Assay Detail
Functional
CHEMBL859622
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Antagonism at 5HT4 receptor in rat tunica muscularis mucosa
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Muscularis mucosa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pyrrolizidine esters and amides as 5-HT4 receptor agonists and antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 7.63 | 8.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201946 | — | — | 1 | 8.93 |
| CHEMBL383577 | — | — | 1 | 8.56 |
| CHEMBL202122 | — | — | 1 | 8.50 |
| CHEMBL201878 | — | — | 1 | 8.48 |
| CHEMBL202434 | — | — | 1 | 8.13 |
| CHEMBL425222 | — | — | 1 | 7.15 |
| CHEMBL372776 | — | — | 1 | 7.09 |
| CHEMBL371883 | — | — | 1 | 7.00 |
| CHEMBL383554 | — | — | 1 | 6.75 |
| CHEMBL202481 | — | — | 1 | 6.75 |
| CHEMBL202149 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201946 | — | Kd | = | 1.175 | nM | 8.93 |
| CHEMBL383577 | — | Kd | = | 2.754 | nM | 8.56 |
| CHEMBL202122 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL201878 | — | Kd | = | 3.311 | nM | 8.48 |
| CHEMBL202434 | — | Kd | = | 7.413 | nM | 8.13 |
| CHEMBL425222 | — | Kd | = | 70.79 | nM | 7.15 |
| CHEMBL372776 | — | Kd | = | 81.28 | nM | 7.09 |
| CHEMBL371883 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL383554 | — | Kd | = | 177.83 | nM | 6.75 |
| CHEMBL202481 | — | Kd | = | 177.83 | nM | 6.75 |
| CHEMBL202149 | — | Kd | = | 275.42 | nM | 6.56 |