Assay Detail
Binding
CHEMBL4331528
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay
10
Total Activities
10
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
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.23 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4593553 | — | — | 1 | 8.77 |
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 7.70 |
| CHEMBL1968380 | — | — | 1 | 7.60 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 7.49 |
| CHEMBL4441082 | — | — | 1 | 7.48 |
| CHEMBL4303404 | PELABRESIB | 3.0 | 1 | 7.41 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 7.04 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 6.29 |
| CHEMBL2326966 | SF-1126 | 2.0 | 1 | 5.28 |
| CHEMBL4438598 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4593553 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1968380 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL4441082 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4303404 | PELABRESIB | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2393130 | APABETALONE | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2326966 | SF-1126 | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4438598 | — | IC50 | < | 5.0 | nM | - |