Assay Detail
Binding
CHEMBL5351864
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Inhibition of BRD4 BD1 (unknown origin)
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Bromodomain and Extra Terminal Domain (BET) Inhibitor with the Selectivity for the Second Bromodomain (BD2) and the Capacity for the Treatment of Inflammatory Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.36 | 5.94 |
| Ki | 1 | 6.28 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4297454 | ABBV-744 | 1.0 | 1 | 6.28 |
| CHEMBL4466553 | — | — | 1 | 5.94 |
| CHEMBL5432981 | — | — | 1 | 5.35 |
| CHEMBL4635134 | GSK620 | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4297454 | ABBV-744 | Ki | = | 521.0 | nM | 6.28 |
| CHEMBL4466553 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL5432981 | — | IC50 | = | 4460.0 | nM | 5.35 |
| CHEMBL4635134 | GSK620 | IC50 | = | 15848.0 | nM | 4.80 |