Assay Detail
Binding
CHEMBL3887989
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PARP-1 Enzymatic Assay: PARP-1 enzymatic assay was conducted using a method modified from HT F Homogeneous PARP Inhibition Assay Kit (Trevigen). 8.8 nM PARP-1 was pre-incubated with different concentrations of compounds in a buffer containing 100 mM Tris-HCl pH 8.0, 100 mM NaCl, 20 mM MgCl2, and 1% DMSO for 30 min at RT. The auto-PARylation reaction was initiated by addition of 500 nM NAD and 20 ng/ul activated DNA (Sigma) and incubated at RT for 40 min. The remaining NAD was detected by incubation with cycling assay solution containing 1% ethanol, 0.30 U/ml alcohol dehydrogenase, 25 uM resazurin, and 0.25 U/ml diaphorase for 50 min at RT. The concentration of NAD is proportional to the fluorescence signal at Ex 540 nm/Em 590 nm.
70
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 70 | 7.96 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4112930 | PAMIPARIB | 3.0 | 1 | 9.05 |
| CHEMBL4107982 | — | — | 1 | 8.96 |
| CHEMBL3983859 | — | — | 1 | 8.64 |
| CHEMBL3970252 | — | — | 2 | 8.59 |
| CHEMBL3984980 | — | — | 1 | 8.54 |
| CHEMBL3926240 | — | — | 1 | 8.48 |
| CHEMBL3922789 | — | — | 1 | 8.48 |
| CHEMBL3925115 | — | — | 1 | 8.48 |
| CHEMBL3905389 | — | — | 1 | 8.42 |
| CHEMBL3917078 | — | — | 1 | 8.35 |
| CHEMBL3908123 | — | — | 1 | 8.32 |
| CHEMBL3931972 | — | — | 1 | 8.29 |
| CHEMBL3914932 | — | — | 2 | 8.28 |
| CHEMBL3911687 | — | — | 1 | 8.28 |
| CHEMBL3975917 | — | — | 1 | 8.26 |
| CHEMBL3900548 | — | — | 1 | 8.24 |
| CHEMBL3908092 | — | — | 1 | 8.24 |
| CHEMBL3910080 | — | — | 1 | 8.22 |
| CHEMBL3929705 | — | — | 1 | 8.22 |
| CHEMBL3907218 | — | — | 1 | 8.22 |
| CHEMBL3972156 | — | — | 1 | 8.20 |
| CHEMBL3892363 | — | — | 1 | 8.20 |
| CHEMBL3962648 | — | — | 1 | 8.19 |
| CHEMBL3929889 | — | — | 1 | 8.19 |
| CHEMBL3947623 | — | — | 1 | 8.18 |
| CHEMBL3969742 | — | — | 1 | 8.17 |
| CHEMBL3933450 | — | — | 1 | 8.15 |
| CHEMBL3907535 | — | — | 1 | 8.15 |
| CHEMBL3906623 | — | — | 1 | 8.14 |
| CHEMBL3915929 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4112930 | PAMIPARIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4107982 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3983859 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3970252 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3984980 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3926240 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3922789 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3925115 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3905389 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3917078 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3908123 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3931972 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3911687 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3914932 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3914932 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3975917 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3908092 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3900548 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3910080 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3929705 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3907218 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3972156 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3892363 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3962648 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3929889 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3947623 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3969742 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3933450 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3907535 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3970252 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3906623 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3915929 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3930740 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3931542 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL3955609 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3901034 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3978425 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3969049 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3891329 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3901638 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3898162 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3978989 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3923029 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3961684 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL3905040 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3963459 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3906567 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL3954603 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3895581 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL3955636 | — | IC50 | = | 16.0 | nM | 7.80 |