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Bioluminescence Resonance Energy Transfer (BRET) Assay from US Patent US20240132519: "NRF2-ACTIVATING COMPOUND"
Assay data:35 Active, 24 Activity ≤ 1 nM, 35 Activity ≤ 1 µM, 35 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Invivo inhibition of Nrf2-Keap1 Kelch domain protein-protein interaction in po dosed Wistar rat kidney assessed as increase in HO-1 protein level by measuring fold change at 30 mg/kg incubated for 6 hrs by ELISA assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Invivo inhibition of Nrf2-Keap1 Kelch domain protein-protein interaction in po dosed Wistar rat kidney assessed as increase in HO-1 protein level incubated for 6 hrs by ELISA assay
Binding affinity to Keap1 Kelch domain (unknown origin) assessed as change in entropy by isothermal titration calorimetry assay
Assay data:3 Tested
Binding affinity to Keap1 Kelch domain (unknown origin) assessed as change in enthalpy by isothermal titration calorimetry assay
Binding affinity to Keap1 Kelch domain (unknown origin) assessed as change in free energy by isothermal titration calorimetry assay
Inhibition of Nrf2-Keap1 Kelch domain (unknown origin) protein-protein interaction in presence of biotin labeled 16mer ETGE peptide AFFAQLQLDEETGEFL
Assay data:5 Active, 2 Activity ≤ 1 µM, 21 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of KEAP1/p62 (unknown origin) protein-protein interaction
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of KEAP1/Nrf2 (unknown origin) protein-protein interaction
Binding affinity to human KEAP1 by fluorescence anisotropy assay
Assay data:2 Active, 2 Tested
Binding affinity to human KEAP1 by fluorescence based assay
Binding affinity to human KEAP1
Inhibition of human Keap1-Nrf2 protein-protein interaction
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to human KEAP1 incubated for 1 hr by absorbance based analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Binding affinity to human KEAP1 by fluorescence polarization assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Inhibition of human Keap1-Nrf2 protein-protein interaction by fluorescence polarization assay
Assay data:12 Active, 10 Activity ≤ 1 µM, 14 Tested
Binding affinity to human KEAP1 by isothermal titration calorimetric assay
Inhibition of human KEAP1 by fluorescence polarization assay
Binding affinity to human KEAP1 Kelch domain (residues Ala321-Thr609) expressed in Escherichia coli BL21(DE3) cells assessed as dissociation constant by isothermal titration calorimetric analysis
Binding affinity to human KEAP1 Kelch domain (residues Ala321-Thr609) expressed in Escherichia coli BL21(DE3) cells assessed as dissociation constant by SPR direct binding assay
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