Assay Detail
Functional
CHEMBL3767929
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against BRCA2-deficient human Capan1 cells
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CAPAN-1 |
| 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 | 42 | 6.50 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 8.30 |
| CHEMBL3765528 | — | — | 1 | 8.10 |
| CHEMBL3763497 | — | — | 1 | 8.05 |
| CHEMBL3763446 | — | — | 1 | 7.43 |
| CHEMBL3764202 | — | — | 1 | 7.41 |
| CHEMBL3764085 | — | — | 1 | 7.25 |
| CHEMBL3765056 | — | — | 1 | 7.15 |
| CHEMBL3765472 | — | — | 1 | 7.06 |
| CHEMBL3763188 | — | — | 1 | 6.97 |
| CHEMBL3764066 | — | — | 1 | 6.91 |
| CHEMBL3765611 | — | — | 1 | 6.87 |
| CHEMBL3764670 | — | — | 1 | 6.84 |
| CHEMBL3764951 | — | — | 1 | 6.84 |
| CHEMBL3765125 | — | — | 1 | 6.77 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 6.59 |
| CHEMBL3763674 | — | — | 1 | 6.56 |
| CHEMBL3763844 | — | — | 1 | 6.53 |
| CHEMBL3763822 | — | — | 1 | 6.52 |
| CHEMBL3765291 | — | — | 1 | 6.44 |
| CHEMBL3764920 | — | — | 1 | 6.41 |
| CHEMBL3764052 | — | — | 1 | 6.41 |
| CHEMBL3765434 | — | — | 1 | 6.38 |
| CHEMBL3763243 | — | — | 1 | 6.36 |
| CHEMBL3765318 | — | — | 1 | 6.34 |
| CHEMBL3763531 | — | — | 1 | 6.29 |
| CHEMBL3764829 | — | — | 1 | 6.22 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 6.21 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | 6.19 |
| CHEMBL3763370 | — | — | 1 | 6.11 |
| CHEMBL3763661 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3765528 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3763497 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3763446 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3764202 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3764085 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3765056 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3765472 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3763188 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL3764066 | — | EC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3765611 | — | EC50 | = | 134.0 | nM | 6.87 |
| CHEMBL3764951 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL3764670 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL3765125 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL521686 | OLAPARIB | EC50 | = | 259.0 | nM | 6.59 |
| CHEMBL3763674 | — | EC50 | = | 276.0 | nM | 6.56 |
| CHEMBL3763844 | — | EC50 | = | 298.0 | nM | 6.53 |
| CHEMBL3763822 | — | EC50 | = | 305.0 | nM | 6.52 |
| CHEMBL3765291 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3764920 | — | EC50 | = | 389.0 | nM | 6.41 |
| CHEMBL3764052 | — | EC50 | = | 387.0 | nM | 6.41 |
| CHEMBL3765434 | — | EC50 | = | 418.0 | nM | 6.38 |
| CHEMBL3763243 | — | EC50 | = | 434.0 | nM | 6.36 |
| CHEMBL3765318 | — | EC50 | = | 454.0 | nM | 6.34 |
| CHEMBL3763531 | — | EC50 | = | 514.0 | nM | 6.29 |
| CHEMBL3764829 | — | EC50 | = | 603.0 | nM | 6.22 |
| CHEMBL1173055 | RUCAPARIB | EC50 | = | 609.0 | nM | 6.21 |
| CHEMBL1094636 | NIRAPARIB | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3763370 | — | EC50 | = | 785.0 | nM | 6.11 |
| CHEMBL3763661 | — | EC50 | = | 818.0 | nM | 6.09 |
| CHEMBL3764188 | — | EC50 | = | 956.0 | nM | 6.02 |
| CHEMBL3764811 | — | EC50 | = | 979.0 | nM | 6.01 |
| CHEMBL3763963 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3764816 | — | EC50 | = | 1135.0 | nM | 5.95 |
| CHEMBL3764422 | — | EC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL3764624 | — | EC50 | = | 1883.0 | nM | 5.72 |
| CHEMBL3763705 | — | EC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL3765670 | — | EC50 | = | 2249.0 | nM | 5.65 |
| CHEMBL3763589 | — | EC50 | = | 2970.0 | nM | 5.53 |
| CHEMBL3764995 | — | EC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL3764990 | — | EC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL506871 | VELIPARIB | EC50 | > | 10000.0 | nM | - |