Assay Detail
Binding
CHEMBL4731452
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 bromodomain1 (unknown origin) using peptide histone H4 (SGRGACKGGACKGLGAC-KGGAACKRHGSGSK-biotin) as substrate incubated for 15 mins followed by substrate addition measured after 1 hr by alphascreen assay
16
Total Activities
16
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
Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.77 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.60 |
| CHEMBL4793308 | — | — | 1 | 8.38 |
| CHEMBL4778807 | — | — | 1 | 8.11 |
| CHEMBL4795650 | — | — | 1 | 7.89 |
| CHEMBL4781744 | — | — | 1 | 7.72 |
| CHEMBL4764687 | — | — | 1 | 7.51 |
| CHEMBL4637198 | — | — | 1 | 7.50 |
| CHEMBL4743695 | — | — | 1 | 7.38 |
| CHEMBL1957266 | — | — | 1 | 7.38 |
| CHEMBL4751282 | — | — | 1 | 7.25 |
| CHEMBL4790523 | — | — | 1 | - |
| CHEMBL4799831 | — | — | 1 | - |
| CHEMBL4758215 | — | — | 1 | - |
| CHEMBL4749258 | — | — | 1 | - |
| CHEMBL4788655 | — | — | 1 | - |
| CHEMBL4756710 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4793308 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4778807 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4795650 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4781744 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4764687 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4637198 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4743695 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1957266 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4751282 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4790523 | — | IC50 | - | — | - | |
| CHEMBL4799831 | — | IC50 | < | 2.1 | nM | - |
| CHEMBL4758215 | — | IC50 | < | 2.1 | nM | - |
| CHEMBL4749258 | — | IC50 | < | 2.1 | nM | - |
| CHEMBL4788655 | — | IC50 | < | 2.1 | nM | - |
| CHEMBL4756710 | — | IC50 | < | 2.1 | nM | - |