Assay Detail
Binding
CHEMBL4322256
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length Myc/His-tagged Parp-1 expressed in baculovirus infected Sf21 insect cells assessed as reduction in auto-PARsylation using activated DNA as substrate incubated for 150 mins in presence of NAD and bio-NAD as co-substrate by TR-FRET assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.05 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4458129 | — | — | 1 | 7.22 |
| CHEMBL4588170 | — | — | 1 | 7.10 |
| CHEMBL4584689 | — | — | 1 | 6.92 |
| CHEMBL336718 | — | — | 1 | 6.54 |
| CHEMBL4447252 | — | — | 1 | 6.46 |
| CHEMBL4455904 | — | — | 1 | 6.43 |
| CHEMBL4567515 | — | — | 1 | 6.41 |
| CHEMBL4514589 | — | — | 1 | 6.39 |
| CHEMBL4545573 | — | — | 1 | 6.29 |
| CHEMBL4450725 | — | — | 1 | 6.21 |
| CHEMBL4524437 | — | — | 1 | 6.20 |
| CHEMBL4437173 | — | — | 1 | 6.11 |
| CHEMBL4551200 | — | — | 1 | 6.10 |
| CHEMBL4548930 | — | — | 1 | 6.08 |
| CHEMBL4475367 | — | — | 1 | 6.04 |
| CHEMBL4558610 | — | — | 1 | 5.96 |
| CHEMBL4454894 | — | — | 1 | 5.89 |
| CHEMBL4566814 | — | — | 1 | 5.85 |
| CHEMBL4077094 | — | — | 1 | 5.77 |
| CHEMBL4536612 | — | — | 1 | 5.64 |
| CHEMBL4585900 | — | — | 1 | 5.60 |
| CHEMBL4444673 | — | — | 1 | 5.43 |
| CHEMBL4586580 | — | — | 1 | 5.41 |
| CHEMBL4457607 | — | — | 1 | 5.37 |
| CHEMBL4440292 | — | — | 1 | 5.24 |
| CHEMBL127066 | — | — | 1 | 4.68 |
| CHEMBL4290134 | — | — | 1 | - |
| CHEMBL4457148 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4458129 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4588170 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4584689 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL336718 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4447252 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL4455904 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4567515 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4514589 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4545573 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL4450725 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4524437 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4437173 | — | IC50 | = | 782.0 | nM | 6.11 |
| CHEMBL4551200 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4548930 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4475367 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4558610 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4454894 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4566814 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4077094 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4536612 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4585900 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4444673 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4586580 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4457607 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4440292 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL127066 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4290134 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4457148 | — | IC50 | - | — | - |