Assay Detail
Functional
CHEMBL1040516
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in melanophores assessed as melanosome dispersion by melanophore assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
G-protein coupled bile acid receptor 1 (CHEMBL5409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 7.30 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575966 | — | — | 1 | 7.50 |
| CHEMBL576138 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575966 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL576138 | — | EC50 | = | 79.43 | nM | 7.10 |