Assay Detail
Binding
CHEMBL3767926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LoVo |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 | 39 | 7.76 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 8.60 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.45 |
| CHEMBL3763674 | — | — | 1 | 8.42 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 8.33 |
| CHEMBL3763446 | — | — | 1 | 8.29 |
| CHEMBL3765528 | — | — | 1 | 8.26 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 8.23 |
| CHEMBL3764052 | — | — | 1 | 8.22 |
| CHEMBL3765611 | — | — | 1 | 8.21 |
| CHEMBL3764920 | — | — | 1 | 8.20 |
| CHEMBL3763661 | — | — | 1 | 8.17 |
| CHEMBL3763822 | — | — | 1 | 8.16 |
| CHEMBL3765056 | — | — | 1 | 8.16 |
| CHEMBL3764670 | — | — | 1 | 8.07 |
| CHEMBL3764188 | — | — | 1 | 8.03 |
| CHEMBL3763844 | — | — | 1 | 8.02 |
| CHEMBL3763243 | — | — | 1 | 8.01 |
| CHEMBL3763531 | — | — | 1 | 7.97 |
| CHEMBL3765670 | — | — | 1 | 7.93 |
| CHEMBL3763164 | — | — | 1 | 7.82 |
| CHEMBL3765291 | — | — | 1 | 7.77 |
| CHEMBL3764085 | — | — | 1 | 7.77 |
| CHEMBL3764202 | — | — | 1 | 7.75 |
| CHEMBL3763188 | — | — | 1 | 7.74 |
| CHEMBL3764422 | — | — | 1 | 7.73 |
| CHEMBL3764811 | — | — | 1 | 7.73 |
| CHEMBL3765434 | — | — | 1 | 7.71 |
| CHEMBL3765318 | — | — | 1 | 7.64 |
| CHEMBL3764464 | — | — | 1 | 7.61 |
| CHEMBL3763963 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | EC50 | = | 2.51 | nM | 8.60 |
| CHEMBL521686 | OLAPARIB | EC50 | = | 3.57 | nM | 8.45 |
| CHEMBL3763674 | — | EC50 | = | 3.81 | nM | 8.42 |
| CHEMBL1173055 | RUCAPARIB | EC50 | = | 4.69 | nM | 8.33 |
| CHEMBL3763446 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3765528 | — | EC50 | = | 5.48 | nM | 8.26 |
| CHEMBL506871 | VELIPARIB | EC50 | = | 5.94 | nM | 8.23 |
| CHEMBL3764052 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3765611 | — | EC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3764920 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3763661 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3763822 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3765056 | — | EC50 | = | 6.94 | nM | 8.16 |
| CHEMBL3764670 | — | EC50 | = | 8.48 | nM | 8.07 |
| CHEMBL3764188 | — | EC50 | = | 9.33 | nM | 8.03 |
| CHEMBL3763844 | — | EC50 | = | 9.47 | nM | 8.02 |
| CHEMBL3763243 | — | EC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3763531 | — | EC50 | = | 10.8 | nM | 7.97 |
| CHEMBL3765670 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL3763164 | — | EC50 | = | 15.2 | nM | 7.82 |
| CHEMBL3764085 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3765291 | — | EC50 | = | 16.9 | nM | 7.77 |
| CHEMBL3764202 | — | EC50 | = | 17.9 | nM | 7.75 |
| CHEMBL3763188 | — | EC50 | = | 18.1 | nM | 7.74 |
| CHEMBL3764422 | — | EC50 | = | 18.5 | nM | 7.73 |
| CHEMBL3764811 | — | EC50 | = | 18.6 | nM | 7.73 |
| CHEMBL3765434 | — | EC50 | = | 19.7 | nM | 7.71 |
| CHEMBL3765318 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3764464 | — | EC50 | = | 24.4 | nM | 7.61 |
| CHEMBL3763963 | — | EC50 | = | 27.2 | nM | 7.57 |
| CHEMBL3764829 | — | EC50 | = | 40.6 | nM | 7.39 |
| CHEMBL3763589 | — | EC50 | = | 58.4 | nM | 7.23 |
| CHEMBL3763370 | — | EC50 | = | 121.0 | nM | 6.92 |
| CHEMBL3765125 | — | EC50 | = | 149.0 | nM | 6.83 |
| CHEMBL3764066 | — | EC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3764624 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3764990 | — | EC50 | = | 285.0 | nM | 6.54 |
| CHEMBL3764816 | — | EC50 | = | 864.0 | nM | 6.06 |
| CHEMBL1094636 | NIRAPARIB | EC50 | - | — | - |