Assay Detail
Functional
CHEMBL4772461
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed as CRE-driven luciferase reporter incubated for 5.5 hrs and measured by Steady Glow reagent based luminescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
G-protein coupled bile acid receptor 1 (CHEMBL1255150) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.45 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4779084 | — | — | 1 | 7.64 |
| CHEMBL4791709 | — | — | 1 | 7.36 |
| CHEMBL4776876 | — | — | 1 | 6.94 |
| CHEMBL4794753 | — | — | 1 | 6.86 |
| CHEMBL4783037 | — | — | 1 | 6.84 |
| CHEMBL4798091 | — | — | 1 | 6.68 |
| CHEMBL4793377 | — | — | 1 | 6.68 |
| CHEMBL3290724 | — | — | 1 | 6.67 |
| CHEMBL567640 | — | — | 1 | 6.60 |
| CHEMBL4784355 | — | — | 1 | 6.41 |
| CHEMBL4782069 | — | — | 1 | 6.25 |
| CHEMBL4794523 | — | — | 1 | 5.86 |
| CHEMBL4778884 | — | — | 1 | 5.46 |
| CHEMBL4792593 | — | — | 1 | 5.22 |
| CHEMBL4783601 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4779084 | — | EC50 | = | 23.1 | nM | 7.64 |
| CHEMBL4791709 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4776876 | — | EC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4794753 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4783037 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4798091 | — | EC50 | = | 209.0 | nM | 6.68 |
| CHEMBL4793377 | — | EC50 | = | 211.0 | nM | 6.68 |
| CHEMBL3290724 | — | EC50 | = | 215.0 | nM | 6.67 |
| CHEMBL567640 | — | EC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4784355 | — | EC50 | = | 388.0 | nM | 6.41 |
| CHEMBL4782069 | — | EC50 | = | 561.0 | nM | 6.25 |
| CHEMBL4794523 | — | EC50 | = | 1372.0 | nM | 5.86 |
| CHEMBL4778884 | — | EC50 | = | 3468.0 | nM | 5.46 |
| CHEMBL4792593 | — | EC50 | = | 6052.0 | nM | 5.22 |
| CHEMBL4783601 | — | EC50 | = | 5953.0 | nM | 5.22 |