Assay Detail
Binding
CHEMBL3887227
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Assay: An expression vector containing cDNA of BRD2, 3 and 4 added with Flag-tag was transfected to CHO cell, and a cell lysate was prepared 24 hr later. Binding of acetylated histone H4 and BRD was confirmed by a Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) method. To a 384-well white plate (manufactured by Coaster) were added 50 nmol/L biotin-labeled acetylated histone H4 peptide (manufactured by Upstate) and a serially diluted test compound. Furthermore, CHO cell lysate transfected with BRD expression vector, a europium-labeled anti-Flag antibody (manufactured by Cisbio), and XL-665-labeled avidin (manufactured by Cisbio) were added, and the mixture was reacted at room temperature for 30 min to 2 hr. The fluorescence by FRET was measured by EnVision 2103 Multilabel Reader (manufactured by Perkin Elmer).
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Antitumor agent
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.19 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3941687 | — | — | 1 | 7.89 |
| CHEMBL3967931 | — | — | 1 | 7.76 |
| CHEMBL3769755 | — | — | 1 | 7.74 |
| CHEMBL3893293 | — | — | 1 | 7.68 |
| CHEMBL3894110 | — | — | 1 | 7.33 |
| CHEMBL3889858 | — | — | 1 | 7.27 |
| CHEMBL3902369 | — | — | 1 | 7.26 |
| CHEMBL3912420 | — | — | 1 | 7.13 |
| CHEMBL3926818 | — | — | 1 | 7.11 |
| CHEMBL3903414 | — | — | 1 | 6.97 |
| CHEMBL3937740 | — | — | 1 | 6.95 |
| CHEMBL3904716 | — | — | 1 | 6.93 |
| CHEMBL3953629 | — | — | 1 | 6.92 |
| CHEMBL3922243 | — | — | 1 | 6.92 |
| CHEMBL3936300 | — | — | 1 | 6.91 |
| CHEMBL3892997 | — | — | 1 | 6.83 |
| CHEMBL3974352 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3941687 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL3967931 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL3769755 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL3893293 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3894110 | — | IC50 | = | 47.1 | nM | 7.33 |
| CHEMBL3889858 | — | IC50 | = | 54.2 | nM | 7.27 |
| CHEMBL3902369 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL3912420 | — | IC50 | = | 73.6 | nM | 7.13 |
| CHEMBL3926818 | — | IC50 | = | 77.2 | nM | 7.11 |
| CHEMBL3903414 | — | IC50 | = | 107.8 | nM | 6.97 |
| CHEMBL3937740 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL3904716 | — | IC50 | = | 116.4 | nM | 6.93 |
| CHEMBL3953629 | — | IC50 | = | 119.8 | nM | 6.92 |
| CHEMBL3922243 | — | IC50 | = | 121.2 | nM | 6.92 |
| CHEMBL3936300 | — | IC50 | = | 123.5 | nM | 6.91 |
| CHEMBL3892997 | — | IC50 | = | 146.8 | nM | 6.83 |
| CHEMBL3974352 | — | IC50 | = | 225.3 | nM | 6.65 |