Assay Detail
Binding
CHEMBL5393048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of Nrf2 in human PathHunter U2OS Keap1-Nrf2 cells assessed as Nrf2 nuclear translocation by chemiluminescent assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PathHunter U2OS Keap1-NRF2 Nuclear Translocation |
| 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
Tuning the Reactivity of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Optimal <i>in Vivo</i> Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.35 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5437928 | — | — | 1 | 7.70 |
| CHEMBL5408914 | — | — | 1 | 6.52 |
| CHEMBL5440555 | — | — | 1 | 6.44 |
| CHEMBL5433953 | — | — | 1 | 6.05 |
| CHEMBL5425309 | — | — | 1 | 5.36 |
| CHEMBL2107333 | DIMETHYL FUMARATE | 4.0 | 1 | 5.10 |
| CHEMBL5393772 | — | — | 1 | 5.06 |
| CHEMBL5413156 | — | — | 1 | 4.98 |
| CHEMBL5430762 | — | — | 1 | 4.49 |
| CHEMBL5422691 | — | — | 1 | 4.30 |
| CHEMBL5415198 | — | — | 1 | 4.21 |
| CHEMBL5393827 | — | — | 1 | 4.02 |
| CHEMBL589586 | MONOMETHYL FUMARATE | 4.0 | 1 | - |
| CHEMBL5404675 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5437928 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5408914 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5440555 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5433953 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5425309 | — | EC50 | = | 4420.0 | nM | 5.36 |
| CHEMBL2107333 | DIMETHYL FUMARATE | EC50 | = | 7930.0 | nM | 5.10 |
| CHEMBL5393772 | — | EC50 | = | 8720.0 | nM | 5.06 |
| CHEMBL5413156 | — | EC50 | = | 10450.0 | nM | 4.98 |
| CHEMBL5430762 | — | EC50 | = | 32410.0 | nM | 4.49 |
| CHEMBL5422691 | — | EC50 | = | 50040.0 | nM | 4.30 |
| CHEMBL5415198 | — | EC50 | = | 60900.0 | nM | 4.21 |
| CHEMBL5393827 | — | EC50 | = | 95240.0 | nM | 4.02 |
| CHEMBL589586 | MONOMETHYL FUMARATE | EC50 | = | 127200.0 | nM | - |
| CHEMBL5404675 | — | EC50 | > | 100000.0 | nM | - |