Assay Detail
Binding
CHEMBL4405928
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 in poly(I:C)-stimulated human SAECs TLR3-inducible IL-6 gene expression pre-incubated for 24 hrs before poly(I:C) stimulation for 4 hrs by qRT-PCR analysis
9
Total Activities
9
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 Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.93 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4557050 | — | — | 1 | 6.51 |
| CHEMBL4549898 | — | — | 1 | 6.27 |
| CHEMBL4517875 | — | — | 1 | 6.12 |
| CHEMBL4453427 | — | — | 1 | 6.01 |
| CHEMBL1957266 | — | — | 1 | 5.99 |
| CHEMBL4455209 | — | — | 1 | 5.96 |
| CHEMBL4543985 | — | — | 1 | 5.55 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 5.48 |
| CHEMBL4555828 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4557050 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4549898 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4517875 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4453427 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL1957266 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4455209 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4543985 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2393130 | APABETALONE | IC50 | = | 3290.0 | nM | 5.48 |
| CHEMBL4555828 | — | IC50 | = | 3500.0 | nM | 5.46 |