Assay Detail
Binding
CHEMBL5152029
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal Avi-6His-TEV tagged PARP2 full length expressed in pFastBac expression system incubated for 4 hrs by fluorescence anisotropy binding assay
25
Total Activities
25
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 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-<i>N</i>-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.74 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.22 |
| CHEMBL3137320 | TALAZOPARIB | 4.0 | 1 | 7.52 |
| CHEMBL1173055 | RUCAPARIB | 4.0 | 1 | 6.76 |
| CHEMBL506871 | VELIPARIB | 3.0 | 1 | 6.65 |
| CHEMBL5177596 | — | — | 1 | 6.31 |
| CHEMBL5191396 | — | — | 1 | 6.22 |
| CHEMBL5197101 | — | — | 1 | 5.96 |
| CHEMBL5209181 | — | — | 1 | 5.96 |
| CHEMBL5095220 | SARUPARIB | 3.0 | 1 | 5.85 |
| CHEMBL4874589 | — | — | 1 | 5.77 |
| CHEMBL1094636 | NIRAPARIB | 4.0 | 1 | 5.75 |
| CHEMBL5183769 | — | — | 1 | 5.62 |
| CHEMBL5200723 | — | — | 1 | 5.41 |
| CHEMBL5193246 | — | — | 1 | 5.40 |
| CHEMBL5181905 | — | — | 1 | 5.38 |
| CHEMBL5188853 | — | — | 1 | 5.31 |
| CHEMBL5195580 | — | — | 1 | 5.23 |
| CHEMBL3606021 | — | — | 1 | 5.18 |
| CHEMBL5178594 | — | — | 1 | 5.18 |
| CHEMBL5202060 | — | — | 1 | 5.13 |
| CHEMBL5197824 | — | — | 1 | 5.04 |
| CHEMBL251030 | — | — | 1 | 4.70 |
| CHEMBL5190481 | — | — | 1 | 4.66 |
| CHEMBL5176615 | — | — | 1 | 4.55 |
| CHEMBL5196187 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521686 | OLAPARIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3137320 | TALAZOPARIB | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1173055 | RUCAPARIB | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL506871 | VELIPARIB | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL5177596 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5191396 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5197101 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5209181 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5095220 | SARUPARIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4874589 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1094636 | NIRAPARIB | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5183769 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5200723 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5193246 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5181905 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5188853 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5195580 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3606021 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5178594 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5202060 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL5197824 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL251030 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5190481 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5176615 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL5196187 | — | IC50 | > | 26000.0 | nM | - |