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Invivo inhibition of human Delta 5 desaturase in atherosclerosis mouse model at 3 mg/kg, po relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Invivo inhibition of human Delta 5 desaturase in C57BL/6J mouse at 3 mg/kg, po relative to control
Inhibition of human Delta 5 desaturase (unknown origin) expressed in human HepG2 cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Delta-5-desaturase (unknown origin) expressed in HEK2936E cell membrane incubated for 1 hr by DGLA-CoA and Arachidonyl-CoA mass spectrometric assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Binding affinity to D5D in Sprague-Dawley rat liver microsomes at 1.2 to 20 nM measured after 2.5 hrs by liquid scintillation counting
Displacement of [3H]T-3364366 from D5D in Sprague-Dawley rat liver microsomes at high concentrations after 150 mins by liquid scintillation counting
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to recombinant wild type D5D (unknown origin) expressed in baculovirus at 5 to 25 nM after 150 mins by liquid scintillation counting
Inhibition of D5D in human HepG2 cells using [14C]DGLA as substrate assessed as suppression of [14C]AA production at 10 uM preincubated for 3 hrs followed by compound washout and addition of substrate measured after 4 hrs by liquid scintillation counting
Ratio of inhibition of D5D in human HepG2 cells preincubated for 30 mins followed by [14C]DGLA substrate addition measured after 3 hrs to inhibition of D5D in human HepG2 cells assessed as inhibition of [14C]AA production preincubated for 3 hrs followed by compound washout and addition of [14C]DGLA substrate measured after 4 hrs
Reversible binding affinity to D5D in Sprague-Dawley rat liver microsomes after 150 mins in presence of trichloroacetate by liquid scintillation counting
Reversible binding affinity to D5D in Sprague-Dawley rat liver microsomes assessed as dissociation half life at 6 nM preincubated for 150 mins followed by 2 fold dilution by 10 uM of T-3364366 by liquid scintillation counting
Reversible binding affinity to D5D in Sprague-Dawley rat liver microsomes assessed as compound bound to protein at 6 nM preincubated for 150 mins followed by 2 fold dilution by 10 uM of T-3364366 measured after 21 hrs by liquid scintillation counting relative to control
Displacement of [3H]T-3364366 from D5D in Sprague-Dawley rat liver microsomes after 150 mins by liquid scintillation counting
Assay data:4 Active, 4 Tested
Binding affinity to D5D in Sprague-Dawley rat liver microsomes at 1.2 to 20 nM measured up to 2.5 hrs by liquid scintillation counting
Binding affinity to D5D in Sprague-Dawley rat liver microsomes after 150 mins by liquid scintillation counting
Inhibition of D5D in rat RLN10 cells using [14C]DGLA as substrate preincubated for 30 mins followed by substrate addition measured after 3 hrs
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of D5D in human HepG2 cells using [14C]DGLA as substrate preincubated for 30 mins followed by substrate addition measured after 3 hrs
Inhibition of D6D in Sprague-Dawley rat liver microsomes using [14C]LA as substrate preincubated for 5 mins measured after 30 mins
Assay data:1 Active, 2 Tested
Inhibition of D5D in Sprague-Dawley rat liver microsomes using [14C]DGLA as substrate preincubated for 5 mins measured after 120 mins
Inhibition of D5D in human HepG2 cells assessed as [14C]AA formation from [14C]DGLA preincubated for 30 mins followed by [14C]eicosatrienoic acid addition measured after 3 hrs by TLC analysis
Assay data:13 Active, 1 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 19 Tested
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