Assay Detail
Binding
CHEMBL5628152
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Inhibition of PARP1 (unknown origin) incubated for 1 hr by ELISA analysis
39
Total Activities
39
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
Identification of [1,2,4]Triazolo[4,3-a]pyrazine PARP1 inhibitors with overcome acquired resistance activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 8.02 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5631710 | — | — | 1 | 9.22 |
| CHEMBL5632420 | — | — | 1 | 9.15 |
| CHEMBL5632796 | — | — | 1 | 8.77 |
| CHEMBL5632854 | — | — | 1 | 8.70 |
| CHEMBL5633982 | — | — | 1 | 8.70 |
| CHEMBL5632428 | — | — | 1 | 8.55 |
| CHEMBL5632340 | — | — | 1 | 8.49 |
| CHEMBL5631531 | — | — | 1 | 8.49 |
| CHEMBL5633486 | — | — | 1 | 8.47 |
| CHEMBL3907010 | — | — | 1 | 8.40 |
| CHEMBL5632118 | — | — | 1 | 8.40 |
| CHEMBL521686 | OLAPARIB | 4.0 | 1 | 8.39 |
| CHEMBL5631466 | — | — | 1 | 8.39 |
| CHEMBL5631857 | — | — | 1 | 8.39 |
| CHEMBL3903910 | — | — | 1 | 8.37 |
| CHEMBL5631243 | — | — | 1 | 8.34 |
| CHEMBL5632074 | — | — | 1 | 8.24 |
| CHEMBL5633663 | — | — | 1 | 8.11 |
| CHEMBL5632868 | — | — | 1 | 8.04 |
| CHEMBL5632742 | — | — | 1 | 8.03 |
| CHEMBL3936349 | — | — | 1 | 7.92 |
| CHEMBL5631862 | — | — | 1 | 7.88 |
| CHEMBL5633084 | — | — | 1 | 7.75 |
| CHEMBL5632703 | — | — | 1 | 7.68 |
| CHEMBL5633542 | — | — | 1 | 7.60 |
| CHEMBL5632172 | — | — | 1 | 7.37 |
| CHEMBL5631371 | — | — | 1 | 7.21 |
| CHEMBL5634039 | — | — | 1 | 7.15 |
| CHEMBL5631781 | — | — | 1 | 6.97 |
| CHEMBL5633569 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5631710 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5632420 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5632796 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5632854 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5633982 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5632428 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5632340 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5631531 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5633486 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3907010 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5632118 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL521686 | OLAPARIB | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5631857 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL5631466 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3903910 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5631243 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5632074 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5633663 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL5632868 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5632742 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3936349 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5631862 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5633084 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL5632703 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5633542 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5632172 | — | IC50 | = | 42.8 | nM | 7.37 |
| CHEMBL5631371 | — | IC50 | = | 61.3 | nM | 7.21 |
| CHEMBL5634039 | — | IC50 | = | 70.7 | nM | 7.15 |
| CHEMBL5631781 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5633569 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL5632685 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5633556 | — | IC50 | = | 947.0 | nM | 6.02 |
| CHEMBL5632530 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL5633862 | — | IC50 | - | — | - | |
| CHEMBL5631422 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5633842 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5633704 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5631418 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5633159 | — | IC50 | > | 1000.0 | nM | - |