Assay Detail
Binding
CHEMBL5036178
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Binding affinity to N-terminal His6-tagged VHL (54 to 213 residues)/BRD4 BD2 (333 to 460 residues) (unknown origin) expressed in Escherichia coli assessed as displacement of HIF-1alpha preincubated with Brd4 BD2 by ternary binding competitive fluorescence polarization assay
8
Total Activities
8
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 |
Target
von Hippel-Lindau disease tumor suppressor/Bromodomain-containing protein 4 (CHEMBL4296140) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| 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 | 8 | 7.98 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215078 | — | — | 1 | 8.60 |
| CHEMBL5074720 | — | — | 1 | 8.52 |
| CHEMBL5075400 | — | — | 1 | 8.43 |
| CHEMBL5087181 | — | — | 1 | 8.14 |
| CHEMBL5086339 | — | — | 1 | 7.75 |
| CHEMBL5079045 | — | — | 1 | 7.68 |
| CHEMBL4226570 | — | — | 1 | 7.41 |
| CHEMBL5081695 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215078 | — | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL5074720 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5075400 | — | Kd | = | 3.7 | nM | 8.43 |
| CHEMBL5087181 | — | Kd | = | 7.3 | nM | 8.14 |
| CHEMBL5086339 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL5079045 | — | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL4226570 | — | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL5081695 | — | Kd | = | 54.0 | nM | 7.27 |