Assay Detail
Binding
CHEMBL5738554
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding Assay: Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo® 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction Biology Company, RD-11-157) solution or the assay buffer was added to each well. After incubating at RT for 15 min, 5 μL of the biotinylated H4 derived acetylated peptide (synthesized by GL Biochem (Shanghai) Ltd) and 10 μL of the detection solution (Cisbio Assay) were added to each well. After incubating for 1 h at RT, the HTRF signal was measure at 615 nm and 665 nm using the EnVision Multilabel Plate Reader (PerkinElmer, USA). Results were analyzed with a two-wavelength signal ratio: intensity (665 nm)/intensity (615 nm). The inhibition percentage in the presence of the compound was calculated according to the equation, Percent inhibition=(Max−Signal)/(Max−Min)*100%. Fit the data in GraphPad Prism V5.0 software (San Diego, Calif.) to obtain IC50 values with nonlinear regression analysis using equation, Y=Bottom+(Top−Bottom)/(1+10{circumflex over ( )}((Log IC50−X)×HillSlope), where Y stands for inhibition percentage and X stands for compound concentration.
81
Total Activities
27
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Tricyclic compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.97 | 9.52 |
| kon | 27 | - | - |
| k_off | 27 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5914594 | — | — | 3 | 9.52 |
| CHEMBL5980250 | — | — | 3 | 9.47 |
| CHEMBL5927816 | — | — | 3 | 9.46 |
| CHEMBL5952972 | — | — | 3 | 9.40 |
| CHEMBL6018004 | — | — | 3 | 9.32 |
| CHEMBL6051531 | — | — | 3 | 9.31 |
| CHEMBL5908102 | — | — | 3 | 9.27 |
| CHEMBL5743600 | — | — | 3 | 9.26 |
| CHEMBL5789417 | — | — | 3 | 9.24 |
| CHEMBL5828701 | — | — | 3 | 9.23 |
| CHEMBL6011004 | — | — | 3 | 9.21 |
| CHEMBL6021830 | — | — | 3 | 9.18 |
| CHEMBL5932344 | — | — | 3 | 9.17 |
| CHEMBL5881619 | — | — | 3 | 9.10 |
| CHEMBL5774736 | — | — | 3 | 9.06 |
| CHEMBL5900152 | — | — | 3 | 9.01 |
| CHEMBL5992577 | — | — | 3 | 9.00 |
| CHEMBL5912569 | — | — | 3 | 8.96 |
| CHEMBL6042563 | — | — | 3 | 8.89 |
| CHEMBL5883744 | — | — | 3 | 8.80 |
| CHEMBL5816607 | — | — | 3 | 8.72 |
| CHEMBL5894520 | — | — | 3 | 8.66 |
| CHEMBL5911397 | — | — | 3 | 8.52 |
| CHEMBL6010533 | — | — | 3 | 8.34 |
| CHEMBL5760907 | — | — | 3 | 8.33 |
| CHEMBL5809443 | — | — | 3 | 7.92 |
| CHEMBL6008826 | — | — | 3 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5914594 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5980250 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL5927816 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL5952972 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL6018004 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL6051531 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL5908102 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL5743600 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5789417 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL5828701 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL6011004 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL6021830 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL5932344 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL5881619 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL5774736 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL5900152 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL5992577 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL5912569 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6042563 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5883744 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5816607 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5894520 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5911397 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6010533 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5760907 | — | IC50 | = | 4.67 | nM | 8.33 |
| CHEMBL5809443 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6008826 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5911397 | — | k_off | = | - | s-1 | - |
| CHEMBL5881619 | — | k_off | = | - | s-1 | - |
| CHEMBL5760907 | — | kon | = | - | — | - |
| CHEMBL5883744 | — | k_off | = | - | s-1 | - |
| CHEMBL5883744 | — | kon | = | - | — | - |
| CHEMBL6010533 | — | k_off | = | - | s-1 | - |
| CHEMBL5760907 | — | k_off | = | - | s-1 | - |
| CHEMBL6010533 | — | kon | = | - | — | - |
| CHEMBL5952972 | — | kon | = | - | — | - |
| CHEMBL6042563 | — | k_off | = | - | s-1 | - |
| CHEMBL6042563 | — | kon | = | - | — | - |
| CHEMBL5952972 | — | k_off | = | - | s-1 | - |
| CHEMBL5911397 | — | kon | = | - | — | - |
| CHEMBL5980250 | — | k_off | = | - | s-1 | - |
| CHEMBL5932344 | — | kon | = | - | — | - |
| CHEMBL5894520 | — | k_off | = | - | s-1 | - |
| CHEMBL5894520 | — | kon | = | - | — | - |
| CHEMBL5992577 | — | k_off | = | - | s-1 | - |
| CHEMBL6011004 | — | kon | = | - | — | - |
| CHEMBL6011004 | — | k_off | = | - | s-1 | - |
| CHEMBL5980250 | — | kon | = | - | — | - |
| CHEMBL5816607 | — | k_off | = | - | s-1 | - |
| CHEMBL5816607 | — | kon | = | - | — | - |