Assay Detail
Functional
CHEMBL4405047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MV4-11 |
| 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 | 26 | 7.46 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | 2.0 | 1 | 8.72 |
| CHEMBL4440098 | — | — | 1 | 8.62 |
| CHEMBL4539863 | — | — | 1 | 8.31 |
| CHEMBL4522212 | — | — | 1 | 8.19 |
| CHEMBL4543167 | — | — | 1 | 7.85 |
| CHEMBL4524758 | — | — | 1 | 7.84 |
| CHEMBL4461077 | — | — | 1 | 7.83 |
| CHEMBL4461662 | — | — | 1 | 7.69 |
| CHEMBL4441348 | — | — | 1 | 7.44 |
| CHEMBL3581647 | BIRABRESIB | 2.0 | 1 | 7.33 |
| CHEMBL4550412 | — | — | 1 | 6.93 |
| CHEMBL4445399 | — | — | 1 | 6.73 |
| CHEMBL4579454 | — | — | 1 | 6.68 |
| CHEMBL4449279 | — | — | 1 | 6.59 |
| CHEMBL4567383 | — | — | 1 | 6.41 |
| CHEMBL4474369 | — | — | 1 | 6.27 |
| CHEMBL4557084 | — | — | 1 | - |
| CHEMBL4564804 | — | — | 1 | - |
| CHEMBL4462005 | — | — | 1 | - |
| CHEMBL4542938 | — | — | 1 | - |
| CHEMBL4466659 | — | — | 1 | - |
| CHEMBL4467880 | — | — | 1 | - |
| CHEMBL4470237 | — | — | 1 | - |
| CHEMBL4579222 | — | — | 1 | - |
| CHEMBL4441706 | — | — | 1 | - |
| CHEMBL4473292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3987016 | MIVEBRESIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4440098 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4539863 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4522212 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4543167 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL4524758 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL4461077 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL4461662 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL4441348 | — | IC50 | = | 36.6 | nM | 7.44 |
| CHEMBL3581647 | BIRABRESIB | IC50 | = | 46.3 | nM | 7.33 |
| CHEMBL4550412 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4445399 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4579454 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL4449279 | — | IC50 | = | 256.9 | nM | 6.59 |
| CHEMBL4567383 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL4474369 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL4557084 | — | IC50 | - | — | - | |
| CHEMBL4564804 | — | IC50 | - | — | - | |
| CHEMBL4462005 | — | IC50 | - | — | - | |
| CHEMBL4542938 | — | IC50 | - | — | - | |
| CHEMBL4466659 | — | IC50 | - | — | - | |
| CHEMBL4467880 | — | IC50 | - | — | - | |
| CHEMBL4470237 | — | IC50 | - | — | - | |
| CHEMBL4579222 | — | IC50 | - | — | - | |
| CHEMBL4441706 | — | IC50 | - | — | - | |
| CHEMBL4473292 | — | IC50 | - | — | - |