Assay Detail
Binding
CHEMBL4626992
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 BRDT BD2 (1 to 397 residues)/BD1 Y66A 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 |
Target
Bromodomain testis-specific protein (CHEMBL1795185) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 5.70 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4635329 | — | — | 1 | 6.50 |
| CHEMBL2017291 | — | — | 1 | 5.80 |
| CHEMBL4639128 | GSK778 | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4635329 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL2017291 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4639128 | GSK778 | IC50 | = | 15848.93 | nM | 4.80 |