Assay Detail
Functional
CHEMBL895768
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
G-protein coupled bile acid receptor 1 (CHEMBL5409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 5.68 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL244785 | — | — | 1 | 7.02 |
| CHEMBL244784 | — | — | 1 | 6.85 |
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 6.12 |
| CHEMBL244783 | — | — | 1 | 5.45 |
| CHEMBL266356 | — | — | 1 | 5.36 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 5.17 |
| CHEMBL205596 | CHOLIC ACID | 4.0 | 1 | 4.87 |
| CHEMBL245001 | — | — | 1 | 4.59 |
| CHEMBL388679 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL244785 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL244784 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 755.0 | nM | 6.12 |
| CHEMBL244783 | — | EC50 | = | 3580.0 | nM | 5.45 |
| CHEMBL266356 | — | EC50 | = | 4390.0 | nM | 5.36 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 6710.0 | nM | 5.17 |
| CHEMBL205596 | CHOLIC ACID | EC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL245001 | — | EC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL388679 | — | EC50 | > | 51900.0 | nM | - |