Assay Detail
Binding
CHEMBL5529138
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Inhibition of Keap1-Nrf2 protein-protein interaction (unknown origin) assessed as inhibition constant by TR-FRET assay
30
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 |
|---|---|---|---|
| Ki | 30 | 7.14 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237245 | — | — | 2 | 9.00 |
| CHEMBL5571025 | — | — | 1 | 8.12 |
| CHEMBL5570595 | — | — | 1 | 8.04 |
| CHEMBL5595521 | — | — | 1 | 7.62 |
| CHEMBL5567570 | — | — | 1 | 7.52 |
| CHEMBL5567314 | — | — | 1 | 7.49 |
| CHEMBL5556087 | — | — | 1 | 7.38 |
| CHEMBL5569386 | — | — | 1 | 7.29 |
| CHEMBL5555837 | — | — | 1 | 7.18 |
| CHEMBL5573658 | — | — | 1 | 7.13 |
| CHEMBL5564155 | — | — | 1 | 7.11 |
| CHEMBL5574547 | — | — | 1 | 7.09 |
| CHEMBL5590204 | — | — | 1 | 6.97 |
| CHEMBL5571910 | — | — | 1 | 6.85 |
| CHEMBL5172581 | — | — | 1 | 6.84 |
| CHEMBL5563080 | — | — | 1 | 6.50 |
| CHEMBL5583856 | — | — | 1 | 6.46 |
| CHEMBL5543048 | — | — | 1 | 6.34 |
| CHEMBL5592263 | — | — | 1 | 6.30 |
| CHEMBL5575136 | — | — | 1 | 6.11 |
| CHEMBL5549871 | — | — | 1 | 5.80 |
| CHEMBL5573742 | — | — | 1 | - |
| CHEMBL5181633 | — | — | 1 | - |
| CHEMBL5590315 | — | — | 1 | - |
| CHEMBL5557583 | — | — | 1 | - |
| CHEMBL5572451 | — | — | 1 | - |
| CHEMBL5573249 | — | — | 1 | - |
| CHEMBL5594768 | — | — | 1 | - |
| CHEMBL5593633 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237245 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5571025 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL5570595 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL3237245 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5595521 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL5567570 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL5567314 | — | Ki | = | 32.2 | nM | 7.49 |
| CHEMBL5556087 | — | Ki | = | 41.4 | nM | 7.38 |
| CHEMBL5569386 | — | Ki | = | 50.7 | nM | 7.29 |
| CHEMBL5555837 | — | Ki | = | 66.1 | nM | 7.18 |
| CHEMBL5573658 | — | Ki | = | 74.2 | nM | 7.13 |
| CHEMBL5564155 | — | Ki | = | 78.3 | nM | 7.11 |
| CHEMBL5574547 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL5590204 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL5571910 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL5172581 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL5563080 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL5583856 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL5543048 | — | Ki | = | 452.0 | nM | 6.34 |
| CHEMBL5592263 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5575136 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL5549871 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL5573742 | — | Ki | - | — | - | |
| CHEMBL5181633 | — | Ki | - | — | - | |
| CHEMBL5590315 | — | Ki | - | — | - | |
| CHEMBL5557583 | — | Ki | - | — | - | |
| CHEMBL5572451 | — | Ki | - | — | - | |
| CHEMBL5573249 | — | Ki | - | — | - | |
| CHEMBL5594768 | — | Ki | - | — | - | |
| CHEMBL5593633 | — | Ki | - | — | - |