Assay Detail
Binding
CHEMBL2406877
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Displacement of MR121-Nrf2 from human N-terminal His-tagged Kelch-DC domain of Keap1 (321 to 609) expressed in Escherichia coli BL21 (DE3) after 40 mins by 2D-FIDA assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Kelch-like ECH-associated protein 1 (CHEMBL2069156) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.53 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2402205 | — | — | 1 | 7.48 |
| CHEMBL2402207 | — | — | 1 | 5.57 |
| CHEMBL2402206 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2402205 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2402207 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2402206 | — | IC50 | = | 118000.0 | nM | - |