Assay Detail
Binding
CHEMBL3635401
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of porcupine in human HEK293 cells assessed as reduction in Wnt secretion by measuring suppression of beta-catenin reporter activity after 24 hrs by STF reporter assay
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein-serine O-palmitoleoyltransferase porcupine (CHEMBL1255163) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The use of porcupine inhibitors to target Wnt-driven cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.70 | 9.30 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3633801 | — | — | 2 | 9.30 |
| CHEMBL3633802 | ETC-159 | 1.0 | 2 | 8.54 |
| CHEMBL3633803 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3633801 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3633802 | ETC-159 | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3633803 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3633801 | — | Inhibition | - | % | - | |
| CHEMBL3633802 | ETC-159 | Inhibition | - | % | - |