Assay Detail
Binding
CHEMBL5260303
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Nrf2-Keap1 Kelch domain (unknown origin) protein-protein interaction in presence of biotin labeled 16mer ETGE peptide AFFAQLQLDEETGEFL
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Methyl and Fluorine Effects in Novel Orally Bioavailable Keap1-Nrf2 PPI Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.73 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5284493 | — | — | 1 | 7.05 |
| CHEMBL2381968 | — | — | 1 | 6.15 |
| CHEMBL5284304 | — | — | 1 | 5.55 |
| CHEMBL5278346 | — | — | 1 | 5.46 |
| CHEMBL5289954 | — | — | 1 | 5.05 |
| CHEMBL5271230 | — | — | 1 | 4.77 |
| CHEMBL5273621 | — | — | 1 | 4.43 |
| CHEMBL5286485 | — | — | 1 | 4.41 |
| CHEMBL5266194 | — | — | 1 | 4.40 |
| CHEMBL5283445 | — | — | 1 | 4.29 |
| CHEMBL5274849 | — | — | 1 | 4.27 |
| CHEMBL5285861 | — | — | 1 | 4.26 |
| CHEMBL5289579 | — | — | 1 | 4.17 |
| CHEMBL5277909 | — | — | 1 | 4.08 |
| CHEMBL5286321 | — | — | 1 | 4.05 |
| CHEMBL5281246 | — | — | 1 | 4.02 |
| CHEMBL5265976 | — | — | 1 | 4.00 |
| CHEMBL5274045 | — | — | 1 | - |
| CHEMBL5273258 | — | — | 1 | - |
| CHEMBL5270092 | — | — | 1 | - |
| CHEMBL5280279 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5284493 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2381968 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5284304 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5278346 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL5289954 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5271230 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5273621 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL5286485 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL5266194 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL5283445 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL5274849 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL5285861 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL5289579 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL5277909 | — | IC50 | = | 83000.0 | nM | 4.08 |
| CHEMBL5286321 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL5281246 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL5265976 | — | IC50 | = | 99000.0 | nM | 4.00 |
| CHEMBL5274045 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5273258 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5270092 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5280279 | — | IC50 | > | 100000.0 | nM | - |