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Inhibition of GST-tagged DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction incubated for 1 hr by HTRF analysis
Assay data:41 Active, 34 Activity ≤ 1 µM, 45 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Reversible inhibition of GST-tagged DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction at 500 nM preincubated for 1 hr followed by Ac-UBC12-biotin addition by HTRF based dilution analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Reversible inhibition of GST-tagged DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction at 500 nM preincubated for 1 hr followed by Ac-UBC12-biotin addition by HTRF based ultrafiltration analysis
Binding affinity to DCN1 in human MGC-803 cells assessed as thermal stabilization incubated for 1 hr followed by heating at 53 degreeC for 3 mins by CETSA assay
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of DCN1 (unknown origin) by TR-FRET analysis
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to DCN1 (unknown origin) assessed as inhibition of constant by fluorescence polarization assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of biotinylated DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction incubated for 1 hr by TR-FRET analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Binding affinity to DCN1 (unknown origin) assessed as inhibitory constant
Binding affinity to DCN1 (unknown origin) assessed as Gibbs free energy change by MM-PBSA method
Assay data:3 Tested
Binding affinity to DCN1 (unknown origin) assessed as change in entropy by MM-PBSA method
Binding affinity to extracellular DCN1 (unknown origin) assessed as dissociation constant incubated for upto 180 secs by label-free biolayer interferometry assay
Inhibition of GST-tagged DCN1 (unknown origin) using AcUBE2M1-21 incubated for 30 mins by HTRF assay
Assay data:54 Active, 1 Activity ≤ 1 nM, 43 Activity ≤ 1 µM, 62 Tested
TR-Fret Assay from US Patent US11116757: "Methods and compositions of inhibiting DCN1-UBC12 interaction"
Assay data:188 Active, 99 Activity ≤ 1 µM, 635 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Competitive FP Binding Assay from US Patent US10500194: "Covalent small molecule DCN1 inhibitors and therapeutic methods using the same"
Assay data:30 Active, 30 Activity ≤ 1 µM, 30 Tested
Potency index, ratio of N-(rel-(4S,5S)-7-Ethyl-4-(4-fluorophenyl)-3-methyl-6-oxo-1-phenyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-b]pyridin-5-yl)-3-methylbenzamide IC50 to test compound IC50 for inhibition of biotinylated DCN1 (unknown origin) - AlexaFluor488 labelled UBE2M (unknown origin) protein-protein interaction after 1 hr by TR-FRET assay
Assay data:1 Tested
Inhibition of DCN1 (unknown origin) dependent cullin neddylation assessed as decrease in NEDD8 transfer from UBE2M to CUL2 using CUL2 as substrate preincubated for 15 mins in presence of ATP followed by substrate addition by fluorescence imaging analysis
Binding affinity to DCN1 in human HCC95 cells assessed as increase in thermal stability measured after 1 hr by CETSA
Inhibition of biotinylated DCN1 (unknown origin) - AlexaFluor488 labelled UBE2M (unknown origin) protein-protein interaction after 1 hr by TR-FRET assay
Assay data:41 Active, 27 Activity ≤ 1 µM, 48 Tested
Inhibition of DCN-1 in human KYSE-70 cell line assessed as increase in HO-1 expression at 5 to 10 uM incubated for 24 hrs by Western blot analysis
Assay data:1 Active, 1 Tested
Inhibition of DCN-1 in human KYSE-70 cell line assessed as increase in NRF2 expression at 5 to 10 uM incubated for 24 hrs by Western blot analysis
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