Assay Detail
Binding
CHEMBL5349003
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Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assay
16
Total Activities
16
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
From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.86 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5424952 | — | — | 1 | 10.00 |
| CHEMBL5440537 | — | — | 1 | 9.70 |
| CHEMBL5432745 | — | — | 1 | 9.70 |
| CHEMBL5401253 | — | — | 1 | 9.52 |
| CHEMBL5440963 | — | — | 1 | 9.52 |
| CHEMBL5422881 | — | — | 1 | 9.40 |
| CHEMBL5403848 | — | — | 1 | 9.22 |
| CHEMBL5436475 | — | — | 1 | 9.15 |
| CHEMBL5422163 | — | — | 1 | 9.00 |
| CHEMBL5439607 | — | — | 1 | 9.00 |
| CHEMBL5400310 | — | — | 1 | 8.52 |
| CHEMBL5399489 | — | — | 1 | 8.22 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 8.05 |
| CHEMBL1957266 | — | — | 1 | 7.89 |
| CHEMBL5420752 | — | — | 1 | 7.58 |
| CHEMBL5398000 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5424952 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5440537 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5432745 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5401253 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5440963 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5422881 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5403848 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5436475 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5422163 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5439607 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5400310 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5399489 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1957266 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5420752 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5398000 | — | IC50 | = | 60.0 | nM | 7.22 |