Assay Detail
Binding
CHEMBL4678541
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 pre-incubated for 30 mins before addition of activated DNA and NAD by fluorescence based assay
58
Total Activities
58
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 |
|---|---|---|---|
| IC50 | 58 | 7.96 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4112930 | PAMIPARIB | 3.0 | 1 | 8.89 |
| CHEMBL3983859 | — | — | 1 | 8.64 |
| CHEMBL3984980 | — | — | 1 | 8.54 |
| CHEMBL3926240 | — | — | 1 | 8.48 |
| CHEMBL3925115 | — | — | 1 | 8.48 |
| CHEMBL3922789 | — | — | 1 | 8.48 |
| CHEMBL3905389 | — | — | 1 | 8.42 |
| CHEMBL3917078 | — | — | 1 | 8.35 |
| CHEMBL3908123 | — | — | 1 | 8.34 |
| CHEMBL4784831 | — | — | 1 | 8.33 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.32 |
| CHEMBL3910080 | — | — | 1 | 8.31 |
| CHEMBL3931972 | — | — | 1 | 8.29 |
| CHEMBL3911687 | — | — | 1 | 8.28 |
| CHEMBL3975917 | — | — | 1 | 8.26 |
| CHEMBL3900548 | — | — | 1 | 8.24 |
| CHEMBL3908092 | — | — | 1 | 8.24 |
| CHEMBL3929705 | — | — | 1 | 8.22 |
| CHEMBL3972156 | — | — | 1 | 8.20 |
| CHEMBL3962648 | — | — | 1 | 8.19 |
| CHEMBL3929889 | — | — | 1 | 8.19 |
| CHEMBL4749094 | — | — | 1 | 8.18 |
| CHEMBL3947623 | — | — | 1 | 8.18 |
| CHEMBL3969742 | — | — | 1 | 8.17 |
| CHEMBL4776661 | — | — | 1 | 8.15 |
| CHEMBL3907535 | — | — | 1 | 8.15 |
| CHEMBL3970252 | — | — | 1 | 8.14 |
| CHEMBL3906623 | — | — | 1 | 8.14 |
| CHEMBL4749300 | — | — | 1 | 8.10 |
| CHEMBL4107982 | — | — | 1 | 8.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3983859 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3984980 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3926240 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3925115 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3922789 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3905389 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3917078 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3908123 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4784831 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3910080 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3931972 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3911687 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3975917 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3900548 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3908092 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3929705 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3972156 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3962648 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3929889 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4749094 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3947623 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3969742 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3907535 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4776661 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3970252 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3906623 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4749300 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4107982 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3931542 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3901034 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4784468 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4748572 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3891329 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL3969049 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL3898162 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL3901638 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL3961684 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL3905040 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4778454 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL3906567 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL3954603 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3983247 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL3895581 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL3970120 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL4788782 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL3910594 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3983342 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3916191 | — | IC50 | = | 25.6 | nM | 7.59 |