Assay Detail
Binding
CHEMBL5539775
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Binding affinity to BRD4 BD1 (unknown origin) by ITC analysis
2
Total Activities
2
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 Novel Phenoxyaryl Pyridones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with High Selectivity for the Second Bromodomain (BD2) to Potentially Treat Acute Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 2 | 5.26 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770724 | — | — | 1 | 5.47 |
| CHEMBL2393130 | APABETALONE | 3.0 | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770724 | — | Kd | = | 3400.0 | nM | 5.47 |
| CHEMBL2393130 | APABETALONE | Kd | = | 8900.0 | nM | 5.05 |