Assay Detail
Binding
CHEMBL5344124
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Binding affinity to recombinant BRD2 BD1 (unknown origin) assessed as dissociation constant measured for 1200 sec by bio-layer interferometry streptavidin sensor based assay
4
Total Activities
4
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 |
Publication
Precise Conformational Control Yielding Highly Potent and Exceptionally Selective BRD4 Degraders with Strong Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 7.32 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5406183 | — | — | 1 | 8.08 |
| CHEMBL5409305 | — | — | 1 | 7.41 |
| CHEMBL4555209 | — | — | 1 | 6.92 |
| CHEMBL5421103 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5406183 | — | Kd | = | 8.3 | nM | 8.08 |
| CHEMBL5409305 | — | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL4555209 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL5421103 | — | Kd | = | 140.0 | nM | 6.85 |