Assay Detail
Functional
CHEMBL2090176
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulation
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous 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 | 1 | 9.20 | 9.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087337 | VELUSETRAG | 2.0 | 1 | 9.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087337 | VELUSETRAG | EC50 | = | 0.631 | nM | 9.20 |