Assay ID | Title | Year | Journal | Article |
AID1354593 | Efflux ratio of apparent permeability in MDCK-MDR1 cells at 10 uM up to 120 mins | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases. |
AID1506526 | Inhibition of fluorescent labelled Nrf2 peptide ligand binding to human Keap1 (321 to 609 residues) expressed in Escherichia coli BL21 DE3 pLysS incubated for 1 hr by fluorescence polarisation assay | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: a novel approach to activate Nrf2 function. |
AID1577808 | Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as thermal stabilization by sypro orange dye based thermal shift assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID1239358 | Inhibition of Keap1-Nrf2 (unknown origin) protein-protein interaction by fluorescence polarization assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Structure-Activity and Structure-Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1-Nrf2 Protein-Protein Interaction Inhibitor. |
AID746546 | Binding affinity to Keap1 kelch domain (unknown origin) by competitive SPR assay | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID746541 | Stability in phosphate buffer after 24 hrs | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID1659349 | Binding affinity to KEAP1 interaction with Nrf2 (unknown origin) by SRP assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases. |
AID1354598 | Ratio of unbound drug level in Mdr1a/1b/Bcrp knock-out mouse brain to plasma | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases. |
AID1577815 | Inhibition of Cys5-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measured after 10 to 15 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID746545 | Inhibition of Keap1-Nrf2 interaction in human HepG2 cells expressing ARE-bla assessed as activation of antioxidant response element by beta-lactamase reporter assay | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID1354589 | Inhibition of Keap1 kelch domain (unknow origin)/Nrf2-ETGE peptide (unknown origin) interaction by fluorescence polarization assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases. |
AID746542 | Metabolic stability of the compound assessed as thiol group addition after 48 hrs in presence of glutathione | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID1577849 | Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as change in melting temperature by sypro orange dye based thermal shift assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID1577839 | Redox cycling activity of the compound assessed as H2O2 production measured after 15 mins in presence of TCEP by phenol red reagent based horseradish peroxidase coupled assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID746540 | Metabolic stability of the compound assessed as thiol group decomposition after 48 hrs in presence of glutathione | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID1655400 | Displacement of AF647-9-mer ETGE peptide from recombinant human biotinylated KEAP1 Kelch domain (322 to 609 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins followed by AF647-9-mer ETGE peptide addition and measured after 60 min | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction. |
AID746543 | Solubility of the compound in phosphate buffer | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID1577810 | Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance analysis | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID1577841 | Inhibition of Cys5-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measured after 10 to 15 mins in presence of 0.01% Triton X-100 by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID1354594 | Ratio of unbound drug level in mouse brain to plasma | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases. |
AID1577814 | Binding affinity to Keap1 in mouse Hepa1c1c7 cells assessed as reduction in Keap1 interaction by measuring induction of NQO1 activity measured after 24 hrs | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
| A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
AID746544 | Inhibition of Keap1-Nrf2 interaction in human U2OS cells assessed as Nrf2 nuclear translocation by beta-lactamase reporter assay | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction. |
AID1248054 | Inhibition of Keap1 (unknown origin) interaction to Nrf2 | 2015 | Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
| Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2014 | ChemMedChem, Apr, Volume: 9, Issue:4
| Binding mode and structure-activity relationships around direct inhibitors of the Nrf2-Keap1 complex. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |