Assay Detail
Binding
CHEMBL5217617
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Binding affinity to Keap1 kelch domain (unknown origin) by surface plasmon resonance assay
41
Total Activities
38
Compounds Tested
2
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
Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 36 | 3.29 | 9.15 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4643134 | — | — | 1 | 9.15 |
| CHEMBL3358228 | — | — | 1 | 4.08 |
| CHEMBL5218656 | — | — | 1 | 3.66 |
| CHEMBL5220573 | — | — | 1 | 3.52 |
| CHEMBL158697 | — | — | 1 | 3.52 |
| CHEMBL5219654 | — | — | 1 | 3.32 |
| CHEMBL1486504 | — | — | 2 | 3.27 |
| CHEMBL5218868 | — | — | 1 | 3.25 |
| CHEMBL4585642 | — | — | 1 | 3.22 |
| CHEMBL5219398 | — | — | 2 | 3.10 |
| CHEMBL5219152 | — | — | 2 | 3.09 |
| CHEMBL1230159 | — | — | 1 | 3.08 |
| CHEMBL5218920 | — | — | 1 | 3.07 |
| CHEMBL5220217 | — | — | 1 | 3.05 |
| CHEMBL5220238 | — | — | 1 | 3.05 |
| CHEMBL5218944 | — | — | 1 | 3.00 |
| CHEMBL4856216 | — | — | 1 | 3.00 |
| CHEMBL1874593 | — | — | 1 | 3.00 |
| CHEMBL3187039 | — | — | 1 | 3.00 |
| CHEMBL5219344 | — | — | 1 | 2.96 |
| CHEMBL5218544 | — | — | 1 | 2.92 |
| CHEMBL4868334 | — | — | 1 | 2.92 |
| CHEMBL190660 | — | — | 1 | 2.80 |
| CHEMBL5219161 | — | — | 1 | 2.77 |
| CHEMBL1555771 | — | — | 1 | 2.75 |
| CHEMBL2018159 | — | — | 1 | 2.75 |
| CHEMBL5220089 | — | — | 1 | 2.75 |
| CHEMBL5220689 | — | — | 1 | 2.48 |
| CHEMBL5219525 | — | — | 1 | - |
| CHEMBL5219260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4643134 | — | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL3358228 | — | Kd | = | 84000.0 | nM | 4.08 |
| CHEMBL5218656 | — | Kd | = | 220000.0 | nM | 3.66 |
| CHEMBL5220573 | — | Kd | = | 300000.0 | nM | 3.52 |
| CHEMBL158697 | — | Kd | = | 300000.0 | nM | 3.52 |
| CHEMBL5219654 | — | Kd | = | 480000.0 | nM | 3.32 |
| CHEMBL1486504 | — | Kd | = | 540000.0 | nM | 3.27 |
| CHEMBL1486504 | — | Kd | = | 540000.0 | nM | 3.27 |
| CHEMBL5218868 | — | Kd | = | 560000.0 | nM | 3.25 |
| CHEMBL4585642 | — | Kd | = | 600000.0 | nM | 3.22 |
| CHEMBL5219398 | — | Kd | = | 790000.0 | nM | 3.10 |
| CHEMBL5219398 | — | Kd | = | 790000.0 | nM | 3.10 |
| CHEMBL5219152 | — | Kd | = | 820000.0 | nM | 3.09 |
| CHEMBL5219152 | — | Kd | = | 820000.0 | nM | 3.09 |
| CHEMBL1230159 | — | Kd | = | 840000.0 | nM | 3.08 |
| CHEMBL5218920 | — | Kd | = | 850000.0 | nM | 3.07 |
| CHEMBL5220217 | — | Kd | = | 900000.0 | nM | 3.05 |
| CHEMBL5220238 | — | Kd | = | 900000.0 | nM | 3.05 |
| CHEMBL3187039 | — | Kd | = | 1000000.0 | nM | 3.00 |
| CHEMBL4856216 | — | Kd | = | 1000000.0 | nM | 3.00 |
| CHEMBL5218944 | — | Kd | = | 1000000.0 | nM | 3.00 |
| CHEMBL1874593 | — | Kd | = | 1000000.0 | nM | 3.00 |
| CHEMBL5219344 | — | Kd | = | 1100000.0 | nM | 2.96 |
| CHEMBL4868334 | — | Kd | = | 1200000.0 | nM | 2.92 |
| CHEMBL5218544 | — | Kd | = | 1200000.0 | nM | 2.92 |
| CHEMBL190660 | — | Kd | = | 1600000.0 | nM | 2.80 |
| CHEMBL5219161 | — | Kd | = | 1700000.0 | nM | 2.77 |
| CHEMBL2018159 | — | Kd | = | 1800000.0 | nM | 2.75 |
| CHEMBL5220089 | — | Kd | = | 1800000.0 | nM | 2.75 |
| CHEMBL1555771 | — | Kd | = | 1800000.0 | nM | 2.75 |
| CHEMBL5220689 | — | Kd | = | 3300000.0 | nM | 2.48 |
| CHEMBL5219196 | — | Kd | = | 360000000.0 | nM | - |
| CHEMBL5219260 | — | Kd | = | 350000000.0 | nM | - |
| CHEMBL5219525 | — | Kd | = | 350000000.0 | nM | - |
| CHEMBL5218914 | — | Activity | - | — | - | |
| CHEMBL1404172 | — | Activity | - | — | - | |
| CHEMBL5218773 | — | Activity | - | — | - | |
| CHEMBL5219387 | — | Activity | - | — | - | |
| CHEMBL5218662 | — | Kd | = | 310000000.0 | nM | - |
| CHEMBL1303660 | — | Kd | = | 190000000.0 | nM | - |
| CHEMBL5220047 | — | Activity | - | — | - |