Assay Detail
Binding
CHEMBL3743853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein mono-ADP-ribosyltransferase PARP6 (CHEMBL2380187) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.34 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3740897 | — | — | 1 | 7.08 |
| CHEMBL3740104 | — | — | 1 | 6.19 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3740897 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3740104 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 1800.0 | nM | 5.75 |