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TBD from US Patent US20240174649: "CULLIN-RING E3 UBIQUITIN LIGASE 4 INHIBITOR COMPOUNDS AND METHODS OF THEIR USE"
Assay data:2 Active, 1 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Inhibition of cullin1 neddylation in UBC/DCN1 overactivated human MGC-803 cells at 1 uM incubated for 24 hrs by Western blot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of cullin1 neddylation in UBC/DCN1 overactivated human MGC-803 cells at 10 uM incubated for 24 hrs by Western blot analysis
Inhibition of cullin1 neddylation in UBC/DCN1 overactivated human MGC-803 cells at 0.3 to 10 uM incubated for 24 hrs by Western blot analysis
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of CUL1 in human U20S cells assessed as reduction in TNF-alpha-induced IkappaB-alpha degradation at 50 uM incubated for 2 hrs followed by TNFalpha stimulation for 15 mins by Western blotting analysis
Assay data:6 Tested
SummaryRelated BioAssays by Target
Competitive inhibition of Nedd8-cullin1 (unknown origin) adduct formation assessed as decrease in cullin1-Nedd8 adduct formation at 50 uM preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis
Inhibition of Nedd8-cullin1 (unknown origin) adduct formation assessed as decrease in cullin1 neddylation at 10 uM preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis
Inhibition of Nedd8-cullin1 adduct formation in human A549 cells assessed as decrease in cullin1 neddylation at 50 uM measured after 6 hrs by Western blot analysis
Assay data:1 Tested
Inhibition of Nedd8-cullin1 adduct formation in human A549 cells assessed as decrease in cullin1 neddylation at 75 uM measured after 6 hrs by Western blot analysis
Inhibition of Nedd8-cullin1 adduct formation in human A549 cells assessed as decrease in cullin1 neddylation at 60 to 80 uM measured after 6 hrs by Western blot analysis
Competitive inhibition of Nedd8-cullin1 (unknown origin) adduct formation at 12.5 to 50 uM assessed as increase in substrate Km by Lineweaver-Burk plot analysis
Competitive inhibition of Nedd8-cullin1 (unknown origin) adduct formation at 12.5 to 50 uM assessed as substrate Vmax by Lineweaver-Burk plot analysis
Inhibition of Nedd8-cullin1 (unknown origin) assessed as decrease in cullin1-Nedd8 adduct formation at 25 to 50 uM preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis
Inhibition of Nedd8-cullin1 adduct formation in human A549 cells assessed as decrease in cullin1 neddylation at 100 uM incubated for 6 to 12 hrs by Western blot analysis
Assay data:1 Active, 4 Tested
Inhibition of Nedd8-cullin1 (unknown origin) adduct formation assessed as decrease in cullin1 neddylation at 50 uM preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis
Assay data:4 Active, 4 Tested
ROC1-CUL1 CTD di-Ub FRET assay
Assay data:2 Active, 12 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
ROC1-CUL1 CTD Inhibitor di-Ub FRET Primary HTS Screen
Assay data:859 Active, 144055 Tested
Inhibition of Cul-1/Skp1 protein interaction in human HCT116 cells after 24 hrs by immunoprecipitation assay
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