Assay Detail
Binding
CHEMBL4415481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incubated for 4 hrs in dark condition by fluorescence anisotropy binding assay
28
Total Activities
28
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
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.02 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4550548 | — | — | 1 | 8.38 |
| CHEMBL4587000 | — | — | 1 | 8.35 |
| CHEMBL4583525 | — | — | 1 | 8.34 |
| CHEMBL4449874 | — | — | 1 | 8.34 |
| CHEMBL4518804 | — | — | 1 | 8.32 |
| CHEMBL4463165 | — | — | 1 | 8.28 |
| CHEMBL4451357 | — | — | 1 | 8.28 |
| CHEMBL4573400 | — | — | 1 | 8.27 |
| CHEMBL4578490 | — | — | 1 | 8.24 |
| CHEMBL4561468 | — | — | 1 | 8.24 |
| CHEMBL4445973 | — | — | 1 | 8.23 |
| CHEMBL4582401 | — | — | 1 | 8.21 |
| CHEMBL4553774 | — | — | 1 | 8.18 |
| CHEMBL4441607 | — | — | 1 | 8.17 |
| CHEMBL4577433 | — | — | 1 | 8.15 |
| CHEMBL4452579 | — | — | 1 | 8.15 |
| CHEMBL4584184 | — | — | 1 | 8.10 |
| CHEMBL4585487 | — | — | 1 | 8.07 |
| CHEMBL4454674 | — | — | 1 | 8.06 |
| CHEMBL4556261 | — | — | 1 | 8.03 |
| CHEMBL4537909 | — | — | 1 | 8.02 |
| CHEMBL4445310 | — | — | 1 | 8.02 |
| CHEMBL4585185 | — | — | 1 | 7.84 |
| CHEMBL4470399 | — | — | 1 | 7.57 |
| CHEMBL1957266 | — | — | 1 | 7.54 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 7.46 |
| CHEMBL4465676 | — | — | 1 | 7.00 |
| CHEMBL4572470 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4550548 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4587000 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4583525 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4449874 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4518804 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4463165 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4451357 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4573400 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4578490 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4561468 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4445973 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4582401 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4553774 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4441607 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4577433 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4452579 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4584184 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4585487 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4454674 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4556261 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4537909 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4445310 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4585185 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL4470399 | — | IC50 | = | 27.2 | nM | 7.57 |
| CHEMBL1957266 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL4465676 | — | IC50 | = | 100.4 | nM | 7.00 |
| CHEMBL4572470 | — | IC50 | = | 142.0 | nM | 6.85 |