Assay Detail
Binding
CHEMBL5529137
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Inhibition of Keap1-Nrf2 protein-protein interaction (unknown origin) by fluorescence polarization assay
29
Total Activities
29
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
Structural modification of C2-substituents on 1,4-bis(arylsulfonamido)benzene or naphthalene-N,N'-diacetic acid derivatives as potent inhibitors of the Keap1-Nrf2 protein-protein interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.28 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237245 | — | — | 1 | 7.20 |
| CHEMBL5570595 | — | — | 1 | 7.16 |
| CHEMBL5571025 | — | — | 1 | 7.05 |
| CHEMBL5595521 | — | — | 1 | 6.96 |
| CHEMBL5567314 | — | — | 1 | 6.87 |
| CHEMBL5567570 | — | — | 1 | 6.65 |
| CHEMBL5572451 | — | — | 1 | 6.64 |
| CHEMBL5569386 | — | — | 1 | 6.49 |
| CHEMBL5555837 | — | — | 1 | 6.40 |
| CHEMBL5573249 | — | — | 1 | 6.39 |
| CHEMBL5590315 | — | — | 1 | 6.39 |
| CHEMBL5573658 | — | — | 1 | 6.36 |
| CHEMBL5181633 | — | — | 1 | 6.35 |
| CHEMBL5564155 | — | — | 1 | 6.34 |
| CHEMBL5574547 | — | — | 1 | 6.32 |
| CHEMBL5593633 | — | — | 1 | 6.25 |
| CHEMBL5590204 | — | — | 1 | 6.23 |
| CHEMBL5557583 | — | — | 1 | 6.19 |
| CHEMBL5571910 | — | — | 1 | 6.12 |
| CHEMBL5172581 | — | — | 1 | 6.11 |
| CHEMBL5563080 | — | — | 1 | 5.79 |
| CHEMBL5594768 | — | — | 1 | 5.75 |
| CHEMBL5583856 | — | — | 1 | 5.75 |
| CHEMBL5543048 | — | — | 1 | 5.65 |
| CHEMBL5592263 | — | — | 1 | 5.60 |
| CHEMBL5575136 | — | — | 1 | 5.42 |
| CHEMBL5549871 | — | — | 1 | 5.12 |
| CHEMBL5573742 | — | — | 1 | - |
| CHEMBL5556087 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237245 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5570595 | — | IC50 | = | 69.3 | nM | 7.16 |
| CHEMBL5571025 | — | IC50 | = | 88.6 | nM | 7.05 |
| CHEMBL5595521 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL5567314 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5567570 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL5572451 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL5569386 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL5555837 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL5573249 | — | IC50 | = | 408.0 | nM | 6.39 |
| CHEMBL5590315 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL5573658 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL5181633 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL5564155 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL5574547 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL5593633 | — | IC50 | = | 565.0 | nM | 6.25 |
| CHEMBL5590204 | — | IC50 | = | 593.0 | nM | 6.23 |
| CHEMBL5557583 | — | IC50 | = | 641.0 | nM | 6.19 |
| CHEMBL5571910 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5172581 | — | IC50 | = | 786.0 | nM | 6.11 |
| CHEMBL5563080 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL5594768 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL5583856 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL5543048 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL5592263 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5575136 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL5549871 | — | IC50 | = | 7680.0 | nM | 5.12 |
| CHEMBL5573742 | — | IC50 | - | — | - | |
| CHEMBL5556087 | — | IC50 | - | — | - |