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Inhibition of recombinant human GSTA1-1
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryRelated BioAssays by Target
Inhibition of recombinant human GSTA1-1 using GSH and CDNB as substrate preincubated for 2 mins followed by substrate addition and measured upto 6 mins in the presence of UV irradiation by spectrophotometric analysis
Assay data:6 Active, 4 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human GSTA1-1 using GSH and CDNB as substrate preincubated for 5 mins followed by substrate addition and measured in the absence of UV irradiation by spectrophotometric analysis
Assay data:4 Active, 2 Activity ≤ 1 µM, 6 Tested
MKNK1 Kinase High ATP Assay from US Patent US9296757: "Substituted benzothienopyrimidines"
Assay data:89 Active, 4 Activity ≤ 1 nM, 89 Activity ≤ 1 µM, 89 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
MKNK1 Kinase High ATP Assay from US Patent US9284319: "Heterocyclyl aminoimidazopyridazines"
Assay data:16 Active, 16 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
MKNK1 Kinase Assay from US Patent US9284319: "Heterocyclyl aminoimidazopyridazines"
Assay data:18 Active, 18 Activity ≤ 1 µM, 18 Tested
Drug level in phosphate buffer assessed as GSTA1 (unknown origin)-mediated compound formation from nitric oxide retained pathway treated with (Z)-1-(4-cyano-5-(4-(methylamino)benzoyloxy)-2-nitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Drug level in phosphate buffer assessed as GSTA1 (unknown origin)-mediated compound formation from nitric oxide release pathway treated with (Z)-1-(4-cyano-5-(4-(methylamino)benzoyloxy)-2-nitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug level in phosphate buffer assessed as GSTA1 (unknown origin)-mediated compound formation from nitric oxide retained pathway treated with (Z)-1-(2-cyano-5-(4-(methylamino)benzoyloxy)-4-nitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug level in phosphate buffer assessed as GSTA1 (unknown origin)-mediated compound formation from nitric oxide release pathway treated with (Z)-1-(2-cyano-5-(4-(methylamino)benzoyloxy)-4-nitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug level in phosphate buffer assessed as GSTA1 (unknown origin)-mediated compound formation from nitric oxide retained pathway treated with (Z)-3,3-dimethyl-1-(5-(4-(methylamino)benzoyloxy)-2,4-dinitrophenoxy)triaz-1-ene 2-oxide at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug level in phosphate buffer assessed as GSTA1 (unknown origin)-mediated compound formation from nitric oxide release pathway treated with (Z)-3,3-dimethyl-1-(5-(4-(methylamino)benzoyloxy)-2,4-dinitrophenoxy)triaz-1-ene 2-oxide at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug metabolism in phosphate buffer assessed as ratio of GSTA1 (unknown origin)-mediated (S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(4-cyano-5-hydroxy-2-nitrophenylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid formation from nitric oxide release pathway to GSTA1 (unknown origin)-mediated (Z)-1-(4-cyano-5-hydroxy-2-nitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide formation from nitric oxide retained pathway at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug metabolism in phosphate buffer assessed as ratio of GSTA1 (unknown origin)-mediated (S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(2-cyano-5-hydroxy-4-nitrophenylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid formation from nitric oxide release pathway to GSTA1 (unknown origin)-mediated (Z)-1-(2-cyano-5-hydroxy-4-nitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide formation from nitric oxide retained pathway at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Drug metabolism in phosphate buffer assessed as ratio of GSTA1 (unknown origin)-mediated (S)-2-amino-5-((R)-1-(carboxymethylamino)-3-(5-hydroxy-2,4-dinitrophenylthio)-1-oxopropan-2-ylamino)-5-oxopentanoic acid formation from nitric oxide release pathway to GSTA1 (unknown origin)-mediated (Z)-1-(5-hydroxy-2,4-dinitrophenoxy)-3,3-dimethyltriaz-1-ene 2-oxide formation from nitric oxide retained pathway at 1 uM at pH 7.4 at 37 degC after 30 mins by LC-MS/MS analysis in presence of GSH
Inhibition of human GSTA1 activity assessed as conjugation between CDNB and GSH at 25 uM
Assay data:12 Tested
Competitive inhibition of human GSTA1 activity by double reciprocal Lineweaver-Burk graph
Assay data:4 Active, 2 Activity ≤ 1 µM, 4 Tested
Inhibition of human GSTA1 activity assessed as conjugation between CDNB and GSH
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
Prodrug conversion assessed as half life for human recombinant GST-A1-mediated metformin formation at 100 uM in presence of 1 mM reduced glutathione by HPLC method
Ratio of prodrug activation in presence of GSH and recombinant GSTA1 (unknown origin) to prodrug activation in presence of GSH by UV-Visible spectrophotometry
Assay data:4 Tested
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