Assay Detail
Binding
CHEMBL4380268
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Inhibition of recombinant human PARP1 using histone as substrate after 1 hr in presence of biotinylated NAD+ by ELISA
19
Total Activities
19
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 Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.71 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4461392 | — | — | 1 | 9.36 |
| CHEMBL4437593 | — | — | 1 | 9.19 |
| CHEMBL4549595 | — | — | 1 | 9.17 |
| CHEMBL4525998 | — | — | 1 | 9.16 |
| CHEMBL4436980 | — | — | 1 | 9.14 |
| CHEMBL4461382 | — | — | 1 | 9.08 |
| CHEMBL4571423 | — | — | 1 | 9.08 |
| CHEMBL4551779 | — | — | 1 | 8.97 |
| CHEMBL4436366 | — | — | 1 | 8.96 |
| CHEMBL4446789 | — | — | 1 | 8.95 |
| CHEMBL4438927 | — | — | 1 | 8.93 |
| CHEMBL4438741 | — | — | 1 | 8.59 |
| CHEMBL4593274 | — | — | 1 | 8.31 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.30 |
| CHEMBL4470724 | — | — | 1 | 8.22 |
| CHEMBL4531016 | — | — | 1 | 8.21 |
| CHEMBL4551630 | — | — | 1 | 8.10 |
| CHEMBL4541731 | — | — | 1 | 8.02 |
| CHEMBL4465869 | — | — | 1 | 7.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4461392 | — | IC50 | = | 0.4365 | nM | 9.36 |
| CHEMBL4437593 | — | IC50 | = | 0.6457 | nM | 9.19 |
| CHEMBL4549595 | — | IC50 | = | 0.6761 | nM | 9.17 |
| CHEMBL4525998 | — | IC50 | = | 0.6918 | nM | 9.16 |
| CHEMBL4436980 | — | IC50 | = | 0.7244 | nM | 9.14 |
| CHEMBL4461382 | — | IC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL4571423 | — | IC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL4551779 | — | IC50 | = | 1.072 | nM | 8.97 |
| CHEMBL4436366 | — | IC50 | = | 1.096 | nM | 8.96 |
| CHEMBL4446789 | — | IC50 | = | 1.122 | nM | 8.95 |
| CHEMBL4438927 | — | IC50 | = | 1.175 | nM | 8.93 |
| CHEMBL4438741 | — | IC50 | = | 2.57 | nM | 8.59 |
| CHEMBL4593274 | — | IC50 | = | 4.898 | nM | 8.31 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL4470724 | — | IC50 | = | 6.026 | nM | 8.22 |
| CHEMBL4531016 | — | IC50 | = | 6.166 | nM | 8.21 |
| CHEMBL4551630 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4541731 | — | IC50 | = | 9.55 | nM | 8.02 |
| CHEMBL4465869 | — | IC50 | = | 15.49 | nM | 7.81 |