Assay Detail
Binding
CHEMBL3826480
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Inhibition of human N-terminal GST-tagged BRD4-BD2 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay
13
Total Activities
13
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 | 13 | 4.39 | 4.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3822990 | — | — | 1 | 4.85 |
| CHEMBL3824146 | — | — | 1 | 4.49 |
| CHEMBL3823599 | — | — | 1 | 4.37 |
| CHEMBL3823551 | — | — | 1 | 4.17 |
| CHEMBL3824133 | — | — | 1 | 4.06 |
| CHEMBL3823101 | — | — | 1 | - |
| CHEMBL3824351 | — | — | 1 | - |
| CHEMBL3824312 | — | — | 1 | - |
| CHEMBL3822539 | — | — | 1 | - |
| CHEMBL3823859 | — | — | 1 | - |
| CHEMBL3823478 | — | — | 1 | - |
| CHEMBL3822909 | — | — | 1 | - |
| CHEMBL3823697 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3822990 | — | IC50 | = | 14256.0 | nM | 4.85 |
| CHEMBL3824146 | — | IC50 | = | 32432.0 | nM | 4.49 |
| CHEMBL3823599 | — | IC50 | = | 42281.0 | nM | 4.37 |
| CHEMBL3823551 | — | IC50 | = | 67479.0 | nM | 4.17 |
| CHEMBL3824133 | — | IC50 | = | 86973.0 | nM | 4.06 |
| CHEMBL3823101 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3824351 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3824312 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3822539 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3823859 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3823478 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3822909 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3823697 | — | IC50 | > | 100000.0 | nM | - |