Assay Detail
Binding
CHEMBL4138520
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Kelch-like ECH-associated protein 1 (CHEMBL2069156) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: a novel approach to activate Nrf2 function.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.34 | 6.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4167793 | — | — | 1 | 6.12 |
| CHEMBL2381968 | — | — | 1 | 5.96 |
| CHEMBL4159561 | — | — | 1 | 5.92 |
| CHEMBL4159153 | — | — | 1 | 5.66 |
| CHEMBL4167472 | — | — | 1 | 5.13 |
| CHEMBL4166378 | — | — | 1 | 5.10 |
| CHEMBL4174294 | — | — | 1 | 4.68 |
| CHEMBL4162919 | — | — | 1 | 4.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4167793 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2381968 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4159561 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4159153 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4167472 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4166378 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4174294 | — | IC50 | = | 20800.0 | nM | 4.68 |
| CHEMBL4162919 | — | IC50 | = | 69700.0 | nM | 4.16 |