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Co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as maximal intensity in the presence of BRD9-BD as complex with compound incubated for 1 hrs by AlphaLISA proximity assay
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as total gibb's free energy change in the presence of BRD9-BD as complex with compound by ITC analysis
Assay data:1 Tested
Negative co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as total gibb's free energy change in the presence of BRD9-BD as complex with compound by ITC analysis
Assay data:2 Tested
Co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant in the presence of BRD9-BD as complex with compound by ITC analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant in the presence of BRD9-BD as complex with compound using FAM-DEALAHypYIPMDDDFQLRSF peptide as substrate by fluorescence polarization assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Negative co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant in the presence of BRD9-BD as complex with compound using FAM-DEALAHypYIPMDDDFQLRSF peptide as substrate by fluorescence polarization assay
Binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant using FAM-DEALAHypYIPMDDDFQLRSF peptide as substrate by fluorescence polarisation
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Negative co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as change in entropy in the presence of BRD9-BD as complex with compound by ITC analysis
Negative co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as change in gibbs free energy in the presence of BRD9-BD as complex with compound by ITC analysis
Negative co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as change in enthalpy in the presence of BRD9-BD as complex with compound by ITC analysis
Negative co-operative binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant in the presence of BRD9-BD as complex with compound by ITC analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as change in entropy by ITC analysis
Binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as gibbs free energy change by ITC analysis
Binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as change in enthalpy by ITC analysis
Binding affinity to 6His-tagged human VHL/ElonginC/ElonginB expressed in Escherichia coli BL21 (DE3) cells assessed as dissociation constant by ITC analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
Binding affinity to GST tagged human SOS1(564 to 1049 residues)-6his tagged human VHL (54 to 213 residues)-human ElonginC (17 to 112 residues)-human ElonginB (1 to 104 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as ternary complex formation by measuring maximal HTRF signals incubated for 15 mins by HTRF analysis
Assay data:1 Active, 7 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to VCB E3 ligase (unknown origin) assessed as binary equilibrium dissociation constant by surface plasmon resonance analysis
Binding affinity to VCB E3 ligase (unknown origin) assessed as binary equilibrium dissociation constant by 19F NMR assay
Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from dual VBC E3 ligase (unknown origin) ternary complex assessed as inhibition constant by 19F NMR assay
Displacement of (2S,4R)-N-(4-bromobenzyl)-4-hydroxy-1-(3,3,3-trifluoropropanoyl)pyrrolidine-2-carboxamide from dual VBC E3 ligase (unknown origin) ternary complex by 19F NMR assay
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