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ROC1-CUL1 CTD Inhibitor di-Ub FRET Primary HTS Screen
Assay data:859 Active, 144055 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of histidine tagged recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) cells using Histone H4(1-20) substrate preincubated for 5 mins measured after 8 mins at 100 uM by liquid scintillation counting
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of histidine tagged recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) cells using Histone H4(1-20) substrate preincubated for 5 mins measured after 8 mins by liquid scintillation counting
Assay data:4 Tested
Competitive inhibition of histidine tagged recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) cells assessed as Ki intercept using Histone H4(1-20) substrate preincubated for 5 mins measured after 8 mins by liquid scintillation counting
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Non competitive inhibition of histidine tagged recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) cells assessed as Ki slope using SAM preincubated for 5 mins measured after 8 mins by liquid scintillation counting
Assay data:2 Tested
Binding affinity to fluorescein-labeled Histone H4(1-20) assessed as peptide fluorescence quenching by spectrofluorometry
Assay data:1 Active, 1 Tested
Inhibition of recombinant p300 HAT domain using Histone H4(1-20) substrate assessed as inhibition of histone acetyltransferase activity after 10 mins by liquid scintillation counting
Assay data:1 Tested
Inhibition of His6x-tagged PRMT1 expressed in Escherichia coli BL21 (DE3) using Histone H4(1-20) substrate in the presence of [14C] SAM assessed as residual activity at 30 uM by liquid scintillation counting
Inhibition of His6x-tagged PRMT4 expressed in Escherichia coli BL21 (DE3) using Histone H3(1-31) substrate in the presence of [14C] SAM assessed as residual activity at 30 uM by liquid scintillation counting
Inhibition of His6x-tagged PRMT5 expressed in Escherichia coli BL21 (DE3) using Histone H4(1-20 substrate in the presence of [14C] SAM assessed as residual activity at 30 uM by liquid scintillation counting
Binding affinity to recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) assessed as enzyme fluorescence quenching by spectrofluorometry
Binding affinity to fluorescein-labeled Histone H4(1-20) by spectrofluorometry
Selectivity ratio for His6x-tagged PRMT1 over His6x-tagged PRMT4
SummaryPubMed Citation
Selectivity ratio for His6x-tagged PRMT1 over His6x-tagged PRMT5
Potency index, ratio of IC50 for AMI-1 to IC50 for compound for histidine tagged recombinant PRMT1 expressed in Escherichia coli BL21 (DE3) cells
Inhibition of cell proliferation of human LNCAP cells in regular medium after 3 days
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