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Enzyme Activity Assay from Article 10.1021/cb700166z: "Picomolar inhibitors as transition-state probes of 5'-methylthioadenosine nucleosidases."
Assay data:8 Active, 8 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
MTAP/MTAN Inhibition Assay from Article 10.1021/jm701265n: "Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases."
Assay data:3 Active, 3 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Binding affinity to recombinant human N-terminal TEV cleavage site-fused-His6-tagged MTAP expressed in Escherichia coli BL21-CodonPlus(DE3)-RIPL competent cells assessed as reduction in MTA hydrolysis at 5 uM measured after 40 mins in presence of xanthine oxidase
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to recombinant human N-terminal TEV cleavage site-fused-His6-tagged MTAP expressed in Escherichia coli BL21-CodonPlus(DE3)-RIPL competent cells assessed as reduction in MTA hydrolysis measured after 40 mins in presence of xanthine oxidase
Assay data:13 Active, 2 Activity ≤ 1 nM, 13 Activity ≤ 1 µM, 13 Tested
Prodrug activation assessed as recombinant human MTAP-mediated compound cleavage at 100 uM by reverse phase HPLC analysis
Assay data:4 Tested
Inhibition of human MTAP using methylthioadenosine as substrate assessed as inhibition constant for slow onset inhibition of enzyme-inhibitor complex by xanthine oxidase coupling enzyme assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human MTAP using methylthioadenosine as substrate by xanthine oxidase coupling enzyme assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB
Assay data:3598 Active, 421 Activity ≤ 1 nM, 2233 Activity ≤ 1 µM, 3598 Tested
Inhibition of human MTAP assessed as reduction in methylthioadenosine phosphorolysis/hydrolysis
Assay data:17 Active, 2 Activity ≤ 1 nM, 17 Activity ≤ 1 µM, 17 Tested
Inhibition of His-tagged human MTAP at 2.5 uM
Assay data:1 Tested
Inhibition of His-tagged human MTAP
Assay data:14 Active, 2 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 14 Tested
Inhibition of MTAP in human CRL2522 cells by by ESI-MS analysis
Inhibition of MTAP in human FaDu cells by ESI-MS analysis
Inhibition of human MTAP
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Ratio of Kcat to Km against human Methylthioadenosine phosphorylase; Not determined
Ratio of Kcat to Km against human Methylthioadenosine phosphorylase
Assay data:32 Tested
Kcat against human methylthioadenosine phosphorylase expressed in Escherichia coli BL21 DE3 cells
Assay data:33 Tested
Inhibition of human MTAP as equilibrium dissociation constant; ND=no slow-onset phase
Inhibition of human MTAP as equilibrium dissociation constant
Assay data:16 Active, 13 Activity ≤ 1 nM, 16 Activity ≤ 1 µM, 16 Tested
Km against human methylthioadenosine phosphorylase expressed in Escherichia coli BL21 DE3 cells; Not determined
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