Assay Detail
Binding
CHEMBL3602923
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Inhibition of Keap1 Kelch domain-Nrf2 ETGE (unknown origin) protein-protein interaction incubated for 30 mins by fluorescence polarization competition assay
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
Structure-Activity and Structure-Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1-Nrf2 Protein-Protein Interaction Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.81 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3601212 | — | — | 1 | 7.84 |
| CHEMBL3601208 | — | — | 1 | 7.74 |
| CHEMBL3237245 | — | — | 1 | 7.51 |
| CHEMBL3601215 | — | — | 1 | 7.46 |
| CHEMBL3601211 | — | — | 1 | 7.44 |
| CHEMBL3601221 | — | — | 1 | 7.38 |
| CHEMBL3601210 | — | — | 1 | 7.37 |
| CHEMBL3601217 | — | — | 1 | 7.32 |
| CHEMBL3601213 | — | — | 1 | 7.30 |
| CHEMBL3601209 | — | — | 1 | 7.26 |
| CHEMBL3601219 | — | — | 1 | 7.18 |
| CHEMBL3601220 | — | — | 1 | 6.93 |
| CHEMBL3601218 | — | — | 1 | 6.91 |
| CHEMBL3601216 | — | — | 1 | 6.75 |
| CHEMBL3600394 | — | — | 1 | 6.22 |
| CHEMBL3601214 | — | — | 1 | 6.01 |
| CHEMBL3601205 | — | — | 1 | 6.01 |
| CHEMBL3600957 | — | — | 1 | 5.84 |
| CHEMBL3601206 | — | — | 1 | 5.78 |
| CHEMBL3601222 | — | — | 1 | 5.73 |
| CHEMBL3601207 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3601212 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL3601208 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL3237245 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL3601215 | — | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL3601211 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL3601221 | — | IC50 | = | 42.2 | nM | 7.38 |
| CHEMBL3601210 | — | IC50 | = | 42.3 | nM | 7.37 |
| CHEMBL3601217 | — | IC50 | = | 47.4 | nM | 7.32 |
| CHEMBL3601213 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL3601209 | — | IC50 | = | 54.3 | nM | 7.26 |
| CHEMBL3601219 | — | IC50 | = | 66.1 | nM | 7.18 |
| CHEMBL3601220 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL3601218 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3601216 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL3600394 | — | IC50 | = | 602.0 | nM | 6.22 |
| CHEMBL3601214 | — | IC50 | = | 979.0 | nM | 6.01 |
| CHEMBL3601205 | — | IC50 | = | 966.0 | nM | 6.01 |
| CHEMBL3600957 | — | IC50 | = | 1448.0 | nM | 5.84 |
| CHEMBL3601206 | — | IC50 | = | 1666.0 | nM | 5.78 |
| CHEMBL3601222 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL3601207 | — | IC50 | = | 10170.0 | nM | 4.99 |