Assay Detail
Binding
CHEMBL3826482
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Inhibition of human N-terminal GST-tagged BRD4-BD1 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay
21
Total Activities
21
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
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.80 | 5.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3823369 | — | — | 1 | 5.95 |
| CHEMBL3823177 | — | — | 1 | 5.94 |
| CHEMBL3822498 | — | — | 1 | 5.43 |
| CHEMBL3823906 | — | — | 1 | 5.42 |
| CHEMBL3822990 | — | — | 1 | 5.23 |
| CHEMBL3824289 | — | — | 1 | 4.72 |
| CHEMBL3823599 | — | — | 1 | 4.64 |
| CHEMBL3824146 | — | — | 1 | 4.63 |
| CHEMBL3823697 | — | — | 1 | 4.51 |
| CHEMBL3822843 | — | — | 1 | 4.50 |
| CHEMBL3822501 | — | — | 1 | 4.49 |
| CHEMBL3823551 | — | — | 1 | 4.36 |
| CHEMBL3822909 | — | — | 1 | 4.33 |
| CHEMBL3824133 | — | — | 1 | 4.33 |
| CHEMBL3824351 | — | — | 1 | 4.21 |
| CHEMBL3822988 | — | — | 1 | 4.09 |
| CHEMBL3822539 | — | — | 1 | - |
| CHEMBL3823859 | — | — | 1 | - |
| CHEMBL3823478 | — | — | 1 | - |
| CHEMBL3824312 | — | — | 1 | - |
| CHEMBL3823101 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3823369 | — | IC50 | = | 1121.0 | nM | 5.95 |
| CHEMBL3823177 | — | IC50 | = | 1147.0 | nM | 5.94 |
| CHEMBL3822498 | — | IC50 | = | 3681.0 | nM | 5.43 |
| CHEMBL3823906 | — | IC50 | = | 3778.0 | nM | 5.42 |
| CHEMBL3822990 | — | IC50 | = | 5861.0 | nM | 5.23 |
| CHEMBL3824289 | — | IC50 | = | 19165.0 | nM | 4.72 |
| CHEMBL3823599 | — | IC50 | = | 23005.0 | nM | 4.64 |
| CHEMBL3824146 | — | IC50 | = | 23576.0 | nM | 4.63 |
| CHEMBL3823697 | — | IC50 | = | 30652.0 | nM | 4.51 |
| CHEMBL3822843 | — | IC50 | = | 31421.0 | nM | 4.50 |
| CHEMBL3822501 | — | IC50 | = | 32430.0 | nM | 4.49 |
| CHEMBL3823551 | — | IC50 | = | 43998.0 | nM | 4.36 |
| CHEMBL3822909 | — | IC50 | = | 47359.0 | nM | 4.33 |
| CHEMBL3824133 | — | IC50 | = | 47095.0 | nM | 4.33 |
| CHEMBL3824351 | — | IC50 | = | 61917.0 | nM | 4.21 |
| CHEMBL3822988 | — | IC50 | = | 81300.0 | nM | 4.09 |
| CHEMBL3822539 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3823859 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3823478 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3824312 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3823101 | — | IC50 | > | 100000.0 | nM | - |