Assay Detail
Binding
CHEMBL4386552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human N-terminal His6-tagged KEAP1 Kelch domain (321 to 609 residues) expressed in baculovirus infected Sf9 insect cells by isothermal titration calorimetry
3
Total Activities
3
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 |
|---|---|---|---|
| Kd | 3 | 7.26 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464511 | — | — | 1 | 7.46 |
| CHEMBL4554007 | — | — | 1 | 7.36 |
| CHEMBL4473977 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464511 | — | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL4554007 | — | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL4473977 | — | Kd | = | 110.0 | nM | 6.96 |