Assay Detail
Binding
CHEMBL5037316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human partial length BRD4 BD2 expressed in bacterial expression system assessed as dissociation constant by BROMOscan 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 | 8.42 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770724 | — | — | 1 | 9.52 |
| CHEMBL4639128 | GSK778 | — | 1 | 9.20 |
| CHEMBL4297454 | ABBV-744 | 1.0 | 1 | 8.68 |
| CHEMBL5080584 | — | — | 1 | 7.55 |
| CHEMBL5083660 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770724 | — | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL4639128 | GSK778 | Kd | = | 0.63 | nM | 9.20 |
| CHEMBL4297454 | ABBV-744 | Kd | = | 2.1 | nM | 8.68 |
| CHEMBL5080584 | — | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL5083660 | — | Kd | = | 67.0 | nM | 7.17 |