Assay Detail
Binding
CHEMBL4615773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of AF647-9-mer ETGE peptide from recombinant human biotinylated KEAP1 Kelch domain (322 to 609 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins followed by AF647-9-mer ETGE peptide addition and measured after 60 mins by TR-FRET assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Kelch-like ECH-associated protein 1 (CHEMBL2069156) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.82 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639381 | — | — | 1 | 7.01 |
| CHEMBL4636738 | — | — | 1 | 6.74 |
| CHEMBL3134422 | — | — | 1 | 6.70 |
| CHEMBL4634711 | — | — | 1 | 6.59 |
| CHEMBL2381968 | — | — | 1 | 6.10 |
| CHEMBL4638389 | — | — | 1 | 6.06 |
| CHEMBL4645065 | — | — | 1 | 5.89 |
| CHEMBL4645109 | — | — | 1 | 5.81 |
| CHEMBL4642536 | — | — | 1 | 5.70 |
| CHEMBL4648717 | — | — | 1 | 5.59 |
| CHEMBL4642135 | — | — | 1 | 5.57 |
| CHEMBL4649380 | — | — | 1 | 5.51 |
| CHEMBL4639835 | — | — | 1 | 5.33 |
| CHEMBL4635272 | — | — | 1 | 5.26 |
| CHEMBL4641843 | — | — | 1 | 5.26 |
| CHEMBL4647979 | — | — | 1 | 5.23 |
| CHEMBL4633579 | — | — | 1 | 4.54 |
| CHEMBL4637259 | — | — | 1 | - |
| CHEMBL4638535 | — | — | 1 | - |
| CHEMBL4648472 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639381 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4636738 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3134422 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4634711 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL2381968 | — | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL4638389 | — | IC50 | = | 862.0 | nM | 6.06 |
| CHEMBL4645065 | — | IC50 | = | 1275.0 | nM | 5.89 |
| CHEMBL4645109 | — | IC50 | = | 1558.0 | nM | 5.81 |
| CHEMBL4642536 | — | IC50 | = | 1976.0 | nM | 5.70 |
| CHEMBL4648717 | — | IC50 | = | 2545.0 | nM | 5.59 |
| CHEMBL4642135 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4649380 | — | IC50 | = | 3102.0 | nM | 5.51 |
| CHEMBL4639835 | — | IC50 | = | 4682.0 | nM | 5.33 |
| CHEMBL4635272 | — | IC50 | = | 5456.0 | nM | 5.26 |
| CHEMBL4641843 | — | IC50 | = | 5539.0 | nM | 5.26 |
| CHEMBL4647979 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4633579 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL4637259 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL4638535 | — | IC50 | > | 64000.0 | nM | - |
| CHEMBL4648472 | — | IC50 | > | 50000.0 | nM | - |