Assay Detail
Functional
CHEMBL3737332
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at wild type human TGR5 expressed in HEK293 cells assessed as rise in intracellular cAMP level incubated for 16 hrs by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 5.37 | 6.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL412272 | TAURODEOXYCHOLIC ACID | 2.0 | 1 | 6.17 |
| CHEMBL185878 | TAUROCHENODEOXYCHOLATE | — | 1 | 5.64 |
| CHEMBL272427 | TAURURSODIOL | 4.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL412272 | TAURODEOXYCHOLIC ACID | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL185878 | TAUROCHENODEOXYCHOLATE | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL272427 | TAURURSODIOL | EC50 | = | 50500.0 | nM | 4.30 |