Assay Detail
Binding
CHEMBL3796544
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Agonist activity at human TGR5 expressed in CHO-K1 cells after 5 hrs by luciferase reporter gene assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 a Potent and Orally Efficacious TGR5 Receptor Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 8.21 | 10.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3793436 | — | — | 1 | 10.24 |
| CHEMBL3794442 | — | — | 1 | 8.83 |
| CHEMBL3793012 | — | — | 1 | 8.64 |
| CHEMBL3793388 | — | — | 1 | 8.24 |
| CHEMBL3792957 | — | — | 1 | 8.11 |
| CHEMBL3793168 | — | — | 1 | 8.07 |
| CHEMBL3794111 | — | — | 1 | 7.78 |
| CHEMBL3794175 | — | — | 1 | 7.77 |
| CHEMBL3793859 | — | — | 1 | 7.71 |
| CHEMBL3794424 | — | — | 1 | 7.50 |
| CHEMBL3794293 | — | — | 1 | 7.42 |
| CHEMBL3794367 | — | — | 1 | - |
| CHEMBL3792938 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3793436 | — | EC50 | = | 0.057 | nM | 10.24 |
| CHEMBL3794442 | — | EC50 | = | 1.48 | nM | 8.83 |
| CHEMBL3793012 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3793388 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3792957 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL3793168 | — | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3794111 | — | EC50 | = | 16.8 | nM | 7.78 |
| CHEMBL3794175 | — | EC50 | = | 17.08 | nM | 7.77 |
| CHEMBL3793859 | — | EC50 | = | 19.6 | nM | 7.71 |
| CHEMBL3794424 | — | EC50 | = | 31.5 | nM | 7.50 |
| CHEMBL3794293 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3794367 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL3792938 | — | EC50 | > | 100.0 | nM | - |