Assay Detail
Functional
CHEMBL4681027
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at TGR5 in human NCI-H716 cells assessed as stimulation of intracellular cAMP accumulation incubated for 60 mins by HTR-FRET assay
10
Total Activities
10
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
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 4.87 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL567640 | — | — | 1 | 6.05 |
| CHEMBL567835 | — | — | 1 | 5.30 |
| CHEMBL566315 | OBETICHOLIC ACID | 4.0 | 1 | 4.82 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 4.48 |
| CHEMBL4758363 | — | — | 1 | 4.38 |
| CHEMBL4740844 | — | — | 1 | 4.21 |
| CHEMBL1551 | URSODIOL | 4.0 | 1 | - |
| CHEMBL4758064 | — | — | 1 | - |
| CHEMBL4740500 | — | — | 1 | - |
| CHEMBL4790262 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL567640 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL567835 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL566315 | OBETICHOLIC ACID | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4758363 | — | EC50 | = | 41500.0 | nM | 4.38 |
| CHEMBL4740844 | — | EC50 | = | 62000.0 | nM | 4.21 |
| CHEMBL1551 | URSODIOL | EC50 | > | 100000.0 | nM | - |
| CHEMBL4758064 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4740500 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL4790262 | — | EC50 | > | 100000.0 | nM | - |