Assay Detail
Binding
CHEMBL5165804
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Inhibition of PARP1 (unknown origin)
3
Total Activities
3
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 of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.97 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 9.10 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.10 |
| CHEMBL5197463 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5197463 | — | IC50 | = | 197.0 | nM | 6.71 |