Assay Detail
Binding
CHEMBL2339910
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at dog TGR5 expressed in uninduced Flp-In-CHO-TO cells assessed as increase in intracellular cAMP measured after 48 hrs by HTRF competitive immunoassay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.18 | 6.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2331649 | — | — | 1 | 6.95 |
| CHEMBL2331648 | — | — | 1 | 6.87 |
| CHEMBL2331646 | — | — | 1 | 6.67 |
| CHEMBL2331653 | — | — | 1 | 6.66 |
| CHEMBL2331650 | — | — | 1 | 6.63 |
| CHEMBL2331654 | — | — | 1 | 6.52 |
| CHEMBL2331651 | — | — | 1 | 6.42 |
| CHEMBL2331655 | — | — | 1 | 6.39 |
| CHEMBL576138 | — | — | 1 | 6.35 |
| CHEMBL604131 | — | — | 1 | 6.23 |
| CHEMBL2331645 | — | — | 1 | 6.08 |
| CHEMBL1258423 | — | — | 1 | 5.69 |
| CHEMBL2331652 | — | — | 1 | 5.50 |
| CHEMBL2331647 | — | — | 1 | 5.37 |
| CHEMBL567640 | — | — | 1 | 5.30 |
| CHEMBL2331644 | — | — | 1 | 5.24 |
| CHEMBL2331643 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2331649 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL2331648 | — | EC50 | = | 135.0 | nM | 6.87 |
| CHEMBL2331646 | — | EC50 | = | 213.0 | nM | 6.67 |
| CHEMBL2331653 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2331650 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL2331654 | — | EC50 | = | 303.0 | nM | 6.52 |
| CHEMBL2331651 | — | EC50 | = | 382.0 | nM | 6.42 |
| CHEMBL2331655 | — | EC50 | = | 407.0 | nM | 6.39 |
| CHEMBL576138 | — | EC50 | = | 445.0 | nM | 6.35 |
| CHEMBL604131 | — | EC50 | = | 584.0 | nM | 6.23 |
| CHEMBL2331645 | — | EC50 | = | 828.0 | nM | 6.08 |
| CHEMBL1258423 | — | EC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL2331652 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2331647 | — | EC50 | = | 4280.0 | nM | 5.37 |
| CHEMBL567640 | — | EC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL2331644 | — | EC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2331643 | — | EC50 | - | — | - |