Assay Detail
Binding
CHEMBL4058601
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Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BRD4 bromodomain-1 measured after 10 mins by TR-FRET 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
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.21 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4072979 | — | — | 1 | 5.66 |
| CHEMBL4080905 | — | — | 1 | 5.51 |
| CHEMBL4060566 | — | — | 1 | 5.40 |
| CHEMBL4088793 | — | — | 1 | 5.39 |
| CHEMBL4098938 | — | — | 1 | 5.38 |
| CHEMBL4076748 | — | — | 1 | 5.38 |
| CHEMBL4083416 | — | — | 1 | 5.38 |
| CHEMBL4099857 | — | — | 1 | 5.32 |
| CHEMBL4097025 | — | — | 1 | 5.29 |
| CHEMBL4061161 | — | — | 1 | 5.27 |
| CHEMBL4061600 | — | — | 1 | 5.25 |
| CHEMBL4062259 | — | — | 1 | 5.14 |
| CHEMBL4069831 | — | — | 1 | 5.02 |
| CHEMBL4091202 | — | — | 1 | 5.02 |
| CHEMBL4095660 | — | — | 1 | 4.92 |
| CHEMBL3897393 | — | — | 1 | 4.89 |
| CHEMBL4104751 | — | — | 1 | 4.82 |
| CHEMBL4077449 | — | — | 1 | 4.70 |
| CHEMBL4080528 | — | — | 1 | - |
| CHEMBL4076770 | — | — | 1 | - |
| CHEMBL4089325 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4072979 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4080905 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4060566 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4088793 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4098938 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4076748 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4083416 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4099857 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4097025 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4061161 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4061600 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4062259 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4069831 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4091202 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4095660 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3897393 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4104751 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4077449 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4080528 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4076770 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4089325 | — | IC50 | > | 100000.0 | nM | - |