Assay Detail
Binding
CHEMBL3767923
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PARP1 using [3H]NAD as substrate after 1 min by microplate scintillation counting analysis
56
Total Activities
55
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| IC50 | 55 | 8.26 | 9.24 |
| Ki | 1 | 8.92 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 2 | 9.24 |
| CHEMBL3764920 | — | — | 1 | 8.96 |
| CHEMBL3763446 | — | — | 1 | 8.84 |
| CHEMBL3764202 | — | — | 1 | 8.80 |
| CHEMBL3764085 | — | — | 1 | 8.73 |
| CHEMBL3764188 | — | — | 1 | 8.73 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.71 |
| CHEMBL3763531 | — | — | 1 | 8.71 |
| CHEMBL3765318 | — | — | 1 | 8.70 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 8.70 |
| CHEMBL3764829 | — | — | 1 | 8.70 |
| CHEMBL3764951 | — | — | 1 | 8.68 |
| CHEMBL3765434 | — | — | 1 | 8.68 |
| CHEMBL3765528 | — | — | 1 | 8.67 |
| CHEMBL3763188 | — | — | 1 | 8.67 |
| CHEMBL3763822 | — | — | 1 | 8.65 |
| CHEMBL3765056 | — | — | 1 | 8.64 |
| CHEMBL3764052 | — | — | 1 | 8.63 |
| CHEMBL3765291 | — | — | 1 | 8.63 |
| CHEMBL3765125 | — | — | 1 | 8.62 |
| CHEMBL3764422 | — | — | 1 | 8.61 |
| CHEMBL3763497 | — | — | 1 | 8.59 |
| CHEMBL3765611 | — | — | 1 | 8.58 |
| CHEMBL3764190 | — | — | 1 | 8.58 |
| CHEMBL3764995 | — | — | 1 | 8.56 |
| CHEMBL3763705 | — | — | 1 | 8.54 |
| CHEMBL3763674 | — | — | 1 | 8.51 |
| CHEMBL3764670 | — | — | 1 | 8.48 |
| CHEMBL3765275 | — | — | 1 | 8.44 |
| CHEMBL3763243 | — | — | 1 | 8.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL3764920 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3137320 | TALAZOPARIB | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3763446 | — | IC50 | = | 1.46 | nM | 8.84 |
| CHEMBL3764202 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3764085 | — | IC50 | = | 1.87 | nM | 8.73 |
| CHEMBL3764188 | — | IC50 | = | 1.84 | nM | 8.73 |
| CHEMBL3763531 | — | IC50 | = | 1.95 | nM | 8.71 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL3764829 | — | IC50 | = | 2.02 | nM | 8.70 |
| CHEMBL3765318 | — | IC50 | = | 2.02 | nM | 8.70 |
| CHEMBL3764951 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL3765434 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL3763188 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL3765528 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL3763822 | — | IC50 | = | 2.25 | nM | 8.65 |
| CHEMBL3765056 | — | IC50 | = | 2.29 | nM | 8.64 |
| CHEMBL3764052 | — | IC50 | = | 2.36 | nM | 8.63 |
| CHEMBL3765291 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL3765125 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3764422 | — | IC50 | = | 2.48 | nM | 8.61 |
| CHEMBL3763497 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3764190 | — | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL3765611 | — | IC50 | = | 2.63 | nM | 8.58 |
| CHEMBL3764995 | — | IC50 | = | 2.76 | nM | 8.56 |
| CHEMBL3763705 | — | IC50 | = | 2.88 | nM | 8.54 |
| CHEMBL3763674 | — | IC50 | = | 3.09 | nM | 8.51 |
| CHEMBL3764670 | — | IC50 | = | 3.29 | nM | 8.48 |
| CHEMBL3765275 | — | IC50 | = | 3.65 | nM | 8.44 |
| CHEMBL3763243 | — | IC50 | = | 3.63 | nM | 8.44 |
| CHEMBL3764811 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL3765472 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3763844 | — | IC50 | = | 4.02 | nM | 8.40 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 4.73 | nM | 8.32 |
| CHEMBL3763963 | — | IC50 | = | 5.27 | nM | 8.28 |
| CHEMBL3765670 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3764640 | — | IC50 | = | 5.85 | nM | 8.23 |
| CHEMBL3763370 | — | IC50 | = | 6.18 | nM | 8.21 |
| CHEMBL3763589 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3763661 | — | IC50 | = | 6.29 | nM | 8.20 |
| CHEMBL3764464 | — | IC50 | = | 7.35 | nM | 8.13 |
| CHEMBL3765661 | — | IC50 | = | 7.62 | nM | 8.12 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 8.05 | nM | 8.09 |
| CHEMBL3765357 | — | IC50 | = | 9.45 | nM | 8.03 |
| CHEMBL3763164 | — | IC50 | = | 9.59 | nM | 8.02 |
| CHEMBL3763348 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL3764066 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL3764974 | — | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL3763492 | — | IC50 | = | 24.5 | nM | 7.61 |