Assay Detail
Functional
CHEMBL861942
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potency at muscarinic receptor M3 in guinea pig ileum
16
Total Activities
7
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL5498) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
Publication
Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Intrinsic activity | 7 | - | - |
| pKb | 5 | - | - |
| Kd | 2 | 5.40 | 6.45 |
| EC50 | 2 | 6.25 | 6.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL199636 | — | — | 3 | 6.45 |
| CHEMBL201016 | — | — | 2 | 4.35 |
| CHEMBL197604 | — | — | 2 | - |
| CHEMBL382846 | — | — | 2 | - |
| CHEMBL381913 | — | — | 2 | - |
| CHEMBL380572 | — | — | 3 | - |
| CHEMBL382659 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL199636 | — | Kd | = | 354.81 | nM | 6.45 |
| CHEMBL199636 | — | EC50 | = | 562.34 | nM | 6.25 |
| CHEMBL201016 | — | Kd | = | 44668.36 | nM | 4.35 |
| CHEMBL197604 | — | Intrinsic activity | = | 0.29 | — | - |
| CHEMBL382846 | — | Intrinsic activity | = | - | — | - |
| CHEMBL381913 | — | Intrinsic activity | = | - | — | - |
| CHEMBL201016 | — | Intrinsic activity | = | 0.34 | — | - |
| CHEMBL380572 | — | pKb | = | 6.0 | — | - |
| CHEMBL382846 | — | pKb | = | 4.78 | — | - |
| CHEMBL381913 | — | pKb | = | 5.26 | — | - |
| CHEMBL197604 | — | pKb | = | 4.57 | — | - |
| CHEMBL199636 | — | Intrinsic activity | = | 0.45 | — | - |
| CHEMBL382659 | — | Intrinsic activity | = | - | — | - |
| CHEMBL380572 | — | EC50 | < | 100000.0 | nM | - |
| CHEMBL382659 | — | pKb | = | 5.53 | — | - |
| CHEMBL380572 | — | Intrinsic activity | = | - | — | - |