Assay Detail
Binding
CHEMBL4307109
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Activation of ED-tagged Nrf2 in human U2OS cells co-expressing Keap1 assessed as induction of NRF2 translocation to nucleus after 6 hrs by beta-galactosidase based chemiluminescent assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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
Antioxidant, Anti-inflammatory, and Neuroprotective Effects of Novel Vinyl Sulfonate Compounds as Nrf2 Activator.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.12 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4584457 | — | — | 1 | 7.12 |
| CHEMBL4444710 | — | — | 1 | 6.78 |
| CHEMBL4468759 | — | — | 1 | 6.62 |
| CHEMBL48802 | SULFORAPHANE | 3.0 | 1 | 6.24 |
| CHEMBL4526321 | — | — | 1 | 6.16 |
| CHEMBL4461002 | — | — | 1 | 6.03 |
| CHEMBL4438169 | — | — | 1 | 6.02 |
| CHEMBL443343 | — | — | 1 | 5.98 |
| CHEMBL4563801 | — | — | 1 | 5.94 |
| CHEMBL4435986 | — | — | 1 | 5.88 |
| CHEMBL469941 | — | — | 1 | 5.83 |
| CHEMBL4567717 | — | — | 1 | 5.75 |
| CHEMBL4446359 | — | — | 1 | 5.20 |
| CHEMBL4464048 | — | — | 1 | - |
| CHEMBL4545539 | — | — | 1 | - |
| CHEMBL4576084 | — | — | 1 | - |
| CHEMBL463270 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4584457 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4444710 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4468759 | — | EC50 | = | 237.0 | nM | 6.62 |
| CHEMBL48802 | SULFORAPHANE | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4526321 | — | EC50 | = | 698.0 | nM | 6.16 |
| CHEMBL4461002 | — | EC50 | = | 943.0 | nM | 6.03 |
| CHEMBL4438169 | — | EC50 | = | 948.0 | nM | 6.02 |
| CHEMBL443343 | — | EC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4563801 | — | EC50 | = | 1155.0 | nM | 5.94 |
| CHEMBL4435986 | — | EC50 | = | 1334.0 | nM | 5.88 |
| CHEMBL469941 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL4567717 | — | EC50 | = | 1778.0 | nM | 5.75 |
| CHEMBL4446359 | — | EC50 | = | 6350.0 | nM | 5.20 |
| CHEMBL4464048 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4545539 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4576084 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL463270 | — | EC50 | > | 10000.0 | nM | - |