Assay Detail
Binding
CHEMBL4152128
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Inhibition of Keap1 Kelch domain (unknown origin) /Nrf2 (unknown origin) interaction using fluorescein-labeled 9-mer peptide containing NRF2 Neh2 domain ETGE motif by fluorescence anisotropy assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Intermediate |
Publication
Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear Factor (Erythroid-derived 2)-like 2 (NRF2) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.61 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237245 | — | — | 1 | 7.60 |
| CHEMBL4174651 | — | — | 1 | 7.22 |
| CHEMBL3632711 | — | — | 1 | 7.20 |
| CHEMBL4166445 | — | — | 1 | 7.00 |
| CHEMBL2402207 | — | — | 1 | 6.03 |
| CHEMBL3600957 | — | — | 1 | 6.01 |
| CHEMBL4173296 | — | — | 1 | 5.96 |
| CHEMBL4169869 | — | — | 1 | 5.89 |
| CHEMBL4160703 | — | — | 1 | - |
| CHEMBL4176664 | — | — | 1 | - |
| CHEMBL4166048 | — | — | 1 | - |
| CHEMBL4162602 | — | — | 1 | - |
| CHEMBL4159226 | — | — | 1 | - |
| CHEMBL4171299 | — | — | 1 | - |
| CHEMBL4166752 | — | — | 1 | - |
| CHEMBL4176126 | — | — | 1 | - |
| CHEMBL3632890 | — | — | 1 | - |
| CHEMBL4174360 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237245 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4174651 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3632711 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4166445 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL2402207 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3600957 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4173296 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4169869 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4160703 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4176664 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4166048 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4162602 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4159226 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4171299 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4166752 | — | IC50 | - | — | - | |
| CHEMBL4176126 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL3632890 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4174360 | — | IC50 | > | 25000.0 | nM | - |