Assay Detail
Binding
CHEMBL4367553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of FITC-LDEETGEFL-NH2 from human KEAP1 Kelch domain (322 to 609 residues) measured after 30 mins by fluorescence polarization assay
38
Total Activities
38
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
Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 5.52 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588743 | — | — | 1 | 7.37 |
| CHEMBL3899754 | — | — | 1 | 6.85 |
| CHEMBL4440603 | — | — | 1 | 6.52 |
| CHEMBL4522423 | — | — | 1 | 6.35 |
| CHEMBL4438752 | — | — | 1 | 6.26 |
| CHEMBL4462141 | — | — | 1 | 6.23 |
| CHEMBL4535811 | — | — | 1 | 5.97 |
| CHEMBL4590033 | — | — | 1 | 5.95 |
| CHEMBL4441181 | — | — | 1 | 5.89 |
| CHEMBL4457575 | — | — | 1 | 5.88 |
| CHEMBL4445846 | — | — | 1 | 5.83 |
| CHEMBL4564764 | — | — | 1 | 5.80 |
| CHEMBL4587621 | — | — | 1 | 5.56 |
| CHEMBL4576001 | — | — | 1 | 5.48 |
| CHEMBL4515546 | — | — | 1 | 5.37 |
| CHEMBL4527377 | — | — | 1 | 5.37 |
| CHEMBL4471657 | — | — | 1 | 5.15 |
| CHEMBL4450491 | — | — | 1 | 5.14 |
| CHEMBL4439070 | — | — | 1 | 5.00 |
| CHEMBL4466277 | — | — | 1 | 4.96 |
| CHEMBL4446724 | — | — | 1 | 4.91 |
| CHEMBL4438367 | — | — | 1 | 4.86 |
| CHEMBL4518400 | — | — | 1 | 4.83 |
| CHEMBL4474076 | — | — | 1 | 4.80 |
| CHEMBL4461055 | — | — | 1 | 4.74 |
| CHEMBL4529979 | — | — | 1 | 4.56 |
| CHEMBL4454849 | — | — | 1 | 4.48 |
| CHEMBL4573058 | — | — | 1 | 4.47 |
| CHEMBL4470508 | — | — | 1 | - |
| CHEMBL4455435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588743 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3899754 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4440603 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4522423 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4438752 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4462141 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4535811 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL4590033 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL4441181 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4457575 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4445846 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL4564764 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL4587621 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL4576001 | — | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL4527377 | — | IC50 | = | 4280.0 | nM | 5.37 |
| CHEMBL4515546 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL4471657 | — | IC50 | = | 7010.0 | nM | 5.15 |
| CHEMBL4450491 | — | IC50 | = | 7260.0 | nM | 5.14 |
| CHEMBL4439070 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL4466277 | — | IC50 | = | 11010.0 | nM | 4.96 |
| CHEMBL4446724 | — | IC50 | = | 12370.0 | nM | 4.91 |
| CHEMBL4438367 | — | IC50 | = | 13760.0 | nM | 4.86 |
| CHEMBL4518400 | — | IC50 | = | 14790.0 | nM | 4.83 |
| CHEMBL4474076 | — | IC50 | = | 15920.0 | nM | 4.80 |
| CHEMBL4461055 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL4529979 | — | IC50 | = | 27740.0 | nM | 4.56 |
| CHEMBL4454849 | — | IC50 | = | 33280.0 | nM | 4.48 |
| CHEMBL4573058 | — | IC50 | = | 33900.0 | nM | 4.47 |
| CHEMBL4562295 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4514275 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4552364 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4469680 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4465581 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4561918 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4457780 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4462357 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4455435 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4470508 | — | IC50 | > | 50000.0 | nM | - |