Assay Detail
Binding
CHEMBL5037308
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Binding affinity to BRD4 BD2 (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 | 5.17 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1957266 | — | — | 1 | 7.14 |
| CHEMBL4557050 | — | — | 1 | 6.14 |
| CHEMBL5080584 | — | — | 1 | 6.07 |
| CHEMBL5083660 | — | — | 1 | 5.99 |
| CHEMBL5089426 | — | — | 1 | 5.61 |
| CHEMBL5075276 | — | — | 1 | 5.59 |
| CHEMBL5094520 | — | — | 1 | 5.51 |
| CHEMBL5077946 | — | — | 1 | 5.35 |
| CHEMBL4552460 | — | — | 1 | 5.31 |
| CHEMBL5089274 | — | — | 1 | 5.28 |
| CHEMBL5069903 | — | — | 1 | 5.21 |
| CHEMBL5088065 | — | — | 1 | 4.96 |
| CHEMBL5088967 | — | — | 1 | 4.91 |
| CHEMBL5084581 | — | — | 1 | 4.90 |
| CHEMBL5082857 | — | — | 1 | 4.90 |
| CHEMBL5076270 | — | — | 1 | 4.89 |
| CHEMBL5093335 | — | — | 1 | 4.89 |
| CHEMBL5087835 | — | — | 1 | 4.88 |
| CHEMBL5080763 | — | — | 1 | 4.87 |
| CHEMBL5094731 | — | — | 1 | 4.70 |
| CHEMBL5091175 | — | — | 1 | 4.65 |
| CHEMBL5093415 | — | — | 1 | 4.63 |
| CHEMBL5093869 | — | — | 1 | 4.62 |
| CHEMBL5080097 | — | — | 1 | 4.58 |
| CHEMBL5077228 | — | — | 1 | 4.47 |
| CHEMBL5093909 | — | — | 1 | 4.27 |
| CHEMBL5093080 | — | — | 1 | - |
| CHEMBL5079822 | — | — | 1 | - |
| CHEMBL5090895 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1957266 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4557050 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL5080584 | — | IC50 | = | 856.0 | nM | 6.07 |
| CHEMBL5083660 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5089426 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL5075276 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL5094520 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL5077946 | — | IC50 | = | 4510.0 | nM | 5.35 |
| CHEMBL4552460 | — | IC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL5089274 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL5069903 | — | IC50 | = | 6120.0 | nM | 5.21 |
| CHEMBL5088065 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL5088967 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL5084581 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL5082857 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL5076270 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5093335 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL5087835 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL5080763 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL5094731 | — | IC50 | = | 20200.0 | nM | 4.70 |
| CHEMBL5091175 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL5093415 | — | IC50 | = | 23300.0 | nM | 4.63 |
| CHEMBL5093869 | — | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL5080097 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL5077228 | — | IC50 | = | 33500.0 | nM | 4.47 |
| CHEMBL5093909 | — | IC50 | = | 53500.0 | nM | 4.27 |
| CHEMBL5093080 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5079822 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5090895 | — | IC50 | > | 100000.0 | nM | - |