Assay Detail
Binding
CHEMBL5528631
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Inhibition of human Keap1 KELCH domain (321 to 609 residues) expressed in Escherichia coli BL21 DE3 pLysS cells/Nrf2 (unknown origin) protein-protein interaction preincubated with Keap1 for 1 hr followed by Nrf2 addition and measured after 1 hr by fluorescence polarization assay
2
Total Activities
2
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
Recent progress and applications of small molecule inhibitors of Keap1-Nrf2 axis for neurodegenerative diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.01 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237245 | — | — | 1 | 8.43 |
| CHEMBL5556774 | — | — | 1 | 7.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237245 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5556774 | — | IC50 | = | 25.7 | nM | 7.59 |