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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
SummaryRelated BioAssays by Target
hABHD6 Endocannabinoid related and lipase panel
Assay data:1 Tested
hFAAH Endocannabinoid related and lipase panel
Assay data:1 Active, 1 Tested
[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
Inhibition of mouse brain FAAH
Inhibition of ABHD6 (unknown origin)
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of human ABHD6 expressed in HEK293T cells assessed as inhibition constant using 2-AG as substrate incubated for 30 mins by fluorescence plate reader assay
Inhibition of human ABHD6 expressed in HEK293 cells using TAMRA-FP as substrate by SDS-PAGE gel based competitive ABPP assay
Inhibition of ABHD6 in mouse brain membrane using HT-01 probe as substrate incubated for 30 mins by gel based competitive ABPP assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of ABHD6 in mouse brain membrane using TAMRA-FP as substrate at 10 uM pre-incubated for 30 mins followed by substrate addition and measured after 20 mins by coomassie staining based gel competitive ABPP assay
Assay data:2 Tested
Inhibition of human recombinant ABHD6
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Inhibition of human ABHD6 expressed in HEK293 cells using 1-AG as substrate incubated for 90 mins by sensitive fluorescence glycerol assay
Inhibition of ABHD6 in mouse brain membrane using FP-biotin as substrate incubated for 1 hr by LC-MS based ABPP-MudPIT analysis
Inhibition of ABHD6 in mouse brain membrane using FP-biotin as substrate at 10 uM incubated for 1 hr by LC-MS based ABPP-MudPIT analysis
Inhibition of human recombinant ABHD6 expressed in COS-7 cells in presence of FP-rhodamine labeled probe by SDS-PAGE based gel fluorescence scanning analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of FAAH in mouse Primary neuron cells using [3H]AEA as substrate at 30 uM incubated for 30 mins by liquid scintillation analysis
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