Assay Detail
Binding
CHEMBL4386553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of Nrf2 in human BEAS2B cells assessed as increase in NQO1 enzymatic activity measured after 48 hrs by MTT assay
10
Total Activities
10
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
Nuclear factor erythroid 2-related factor 2 (CHEMBL1075094) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.37 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4450921 | — | — | 1 | 7.96 |
| CHEMBL4447060 | — | — | 1 | 7.52 |
| CHEMBL4578025 | — | — | 1 | 7.08 |
| CHEMBL4540327 | — | — | 1 | 6.24 |
| CHEMBL4457466 | — | — | 1 | 6.12 |
| CHEMBL4554007 | — | — | 1 | 6.07 |
| CHEMBL4567490 | — | — | 1 | 5.85 |
| CHEMBL4464511 | — | — | 1 | 5.80 |
| CHEMBL4454051 | — | — | 1 | 5.54 |
| CHEMBL4473977 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4450921 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4447060 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4578025 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4540327 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4457466 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4554007 | — | EC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4567490 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4464511 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4454051 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4473977 | — | EC50 | = | 3400.0 | nM | 5.47 |