Assay Detail
Binding
CHEMBL5261614
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Binding affinity to ZsGreen fused-BRD9 (M1 to T597 residues) (unknown origin) expressed in human U2OS-C433 cells assessed as induction of protein bromodomain localization from chromatin by measuring formation of large nuclear puncta by fluorescence based assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 7.25 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5279182 | — | — | 1 | 8.00 |
| CHEMBL5268484 | — | — | 1 | 7.89 |
| CHEMBL5268936 | — | — | 1 | 7.51 |
| CHEMBL5289762 | — | — | 1 | 7.47 |
| CHEMBL5280605 | — | — | 1 | 7.46 |
| CHEMBL5284261 | — | — | 1 | 7.35 |
| CHEMBL5285110 | — | — | 1 | 7.10 |
| CHEMBL5282240 | — | — | 1 | 6.72 |
| CHEMBL5286608 | — | — | 1 | 6.62 |
| CHEMBL5270178 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5279182 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5268484 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5268936 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5289762 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5280605 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5284261 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5285110 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5282240 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5286608 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5270178 | — | EC50 | = | 380.0 | nM | 6.42 |