Assay Detail
Binding
CHEMBL5036171
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Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues) (unknown origin) expressed in Escherichia coli assessed as displacement of HIF-1alpha by fluorescence polarization assay
9
Total Activities
9
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
von Hippel-Lindau disease tumor suppressor (CHEMBL3108660) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 6.82 | 6.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3344081 | — | — | 1 | 6.95 |
| CHEMBL5087145 | — | — | 1 | 6.92 |
| CHEMBL5082521 | — | — | 1 | 6.87 |
| CHEMBL4793272 | — | — | 1 | 6.86 |
| CHEMBL5081396 | — | — | 1 | 6.84 |
| CHEMBL5087530 | — | — | 1 | 6.77 |
| CHEMBL5094871 | — | — | 1 | 6.77 |
| CHEMBL5086047 | — | — | 1 | 6.70 |
| CHEMBL5086897 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3344081 | — | Kd | = | 113.0 | nM | 6.95 |
| CHEMBL5087145 | — | Kd | = | 119.0 | nM | 6.92 |
| CHEMBL5082521 | — | Kd | = | 136.0 | nM | 6.87 |
| CHEMBL4793272 | — | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL5081396 | — | Kd | = | 144.0 | nM | 6.84 |
| CHEMBL5087530 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL5094871 | — | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL5086047 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL5086897 | — | Kd | = | 200.0 | nM | 6.70 |