Assay Detail
Binding
CHEMBL3762973
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Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.37 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3759860 | — | — | 1 | 7.34 |
| CHEMBL3759944 | — | — | 1 | 7.00 |
| CHEMBL74656 | REL-CISAPRIDE | — | 1 | 6.99 |
| CHEMBL3758199 | — | — | 1 | 6.60 |
| CHEMBL3759259 | — | — | 1 | 6.42 |
| CHEMBL3758932 | — | — | 1 | 6.17 |
| CHEMBL3759601 | — | — | 1 | 6.15 |
| CHEMBL3758945 | — | — | 1 | 5.98 |
| CHEMBL3759348 | — | — | 1 | 5.81 |
| CHEMBL3759928 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3759860 | — | EC50 | = | 45.71 | nM | 7.34 |
| CHEMBL3759944 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL74656 | REL-CISAPRIDE | EC50 | = | 102.33 | nM | 6.99 |
| CHEMBL3758199 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3759259 | — | EC50 | = | 380.19 | nM | 6.42 |
| CHEMBL3758932 | — | EC50 | = | 676.08 | nM | 6.17 |
| CHEMBL3759601 | — | EC50 | = | 707.95 | nM | 6.15 |
| CHEMBL3758945 | — | EC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL3759348 | — | EC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL3759928 | — | EC50 | = | 6025.6 | nM | 5.22 |