Assay Detail
Binding
CHEMBL3887955
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ELISA Assay: The HTb-PARP1 positive clones were obtained using the full-length PARP1 plasmid, through PCR amplification, enzyme digestion, ligation, and transformation into DH5a. The plasmids were extracted and determined by enzyme cleavage, and then transformed into DH10Bac. Bacmid/PARP is determined by PCR and sequencing. TNI was transfected, the viruses were collected, and cells were lysed. PARP1 protein was purified by affinity chromatography and determined by Western blotting. A plate was coated by substrate histone, NAD+ and DNA, as well as expressed PARP1 enzyme, was placed into 96-well plate reaction system. Various reaction conditions were optimized and ultimately determined.
27
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.40 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3961901 | — | — | 1 | 8.15 |
| CHEMBL3907010 | — | — | 2 | 8.00 |
| CHEMBL4109341 | — | — | 1 | 7.82 |
| CHEMBL521686 | OLAPARIB | 4.0 | 2 | 7.37 |
| CHEMBL3947382 | — | — | 1 | 6.52 |
| CHEMBL3902201 | — | — | 1 | 6.51 |
| CHEMBL3949270 | — | — | 1 | - |
| CHEMBL3921468 | — | — | 1 | - |
| CHEMBL3961502 | — | — | 1 | - |
| CHEMBL3960883 | — | — | 1 | - |
| CHEMBL3891009 | — | — | 1 | - |
| CHEMBL3927402 | — | — | 1 | - |
| CHEMBL3958419 | — | — | 1 | - |
| CHEMBL3921987 | — | — | 1 | - |
| CHEMBL3912508 | — | — | 1 | - |
| CHEMBL3977995 | — | — | 1 | - |
| CHEMBL3903910 | — | — | 1 | - |
| CHEMBL3936349 | — | — | 1 | - |
| CHEMBL3966173 | — | — | 1 | - |
| CHEMBL3893902 | — | — | 1 | - |
| CHEMBL3925404 | — | — | 1 | - |
| CHEMBL3891552 | — | — | 1 | - |
| CHEMBL3943929 | — | — | 1 | - |
| CHEMBL3934965 | — | — | 1 | - |
| CHEMBL3949758 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3961901 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3907010 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4109341 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3947382 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3902201 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3949270 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3921468 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3961502 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3960883 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3891009 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3927402 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3958419 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3921987 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3949758 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3912508 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3903910 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3936349 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3966173 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3893902 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3925404 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3891552 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL3943929 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3907010 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL3934965 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL521686 | OLAPARIB | IC50 | < | 50.0 | nM | - |
| CHEMBL3977995 | — | IC50 | < | 20.0 | nM | - |