Assay Detail
Binding
CHEMBL4331808
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of 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
54
Total Activities
54
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
Optimization of Vinyl Sulfone Derivatives as Potent Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Parkinson's Disease Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 54 | 5.98 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4585959 | — | — | 1 | 7.01 |
| CHEMBL4565846 | — | — | 1 | 6.91 |
| CHEMBL4575846 | — | — | 1 | 6.88 |
| CHEMBL4561432 | — | — | 1 | 6.85 |
| CHEMBL4534364 | — | — | 1 | 6.83 |
| CHEMBL4590075 | — | — | 1 | 6.75 |
| CHEMBL4467057 | — | — | 1 | 6.70 |
| CHEMBL4473995 | — | — | 1 | 6.61 |
| CHEMBL4578412 | — | — | 1 | 6.49 |
| CHEMBL4563234 | — | — | 1 | 6.46 |
| CHEMBL4465428 | — | — | 1 | 6.46 |
| CHEMBL4455181 | — | — | 1 | 6.46 |
| CHEMBL4565692 | — | — | 1 | 6.46 |
| CHEMBL4552886 | — | — | 1 | 6.35 |
| CHEMBL3125749 | — | — | 1 | 6.28 |
| CHEMBL48802 | SULFORAPHANE | 3.0 | 1 | 6.24 |
| CHEMBL4475115 | — | — | 1 | 6.18 |
| CHEMBL4463072 | — | — | 1 | 6.11 |
| CHEMBL4439975 | — | — | 1 | 6.07 |
| CHEMBL4457010 | — | — | 1 | 6.06 |
| CHEMBL4541592 | — | — | 1 | 6.04 |
| CHEMBL4459567 | — | — | 1 | 6.02 |
| CHEMBL4564090 | — | — | 1 | 6.00 |
| CHEMBL4457276 | — | — | 1 | 5.96 |
| CHEMBL4575585 | — | — | 1 | 5.94 |
| CHEMBL4467316 | — | — | 1 | 5.92 |
| CHEMBL4455621 | — | — | 1 | 5.92 |
| CHEMBL4438395 | — | — | 1 | 5.82 |
| CHEMBL4522696 | — | — | 1 | 5.66 |
| CHEMBL4439009 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4585959 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4565846 | — | EC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4575846 | — | EC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4561432 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4534364 | — | EC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4590075 | — | EC50 | = | 178.0 | nM | 6.75 |
| CHEMBL4467057 | — | EC50 | = | 202.0 | nM | 6.70 |
| CHEMBL4473995 | — | EC50 | = | 246.0 | nM | 6.61 |
| CHEMBL4578412 | — | EC50 | = | 327.0 | nM | 6.49 |
| CHEMBL4563234 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4465428 | — | EC50 | = | 346.0 | nM | 6.46 |
| CHEMBL4455181 | — | EC50 | = | 347.0 | nM | 6.46 |
| CHEMBL4565692 | — | EC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4552886 | — | EC50 | = | 444.0 | nM | 6.35 |
| CHEMBL3125749 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL48802 | SULFORAPHANE | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4475115 | — | EC50 | = | 655.0 | nM | 6.18 |
| CHEMBL4463072 | — | EC50 | = | 786.0 | nM | 6.11 |
| CHEMBL4439975 | — | EC50 | = | 849.0 | nM | 6.07 |
| CHEMBL4457010 | — | EC50 | = | 877.0 | nM | 6.06 |
| CHEMBL4541592 | — | EC50 | = | 908.0 | nM | 6.04 |
| CHEMBL4459567 | — | EC50 | = | 955.0 | nM | 6.02 |
| CHEMBL4564090 | — | EC50 | = | 1007.0 | nM | 6.00 |
| CHEMBL4457276 | — | EC50 | = | 1083.0 | nM | 5.96 |
| CHEMBL4575585 | — | EC50 | = | 1155.0 | nM | 5.94 |
| CHEMBL4467316 | — | EC50 | = | 1204.0 | nM | 5.92 |
| CHEMBL4455621 | — | EC50 | = | 1198.0 | nM | 5.92 |
| CHEMBL4438395 | — | EC50 | = | 1517.0 | nM | 5.82 |
| CHEMBL4522696 | — | EC50 | = | 2171.0 | nM | 5.66 |
| CHEMBL4439009 | — | EC50 | = | 2642.0 | nM | 5.58 |
| CHEMBL4534415 | — | EC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL4462796 | — | EC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL4466191 | — | EC50 | = | 6287.0 | nM | 5.20 |
| CHEMBL4518418 | — | EC50 | = | 6312.0 | nM | 5.20 |
| CHEMBL4544775 | — | EC50 | = | 6845.0 | nM | 5.17 |
| CHEMBL4455036 | — | EC50 | = | 7021.0 | nM | 5.15 |
| CHEMBL4447883 | — | EC50 | = | 7383.0 | nM | 5.13 |
| CHEMBL4565873 | — | EC50 | = | 7610.0 | nM | 5.12 |
| CHEMBL4514932 | — | EC50 | = | 7978.0 | nM | 5.10 |
| CHEMBL4459514 | — | EC50 | = | 8659.0 | nM | 5.06 |
| CHEMBL4469709 | — | EC50 | = | 9070.0 | nM | 5.04 |
| CHEMBL4585054 | — | EC50 | = | 9355.0 | nM | 5.03 |
| CHEMBL4457860 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4448848 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4460009 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4436436 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4581037 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4560990 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4461918 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4473139 | — | EC50 | > | 10000.0 | nM | - |