Assay Detail
Binding
CHEMBL4625974
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to 6His-Thr-BRD3 (1 to 435 residues) BD2 domain Y348A or Y73A mutant (unknown origin) incubated for 30 mins by TR-FRET assay
5
Total Activities
5
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
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.24 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648431 | — | — | 1 | 7.80 |
| CHEMBL4635134 | GSK620 | — | 1 | 7.10 |
| CHEMBL4633353 | — | — | 1 | 6.30 |
| CHEMBL4637442 | — | — | 1 | 5.00 |
| CHEMBL4639878 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648431 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4635134 | GSK620 | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4633353 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4637442 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4639878 | — | IC50 | = | 10000.0 | nM | 5.00 |