Assay Detail
Binding
CHEMBL4003518
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Inhibition of recombinant human N-terminal GST-tagged PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells measured after 1 hr by chemiluminescence assay
12
Total Activities
7
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
Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.14 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1892587 | — | — | 2 | 6.90 |
| CHEMBL4059827 | — | — | 2 | 6.85 |
| CHEMBL4080163 | — | — | 2 | 6.84 |
| CHEMBL4098188 | — | — | 2 | 5.16 |
| CHEMBL4069447 | — | — | 2 | 4.94 |
| CHEMBL4063631 | — | — | 1 | - |
| CHEMBL1956162 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1892587 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1892587 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4059827 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL4059827 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4080163 | — | IC50 | = | 144.54 | nM | 6.84 |
| CHEMBL4080163 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4098188 | — | IC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL4098188 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL4069447 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL4069447 | — | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL4063631 | — | IC50 | - | — | - | |
| CHEMBL1956162 | — | IC50 | > | 100000.0 | nM | - |