Assay Detail
Binding
CHEMBL2330729
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Inhibition of human recombinant PARP1 after 1 hr by ELISA
35
Total Activities
35
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
Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.11 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2322618 | — | — | 1 | 9.51 |
| CHEMBL2323218 | — | — | 1 | 8.74 |
| CHEMBL2323222 | — | — | 1 | 8.72 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.40 |
| CHEMBL2323545 | — | — | 1 | 7.72 |
| CHEMBL2323220 | — | — | 1 | 7.48 |
| CHEMBL2322612 | — | — | 1 | 7.44 |
| CHEMBL2323221 | — | — | 1 | 7.35 |
| CHEMBL2323544 | — | — | 1 | 6.68 |
| CHEMBL2323219 | — | — | 1 | 6.68 |
| CHEMBL2323539 | — | — | 1 | 6.52 |
| CHEMBL2322617 | — | — | 1 | 6.31 |
| CHEMBL2323530 | — | — | 1 | 6.25 |
| CHEMBL2323534 | — | — | 1 | 6.24 |
| CHEMBL2323543 | — | — | 1 | 5.96 |
| CHEMBL2323224 | — | — | 1 | 5.86 |
| CHEMBL2323226 | — | — | 1 | 5.46 |
| CHEMBL2323533 | — | — | 1 | 5.32 |
| CHEMBL2323542 | — | — | 1 | 5.07 |
| CHEMBL2323540 | — | — | 1 | 5.06 |
| CHEMBL2323535 | — | — | 1 | 5.06 |
| CHEMBL2323541 | — | — | 1 | 5.05 |
| CHEMBL2321894 | — | — | 1 | 5.05 |
| CHEMBL2323537 | — | — | 1 | 5.03 |
| CHEMBL2323536 | — | — | 1 | 5.03 |
| CHEMBL2322613 | — | — | 1 | 4.95 |
| CHEMBL2323531 | — | — | 1 | 4.12 |
| CHEMBL2323532 | — | — | 1 | 4.08 |
| CHEMBL2323227 | — | — | 1 | 4.06 |
| CHEMBL2322614 | — | — | 1 | 4.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2322618 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL2323218 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2323222 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2323545 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2323220 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2322612 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2323221 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2323544 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2323219 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL2323539 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2322617 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2323530 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL2323534 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2323543 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2323224 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL2323226 | — | IC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL2323533 | — | IC50 | = | 4810.0 | nM | 5.32 |
| CHEMBL2323542 | — | IC50 | = | 8520.0 | nM | 5.07 |
| CHEMBL2323540 | — | IC50 | = | 8720.0 | nM | 5.06 |
| CHEMBL2323535 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL2323541 | — | IC50 | = | 8960.0 | nM | 5.05 |
| CHEMBL2321894 | — | IC50 | = | 8890.0 | nM | 5.05 |
| CHEMBL2323537 | — | IC50 | = | 9350.0 | nM | 5.03 |
| CHEMBL2323536 | — | IC50 | = | 9380.0 | nM | 5.03 |
| CHEMBL2322613 | — | IC50 | = | 11230.0 | nM | 4.95 |
| CHEMBL2323531 | — | IC50 | = | 76600.0 | nM | 4.12 |
| CHEMBL2323532 | — | IC50 | = | 83900.0 | nM | 4.08 |
| CHEMBL2323227 | — | IC50 | = | 86200.0 | nM | 4.06 |
| CHEMBL2322614 | — | IC50 | = | 86340.0 | nM | 4.06 |
| CHEMBL2323223 | — | IC50 | = | 156000.0 | nM | - |
| CHEMBL2322616 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2323225 | — | IC50 | = | 387000.0 | nM | - |
| CHEMBL2323538 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2322615 | — | IC50 | = | 145750.0 | nM | - |