Assay Detail
Functional
CHEMBL745482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
M2/M3 agonist activity estimated by contraction of isolated guinea pig ileum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptors; M2 & M3 (CHEMBL2095187) ↗| Type | SELECTIVITY GROUP |
| Organism | Homo sapiens |
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 | 8 | 6.23 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129886 | — | — | 1 | 6.89 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 6.85 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.72 |
| CHEMBL273308 | — | — | 1 | 6.37 |
| CHEMBL133905 | — | — | 1 | 6.11 |
| CHEMBL131095 | — | — | 1 | 6.03 |
| CHEMBL131428 | ALVAMELINE | 2.0 | 1 | 5.50 |
| CHEMBL131777 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129886 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL7303 | ARECOLINE | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL14 | CARBACHOL | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL273308 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL133905 | — | EC50 | = | 770.0 | nM | 6.11 |
| CHEMBL131095 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL131428 | ALVAMELINE | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL131777 | — | EC50 | = | 4300.0 | nM | 5.37 |