Assay Detail
Functional
CHEMBL2343386
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Ex vivo activation of TGR5 in human PBMC assessed as elevation of cAMP level by cAMP assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 6.53 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331648 | — | — | 1 | 6.96 |
| CHEMBL2336222 | — | — | 1 | 6.42 |
| CHEMBL576138 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331648 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2336222 | — | EC50 | = | 379.0 | nM | 6.42 |
| CHEMBL576138 | — | EC50 | = | 600.0 | nM | 6.22 |