Assay Detail
Binding
CHEMBL3817161
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Inhibition of Halo-tagged histone H3.3 binding to CBP (unknown origin) expressed in HEK293 cells after overnight incubation by luciferase reporter gene based BRET assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 5.59 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3814752 | — | — | 1 | 6.52 |
| CHEMBL3814896 | — | — | 1 | 5.92 |
| CHEMBL3813929 | — | — | 1 | 5.72 |
| CHEMBL3814550 | — | — | 1 | 5.52 |
| CHEMBL3815023 | — | — | 1 | 5.47 |
| CHEMBL3814246 | — | — | 1 | 5.30 |
| CHEMBL3814602 | — | — | 1 | 5.16 |
| CHEMBL3814197 | — | — | 1 | 5.09 |
| CHEMBL3814595 | — | — | 1 | - |
| CHEMBL3813846 | — | — | 1 | - |
| CHEMBL3814881 | — | — | 1 | - |
| CHEMBL3813915 | — | — | 1 | - |
| CHEMBL3815086 | — | — | 1 | - |
| CHEMBL3813744 | — | — | 1 | - |
| CHEMBL3813713 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3814752 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3814896 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3813929 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3814550 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3815023 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3814246 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3814602 | — | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3814197 | — | EC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL3814595 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3813846 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3814881 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3813915 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3815086 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3813744 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3813713 | — | EC50 | > | 10000.0 | nM | - |