Assay Detail
Binding
CHEMBL4835524
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of interaction between human KEAP1 Kelch domain/FAM-Nrf2 using Cy5-Nrf2 incubated for 10 to 15 mins by competitive fluorescence polarization assay
56
Total Activities
56
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
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 56 | 5.44 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4860934 | — | — | 1 | 7.40 |
| CHEMBL4857893 | — | — | 1 | 7.10 |
| CHEMBL4861831 | — | — | 1 | 7.01 |
| CHEMBL4847104 | — | — | 1 | 6.89 |
| CHEMBL4847787 | — | — | 1 | 6.77 |
| CHEMBL4856469 | — | — | 1 | 6.68 |
| CHEMBL4850809 | — | — | 1 | 6.47 |
| CHEMBL4861607 | — | — | 1 | 6.43 |
| CHEMBL4872361 | — | — | 1 | 6.40 |
| CHEMBL4875171 | — | — | 1 | 6.28 |
| CHEMBL4860948 | — | — | 1 | 6.24 |
| CHEMBL4847150 | — | — | 1 | 6.20 |
| CHEMBL4865528 | — | — | 1 | 6.18 |
| CHEMBL4868608 | — | — | 1 | 6.14 |
| CHEMBL4867014 | — | — | 1 | 5.96 |
| CHEMBL4863502 | — | — | 1 | 5.85 |
| CHEMBL4866786 | — | — | 1 | 5.82 |
| CHEMBL4872869 | — | — | 1 | 5.82 |
| CHEMBL4856515 | — | — | 1 | 5.72 |
| CHEMBL4860409 | — | — | 1 | 5.66 |
| CHEMBL4865784 | — | — | 1 | 5.58 |
| CHEMBL4847187 | — | — | 1 | 5.57 |
| CHEMBL4852755 | — | — | 1 | 5.47 |
| CHEMBL4865277 | — | — | 1 | 5.34 |
| CHEMBL4872029 | — | — | 1 | 5.22 |
| CHEMBL4851543 | — | — | 1 | 5.03 |
| CHEMBL4875014 | — | — | 1 | 5.01 |
| CHEMBL4850911 | — | — | 1 | 4.91 |
| CHEMBL4848597 | — | — | 1 | 4.89 |
| CHEMBL4867068 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4860934 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4857893 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL4861831 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4847104 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4847787 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4856469 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4850809 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4861607 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL4872361 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL4875171 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL4860948 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL4847150 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL4865528 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL4868608 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL4867014 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4863502 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL4866786 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4872869 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4856515 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL4860409 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4865784 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL4847187 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL4852755 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL4865277 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL4872029 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL4851543 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL4875014 | — | Ki | = | 9700.0 | nM | 5.01 |
| CHEMBL4850911 | — | Ki | = | 12300.0 | nM | 4.91 |
| CHEMBL4848597 | — | Ki | = | 12800.0 | nM | 4.89 |
| CHEMBL4867068 | — | Ki | = | 15300.0 | nM | 4.82 |
| CHEMBL4865680 | — | Ki | = | 15600.0 | nM | 4.81 |
| CHEMBL4877966 | — | Ki | = | 23200.0 | nM | 4.63 |
| CHEMBL4864348 | — | Ki | = | 24800.0 | nM | 4.61 |
| CHEMBL4869426 | — | Ki | = | 26900.0 | nM | 4.57 |
| CHEMBL4878476 | — | Ki | = | 41200.0 | nM | 4.38 |
| CHEMBL4860520 | — | Ki | = | 75400.0 | nM | 4.12 |
| CHEMBL4861791 | — | Ki | = | 75700.0 | nM | 4.12 |
| CHEMBL4871793 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL4877778 | — | Ki | = | 164000.0 | nM | 3.79 |
| CHEMBL4879253 | — | Ki | = | 3100000.0 | nM | 2.51 |
| CHEMBL4867889 | — | Ki | = | 3500000.0 | nM | 2.46 |
| CHEMBL4876390 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4878728 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4851549 | — | Ki | = | 672000.0 | nM | - |
| CHEMBL4872323 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4859696 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4859873 | — | Ki | > | 4000000.0 | nM | - |
| CHEMBL4858927 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4869188 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL4868310 | — | Ki | = | 194000.0 | nM | - |