Assay Detail
Functional
CHEMBL2090178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 2 | 8.05 | 8.20 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76370 | TEGASEROD | 4.0 | 1 | 8.20 |
| CHEMBL2087337 | VELUSETRAG | 2.0 | 2 | 7.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76370 | TEGASEROD | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL2087337 | VELUSETRAG | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL2087337 | VELUSETRAG | Activity | - | — | - |