Assay Detail
Binding
CHEMBL5054300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BRD4 (1 to 477 residues) measured after 60 mins by TR-FRET assay
18
Total Activities
18
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
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.84 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5080354 | — | — | 1 | 9.00 |
| CHEMBL4297458 | EZOBRESIB | 2.0 | 1 | 8.96 |
| CHEMBL5093440 | — | — | 1 | 8.82 |
| CHEMBL5087175 | — | — | 1 | 8.72 |
| CHEMBL5082474 | — | — | 1 | 8.72 |
| CHEMBL5074438 | — | — | 1 | 8.38 |
| CHEMBL3786449 | — | — | 1 | 8.36 |
| CHEMBL5074708 | — | — | 1 | 8.35 |
| CHEMBL5075046 | — | — | 1 | 8.27 |
| CHEMBL5075119 | — | — | 1 | 8.02 |
| CHEMBL5089900 | — | — | 1 | 7.64 |
| CHEMBL5085106 | — | — | 1 | 7.46 |
| CHEMBL5090216 | — | — | 1 | 7.41 |
| CHEMBL5094725 | — | — | 1 | 7.16 |
| CHEMBL5080617 | — | — | 1 | 6.88 |
| CHEMBL5093519 | — | — | 1 | 6.54 |
| CHEMBL5090264 | — | — | 1 | 6.28 |
| CHEMBL5083442 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080354 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4297458 | EZOBRESIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5093440 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5087175 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5082474 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5074438 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3786449 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5074708 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5075046 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5075119 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL5089900 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5085106 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5090216 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5094725 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5080617 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5093519 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL5090264 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5083442 | — | IC50 | = | 712.0 | nM | 6.15 |