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Biological Data from US Patent US11891387: "Monoacylglycerol lipase modulators"
Assay data:105 Active, 1 Activity ≤ 1 nM, 85 Activity ≤ 1 µM, 108 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
hFAAH Endocannabinoid related and lipase panel
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
[3H] 2-OG cleavage activity assay (rat brain)
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
[3H] 2-OG cleavage activity assay (mouse brain)
[3H] 2-OG cleavage activity assay (PBMC)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
[3H] 2-OG cleavage activity assay (HeLa)
Inhibition of MGL activity in human HeLa cells assessed as reduction in cleaved [1,3-3H glycerol] level using [glycerol-1,3-3H]-oleoyl glycerol as substrate incubated for 1 hr
Assay data:6 Active, 6 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of mouse brain FAAH
Inhibition of FAAH in mouse Primary neuron cells using [3H]AEA as substrate at 30 uM incubated for 30 mins by liquid scintillation analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of mouse FAAH expressed in COS-7 cells using [3H]AEA as substrate incubated for 30 mins by liquid scintillation analysis
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of mouse MAGL expressed in COS-7 cells using 2-[3H]AG as substrate incubated for 30 mins by liquid scintillation analysis
Binding affinity to MAGL in rat cerebellum incubated for 1 hr in presence of MAGL inhibitor, (1-(4-fluorophenyl)-1H-indol-5-yl)(3-(4-(pyrimidin-2-yl)piperazin-1-yl)azetidin-1-yl)methanone by autoradiography
Binding affinity to MAGL in rat striatum incubated for 1 hr in presence of MAGL inhibitor, (1-(4-fluorophenyl)-1H-indol-5-yl)(3-(4-(pyrimidin-2-yl)piperazin-1-yl)azetidin-1-yl)methanone by autoradiography
Binding affinity to MAGL in rat thalamus incubated for 1 hr in presence of MAGL inhibitor, (1-(4-fluorophenyl)-1H-indol-5-yl)(3-(4-(pyrimidin-2-yl)piperazin-1-yl)azetidin-1-yl)methanone by autoradiography
Binding affinity to MAGL in rat cortex incubated for 1 hr in presence of MAGL inhibitor, (1-(4-fluorophenyl)-1H-indol-5-yl)(3-(4-(pyrimidin-2-yl)piperazin-1-yl)azetidin-1-yl)methanone by autoradiography
Binding affinity to MAGL in rat hippocampus incubated for 1 hr in presence of MAGL inhibitor, (1-(4-fluorophenyl)-1H-indol-5-yl)(3-(4-(pyrimidin-2-yl)piperazin-1-yl)azetidin-1-yl)methanone by autoradiography
Binding affinity to MAGL in rat cerebellum incubated for 1 hr in presence of MAGL inhibitor, JNJ-42226314 by autoradiography
Assay data:2 Tested
Binding affinity to MAGL in rat striatum incubated for 1 hr in presence of MAGL inhibitor, JNJ-42226314 by autoradiography
Binding affinity to MAGL in rat thalamus incubated for 1 hr in presence of MAGL inhibitor, JNJ-42226314 by autoradiography
Binding affinity to MAGL in rat cortex incubated for 1 hr in presence of MAGL inhibitor, JNJ-42226314 by autoradiography
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