Assay Detail
Binding
CHEMBL5164016
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Inhibition of BRD4-BD1 (unknown origin) preincubated for 30 mins followed by substrate addition and measured after 3 hr by HTRF assay
17
Total Activities
17
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
Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.99 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5169455 | — | — | 1 | 7.64 |
| CHEMBL5181042 | — | — | 1 | 7.61 |
| CHEMBL5172487 | — | — | 1 | 7.53 |
| CHEMBL5209531 | — | — | 1 | 7.46 |
| CHEMBL5186542 | — | — | 1 | 7.34 |
| CHEMBL4303781 | — | — | 1 | 7.30 |
| CHEMBL5188851 | — | — | 1 | 7.26 |
| CHEMBL5193742 | — | — | 1 | 7.08 |
| CHEMBL5200802 | — | — | 1 | 7.00 |
| CHEMBL5185340 | — | — | 1 | 6.93 |
| CHEMBL5175586 | — | — | 1 | 6.73 |
| CHEMBL5203560 | — | — | 1 | 6.62 |
| CHEMBL5175450 | — | — | 1 | 6.56 |
| CHEMBL4297454 | ABBV-744 | 1.0 | 1 | 6.52 |
| CHEMBL5189384 | — | — | 1 | 6.48 |
| CHEMBL5206001 | — | — | 1 | 6.36 |
| CHEMBL5203520 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5169455 | — | IC50 | = | 22.75 | nM | 7.64 |
| CHEMBL5181042 | — | IC50 | = | 24.55 | nM | 7.61 |
| CHEMBL5172487 | — | IC50 | = | 29.54 | nM | 7.53 |
| CHEMBL5209531 | — | IC50 | = | 34.58 | nM | 7.46 |
| CHEMBL5186542 | — | IC50 | = | 45.41 | nM | 7.34 |
| CHEMBL4303781 | — | IC50 | = | 50.21 | nM | 7.30 |
| CHEMBL5188851 | — | IC50 | = | 54.31 | nM | 7.26 |
| CHEMBL5193742 | — | IC50 | = | 83.65 | nM | 7.08 |
| CHEMBL5200802 | — | IC50 | = | 99.75 | nM | 7.00 |
| CHEMBL5185340 | — | IC50 | = | 118.6 | nM | 6.93 |
| CHEMBL5175586 | — | IC50 | = | 185.35 | nM | 6.73 |
| CHEMBL5203560 | — | IC50 | = | 241.45 | nM | 6.62 |
| CHEMBL5175450 | — | IC50 | = | 277.55 | nM | 6.56 |
| CHEMBL4297454 | ABBV-744 | IC50 | = | 299.75 | nM | 6.52 |
| CHEMBL5189384 | — | IC50 | = | 331.9 | nM | 6.48 |
| CHEMBL5206001 | — | IC50 | = | 440.7 | nM | 6.36 |
| CHEMBL5203520 | — | IC50 | = | 471.8 | nM | 6.33 |