Assay Detail
Functional
CHEMBL2343387
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human TGR5 receptor in CHO cells assessed as elevation of cAMP level by uninduced cAMP detection method in absence of doxycycline
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 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 | 35 | 6.38 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2336232 | — | — | 1 | 7.48 |
| CHEMBL2336233 | — | — | 1 | 7.31 |
| CHEMBL2331604 | — | — | 1 | 7.22 |
| CHEMBL2336234 | — | — | 1 | 7.16 |
| CHEMBL2331648 | — | — | 1 | 7.12 |
| CHEMBL2336231 | — | — | 1 | 6.98 |
| CHEMBL2336222 | — | — | 1 | 6.80 |
| CHEMBL2336238 | — | — | 1 | 6.67 |
| CHEMBL2336211 | — | — | 1 | 6.64 |
| CHEMBL2336216 | — | — | 1 | 6.45 |
| CHEMBL576138 | — | — | 1 | 6.34 |
| CHEMBL2336213 | — | — | 1 | 6.26 |
| CHEMBL2336235 | — | — | 1 | 6.04 |
| CHEMBL2336236 | — | — | 1 | 5.99 |
| CHEMBL2336237 | — | — | 1 | 5.97 |
| CHEMBL2336210 | — | — | 1 | 5.84 |
| CHEMBL2336212 | — | — | 1 | 5.50 |
| CHEMBL2336215 | — | — | 1 | 5.42 |
| CHEMBL2336239 | — | — | 1 | 5.24 |
| CHEMBL2336227 | — | — | 1 | 5.07 |
| CHEMBL2336214 | — | — | 1 | - |
| CHEMBL2336209 | — | — | 1 | - |
| CHEMBL2336208 | — | — | 1 | - |
| CHEMBL2336217 | — | — | 1 | - |
| CHEMBL2336218 | — | — | 1 | - |
| CHEMBL2336219 | — | — | 1 | - |
| CHEMBL2336220 | — | — | 1 | - |
| CHEMBL2336221 | — | — | 1 | - |
| CHEMBL2336223 | — | — | 1 | - |
| CHEMBL2336224 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2336232 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2336233 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL2331604 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2336234 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2331648 | — | EC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2336231 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL2336222 | — | EC50 | = | 159.0 | nM | 6.80 |
| CHEMBL2336238 | — | EC50 | = | 212.0 | nM | 6.67 |
| CHEMBL2336211 | — | EC50 | = | 231.0 | nM | 6.64 |
| CHEMBL2336216 | — | EC50 | = | 352.0 | nM | 6.45 |
| CHEMBL576138 | — | EC50 | = | 457.0 | nM | 6.34 |
| CHEMBL2336213 | — | EC50 | = | 549.0 | nM | 6.26 |
| CHEMBL2336235 | — | EC50 | = | 922.0 | nM | 6.04 |
| CHEMBL2336236 | — | EC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL2336237 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL2336210 | — | EC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL2336212 | — | EC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL2336215 | — | EC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL2336239 | — | EC50 | = | 5780.0 | nM | 5.24 |
| CHEMBL2336227 | — | EC50 | = | 8460.0 | nM | 5.07 |
| CHEMBL2336230 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336229 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336228 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336226 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336225 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336224 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336223 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336221 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336220 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336219 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336218 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336217 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336208 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336209 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336214 | — | EC50 | > | 10000.0 | nM | - |