Assay Detail
Functional
CHEMBL1768539
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H716 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
G-protein coupled bile acid receptor 1 (CHEMBL5409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3α,7α-dihydroxy-6α-ethyl-24-nor-5β-cholan-23-amine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 4.49 | 4.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 4.70 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.52 |
| CHEMBL1765565 | — | — | 1 | 4.26 |
| CHEMBL3138092 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL1765565 | — | EC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL3138092 | — | EC50 | > | 100000.0 | nM | - |