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Inhibition of C-terminal Hexahistidine-tagged recombinant human LTAH4 expressed in Escherichia coli BL21 (DE3) using L-arginine-7-amino-4-methylcoumarine as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence based method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
LTA4H Enzyme Assay from US Patent US9303018: "Inhibitors of leukotriene production"
Assay data:23 Active, 6 Activity ≤ 1 nM, 23 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Peptidase Assay from Article 10.1016/j.bmc.2008.03.042: "Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase."
Assay data:46 Active, 34 Activity ≤ 1 µM, 56 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Epoxide Hydrolase Assay from Article 10.1021/jm701575k: "Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity."
Assay data:42 Active, 41 Activity ≤ 1 µM, 42 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Enzyme Inhibition Assay from Article 10.1016/j.bmc.2006.06.050: "Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors."
Assay data:7 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 19 Tested
LTA4 hydrolase assay from US Patent US10202362: "Inhibitors of leukotriene A4 hydrolase"
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Enzyme Assay from US Patent US9662339: "Benzodioxane inhibitors of leukotriene production for combination therapy"
Assay data:295 Active, 203 Activity ≤ 1 nM, 295 Activity ≤ 1 µM, 295 Tested
Enzymatic Assay from US Patent US9573957: "Inhibitors of leukotriene production"
Assay data:151 Active, 79 Activity ≤ 1 nM, 151 Activity ≤ 1 µM, 151 Tested
Inhibition of LTA4H in human PBMC assessed as increase of LXA4 generation at 1 uM preincubated for 15 mins followed by calcium ionophore A23187 stimulation and measured after 2 hrs by LCMS/MS analysis
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated thromboxane B2 generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated prostaglandin D2 generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated prostaglandin E2 generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Inhibition of recombinant full length N-terminal His6-tagged LTA4H (unknown origin) expressed in Escherichia coli BL21 DE3 cells at enzyme concentration <1 nM using Arg-AMC as substrate preincubated for 15 mins followed by substrate addition and measured every 10 mins for 300 mins by fluorescence based assay
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated LTB4 generation preincubated for 4 hrs followed by ionophore stimulation and measured after 2 hrs by EIA assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of LTA4H in human whole blood assessed as reduction of calcium ionophore A23187-stimulated LTB4 generation preincubated for 4 hrs followed by ionophore stimulation and measured after 15 hrs by EIA assay
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated LTB4 generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated LTC4 generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated LXA4 generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated arachidonic acid generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
Inhibition of LTA4H in human PBMC assessed as reduction of calcium ionophore A23187-stimulated 12-HETE generation at 1 uM preincubated for 15 mins followed by ionophore stimulation and measured after 2 hrs by LCMS/MS analysis relative to control
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