Assay Detail
Functional
CHEMBL931112
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human Dvl3 assessed as inhibition of interaction between Dvl3 PDZ domain and Fz7 PDZ domain by alphaScreen assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Segment polarity protein dishevelled homolog DVL-3 (CHEMBL6028) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Indole-2-amide based biochemical antagonist of Dishevelled PDZ domain interaction down-regulates Dishevelled-driven Tcf transcriptional activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.31 | 4.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL255779 | — | — | 1 | 4.64 |
| CHEMBL272948 | — | — | 1 | 4.24 |
| CHEMBL402939 | — | — | 1 | 4.04 |
| CHEMBL410400 | — | — | 1 | - |
| CHEMBL252273 | — | — | 1 | - |
| CHEMBL401537 | — | — | 1 | - |
| CHEMBL256605 | — | — | 1 | - |
| CHEMBL255988 | — | — | 1 | - |
| CHEMBL404331 | — | — | 1 | - |
| CHEMBL256431 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL255779 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL272948 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL402939 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL410400 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL252273 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL401537 | — | IC50 | = | 291000.0 | nM | - |
| CHEMBL256605 | — | IC50 | = | 309000.0 | nM | - |
| CHEMBL255988 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL404331 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL256431 | — | IC50 | = | 160000.0 | nM | - |