Assay Detail
Functional
CHEMBL1040510
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at TGR5 expressed in human U2-OS cells assessed as increase in MRE/CRE-driven gene expression by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | U2OS |
| Confidence | 8 — Homologous 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 | 3 | 6.13 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575966 | — | — | 1 | 6.80 |
| CHEMBL576138 | — | — | 1 | 6.30 |
| CHEMBL583110 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575966 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL576138 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL583110 | — | EC50 | = | 5011.87 | nM | 5.30 |