Assay Detail
Functional
CHEMBL3767931
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Cytotoxicity against BRCA1-deficient human MX1 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MX1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 8.48 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 9.52 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 8.28 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 7.63 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | - |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1173055 | RUCAPARIB | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL521686 | OLAPARIB | EC50 | = | 23.2 | nM | 7.63 |
| CHEMBL506871 | VELIPARIB | EC50 | - | — | - | |
| CHEMBL1094636 | NIRAPARIB | EC50 | - | — | - |