Assay Detail
Binding
CHEMBL5029985
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Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis
8
Total Activities
8
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
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 6.74 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4760892 | — | — | 1 | 7.27 |
| CHEMBL1957266 | — | — | 1 | 7.15 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 6.95 |
| CHEMBL2012582 | — | — | 1 | 6.71 |
| CHEMBL2381340 | — | — | 1 | 6.67 |
| CHEMBL2392553 | — | — | 1 | 6.57 |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | 6.50 |
| CHEMBL1673046 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4760892 | — | Kd | = | 54.0 | nM | 7.27 |
| CHEMBL1957266 | — | Kd | = | 71.0 | nM | 7.15 |
| CHEMBL513909 | BI-2536 | Kd | = | 112.0 | nM | 6.95 |
| CHEMBL2012582 | — | Kd | = | 194.0 | nM | 6.71 |
| CHEMBL2381340 | — | Kd | = | 213.0 | nM | 6.67 |
| CHEMBL2392553 | — | Kd | = | 267.0 | nM | 6.57 |
| CHEMBL1233528 | VOLASERTIB | Kd | = | 317.0 | nM | 6.50 |
| CHEMBL1673046 | — | Kd | = | 735.0 | nM | 6.13 |