Assay Detail
Binding
CHEMBL860595
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human PARP1
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of novel pyrrolocarbazole lactam analogs as potent and cell-permeable inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.84 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383442 | — | — | 1 | 7.75 |
| CHEMBL204542 | — | — | 1 | 7.57 |
| CHEMBL383716 | — | — | 1 | 7.52 |
| CHEMBL204250 | — | — | 1 | 7.44 |
| CHEMBL201931 | — | — | 1 | 7.25 |
| CHEMBL381977 | — | — | 1 | 7.23 |
| CHEMBL203597 | — | — | 1 | 7.19 |
| CHEMBL378794 | — | — | 1 | 7.10 |
| CHEMBL204849 | — | — | 1 | 7.10 |
| CHEMBL203982 | — | — | 1 | 7.08 |
| CHEMBL381475 | — | — | 1 | 6.98 |
| CHEMBL380488 | — | — | 1 | 6.92 |
| CHEMBL203884 | — | — | 1 | 6.79 |
| CHEMBL204898 | — | — | 1 | 6.79 |
| CHEMBL204440 | — | — | 1 | 6.78 |
| CHEMBL201883 | — | — | 1 | 6.70 |
| CHEMBL202848 | — | — | 1 | 6.62 |
| CHEMBL205135 | — | — | 1 | 6.17 |
| CHEMBL204643 | — | — | 1 | 6.10 |
| CHEMBL381153 | — | — | 1 | 5.52 |
| CHEMBL382430 | — | — | 1 | 5.00 |
| CHEMBL202426 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383442 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL204542 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL383716 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL204250 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL201931 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL381977 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL203597 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL378794 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL204849 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL203982 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL381475 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL380488 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL203884 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL204898 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL204440 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL201883 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL202848 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL205135 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL204643 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL381153 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL382430 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL202426 | — | IC50 | > | 10000.0 | nM | - |