Assay Detail
Functional
CHEMBL2343388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at doxycycline-promoter regulated overexpressed human TGR5 receptor in CHO cells assessed as elevation of cAMP level by induced-cAMP assay
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 | 7.19 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2336232 | — | — | 1 | 9.52 |
| CHEMBL2336231 | — | — | 1 | 8.92 |
| CHEMBL2336233 | — | — | 1 | 8.92 |
| CHEMBL2331604 | — | — | 1 | 8.74 |
| CHEMBL2331648 | — | — | 1 | 8.64 |
| CHEMBL2336234 | — | — | 1 | 8.62 |
| CHEMBL2336238 | — | — | 1 | 8.26 |
| CHEMBL2336222 | — | — | 1 | 8.17 |
| CHEMBL2336236 | — | — | 1 | 8.10 |
| CHEMBL2336211 | — | — | 1 | 8.10 |
| CHEMBL2336213 | — | — | 1 | 7.92 |
| CHEMBL2336235 | — | — | 1 | 7.85 |
| CHEMBL2336210 | — | — | 1 | 7.82 |
| CHEMBL2336216 | — | — | 1 | 7.82 |
| CHEMBL2336237 | — | — | 1 | 7.75 |
| CHEMBL576138 | — | — | 1 | 7.64 |
| CHEMBL2336212 | — | — | 1 | 7.19 |
| CHEMBL2336215 | — | — | 1 | 6.95 |
| CHEMBL2336239 | — | — | 1 | 6.92 |
| CHEMBL2336208 | — | — | 1 | 6.47 |
| CHEMBL2336209 | — | — | 1 | 6.46 |
| CHEMBL2336227 | — | — | 1 | 6.41 |
| CHEMBL2336220 | — | — | 1 | 6.04 |
| CHEMBL2336226 | — | — | 1 | 5.85 |
| CHEMBL2336214 | — | — | 1 | 5.83 |
| CHEMBL2336217 | — | — | 1 | 5.54 |
| CHEMBL2336225 | — | — | 1 | 5.50 |
| CHEMBL2336223 | — | — | 1 | 5.33 |
| CHEMBL2336218 | — | — | 1 | 5.31 |
| CHEMBL2336228 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2336232 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL2336231 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2336233 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2331604 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL2331648 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2336234 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2336238 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL2336222 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2336236 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL2336211 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL2336213 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2336235 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2336210 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2336216 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2336237 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL576138 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2336212 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2336215 | — | EC50 | = | 113.0 | nM | 6.95 |
| CHEMBL2336239 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2336208 | — | EC50 | = | 337.0 | nM | 6.47 |
| CHEMBL2336209 | — | EC50 | = | 349.0 | nM | 6.46 |
| CHEMBL2336227 | — | EC50 | = | 393.0 | nM | 6.41 |
| CHEMBL2336220 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2336226 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2336214 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL2336217 | — | EC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL2336225 | — | EC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL2336223 | — | EC50 | = | 4680.0 | nM | 5.33 |
| CHEMBL2336218 | — | EC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL2336228 | — | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2336224 | — | EC50 | = | 9530.0 | nM | 5.02 |
| CHEMBL2336221 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336219 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336229 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2336230 | — | EC50 | > | 10000.0 | nM | - |