Assay Detail
Binding
CHEMBL4334744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NOTUM in human HEK293S cells harbouring TCF/LEF luciferase reporter gene assessed as activation wnt signalling pathway incubated for 10 mins followed by wnt-3A addition further incubated for 1 hr by steady-glo luciferase assay
3
Total Activities
3
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 |
Target
Palmitoleoyl-protein carboxylesterase NOTUM (CHEMBL3714531) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 6.44 | 6.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774760 | — | — | 1 | 6.86 |
| CHEMBL4446980 | — | — | 1 | 6.43 |
| CHEMBL4539054 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774760 | — | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4446980 | — | EC50 | = | 368.0 | nM | 6.43 |
| CHEMBL4539054 | — | EC50 | = | 934.0 | nM | 6.03 |