Assay Detail
Functional
CHEMBL696086
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.73 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68131 | — | — | 1 | 10.00 |
| CHEMBL334818 | — | — | 1 | 9.00 |
| CHEMBL130040 | — | — | 1 | 8.20 |
| CHEMBL130809 | — | — | 1 | 8.00 |
| CHEMBL130118 | — | — | 1 | 7.30 |
| CHEMBL132826 | — | — | 1 | 7.20 |
| CHEMBL287045 | — | — | 1 | 6.60 |
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68131 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL334818 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL130040 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL130809 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL130118 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL132826 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL287045 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL56564 | TROPISETRON | IC50 | = | 3162.28 | nM | 5.50 |