Assay Detail
Functional
CHEMBL3406768
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay
12
Total Activities
12
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
Stereoselective synthesis, biological evaluation, and modeling of novel bile acid-derived G-protein coupled bile acid receptor 1 (GP-BAR1, TGR5) agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.79 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3401351 | — | — | 1 | 6.66 |
| CHEMBL3401354 | — | — | 1 | 6.24 |
| CHEMBL1478 | LITHOCHOLIC ACID | — | 1 | 6.17 |
| CHEMBL3401356 | — | — | 1 | 6.14 |
| CHEMBL3401353 | — | — | 1 | 6.12 |
| CHEMBL3401352 | — | — | 1 | 5.98 |
| CHEMBL3401355 | — | — | 1 | 5.83 |
| CHEMBL1551 | URSODIOL | 4.0 | 1 | 5.62 |
| CHEMBL583611 | — | — | 1 | 5.55 |
| CHEMBL240597 | CHENODIOL | 4.0 | 1 | 5.21 |
| CHEMBL3401357 | — | — | 1 | 5.04 |
| CHEMBL1254261 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3401351 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3401354 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL1478 | LITHOCHOLIC ACID | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL3401356 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3401353 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3401352 | — | EC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3401355 | — | EC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL1551 | URSODIOL | EC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL583611 | — | EC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL240597 | CHENODIOL | EC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3401357 | — | EC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL1254261 | — | EC50 | = | 10930.0 | nM | 4.96 |