Assay Detail
Binding
CHEMBL4040031
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of porcupine (unknown origin) expressed in HEK293 cells after day 1 post treatment by Super-top flash reporter gene assay
19
Total Activities
19
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
Protein-serine O-palmitoleoyltransferase porcupine (CHEMBL1255163) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.97 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4080208 | — | — | 1 | 9.40 |
| CHEMBL4096728 | — | — | 1 | 9.00 |
| CHEMBL4080021 | — | — | 1 | 9.00 |
| CHEMBL4069295 | — | — | 1 | 8.22 |
| CHEMBL4104447 | — | — | 1 | 8.10 |
| CHEMBL4066589 | — | — | 1 | 8.05 |
| CHEMBL4096529 | — | — | 1 | 7.96 |
| CHEMBL4095609 | — | — | 1 | 7.96 |
| CHEMBL4087906 | — | — | 1 | 7.92 |
| CHEMBL4103356 | — | — | 1 | 7.92 |
| CHEMBL4066796 | — | — | 1 | 7.92 |
| CHEMBL4061069 | — | — | 1 | 7.82 |
| CHEMBL4094309 | — | — | 1 | 7.82 |
| CHEMBL4066798 | — | — | 1 | 7.62 |
| CHEMBL4104257 | — | — | 1 | 7.54 |
| CHEMBL4075204 | — | — | 1 | 7.54 |
| CHEMBL4102043 | — | — | 1 | 7.38 |
| CHEMBL4086549 | — | — | 1 | 7.17 |
| CHEMBL4078705 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4080208 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4096728 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4080021 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4069295 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4104447 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4066589 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4096529 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4095609 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4087906 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4103356 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4066796 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4061069 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4094309 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4066798 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4104257 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4075204 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4102043 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4086549 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4078705 | — | IC50 | = | 72.0 | nM | 7.14 |