Assay Detail
Binding
CHEMBL4153114
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Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed by poly(I:C) addition and measured after 4 hrs by SYBR green dye-based qRT-PCR analysis
5
Total Activities
5
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
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.79 | 6.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4176038 | — | — | 1 | 6.31 |
| CHEMBL4159382 | — | — | 1 | 6.09 |
| CHEMBL1957266 | — | — | 1 | 5.86 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 5.58 |
| CHEMBL4173521 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4176038 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4159382 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL1957266 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL2393130 | APABETALONE | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL4173521 | — | IC50 | = | 7900.0 | nM | 5.10 |