Assay Detail
Binding
CHEMBL4626977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Alexa Fluor 647 labelled I-BET762 from N-terminal His6-tagged human BRD3 BD2 (1 to 435 residues)/BD1 Y73A mutant expressed in Escherichia coli after 1 hr by TR-FRET assay
3
Total Activities
3
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
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.97 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4635329 | — | — | 1 | 7.80 |
| CHEMBL2017291 | — | — | 1 | 7.10 |
| CHEMBL4639128 | GSK778 | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4635329 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2017291 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4639128 | GSK778 | IC50 | = | 1000.0 | nM | 6.00 |