Assay Detail
Binding
CHEMBL3870929
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Inhibition of recombinant GST-His-tagged Keap1-DC domain (321 to 609 residues) (unknown origin) expressed in Escherichia coli/FAM-labeled Nrf2 (unknown origin) interaction measured after 30 mins by fluorescence polarization assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis of Keap1-phosphorylated p62 and Keap1-Nrf2 protein-protein interaction inhibitors and their inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.07 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3962296 | — | — | 1 | 6.82 |
| CHEMBL3925906 | — | — | 1 | 6.70 |
| CHEMBL3928944 | — | — | 1 | 6.64 |
| CHEMBL3906697 | — | — | 1 | 6.50 |
| CHEMBL3953535 | — | — | 1 | 6.14 |
| CHEMBL3934789 | — | — | 1 | 5.89 |
| CHEMBL2402207 | — | — | 1 | 5.75 |
| CHEMBL3939457 | — | — | 1 | 5.55 |
| CHEMBL3977467 | — | — | 1 | 5.50 |
| CHEMBL3948237 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3962296 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3925906 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3928944 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3906697 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3953535 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3934789 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2402207 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3939457 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3977467 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3948237 | — | IC50 | = | 6200.0 | nM | 5.21 |