Assay Detail
Binding
CHEMBL1010817
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PARP1 in human C41 cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | C41 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 8.00 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL498007 | — | — | 1 | 9.00 |
| CHEMBL498015 | — | — | 1 | 8.70 |
| CHEMBL495743 | — | — | 1 | 8.70 |
| CHEMBL496976 | — | — | 1 | 8.70 |
| CHEMBL521712 | — | — | 1 | 8.70 |
| CHEMBL495969 | — | — | 1 | 8.70 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 8.70 |
| CHEMBL497609 | — | — | 1 | 8.52 |
| CHEMBL497608 | — | — | 1 | 8.52 |
| CHEMBL521880 | — | — | 1 | 8.52 |
| CHEMBL506516 | — | — | 1 | 8.52 |
| CHEMBL450698 | — | — | 1 | 8.40 |
| CHEMBL498008 | — | — | 1 | 8.40 |
| CHEMBL525535 | — | — | 1 | 8.40 |
| CHEMBL522549 | — | — | 1 | 8.40 |
| CHEMBL445016 | — | — | 1 | 8.30 |
| CHEMBL497597 | — | — | 1 | 8.22 |
| CHEMBL507412 | — | — | 1 | 8.15 |
| CHEMBL495951 | — | — | 1 | 8.10 |
| CHEMBL521714 | — | — | 1 | 8.10 |
| CHEMBL504096 | — | — | 1 | 7.89 |
| CHEMBL488831 | — | — | 1 | 7.80 |
| CHEMBL526668 | — | — | 1 | 7.77 |
| CHEMBL505909 | — | — | 1 | 7.75 |
| CHEMBL488830 | — | — | 1 | 7.75 |
| CHEMBL523083 | — | — | 1 | 7.70 |
| CHEMBL495975 | — | — | 1 | 7.60 |
| CHEMBL497181 | — | — | 1 | 7.55 |
| CHEMBL488053 | — | — | 1 | 7.51 |
| CHEMBL509153 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL498007 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL498015 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL506871 | VELIPARIB | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL495969 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL521712 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL496976 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL495743 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL497609 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL497608 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL521880 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL506516 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL450698 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL498008 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL525535 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL522549 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL445016 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL497597 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL507412 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL495951 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL521714 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL504096 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL488831 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL526668 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL505909 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL488830 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL523083 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL495975 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL497181 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL488053 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL509153 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL495782 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL495942 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL525192 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL488496 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL527654 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL495950 | — | EC50 | > | 1000.0 | nM | - |