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Inhibition of UAE (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant C-terminal His-tagged human full length UAE1 expressed in Escherichia coli BL21 (lambdaDE3) assessed as reduction in transfer of Ub to UBE2C enzyme
Binding affinity to UBA1 in human HepG2 cells at 10 uM incubated for 8 hrs by pull-down/LC-MS/MS analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Ubiquitin Thioester Inhibtion Assay from Article 10.1074/jbc.M111.279984: "Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues."
Ubiquitin Activating Enzyme (UAE) HTRF Assay from US Patent US10202389: "Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme"
Assay data:120 Active, 120 Activity ≤ 1 µM, 120 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of Ubiquitin/Ubiquitin-activating enzyme E1 (unknown origin)
Assay data:5 Tested
SummaryPubMed CitationRelated BioAssays by Target
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of ubiquitin/ubiquitin-activating enzyme E1 (unknown origin)
Assay data:3 Tested
Binding affinity to UBA1 in human NCI-H358 cells at 1 uM by mass spectrometry based pull down assay
Binding affinity to UBA1 in human NCI-H23 cells at 1 uM by mass spectrometry based pull down assay
Inhibition of E1 in human MCF7 cells assessed as increase in p53 levels at 100 uM measured after 24 hrs by Western blot analysis
Inhibition of E1 in human MCF7 cells assessed as increase in p53 levels at 30 uM measured after 24 hrs by Western blot analysis
Reversible inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation at 100 uM pretreated for 60 mins followed by 2.5 uM biotin-labelled ubiquitin addition for 30 mins and subsequent 5 uM biotin-labelled ubiquitin addition measured after 30 mins by Western blot analysis
Reversible inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation at 100 uM pretreated for 60 mins followed by 2.5 uM biotin-labelled ubiquitin addition for 30 mins and subsequent 5 uM biotin-labelled ubiquitin addition by Western blot analysis
Irreversible inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation at 10 uM pretreated for 60 mins followed by 2.5 uM biotin-labelled ubiquitin addition for 30 mins and subsequent 5 uM biotin-labelled ubiquitin addition measured after 30 mins by Western blot analysis
Irreversible inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation at 10 uM pretreated for 60 mins followed by 2.5 uM biotin-labelled ubiquitin addition for 30 mins and subsequent 5 uM biotin-labelled ubiquitin addition by Western blot analysis
Inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation at 3 to 300 uM pretreated for 30 mins followed by biotin-labelled ubiquitin addition and measured after 30 mins by Western blot analysis
Inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation pretreated for 30 mins followed by biotin-labelled ubiquitin addition and measured after 30 mins by Western blot analysis
Assay data:1 Tested
Inhibition of recombinant human E1 expressed in Escherichia coli BL21(DE3) assessed as reduction in biotin-labelled ubiquitin-E1 conjugate formation up to 1000 uM pretreated for 30 mins followed by biotin-labelled ubiquitin addition and measured after 30 mins by Western blot analysis
Assay data:1 Active, 2 Tested
Inhibition of UAE1-mediated Ubc10-ubiquitin conjugation in human Caco2 cells up to 10 uM preincubated for 10 mins followed by ATP and Mg2+ addition measured after 60 mins by Western blot analysis
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