Assay Detail
Binding
CHEMBL5373879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PARP2 (unknown origin)
6
Total Activities
6
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 Quinazoline-2,4(1<i>H</i>,3<i>H</i>)-dione Derivatives Containing a Piperizinone Moiety as Potent PARP-1/2 Inhibitors─Design, Synthesis, <i>In Vivo</i> Antitumor Activity, and X-ray Crystal Structure Analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.20 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 9.52 |
| CHEMBL4112930 | PAMIPARIB | 3.0 | 1 | 9.52 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 9.30 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 9.00 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | 8.68 |
| CHEMBL5402698 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5402698 | — | IC50 | < | 0.001 | nM | - |