Assay Detail
Binding
CHEMBL4625972
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to 6His-Thr-BRD2 (1 to 473 residues) BD2 domain Y386A or Y113A 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 | 5.70 | 7.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648431 | — | — | 1 | 7.20 |
| CHEMBL4635134 | GSK620 | — | 1 | 6.50 |
| CHEMBL4633353 | — | — | 1 | 5.60 |
| CHEMBL4637442 | — | — | 1 | 4.60 |
| CHEMBL4639878 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648431 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4635134 | GSK620 | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4633353 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4637442 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4639878 | — | IC50 | = | 25118.86 | nM | 4.60 |