Assay Detail
Functional
CHEMBL751165
Review assay metadata, readout intent, target linkage, and publication context from the same page.
M2 agonist activity estimated by depression of isolated guinea pig left atrium
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 6.27 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.96 |
| CHEMBL133905 | — | — | 1 | 6.57 |
| CHEMBL273308 | — | — | 1 | 6.40 |
| CHEMBL131777 | — | — | 3 | 6.17 |
| CHEMBL337676 | — | — | 1 | 5.72 |
| CHEMBL131095 | — | — | 1 | - |
| CHEMBL131428 | ALVAMELINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14 | CARBACHOL | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL133905 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL273308 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL131777 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL131777 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL131777 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL337676 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL131095 | — | EC50 | > | 51000.0 | nM | - |
| CHEMBL131428 | ALVAMELINE | EC50 | > | 51000.0 | nM | - |