Assay Detail
Binding
CHEMBL3817157
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Displacement of biotinylated ligand from recombinant His-tagged CBP (unknown origin) incubated for 10 mins by TR-FRET assay
29
Total Activities
29
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
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.89 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3814752 | — | — | 1 | 7.52 |
| CHEMBL3814550 | — | — | 1 | 7.48 |
| CHEMBL3814896 | — | — | 1 | 7.41 |
| CHEMBL3813929 | — | — | 1 | 7.11 |
| CHEMBL3813846 | — | — | 1 | 6.96 |
| CHEMBL3814246 | — | — | 1 | 6.89 |
| CHEMBL3815023 | — | — | 1 | 6.80 |
| CHEMBL3814197 | — | — | 1 | 6.62 |
| CHEMBL3814602 | — | — | 1 | 6.60 |
| CHEMBL3814891 | — | — | 1 | 6.28 |
| CHEMBL3813915 | — | — | 1 | 6.21 |
| CHEMBL3814881 | — | — | 1 | 6.17 |
| CHEMBL3813713 | — | — | 1 | 6.05 |
| CHEMBL3813731 | — | — | 1 | 5.72 |
| CHEMBL3814595 | — | — | 1 | 5.47 |
| CHEMBL3814772 | — | — | 1 | 5.39 |
| CHEMBL3813744 | — | — | 1 | 5.30 |
| CHEMBL3815086 | — | — | 1 | 5.19 |
| CHEMBL3813884 | — | — | 1 | 5.16 |
| CHEMBL2282031 | — | — | 1 | 5.00 |
| CHEMBL3814217 | — | — | 1 | 4.92 |
| CHEMBL3814920 | — | — | 1 | 4.57 |
| CHEMBL2142704 | — | — | 1 | 4.50 |
| CHEMBL3813701 | — | — | 1 | 3.92 |
| CHEMBL3815068 | — | — | 1 | 3.89 |
| CHEMBL3813958 | — | — | 1 | - |
| CHEMBL3813890 | — | — | 1 | - |
| CHEMBL3814945 | — | — | 1 | - |
| CHEMBL3814706 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3814752 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3814550 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3814896 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3813929 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL3813846 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3814246 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3815023 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3814197 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3814602 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3814891 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3813915 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL3814881 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3813713 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3813731 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3814595 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3814772 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3813744 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3815086 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3813884 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2282031 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3814217 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3814920 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2142704 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL3813701 | — | IC50 | = | 120000.0 | nM | 3.92 |
| CHEMBL3815068 | — | IC50 | = | 130000.0 | nM | 3.89 |
| CHEMBL3813958 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3813890 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3814945 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL3814706 | — | IC50 | > | 2000000.0 | nM | - |