Assay Detail
Binding
CHEMBL3887956
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Cellular Assay: Based on the preliminary PARP1 inhibition evaluation of compounds at molecular level by ELISA, compounds were further evaluated for their cellular inhibition against PARP1 using a proliferation inhibition model.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.45 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936349 | — | — | 1 | 8.15 |
| CHEMBL3907010 | — | — | 1 | 7.76 |
| CHEMBL3903910 | — | — | 1 | 7.61 |
| CHEMBL3943929 | — | — | 1 | 7.45 |
| CHEMBL3960883 | — | — | 1 | 7.08 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 7.06 |
| CHEMBL3912508 | — | — | 1 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936349 | — | IC50 | = | 7.15 | nM | 8.15 |
| CHEMBL3907010 | — | IC50 | = | 17.33 | nM | 7.76 |
| CHEMBL3903910 | — | IC50 | = | 24.77 | nM | 7.61 |
| CHEMBL3943929 | — | IC50 | = | 35.52 | nM | 7.45 |
| CHEMBL3960883 | — | IC50 | = | 83.97 | nM | 7.08 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 86.32 | nM | 7.06 |
| CHEMBL3912508 | — | IC50 | = | 98.74 | nM | 7.01 |