Assay Detail
Binding
CHEMBL4141610
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Inhibition of FITC-labeled Nrf2 binding to human Keap1 Kelch domain (322 to 609 residues) expressed in Escherichia coli (DE3) after 30 mins 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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Kelch-like ECH-associated protein 1 (CHEMBL2069156) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a head-to-tail cyclic peptide as the Keap1-Nrf2 protein-protein interaction inhibitor with high cell potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.47 | 7.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4169002 | — | — | 1 | 7.74 |
| CHEMBL4174405 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4169002 | — | IC50 | = | 18.31 | nM | 7.74 |
| CHEMBL4174405 | — | IC50 | = | 63.15 | nM | 7.20 |