Assay Detail
Binding
CHEMBL5037307
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Binding affinity to BRD4 BD1 (unknown origin) by fluorescence anisotropy method
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
4-Methyl-1,2,3-Triazoles as <i>N</i>-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.50 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.11 |
| CHEMBL5083660 | — | — | 1 | 6.86 |
| CHEMBL5094520 | — | — | 1 | 6.10 |
| CHEMBL5080097 | — | — | 1 | 6.03 |
| CHEMBL5089426 | — | — | 1 | 6.01 |
| CHEMBL5080584 | — | — | 1 | 5.99 |
| CHEMBL5088065 | — | — | 1 | 5.85 |
| CHEMBL5075276 | — | — | 1 | 5.84 |
| CHEMBL5069903 | — | — | 1 | 5.82 |
| CHEMBL5077946 | — | — | 1 | 5.80 |
| CHEMBL5089274 | — | — | 1 | 5.62 |
| CHEMBL5076270 | — | — | 1 | 5.62 |
| CHEMBL5082857 | — | — | 1 | 5.58 |
| CHEMBL5093335 | — | — | 1 | 5.56 |
| CHEMBL4552460 | — | — | 1 | 5.54 |
| CHEMBL5080763 | — | — | 1 | 5.49 |
| CHEMBL5084581 | — | — | 1 | 5.49 |
| CHEMBL5087835 | — | — | 1 | 5.45 |
| CHEMBL5093415 | — | — | 1 | 5.32 |
| CHEMBL5088967 | — | — | 1 | 5.22 |
| CHEMBL4557050 | — | — | 1 | 5.08 |
| CHEMBL5091175 | — | — | 1 | 5.05 |
| CHEMBL5077228 | — | — | 1 | 4.90 |
| CHEMBL5093869 | — | — | 1 | 4.84 |
| CHEMBL5093909 | — | — | 1 | 4.66 |
| CHEMBL5094731 | — | — | 1 | 4.65 |
| CHEMBL5093080 | — | — | 1 | 4.39 |
| CHEMBL5090895 | — | — | 1 | 4.12 |
| CHEMBL5079822 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5083660 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5094520 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL5080097 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5089426 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL5080584 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5088065 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL5075276 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL5069903 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5077946 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL5089274 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5076270 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5082857 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5093335 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4552460 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL5080763 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL5084581 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL5087835 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL5093415 | — | IC50 | = | 4750.0 | nM | 5.32 |
| CHEMBL5088967 | — | IC50 | = | 5970.0 | nM | 5.22 |
| CHEMBL4557050 | — | IC50 | = | 8220.0 | nM | 5.08 |
| CHEMBL5091175 | — | IC50 | = | 8960.0 | nM | 5.05 |
| CHEMBL5077228 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL5093869 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL5093909 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL5094731 | — | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL5093080 | — | IC50 | = | 40900.0 | nM | 4.39 |
| CHEMBL5090895 | — | IC50 | = | 75800.0 | nM | 4.12 |
| CHEMBL5079822 | — | IC50 | > | 100000.0 | nM | - |