Assay Detail
Binding
CHEMBL923346
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Displacement of [3H]N-methylscopolamine from muscarinic M2 receptor in rat heart
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 6.26 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248811 | — | — | 1 | 7.41 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 7.20 |
| CHEMBL437781 | — | — | 1 | 6.81 |
| CHEMBL249205 | — | — | 1 | 6.56 |
| CHEMBL249007 | — | — | 1 | 6.53 |
| CHEMBL249830 | — | — | 1 | 6.47 |
| CHEMBL248614 | — | — | 1 | 6.46 |
| CHEMBL249204 | — | — | 1 | 6.27 |
| CHEMBL400167 | — | — | 1 | 6.25 |
| CHEMBL248809 | — | — | 1 | 6.20 |
| CHEMBL250834 | — | — | 1 | 6.19 |
| CHEMBL249206 | — | — | 1 | 6.11 |
| CHEMBL401154 | — | — | 1 | 6.09 |
| CHEMBL400953 | — | — | 1 | 6.03 |
| CHEMBL250031 | — | — | 1 | 5.94 |
| CHEMBL249006 | — | — | 1 | 5.91 |
| CHEMBL250030 | — | — | 1 | 5.86 |
| CHEMBL250203 | — | — | 1 | 5.85 |
| CHEMBL1162964 | — | — | 1 | 5.58 |
| CHEMBL249005 | — | — | 1 | 5.40 |
| CHEMBL248616 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248811 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1346 | DARIFENACIN | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL437781 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL249205 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL249007 | — | Ki | = | 298.3 | nM | 6.53 |
| CHEMBL249830 | — | Ki | = | 335.3 | nM | 6.47 |
| CHEMBL248614 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL249204 | — | Ki | = | 537.0 | nM | 6.27 |
| CHEMBL400167 | — | Ki | = | 564.0 | nM | 6.25 |
| CHEMBL248809 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL250834 | — | Ki | = | 646.0 | nM | 6.19 |
| CHEMBL249206 | — | Ki | = | 778.3 | nM | 6.11 |
| CHEMBL401154 | — | Ki | = | 812.0 | nM | 6.09 |
| CHEMBL400953 | — | Ki | = | 943.3 | nM | 6.03 |
| CHEMBL250031 | — | Ki | = | 1139.0 | nM | 5.94 |
| CHEMBL249006 | — | Ki | = | 1230.0 | nM | 5.91 |
| CHEMBL250030 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL250203 | — | Ki | = | 1422.3 | nM | 5.85 |
| CHEMBL1162964 | — | Ki | = | 2630.0 | nM | 5.58 |
| CHEMBL249005 | — | Ki | = | 3981.0 | nM | 5.40 |
| CHEMBL248616 | — | Ki | > | 1000.0 | nM | - |