Assay Detail
Binding
CHEMBL5164017
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Inhibition of BRD4-BD2 (unknown origin) preincubated for 30 mins followed by substrate addition and measured after 3 hr by HTRF
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 | 7.45 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297454 | ABBV-744 | 1.0 | 1 | 8.75 |
| CHEMBL5172487 | — | — | 1 | 8.42 |
| CHEMBL5169455 | — | — | 1 | 8.11 |
| CHEMBL5181042 | — | — | 1 | 7.86 |
| CHEMBL5175586 | — | — | 1 | 7.61 |
| CHEMBL5209531 | — | — | 1 | 7.57 |
| CHEMBL5189384 | — | — | 1 | 7.45 |
| CHEMBL5175450 | — | — | 1 | 7.41 |
| CHEMBL5206001 | — | — | 1 | 7.41 |
| CHEMBL5186542 | — | — | 1 | 7.14 |
| CHEMBL5203560 | — | — | 1 | 7.13 |
| CHEMBL4303781 | — | — | 1 | 7.09 |
| CHEMBL5203520 | — | — | 1 | 7.07 |
| CHEMBL5193742 | — | — | 1 | 7.04 |
| CHEMBL5188851 | — | — | 1 | 7.02 |
| CHEMBL5185340 | — | — | 1 | 7.00 |
| CHEMBL5200802 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297454 | ABBV-744 | IC50 | = | 1.78 | nM | 8.75 |
| CHEMBL5172487 | — | IC50 | = | 3.82 | nM | 8.42 |
| CHEMBL5169455 | — | IC50 | = | 7.79 | nM | 8.11 |
| CHEMBL5181042 | — | IC50 | = | 13.92 | nM | 7.86 |
| CHEMBL5175586 | — | IC50 | = | 24.33 | nM | 7.61 |
| CHEMBL5209531 | — | IC50 | = | 27.22 | nM | 7.57 |
| CHEMBL5189384 | — | IC50 | = | 35.72 | nM | 7.45 |
| CHEMBL5175450 | — | IC50 | = | 38.84 | nM | 7.41 |
| CHEMBL5206001 | — | IC50 | = | 39.37 | nM | 7.41 |
| CHEMBL5186542 | — | IC50 | = | 72.98 | nM | 7.14 |
| CHEMBL5203560 | — | IC50 | = | 74.12 | nM | 7.13 |
| CHEMBL4303781 | — | IC50 | = | 80.53 | nM | 7.09 |
| CHEMBL5203520 | — | IC50 | = | 84.94 | nM | 7.07 |
| CHEMBL5193742 | — | IC50 | = | 91.49 | nM | 7.04 |
| CHEMBL5188851 | — | IC50 | = | 96.4 | nM | 7.02 |
| CHEMBL5185340 | — | IC50 | = | 100.53 | nM | 7.00 |
| CHEMBL5200802 | — | IC50 | = | 295.6 | nM | 6.53 |