Assay Detail
Binding
CHEMBL4678516
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PARP-1 catalytic domain (662 to 1011 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 0.5 hrs by fluorescence polarization assay based DNA trapping activity assay
5
Total Activities
5
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 Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.64 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 8.49 |
| CHEMBL4112930 | PAMIPARIB | 3.0 | 1 | 7.89 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 7.77 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 6.40 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137320 | TALAZOPARIB | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4112930 | PAMIPARIB | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1173055 | RUCAPARIB | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL506871 | VELIPARIB | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL521686 | OLAPARIB | EC50 | = | 16.0 | nM | - |