| Assay ID | Title | Year | Journal | Article |
|---|
| AID1573818 | Inhibition of rat FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model. |
| AID1194116 | Inhibition of recombinant human FAAH assessed as dissociation half life | 2015 | Bioorganic & medicinal chemistry letters, , Volume: 25, Issue:10
| Design strategies to address kinetics of drug binding and residence time. |
| AID690261 | Reversible inhibition of human recombinant FAAH assessed as hydrolysis of [3H]-AEA after 10 mins by liquid scintillation counting | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
| SAR and LC/MS studies of β-lactamic inhibitors of human fatty acid amide hydrolase (hFAAH): evidence of a nonhydrolytic process. |
| AID241449 | Inhibitory concentration against Fatty-acid amide hydrolase | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. |
| AID409622 | Selectivity ratio of IC50 for TGH to IC50 for rat FAAH | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. |
| AID430488 | Inhibition of rat FAAH incubated 3 hrs prior to addition of arachidonyl-amino-methyl-coumarin amide | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. |
| AID280033 | Selectivity for FAAH over TGH | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
| Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. |
| AID593883 | Half life in rat liver microsomes | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID1075082 | Competitive reversible inhibition of recombinant rat FAAH expressed in Escherichia coli using [14C]-oleamide as substrate at 1 to 10 nM preincubated for 3 hrs by Lineweaver-Burk plot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID280031 | Inhibition of TGH | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
| Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. |
| AID316866 | Inhibition of KIAA1363 | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID316865 | Inhibition of TGH | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID430491 | Inhibition of FAAH | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. |
| AID365832 | Inhibition of rat FAAH expressed in Escherichia coli at pH 9.0 | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID409628 | Inhibition of FAAH at pH 9 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase. |
| AID1075069 | In vivo inhibition of FAAH in C57Bl/6J mouse assessed as increase in OEA level in brain at 30 mg/kg, ip measured within 2 to 3 hrs | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID1075102 | Time-dependent inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as breakdown of [14C]-oleamide preincubated for 3 hrs by Dixon plot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID1139400 | Inhibition of rat recombinant FAAH expressed in Escherichia coli using [14C]oleamide as substrate assessed as oleic acid formation by Dixon plot analysis | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| α-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain. |
| AID765035 | Inhibition of human recombinant FAAH using N-arachidonyl-7-amino-4-methylcoumarin as substrate preincubated at 500 uM for 20 mins before substrate addition by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Macamides and their synthetic analogs: evaluation of in vitro FAAH inhibition. |
| AID241282 | Concentration of 50% inhibition of KIAA1363 was determined using FP-Rh as radioligand | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity. |
| AID1075071 | In vivo inhibition of FAAH in C57Bl/6J mouse assessed as increase in AEA level in brain at 30 mg/kg, ip measured within 2 to 3 hrs | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID363690 | Inhibition of rat FAAH assessed as recovery of enzyme activity at IC80 concentration after 18 hrs at 22 degC by dialysis | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
| Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. |
| AID316863 | Inhibition of rat recombinant FAAH expressed in Escherichia coli | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID363689 | Inhibition of rat FAAH assessed as recovery of enzyme activity at IC80 concentration after 18 hrs at 4 degC by dialysis | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
| Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. |
| AID239544 | Inhibitory constant determined against recombinant Fatty-acid amide hydrolase from rat expressed in Escherichia coli | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. |
| AID409626 | Selectivity ratio of IC50 for KIAA1363 to IC50 for rat FAAH | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. |
| AID1573817 | Inhibition of human transmembrane domain deficient FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model. |
| AID316871 | Inhibition of FAAH | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID1075103 | Time-dependent inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as breakdown of [14C]-oleamide preincubated for 1 hr by Dixon plot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID1075080 | In vivo inhibition of FAAH in C57Bl/6J mouse assessed as increase in AEA level in brain at 30 mg/kg, ip after 3 hrs relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID321261 | Selectivity for rat FAAH over monoacylglycerol lipase | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID316867 | Selectivity for rat recombinant FAAH over KIAA1363 | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID280030 | Inhibition of KIAA1363 | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
| Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. |
| AID409625 | Inhibition of KIAA1363 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. |
| AID321258 | Inhibition of human recombinant FAAH | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID1075070 | In vivo inhibition of FAAH in C57Bl/6J mouse assessed as increase in PEA level in brain at 30 mg/kg, ip measured within 2 to 3 hrs | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID593787 | Inhibition of FAAH in C57Bl/6J mouse liver assessed as increase of N-palmitoyl ethanolamine level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID593784 | Inhibition of FAAH in C57Bl/6J mouse brain assessed as increase of 2-arachidonoylglycerol level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID241829 | Inhibitory concentration of fatty acid amide hydrolase using FP-Rh radioligand | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity. |
| AID316310 | Aqueous solubility in water | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH). |
| AID637231 | Inhibition of rat recombinant FAAH expressed in Escherichia coli | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH. |
| AID321260 | Selectivity for rat FAAH over lipoprotein lipase | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID412539 | Inhibition of rat cortex FAAH by [3H]anandamide carbon filtration assay | 2009 | Journal of medicinal chemistry, Jan-08, Volume: 52, Issue:1
| Synthesis and evaluation of benzothiazole-based analogues as novel, potent, and selective fatty acid amide hydrolase inhibitors. |
| AID321259 | Selectivity for rat FAAH over triacylglycerol hydrolase | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID241808 | Inhibitory concentration of triacylgylcerol hydrolase using FP-Rh radioligand | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity. |
| AID697520 | Inhibition of human recombinant FAAH | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases. |
| AID409623 | Inhibition of TGH | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. |
| AID316311 | Inhibition of human FAAH | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
| Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH). |
| AID363656 | Inhibition of rat FAAH preincubated for 20 mins | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
| Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. |
| AID593783 | Inhibition of FAAH in C57Bl/6J mouse brain assessed as increase of N-palmitoyl ethanolamine level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID365831 | Inhibition of rat FAAH expressed in Escherichia coli | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID365835 | Inhibition of human recombinant FAAH expressed in african green monkey COS7 cells | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID239516 | Inhibitory constant determined against recombinant Fatty-acid amide hydrolase from human expressed in COS-7 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. |
| AID612783 | Inhibition of FAAH | 2011 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
| The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH). |
| AID445063 | Inhibition of rat recombinant FAAH expressed in Escherichia coli | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase. |
| AID1075078 | In vivo inhibition of FAAH in C57Bl/6J mouse assessed as increase in PEA level in brain at 30 mg/kg, ip after 3 hrs relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID316869 | Selectivity for rat recombinant FAAH over TGH | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID765036 | Inhibition of human recombinant FAAH using N-arachidonyl-7-amino-4-methylcoumarin as substrate preincubated at 10 uM for 20 mins before substrate addition by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Macamides and their synthetic analogs: evaluation of in vitro FAAH inhibition. |
| AID321262 | Selectivity for rat FAAH over carboxylesterase 1 lipase | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID593789 | Inhibition of FAAH in C57Bl/6J mouse brain assessed as increase of anandamide level at 50 mg/kg, po after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID409630 | Binding affinity to FAAH assessed as thermal stability by measuring melting temperature | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase. |
| AID365838 | Inhibition of KIAA1363 hydrolase | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID291341 | Inhibition of rat recombinant FAAH expressed in Escherichia coli | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
| Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID280032 | Selectivity for FAAH over KIAA1363 | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
| Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. |
| AID593782 | Inhibition of FAAH in C57Bl/6J mouse brain assessed as increase of anandamide level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID280028 | Inhibition of rat recombinant FAAH expressed in Escherichia coli by [14C]oleamide breakdown | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5
| Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase. |
| AID239559 | Binding affinity against purified rat Fatty-acid amide hydrolase (FAAH) expressed in Escherichia coli | 2005 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1
| Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase. |
| AID291343 | Selectivity for rat recombinant FAAH over KIAA1363 | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
| Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID365837 | Selectivity ratio of IC50 for rat FAAH expressed in Escherichia coli over IC50 for TGH | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID593785 | Inhibition of FAAH in C57Bl/6J mouse brain assessed as increase of arachidonic acid level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID291344 | Selectivity for rat recombinant FAAH over TGH | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
| Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID765033 | Reversible inhibition of human recombinant FAAH using N-arachidonyl-7-amino-4-methylcoumarin as substrate preincubated for 20 mins before substrate addition by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Macamides and their synthetic analogs: evaluation of in vitro FAAH inhibition. |
| AID1075091 | Reversible inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as remaining activity at IC80 preincubated for 3 hrs followed by 370 fold dilution measured after 18 hrs | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID1363927 | Inhibition of recombinant human N-terminal FLAG-tagged/C-terminal Myc-His6 tagged FAAH2 (32 to 579 residues) expressed in COS7 cell membranes | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors. |
| AID430487 | Inhibition of rat FAAH incubated 1 hr prior to addition of arachidonyl-amino-methyl-coumarin amide | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. |
| AID321257 | Inhibition of rat FAAH | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID321263 | Analgesic activity in iv dosed mouse | 2008 | Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
| Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality. |
| AID593788 | Inhibition of FAAH in C57Bl/6J mouse liver assessed as increase of 2-arachidonoylglycerol level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID239636 | Inhibitor affinity towards enzymes of class serine hydrolase was determined using biotin or fluorescent as radioligand (FP-biotin or FP-Rh) | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5
| Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity. |
| AID430485 | Inhibition of human FAAH incubated 1 hr prior to addition of arachidonyl-amino-methyl-coumarin amide | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas. |
| AID363662 | Inhibition of rat liver esterase assessed as ester (4-nitrophenyl-acetate) hydrolysis at 10 uM after 30 mins | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
| Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. |
| AID365839 | Inhibition of TGH | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID593786 | Inhibition of FAAH in C57Bl/6J mouse liver assessed as increase of anandamide level at 30 mg/kg, ip after 1 hr relative to control | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics. |
| AID409624 | Inhibition of rat FAAH | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase. |
| AID1573861 | Reversible inhibition of human transmembrane domain deficient FFAH expressed in Escherichia coli assessed as residual activity at 10 times IC50 using AAMCA as substrate preincubated for 1 hr followed by substrate addition and subsequent 10 fold compound d | 2019 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
| Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model. |
| AID346660 | Inhibition of FAAH | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors. |
| AID1075079 | In vivo inhibition of FAAH in C57Bl/6J mouse assessed as increase in OEA level in brain at 30 mg/kg, ip after 3 hrs relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID1139409 | Inhibition of mouse FAAH | 2014 | Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
| α-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain. |
| AID1298614 | Inhibition of MBP-fused human recombinant FAAH with truncated N-terminal transmembrane domain expressed in Escherichia coli T7 using D-AMC substrate measured over 40 mins by fluorescence based assay | 2016 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
| Piperidinyl thiazole isoxazolines: A new series of highly potent, slowly reversible FAAH inhibitors with analgesic properties. |
| AID1075101 | Time-dependent inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as breakdown of [14C]-oleamide preincubated for 6 hrs by Dixon plot analysis | 2014 | Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
| Design, synthesis, and characterization of α-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase. |
| AID241415 | Inhibitory concentration against Triacylglycerol hydrolase | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. |
| AID365836 | Selectivity ratio of IC50 for rat FAAH expressed in Escherichia coli over IC50 for KIAA1363 hydrolase | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase. |
| AID765031 | Reversible inhibition of human recombinant FAAH using N-arachidonyl-7-amino-4-methylcoumarin as substrate preincubated for 20 mins before substrate addition by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
| Macamides and their synthetic analogs: evaluation of in vitro FAAH inhibition. |
| AID697519 | Reversible inhibition of mouse FAAH isolated from brain homogenate using [3H-ethanolamine]AEA as substrate incubated for 20 mins prior to substrate addition measured after 18 hrs by microdialysis method | 2012 | Journal of medicinal chemistry, Aug-09, Volume: 55, Issue:15
| Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases. |
| AID242589 | Inhibitory concentration against KIAA1363 hydrolase | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics. |
| AID1345254 | Human Fatty acid amide hydrolase-2 (N-Acylethanolamine turnover) | 2006 | The Journal of biological chemistry, Dec-01, Volume: 281, Issue:48
| A second fatty acid amide hydrolase with variable distribution among placental mammals. |
| AID1345299 | Human Fatty acid amide hydrolase (Hydrolases) | 2006 | The Journal of biological chemistry, Dec-01, Volume: 281, Issue:48
| A second fatty acid amide hydrolase with variable distribution among placental mammals. |
| AID1345254 | Human Fatty acid amide hydrolase-2 (N-Acylethanolamine turnover) | 2009 | Anesthesia and analgesia, Jan, Volume: 108, Issue:1
| Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. |
| AID1798724 | FAAH Inhibition Assay (5 min Preincubation) from Article 10.1021/bi701378g: \\Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.\\ | 2007 | Biochemistry, Nov-13, Volume: 46, Issue:45
| Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
| AID1798726 | FAAH Inhibition Assay (30 min Preincubation) from Article 10.1021/bi701378g: \\Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.\\ | 2007 | Biochemistry, Nov-13, Volume: 46, Issue:45
| Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
| AID1798727 | FAAH Inhibition Assay (60 min Preincubation) from Article 10.1021/bi701378g: \\Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.\\ | 2007 | Biochemistry, Nov-13, Volume: 46, Issue:45
| Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
| AID1798285 | FAAH Inhibition Assay from Article 10.1021/jm061414r: \\Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.\\ | 2007 | Journal of medicinal chemistry, Jul-12, Volume: 50, Issue:14
| Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase. |
| AID1798725 | FAAH Inhibition Assay (15 min Preincubation) from Article 10.1021/bi701378g: \\Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.\\ | 2007 | Biochemistry, Nov-13, Volume: 46, Issue:45
| Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |