Assay Detail
Binding
CHEMBL5369308
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Inhibition of BRD4 BD1 (unknown origin) by TR-FRET assay
16
Total Activities
16
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
Design and Characterization of 1,3-Dihydro-2<i>H</i>-benzo[<i>d</i>]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.81 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5426022 | — | — | 1 | 8.50 |
| CHEMBL4438171 | — | — | 1 | 7.90 |
| CHEMBL5433432 | — | — | 1 | 7.80 |
| CHEMBL2017291 | — | — | 1 | 7.60 |
| CHEMBL5403564 | — | — | 1 | 7.40 |
| CHEMBL1957266 | — | — | 1 | 7.40 |
| CHEMBL4639128 | GSK778 | — | 1 | 7.40 |
| CHEMBL5422047 | — | — | 1 | 7.20 |
| CHEMBL5408181 | — | — | 1 | 7.10 |
| CHEMBL5426762 | — | — | 1 | 7.00 |
| CHEMBL5220623 | — | — | 1 | 6.80 |
| CHEMBL4078100 | AZD-5153 | 1.0 | 1 | 6.40 |
| CHEMBL5427202 | — | — | 1 | 6.20 |
| CHEMBL5417286 | — | — | 1 | 5.50 |
| CHEMBL4519518 | — | — | 1 | 4.60 |
| CHEMBL4636881 | GSK046 | — | 1 | 4.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5426022 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL4438171 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL5433432 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2017291 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5403564 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL1957266 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4639128 | GSK778 | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5422047 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5408181 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL5426762 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5220623 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4078100 | AZD-5153 | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5427202 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5417286 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4519518 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4636881 | GSK046 | IC50 | = | 63095.73 | nM | 4.20 |