Assay Detail
Binding
CHEMBL5037314
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Binding affinity to BRD4 BD1 (unknown origin) assessed as dissociation constant by Discover X 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
4-Methyl-1,2,3-Triazoles as <i>N</i>-Acetyl-Lysine Mimics Afford Potent BET Bromodomain Inhibitors with Improved Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 7.45 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639128 | GSK778 | — | 1 | 8.20 |
| CHEMBL5080584 | — | — | 1 | 8.19 |
| CHEMBL5083660 | — | — | 1 | 7.92 |
| CHEMBL4297454 | ABBV-744 | 1.0 | 1 | 5.48 |
| CHEMBL3770724 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4639128 | GSK778 | Kd | = | 6.3 | nM | 8.20 |
| CHEMBL5080584 | — | Kd | = | 6.4 | nM | 8.19 |
| CHEMBL5083660 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL4297454 | ABBV-744 | Kd | = | 3300.0 | nM | 5.48 |
| CHEMBL3770724 | — | Kd | = | 3.4 | nM | - |