Assay Detail
Binding
CHEMBL752971
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Reduction of dissociation rate of [3H]N-methylscopolamine ([3H]NMS) from muscarinic acetylcholine receptor M2 of pig heart
14
Total Activities
14
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
Search for the pharmacophore of bispyridinium-type allosteric modulators of muscarinic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 4.96 | 5.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202148 | — | — | 1 | 5.38 |
| CHEMBL33656 | — | — | 1 | 5.35 |
| CHEMBL590603 | — | — | 1 | 5.33 |
| CHEMBL32609 | — | — | 1 | 5.22 |
| CHEMBL32329 | — | — | 1 | 5.03 |
| CHEMBL1202147 | — | — | 1 | 4.96 |
| CHEMBL1202149 | — | — | 1 | 4.92 |
| CHEMBL1202150 | — | — | 1 | 4.77 |
| CHEMBL1202151 | — | — | 1 | 4.68 |
| CHEMBL539621 | — | — | 1 | 4.64 |
| CHEMBL1202152 | — | — | 1 | 4.60 |
| CHEMBL32688 | — | — | 1 | 4.58 |
| CHEMBL33595 | — | — | 1 | - |
| CHEMBL32778 | TRIMEDOXIME | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202148 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL33656 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL590603 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL32609 | — | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL32329 | — | EC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL1202147 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1202149 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1202150 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1202151 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL539621 | — | EC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL1202152 | — | EC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL32688 | — | EC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL33595 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL32778 | TRIMEDOXIME | EC50 | > | 1000000.0 | nM | - |