Assay Detail
Binding
CHEMBL861933
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Inhibition of [3H]NMS dissociation from porcine heart muscarinic receptor M2
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.07 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274413 | NAPHMETHONIUM | — | 1 | 9.29 |
| CHEMBL380572 | — | — | 1 | 8.96 |
| CHEMBL381913 | — | — | 1 | 8.63 |
| CHEMBL199636 | — | — | 1 | 8.61 |
| CHEMBL266295 | — | — | 1 | 7.87 |
| CHEMBL382659 | — | — | 1 | 7.67 |
| CHEMBL382846 | — | — | 1 | 7.30 |
| CHEMBL197604 | — | — | 1 | 7.22 |
| CHEMBL201016 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274413 | NAPHMETHONIUM | EC50 | = | 0.5129 | nM | 9.29 |
| CHEMBL380572 | — | EC50 | = | 1.096 | nM | 8.96 |
| CHEMBL381913 | — | EC50 | = | 2.344 | nM | 8.63 |
| CHEMBL199636 | — | EC50 | = | 2.455 | nM | 8.61 |
| CHEMBL266295 | — | EC50 | = | 13.49 | nM | 7.87 |
| CHEMBL382659 | — | EC50 | = | 21.38 | nM | 7.67 |
| CHEMBL382846 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL197604 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL201016 | — | EC50 | = | 83.18 | nM | 7.08 |