Assay Detail
Binding
CHEMBL4386551
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5'-TAMRA-labelled NRF2 peptide from human N-terminal His6-tagged KEAP1 Kelch domain (321 to 609 residues) expressed in baculovirus infected Sf9 insect cells by fluorescence polarization assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Kelch-like ECH-associated protein 1 (CHEMBL2069156) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.66 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4450921 | — | — | 1 | 8.00 |
| CHEMBL4447060 | — | — | 1 | 7.70 |
| CHEMBL4578025 | — | — | 1 | 7.62 |
| CHEMBL4540327 | — | — | 1 | 7.43 |
| CHEMBL4457466 | — | — | 1 | 7.38 |
| CHEMBL4464511 | — | — | 1 | 7.33 |
| CHEMBL4554007 | — | — | 1 | 7.16 |
| CHEMBL4473977 | — | — | 1 | 6.89 |
| CHEMBL4454051 | — | — | 1 | 6.75 |
| CHEMBL4567490 | — | — | 1 | 6.58 |
| CHEMBL4542179 | — | — | 1 | 6.50 |
| CHEMBL4570791 | — | — | 1 | 6.24 |
| CHEMBL4452805 | — | — | 1 | 5.62 |
| CHEMBL4552527 | — | — | 1 | 4.36 |
| CHEMBL4436743 | — | — | 1 | 4.33 |
| CHEMBL4443801 | — | — | 1 | - |
| CHEMBL4528658 | — | — | 1 | - |
| CHEMBL4461044 | — | — | 1 | - |
| CHEMBL4572418 | — | — | 1 | - |
| CHEMBL4588168 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4450921 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4447060 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4578025 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4540327 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4457466 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4464511 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4554007 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4473977 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4454051 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4567490 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4542179 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4570791 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4452805 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4552527 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4436743 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL4443801 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4528658 | — | IC50 | = | 140000.0 | nM | - |
| CHEMBL4461044 | — | IC50 | = | 330000.0 | nM | - |
| CHEMBL4572418 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL4588168 | — | IC50 | = | 260000.0 | nM | - |