Assay Detail
Functional
CHEMBL4405077
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RS4-11 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of 8-Methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one Derivatives as Highly Potent and Selective Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.41 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.19 |
| CHEMBL4440098 | — | — | 1 | 7.66 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4440098 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 416.0 | nM | 6.38 |