Assay Detail
Functional
CHEMBL5339491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse TGR5 expressed in human HEK293 cells co-expressing CRE-driven luciferase reporter gene assessed as luciferase activity incubated for 5.5 hrs by Steady-Glo based luciferase 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 and exploration of gut-restricted bifunctional molecule with TGR5 agonistic and DPP4 inhibitory effects for treating ulcerative colitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 8.34 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5437749 | — | — | 1 | 8.68 |
| CHEMBL5394421 | — | — | 1 | 8.68 |
| CHEMBL5427760 | — | — | 1 | 8.64 |
| CHEMBL5414305 | — | — | 1 | 8.64 |
| CHEMBL5415272 | — | — | 1 | 8.64 |
| CHEMBL5422904 | — | — | 1 | 8.64 |
| CHEMBL5395284 | — | — | 1 | 8.62 |
| CHEMBL5439914 | — | — | 1 | 8.57 |
| CHEMBL5398966 | — | — | 1 | 8.47 |
| CHEMBL5413666 | — | — | 1 | 8.43 |
| CHEMBL5432337 | — | — | 1 | 8.37 |
| CHEMBL5483060 | — | — | 1 | 8.22 |
| CHEMBL5399395 | — | — | 1 | 7.98 |
| CHEMBL567640 | — | — | 1 | 6.23 |
| CHEMBL390853 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5437749 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5394421 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5427760 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5414305 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5415272 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5422904 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5395284 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5439914 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5398966 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5413666 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5432337 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5483060 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5399395 | — | EC50 | = | 10.5 | nM | 7.98 |
| CHEMBL567640 | — | EC50 | = | 586.0 | nM | 6.23 |
| CHEMBL390853 | — | EC50 | > | 1000.0 | nM | - |