Assay Detail
Binding
CHEMBL5029989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT 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 |
Target
Bromodomain testis-specific protein (CHEMBL1795185) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 8 | 6.05 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4760892 | — | — | 1 | 7.23 |
| CHEMBL1957266 | — | — | 1 | 6.73 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 6.09 |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | 5.77 |
| CHEMBL2012582 | — | — | 1 | 5.77 |
| CHEMBL2392553 | — | — | 1 | 5.75 |
| CHEMBL2381340 | — | — | 1 | 5.68 |
| CHEMBL1673046 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4760892 | — | Kd | = | 59.0 | nM | 7.23 |
| CHEMBL1957266 | — | Kd | = | 188.0 | nM | 6.73 |
| CHEMBL513909 | BI-2536 | Kd | = | 806.0 | nM | 6.09 |
| CHEMBL1233528 | VOLASERTIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL2012582 | — | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL2392553 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL2381340 | — | Kd | = | 2100.0 | nM | 5.68 |
| CHEMBL1673046 | — | Kd | = | 4200.0 | nM | 5.38 |