Assay Detail
Binding
CHEMBL4058600
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Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged CBP 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 | 8.10 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097025 | — | — | 1 | 9.03 |
| CHEMBL4069831 | — | — | 1 | 9.00 |
| CHEMBL4088793 | — | — | 1 | 9.00 |
| CHEMBL4076748 | — | — | 1 | 8.96 |
| CHEMBL4061161 | — | — | 1 | 8.92 |
| CHEMBL4060566 | — | — | 1 | 8.92 |
| CHEMBL4061600 | — | — | 1 | 8.85 |
| CHEMBL4080905 | — | — | 1 | 8.82 |
| CHEMBL4083416 | — | — | 1 | 8.82 |
| CHEMBL4098938 | — | — | 1 | 8.70 |
| CHEMBL4091202 | — | — | 1 | 8.51 |
| CHEMBL4099857 | — | — | 1 | 8.37 |
| CHEMBL4062259 | — | — | 1 | 8.36 |
| CHEMBL4072979 | — | — | 1 | 8.33 |
| CHEMBL4077449 | — | — | 1 | 7.80 |
| CHEMBL3897393 | — | — | 1 | 7.70 |
| CHEMBL4080528 | — | — | 1 | 7.51 |
| CHEMBL4095660 | — | — | 1 | 7.51 |
| CHEMBL4104751 | — | — | 1 | 6.51 |
| CHEMBL4076770 | — | — | 1 | 5.75 |
| CHEMBL4089325 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097025 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL4069831 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4088793 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4076748 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4061161 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4060566 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4061600 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4080905 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4083416 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4098938 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4091202 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4099857 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4062259 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4072979 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4077449 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3897393 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4080528 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4095660 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4104751 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4076770 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4089325 | — | IC50 | = | 18000.0 | nM | 4.75 |