Assay Detail
Binding
CHEMBL4345397
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TNKS/TNKS2 (unknown origin) expressed in human DLD1 cells assessed as reduction in Wnt-signaling measured after 24 hrs by TCF-luciferase reporter gene assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 8.00 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4572668 | — | — | 1 | 8.89 |
| CHEMBL4532667 | — | — | 1 | 8.80 |
| CHEMBL4446044 | — | — | 1 | 8.70 |
| CHEMBL4463639 | — | — | 1 | 8.64 |
| CHEMBL4470270 | — | — | 1 | 8.62 |
| CHEMBL4553990 | — | — | 1 | 8.57 |
| CHEMBL4544771 | — | — | 1 | 8.55 |
| CHEMBL4466701 | — | — | 1 | 8.52 |
| CHEMBL4449082 | — | — | 1 | 8.51 |
| CHEMBL4445363 | — | — | 1 | 8.41 |
| CHEMBL4539435 | — | — | 1 | 8.37 |
| CHEMBL4470218 | — | — | 1 | 8.35 |
| CHEMBL4585076 | — | — | 1 | 8.32 |
| CHEMBL4471663 | — | — | 1 | 8.30 |
| CHEMBL4442053 | — | — | 1 | 8.24 |
| CHEMBL4457037 | — | — | 1 | 8.21 |
| CHEMBL4460022 | — | — | 1 | 8.20 |
| CHEMBL4441668 | — | — | 1 | 8.20 |
| CHEMBL4467730 | — | — | 1 | 8.19 |
| CHEMBL4525942 | — | — | 1 | 8.18 |
| CHEMBL4441063 | — | — | 1 | 8.15 |
| CHEMBL4518341 | — | — | 1 | 8.15 |
| CHEMBL4581567 | — | — | 1 | 8.14 |
| CHEMBL4582280 | — | — | 1 | 8.08 |
| CHEMBL4566625 | — | — | 1 | 7.86 |
| CHEMBL4464007 | — | — | 1 | 7.84 |
| CHEMBL4439372 | — | — | 1 | 7.84 |
| CHEMBL4442841 | — | — | 1 | 7.68 |
| CHEMBL2325503 | — | — | 1 | 7.57 |
| CHEMBL4574717 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4572668 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4532667 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4446044 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4463639 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4470270 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4553990 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4544771 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4466701 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4449082 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4445363 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4539435 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4470218 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4585076 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4471663 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4442053 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4457037 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4460022 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4441668 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4467730 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4525942 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4441063 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4518341 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4581567 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4582280 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4566625 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4464007 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL4439372 | — | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL4442841 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL2325503 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL4574717 | — | IC50 | = | 29.1 | nM | 7.54 |
| CHEMBL4439240 | — | IC50 | = | 32.9 | nM | 7.48 |
| CHEMBL4554146 | — | IC50 | = | 71.2 | nM | 7.15 |
| CHEMBL4448872 | — | IC50 | = | 77.6 | nM | 7.11 |
| CHEMBL4555632 | — | IC50 | = | 140.6 | nM | 6.85 |
| CHEMBL4466165 | — | IC50 | = | 1185.0 | nM | 5.93 |
| CHEMBL4466181 | — | IC50 | = | 1877.0 | nM | 5.73 |