Assay Detail
Binding
CHEMBL3887960
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Assay: In order to test the selectivity of substituents on piperazinotriazole ring within the PARP family, the selectivity of compound S3 and positive compound AZD2281 were tested.
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Poly [ADP-ribose] polymerase tankyrase-1 (CHEMBL6164) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.59 | 7.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521686 | OLAPARIB | 4.0 | 2 | 7.98 |
| CHEMBL3907010 | — | — | 2 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521686 | OLAPARIB | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL3907010 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL3907010 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 1700.0 | nM | 5.77 |