Assay Detail
Binding
CHEMBL5167218
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Inhibition of Keap1-Nrf2 (unknown origin) protein-protein interaction expressed in Escherichia coli BL21 codon plus cells using FITC-beta-DEETGEF-OH as substrate incubated for 30 mins by fluorescence polarization assay
18
Total Activities
18
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
Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein-Protein Interaction Inhibitors with an Alternative Binding Mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.29 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3601212 | — | — | 1 | 7.84 |
| CHEMBL3237245 | — | — | 1 | 7.54 |
| CHEMBL4174651 | — | — | 1 | 7.22 |
| CHEMBL3617852 | — | — | 1 | 7.21 |
| CHEMBL3632882 | — | — | 1 | 7.07 |
| CHEMBL3899754 | — | — | 1 | 6.85 |
| CHEMBL5172581 | — | — | 1 | 6.24 |
| CHEMBL5207192 | — | — | 1 | 6.17 |
| CHEMBL5195422 | — | — | 1 | 6.09 |
| CHEMBL5203566 | — | — | 1 | 6.09 |
| CHEMBL2402207 | — | — | 1 | 6.03 |
| CHEMBL5189014 | — | — | 1 | 5.96 |
| CHEMBL5174036 | — | — | 1 | 5.92 |
| CHEMBL5173969 | — | — | 1 | 5.82 |
| CHEMBL3600394 | — | — | 1 | 5.74 |
| CHEMBL3235901 | — | — | 1 | 5.54 |
| CHEMBL5181288 | — | — | 1 | 5.53 |
| CHEMBL5179855 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3601212 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL3237245 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL4174651 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3617852 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3632882 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3899754 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5172581 | — | IC50 | = | 575.0 | nM | 6.24 |
| CHEMBL5207192 | — | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL5195422 | — | IC50 | = | 805.0 | nM | 6.09 |
| CHEMBL5203566 | — | IC50 | = | 815.0 | nM | 6.09 |
| CHEMBL2402207 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5189014 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL5174036 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5173969 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3600394 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL3235901 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5181288 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL5179855 | — | IC50 | = | 37000.0 | nM | 4.43 |