Assay Detail
Binding
CHEMBL4363365
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assay
6
Total Activities
6
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, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.91 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4528047 | — | — | 1 | 8.51 |
| CHEMBL4438006 | — | — | 1 | 8.05 |
| CHEMBL4471776 | — | — | 1 | 8.04 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 7.99 |
| CHEMBL4533303 | — | — | 1 | 7.72 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 7.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4528047 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL4438006 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL4471776 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL3581647 | BIRABRESIB | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL4533303 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL1232461 | MOLIBRESIB | Ki | = | 74.0 | nM | 7.13 |