Assay Detail
Binding
CHEMBL4200424
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Inhibition of BRD4-BD1 (unknown origin) incubated for 1 hr by AlphaScreen biotin-JQ1 competition assay
27
Total Activities
27
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-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.49 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4207437 | — | — | 1 | 7.55 |
| CHEMBL1957266 | — | — | 1 | 7.50 |
| CHEMBL4206381 | — | — | 1 | 7.23 |
| CHEMBL4209902 | — | — | 1 | 7.08 |
| CHEMBL4202678 | — | — | 1 | 7.03 |
| CHEMBL4216442 | — | — | 1 | 7.02 |
| CHEMBL4210571 | — | — | 1 | 6.98 |
| CHEMBL4216875 | — | — | 1 | 6.97 |
| CHEMBL4210414 | — | — | 1 | 6.97 |
| CHEMBL4213276 | — | — | 1 | 6.96 |
| CHEMBL4203571 | — | — | 1 | 6.74 |
| CHEMBL4207165 | — | — | 1 | 6.73 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 6.69 |
| CHEMBL4212346 | — | — | 1 | 6.60 |
| CHEMBL4202820 | — | — | 1 | 6.51 |
| CHEMBL4206052 | — | — | 1 | 6.38 |
| CHEMBL3609305 | — | — | 1 | 6.31 |
| CHEMBL4209192 | — | — | 1 | 6.22 |
| CHEMBL4215729 | — | — | 1 | 6.19 |
| CHEMBL4205459 | — | — | 1 | 6.16 |
| CHEMBL4206171 | — | — | 1 | 5.59 |
| CHEMBL3609304 | — | — | 1 | 5.18 |
| CHEMBL4215910 | — | — | 1 | 4.73 |
| CHEMBL4212237 | — | — | 1 | 4.38 |
| CHEMBL4207347 | — | — | 1 | - |
| CHEMBL4214823 | — | — | 1 | - |
| CHEMBL4218106 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4207437 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1957266 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4206381 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4209902 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4202678 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4216442 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4210571 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4216875 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4210414 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4213276 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4203571 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL4207165 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL513909 | BI-2536 | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4212346 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL4202820 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4206052 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL3609305 | — | IC50 | = | 489.0 | nM | 6.31 |
| CHEMBL4209192 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL4215729 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4205459 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4206171 | — | IC50 | = | 2579.0 | nM | 5.59 |
| CHEMBL3609304 | — | IC50 | = | 6633.0 | nM | 5.18 |
| CHEMBL4215910 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL4212237 | — | IC50 | = | 41900.0 | nM | 4.38 |
| CHEMBL4207347 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4214823 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4218106 | — | IC50 | > | 10000.0 | nM | - |