido)xylene Drug Info [17]
1,8-bis-maleimidodiethyleneglycol Drug Info [17]
1-(1,2,4-Oxadiazol-3-yl)-7-phenylheptan-1-one Drug Info [18]
1-(1,2,4-Oxadiazol-5-yl)-7-phenylheptan-1-one Drug Info [18]
1-(1,3,4-Oxadiazol-2-yl)-7-phenylheptan-1-one Drug Info [18]
1-(1,3,4-oxadiazol-2-yl)octadec-9-en-1-one Drug Info [18]
1-(1,3,4-thiadiazol-2-yl)octadec-9-en-1-one Drug Info [18]
1-(4-acetyloxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(4-bromooxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(4-chlorooxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(4-iodooxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(4-methoxyoxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(4-methyloxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(5-(furan-2-yl)oxazol-2-yl)octadec-9-en-1-one Drug Info [18]
1-(5-(pyridin-2-yl)oxazol-2-yl)dodecan-1-one Drug Info [14]
1-(5-(pyridin-2-yl)oxazol-2-yl)octadec-9-en-1-one Drug Info [18]
1-(5-(pyridin-2-yl)oxazol-2-yl)octan-1-one Drug Info [14]
1-(5-(pyridin-2-yl)oxazol-2-yl)pentan-1-one Drug Info [14]
1-(5-fluorooxazol-2-yl)-7-phenylheptan-1-one Drug Info [14]
1-(5-methyloxazol-2-yl)-7-phenylheptan-1-one Drug Info [14]
1-(5-phenyloxazol-2-yl)octadec-9-en-1-one Drug Info [18]
1-(5-Pyridin-2-yl-oxazol-2-yl)-octadec-9-yn-1-one Drug Info [13]
1-(oxazol-2-yl)-3-(4-phenoxyphenyl)propan-1-one Drug Info [20]
1-(oxazol-2-yl)-4-(piperidin-4-yl)butan-1-one Drug Info [21]
1-(oxazol-2-yl)-7-phenylheptan-1-one Drug Info [19]
1-(oxazol-2-yl)octadec-9-en-1-one Drug Info [18]
1-(oxazolo[4,5-b]pyridin-2-yl)dodecan-1-one Drug Info [14]
1-(oxazolo[4,5-b]pyridin-2-yl)octan-1-one Drug Info [14]
1-(oxazolo[4,5-b]pyridin-2-yl)pentan-1-one Drug Info [14]
1-Benzooxazol-2-yl-6-phenyl-hexan-1-one Drug Info [13]
1-Biphenyl-4-ylmaleimide Drug Info [17]
1-Biphenyl-4-ylmethylmaleimide Drug Info [17]
1-DODECANOL Drug Info [22]
1-Imidazol-1-yl-3-(4-octylphenoxy)propan-2-one Drug Info [23]
1-Oxazolo[4,5-b]pyridin-2-yl-6-phenyl-hexan-1-one Drug Info [24]
1-Oxazolo[4,5-b]pyridin-2-yl-octadec-9-yn-1-one Drug Info [13]
2,2-dimethyl-3-methyleneheptadecane Drug Info [16]
2,4-difluorophenyl 4-butoxybenzylcarbamate Drug Info [25]
2-(7-phenylheptanoyl)oxazole-4-carbaldehyde Drug Info [19]
2-(7-phenylheptanoyl)oxazole-4-carbonitrile Drug Info [19]
2-(7-phenylheptanoyl)oxazole-4-carboxamide Drug Info [19]
2-(7-phenylheptanoyl)oxazole-4-carboxylic acid Drug Info [19]
2-(7-phenylheptanoyl)oxazole-5-carbonitrile Drug Info [19]
2-(7-phenylheptanoyl)oxazole-5-carboxylic acid Drug Info [19]
2-(biphenyl-4-yl)vinylboronic acid Drug Info [26]
2-arachidonoylglycerol Drug Info [27]
2-chloro-1-(5-(pyridin-2-yl)oxazol-2-yl)ethanone Drug Info [28]
2-Cyclohexylacetic acidbiphenyl-3-yl ester Drug Info [29]
2-fluorophenyl 1-(4-butoxyphenyl)propylcarbamate Drug Info [25]
2-fluorophenyl 4'-ethylbiphenyl-4-ylcarbamate Drug Info [25]
2-fluorophenyl 4-(decyloxy)phenylcarbamate Drug Info [25]
2-fluorophenyl 4-(dodecyloxy)phenylcarbamate Drug Info [25]
2-fluorophenyl 4-(heptyloxy)phenylcarbamate Drug Info [25]
2-fluorophenyl 4-(hexyloxy)phenylcarbamate Drug Info [25]
2-fluorophenyl 4-(octyloxy)phenylcarbamate Drug Info [25]
2-fluorophenyl 4-(undecyloxy)phenylcarbamate Drug Info [25]
2-fluorophenyl 4-butoxybenzylcarbamate Drug Info [25]
2-fluorophenyl 4-butoxyphenylcarbamate Drug Info [25]
2-fluorophenyl 4-phenoxyphenylcarbamate Drug Info [25]
2-fluorophenylboronic acid Drug Info [26]
2-methoxyphenylboronic acid Drug Info [26]
3'-carbamoylbiphenyl-3-yl 6-phenylhexylcarbamate Drug Info [30]
3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate Drug Info [23]
3,3-di(pent-4-enyl)azetidin-2-one Drug Info [11]
3-(4,5-Dihydrooxazol-2-yl)phenyl propylcarbamate Drug Info [31]
3-(benzo[d]oxazol-2-yl)phenyl propylcarbamate Drug Info [31]
3-(biphenyl-4-yl)-1-(oxazol-2-yl)propan-1-one Drug Info [20]
3-(decylsulfinyl)-1,1,1-trifluoropropan-2-one Drug Info [16]
3-(decylsulfonyl)-1,1,1-trifluoropropan-2-one Drug Info [16]
3-(decylthio)-1,1,1-trifluoropropan-2-one Drug Info [16]
3-(dodecylsulfinyl)-1,1,1-trifluoropropan-2-one Drug Info [16]
3-(dodecylsulfonyl)-1,1,1-trifluoropropan-2-one Drug Info [16]
3-(ethoxycarbonyl)phenylboronic acid Drug Info [26]
3-(trifluoromethyl)phenyl 4-butoxybenzylcarbamate Drug Info [25]
3-(trifluoromethyl)phenylboronic acid Drug Info [26]
3-chlorophenyl 4-butoxybenzylcarbamate Drug Info [25]
3-cyanophenylboronic acid Drug Info [26]
3-methoxyphenylboronic acid Drug Info [26]
4-(1,2,3-thiadiazol-4-yl)phenyl butylcarbamate Drug Info [32]
4-(1,2,3-thiadiazol-4-yl)phenyl hexylcarbamate Drug Info [32]
4-(4,5-dihydrothiazol-2-yl)phenyl butylcarbamate Drug Info [32]
4-(cyclohexylmethylcarbamoyloxy)benzoic acid Drug Info [30]
4-(thiazol-2-yl)phenyl butylcarbamate Drug Info [33]
4-(trifluoromethyl)phenylboronic acid Drug Info [26]
4-cyanophenyl ethyl dodecylphosphonate Drug Info [34]
4-cyanophenylboronic acid Drug Info [26]
4-fluorophenyl 1-(4-butoxyphenyl)propylcarbamate Drug Info [25]
4-fluorophenyl 4-butoxybenzylcarbamate Drug Info [25]
4-fluorophenylboronic acid Drug Info [26]
4-methoxyphenyl 1-(4-butoxyphenyl)propylcarbamate Drug Info [25]
4-methoxyphenylboronic acid Drug Info [26]
4-Nitrophenyl 4-Benzylpiperazine-1-carboxylate Drug Info [35]
4-nitrophenylboronic acid Drug Info [26]
4-nonylphenylboronic acid Drug Info [26]
4-Phenylbutylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
6-fluoropyridin-3-ylboronic acid Drug Info [26]
6-Phenylhexylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
7-Phenyl-1-(1,3,4-thiadiazol-2-yl)-heptan-1-one Drug Info [18]
7-Phenyl-1-(2H-tetrazol-5-yl)-heptan-1-one Drug Info [18]
7-phenyl-1-(4-phenyloxazol-2-yl)heptan-1-one Drug Info [19]
7-phenyl-1-(5-phenyloxazol-2-yl)heptan-1-one Drug Info [18]
7-Phenyl-1-(pyridazin-3-yl)-heptan-1-one Drug Info [18]
7-Phenyl-1-(thiazol-2-yl)-heptan-1-one Drug Info [18]
8-Phenyloctylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Adamant-1-ylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Allylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
AM-404 Drug Info [36]
AR-C70484XX Drug Info [23]
ARACHIDONYL TRIFLUOROMETHYLKETONE Drug Info [23]
Benzaldehyde O-4-(decyloxy)phenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-(heptyloxy)phenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-(hexyloxy)phenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-(nonyloxy)phenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-(octyloxy)phenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-(pentyloxy)phenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-butoxyphenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-ethoxyphenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-methoxyphenylcarbamoyl oxime Drug Info [25]
Benzaldehyde O-4-propoxyphenylcarbamoyl oxime Drug Info [25]
Benzofuran-2-ylboronic acid Drug Info [26]
Benzo[b]thiophen-2-ylboronic acid Drug Info [26]
Benzylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Biphenyl-3-ylboronic acid Drug Info [26]
Biphenyl-3-ylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Biphenyl-3-ylcarbamic acid cyclohexyl ester Drug Info [17]
Biphenyl-4-ylboronic acid Drug Info [26]
BMS-1 Drug Info [37]
BTNP Drug Info [30]
Chlorphrifos oxon Drug Info [38]
Cyclobutylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Cyclohexyl biphenyl-4-ylcarbamate Drug Info [32]
Cyclohexylcarbamic acidbiphenyl-3-yl ester Drug Info [29]
Cyclohexylmethylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Cyclopentyl(5-(pyridin-2-yl)oxazol-2-yl)methanone Drug Info [28]
Cyclopentylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Dodecane-1-sulfonyl fluoride Drug Info [34]
Ethyl octylfluorophosphonate Drug Info [38]
Fatty acid amide hydrolase inhibitors Drug Info [39]
Furan-2-ylmethylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
HTS-00798 Drug Info [33]
Indan-2-ylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
IPI-940 Drug Info [39]
Isopropyl 4-nitrophenyl dodecylphosphonate Drug Info [34]
Isopropyl dodecylfluorophosphonate Drug Info [38]
Isopropylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
JNJ-1661010 Drug Info [40]
LY-2183240 Drug Info [30]
LY-2318912 Drug Info [41]
Methoxy arachidonyl fluorophosphonate Drug Info [42]
Methyl 2-(7-phenylheptanoyl)oxazole-4-carboxylate Drug Info [19]
Methyl 2-(7-phenylheptanoyl)oxazole-5-carboxylate Drug Info [18]
Methyl icosylphosphonofluoridate Drug Info [34]
Methylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
N-(2-hydroxyethyl)linoleoylamide Drug Info [43]
N-(2-iodethyl)arachidonylamide Drug Info [43]
N-(2-iodoethyl)linoleoylamide Drug Info [43]
N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide Drug Info [36]
N-arachidonylmaleimide Drug Info [17]
N-Butylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
N-Hexylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
N-Octylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Naphthalen-2-yl cyclohexylcarbamate Drug Info [30]
NICARBAZIN Drug Info [44]
Nicotinaldehyde O-4-butoxyphenylcarbamoyl oxime Drug Info [25]
Nicotinaldehyde O-4-ethoxyphenylcarbamoyl oxime Drug Info [25]
Nicotinaldehyde O-4-propoxyphenylcarbamoyl oxime Drug Info [25]
Octane-1-sulfonyl fluoride Drug Info [34]
OL-135 Drug Info [45]
OL-92 Drug Info [37]
Org-231295 Drug Info [39]
PARAOXON Drug Info [38]
PF-04457845 Drug Info [46]
PF3845 Drug Info [47]
PF750 Drug Info [48]
Phenethylboronic acid Drug Info [26]
Phenethylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
PHENMEDIPHAM Drug Info [44]
Phenyl 1-(4-butoxyphenyl)propylcarbamate Drug Info [25]
Phenyl 4-(decyloxy)phenylcarbamate Drug Info [25]
Phenyl 4-(dodecyloxy)phenylcarbamate Drug Info [25]
Phenyl 4-(heptyloxy)phenylcarbamate Drug Info [25]
Phenyl 4-(hexyloxy)phenylcarbamate Drug Info [25]
Phenyl 4-(octyloxy)phenylcarbamate Drug Info [25]
Phenyl 4-(undecyloxy)phenylcarbamate Drug Info [25]
Phenyl Boronic acid Drug Info [26]
Phenyl-1,4-bismaleimide Drug Info [17]
Phenylcarbamic Acid Biphenyl-3-yl Ester Drug Info [29]
Propan-2-one O-3-butoxyphenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-(decyloxy)phenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-(heptyloxy)phenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-(hexyloxy)phenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-(nonyloxy)phenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-(octyloxy)phenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-(pentyloxy)phenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-butoxybenzylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-butoxyphenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-ethoxyphenylcarbamoyl oxime Drug Info [25]
Propan-2-one O-4-propoxyphenylcarbamoyl oxime Drug Info [25]
Propofol Drug Info [9], [10]
Pyridin-3-yl 4-butoxybenzylcarbamate Drug Info [25]
SSR411298 Drug Info [49]
Thiopental Drug Info [9]
VER-156084 Drug Info [50]
Modulator IW-6118 Drug Info [51]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Anandamide degradation
KEGG Pathway Retrograde endocannabinoid signaling
PANTHER Pathway Anandamide degradation
References
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REF 2(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5464).
REF 3FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011679.
REF 4(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2579).
REF 5ClinicalTrials.gov (NCT01107236) Study to Evaluate Efficacy and Safety of IW-6118 in Patients Undergoing Third Molar Extraction. U.S. National Institutes of Health.
REF 6(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6694).
REF 7ClinicalTrials.gov (NCT00822744) An Eight-week Study of SSR411298 as Treatment for Major Depressive Disorder in Elderly Patients. U.S. National Institutes of Health.
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029245)
REF 9The general anesthetic propofol increases brain N-arachidonylethanolamine (anandamide) content and inhibits fatty acid amide hydrolase. Br J Pharmacol. 2003 Jul;139(5):1005-13.
REF 10Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
REF 11Bioorg Med Chem Lett. 2008 Jul 15;18(14):4163-7. Epub 2008 May 24.3-Alkenyl-2-azetidinones as fatty acid amide hydrolase inhibitors.
REF 12J Med Chem. 2007 Oct 4;50(20):5012-23. Epub 2007 Sep 1.Structure-activity relationship of a series of inhibitors of monoacylglycerol hydrolysis--comparison with effects upon fatty acid amide hydrolase.
REF 13J Med Chem. 2005 Mar 24;48(6):1849-56.Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
REF 14Bioorg Med Chem. 2008 Feb 15;16(4):1562-95. Epub 2007 Nov 6.Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
REF 15Bioorg Med Chem Lett. 2001 Jun 18;11(12):1517-20.alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution.
REF 16Bioorg Med Chem. 2008 Feb 15;16(4):2114-30. Epub 2007 Nov 26.Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH).
REF 17J Med Chem. 2009 Dec 10;52(23):7410-20.Synthesis and in vitro evaluation of N-substituted maleimide derivatives as selective monoglyceride lipase inhibitors.
REF 18J Med Chem. 2008 Aug 14;51(15):4392-403. Epub 2008 Jul 16.Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.
REF 19Bioorg Med Chem Lett. 2008 Nov 15;18(22):5842-6. Epub 2008 Jun 28.Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fattyacid amide hydrolase.
REF 20J Med Chem. 2008 Feb 28;51(4):937-47. Epub 2008 Feb 5.Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
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REF 23Bioorg 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 amidehydrolase.
REF 24J Med Chem. 2005 Aug 11;48(16):5059-87.The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
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.
REF 26J Med Chem. 2008 Nov 27;51(22):7057-60.Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase.
REF 27Bioorg Med Chem Lett. 2007 Nov 1;17(21):5959-63. Epub 2007 Aug 21.Conformationally constrained analogues of 2-arachidonoylglycerol.
REF 28J Med Chem. 2007 Jul 12;50(14):3359-68. Epub 2007 Jun 9.Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
REF 29J 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.
REF 30J Med Chem. 2008 Dec 11;51(23):7327-43.Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors.
REF 31Eur J Med Chem. 2009 Oct;44(10):4179-91. Epub 2009 May 22.Chiral 3-(4,5-dihydrooxazol-2-yl)phenyl alkylcarbamates as novel FAAH inhibitors: Insight into FAAH enantioselectivity by molecular docking and interaction fields.
REF 32Eur J Med Chem. 2009 Jul;44(7):2994-3008. Epub 2009 Jan 20.The synthesis and biological evaluation of para-substituted phenolic N-alkyl carbamates as endocannabinoid hydrolyzing enzyme inhibitors.
REF 33J Med Chem. 2006 Jul 27;49(15):4650-6.Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system.
REF 34Bioorg Med Chem Lett. 2008 Nov 15;18(22):5875-8. Epub 2008 Aug 6.Monoacylglycerol lipase regulates 2-arachidonoylglycerol action and arachidonic acid levels.
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