Assay Detail
Functional
CHEMBL2187733
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at mouse TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
28
Total Activities
28
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, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 7.89 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181229 | — | — | 1 | 9.01 |
| CHEMBL2181227 | — | — | 1 | 8.70 |
| CHEMBL2181228 | — | — | 1 | 8.68 |
| CHEMBL2181230 | — | — | 1 | 8.64 |
| CHEMBL2181226 | — | — | 1 | 8.21 |
| CHEMBL2181225 | — | — | 1 | 7.82 |
| CHEMBL2181239 | — | — | 1 | 7.75 |
| CHEMBL2181235 | — | — | 1 | 7.62 |
| CHEMBL2181223 | — | — | 1 | 7.58 |
| CHEMBL2181221 | — | — | 1 | 7.52 |
| CHEMBL2181256 | — | — | 1 | 7.52 |
| CHEMBL2181222 | — | — | 1 | 7.51 |
| CHEMBL2181240 | — | — | 1 | 7.51 |
| CHEMBL2181238 | — | — | 1 | 7.18 |
| CHEMBL2181236 | — | — | 1 | 7.12 |
| CHEMBL2181237 | — | — | 1 | - |
| CHEMBL2181234 | — | — | 1 | - |
| CHEMBL2181233 | — | — | 1 | - |
| CHEMBL2181232 | — | — | 1 | - |
| CHEMBL2181231 | — | — | 1 | - |
| CHEMBL2181257 | — | — | 1 | - |
| CHEMBL2181255 | — | — | 1 | - |
| CHEMBL2181254 | — | — | 1 | - |
| CHEMBL2181253 | — | — | 1 | - |
| CHEMBL2181252 | — | — | 1 | - |
| CHEMBL2181251 | — | — | 1 | - |
| CHEMBL2181224 | — | — | 1 | - |
| CHEMBL2181220 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181229 | — | EC50 | = | 0.98 | nM | 9.01 |
| CHEMBL2181227 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2181228 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2181230 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2181226 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2181225 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2181239 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2181235 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2181223 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2181221 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2181256 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2181222 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2181240 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2181238 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2181236 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2181237 | — | EC50 | - | — | - | |
| CHEMBL2181234 | — | EC50 | - | — | - | |
| CHEMBL2181233 | — | EC50 | - | — | - | |
| CHEMBL2181232 | — | EC50 | - | — | - | |
| CHEMBL2181231 | — | EC50 | - | — | - | |
| CHEMBL2181257 | — | EC50 | - | — | - | |
| CHEMBL2181255 | — | EC50 | - | — | - | |
| CHEMBL2181254 | — | EC50 | - | — | - | |
| CHEMBL2181253 | — | EC50 | - | — | - | |
| CHEMBL2181252 | — | EC50 | - | — | - | |
| CHEMBL2181251 | — | EC50 | - | — | - | |
| CHEMBL2181224 | — | EC50 | - | — | - | |
| CHEMBL2181220 | — | EC50 | - | — | - |