Page last updated: 2024-08-07 16:56:27
Fatty-acid amide hydrolase 1
A fatty-acid amide hydrolase 1 that is encoded in the genome of rat. [OMA:P97612, PRO:DNx]
Synonyms
EC 3.5.1.99;
Anandamide amidase;
Anandamide amidohydrolase 1;
Fatty acid ester hydrolase;
3.1.1.-;
Oleamide hydrolase 1
Research
Bioassay Publications (63)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (1.59) | 18.2507 |
| 2000's | 31 (49.21) | 29.6817 |
| 2010's | 28 (44.44) | 24.3611 |
| 2020's | 3 (4.76) | 2.80 |
Compounds (76)
Drugs with Potency Measurements
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| anandamide | Rattus norvegicus (Norway rat) | Km | 2.7800 | 1 | 1 |
| arachidonoyl amine | Rattus norvegicus (Norway rat) | Km | 2.3400 | 1 | 1 |
| am-356 | Rattus norvegicus (Norway rat) | Km | 33.0000 | 1 | 1 |
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Assay and inhibition of diacylglycerol lipase activity.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Arylboronic acids as dual-action FAAH and TRPV1 ligands.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 26, Issue:5, 2016
Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Acylated 1Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
New Approaches to Cancer Therapy: Combining Fatty Acid Amide Hydrolase (FAAH) Inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) Activation.Journal of medicinal chemistry, , 12-26, Volume: 62, Issue:24, 2019
Novel propanamides as fatty acid amide hydrolase inhibitors.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).European journal of medicinal chemistry, , Volume: 63, 2013
Assay and inhibition of diacylglycerol lipase activity.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
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.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
The synthesis and biological evaluation of para-substituted phenolic N-alkyl carbamates as endocannabinoid hydrolyzing enzyme inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain.Chemistry & biology, , Apr-24, Volume: 16, Issue:4, 2009
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 18, Issue:17, 2008
Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system.Journal of medicinal chemistry, , Jul-27, Volume: 49, Issue:15, 2006
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 18, Issue:17, 2008
Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Substrate specificity and stereoselectivity of rat brain microsomal anandamide amidohydrolase.Journal of medicinal chemistry, , Mar-11, Volume: 42, Issue:5, 1999
Radiosynthesis, in vitro and in vivo evaluation of 123I-labeled anandamide analogues for mapping brain FAAH.Bioorganic & medicinal chemistry, , Jan-01, Volume: 17, Issue:1, 2009
Synthesis, in vitro and in vivo evaluation, and radiolabeling of aryl anandamide analogues as candidate radioligands for in vivo imaging of fatty acid amide hydrolase in the brain.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.Journal of medicinal chemistry, , 06-11, Volume: 63, Issue:11, 2020
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).European journal of medicinal chemistry, , Volume: 63, 2013
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
Biphenyl-3-yl alkylcarbamates as fatty acid amide hydrolase (FAAH) inhibitors: steric effects of N-alkyl chain on rat plasma and liver stability.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Synthesis and structure-activity relationships of FAAH inhibitors: cyclohexylcarbamic acid biphenyl esters with chemical modulation at the proximal phenyl ring.ChemMedChem, , Volume: 1, Issue:1, 2006
Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies.Journal of medicinal chemistry, , Oct-07, Volume: 47, Issue:21, 2004
Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
α-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain.Bioorganic & medicinal chemistry, , May-01, Volume: 22, Issue:9, 2014
Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 18, Issue:17, 2008
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.Bioorganic & medicinal chemistry, , Feb-15, Volume: 16, Issue:4, 2008
Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 18, Issue:22, 2008
Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.Journal of medicinal chemistry, , Feb-28, Volume: 51, Issue:4, 2008
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.Bioorganic & medicinal chemistry letters, , Jan-03, Volume: 15, Issue:1, 2005
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).European journal of medicinal chemistry, , Volume: 63, 2013
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors.Journal of medicinal chemistry, , Jan-08, Volume: 52, Issue:1, 2009
Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 29, Issue:2, 2019
Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.ACS medicinal chemistry letters, , Feb-10, Volume: 2, Issue:2, 2011
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 29, Issue:2, 2019
Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain.Chemistry & biology, , Apr-24, Volume: 16, Issue:4, 2009
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012