Assay Detail
Binding
CHEMBL923345
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Displacement of [3H]N-methylscopolamine from muscarinic M3 receptor in rat submandibular gland
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Submandibular gland |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Muscarinic acetylcholine receptor M3 (CHEMBL320) ↗| 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 | 7.56 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248811 | — | — | 1 | 8.74 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 8.60 |
| CHEMBL437781 | — | — | 1 | 8.23 |
| CHEMBL248614 | — | — | 1 | 8.17 |
| CHEMBL249830 | — | — | 1 | 8.03 |
| CHEMBL250834 | — | — | 1 | 7.91 |
| CHEMBL400167 | — | — | 1 | 7.91 |
| CHEMBL249205 | — | — | 1 | 7.70 |
| CHEMBL248809 | — | — | 1 | 7.60 |
| CHEMBL400953 | — | — | 1 | 7.50 |
| CHEMBL249007 | — | — | 1 | 7.50 |
| CHEMBL250030 | — | — | 1 | 7.48 |
| CHEMBL249206 | — | — | 1 | 7.38 |
| CHEMBL401154 | — | — | 1 | 7.36 |
| CHEMBL249204 | — | — | 1 | 7.36 |
| CHEMBL249006 | — | — | 1 | 7.23 |
| CHEMBL250031 | — | — | 1 | 7.15 |
| CHEMBL250203 | — | — | 1 | 7.02 |
| CHEMBL249005 | — | — | 1 | 6.28 |
| CHEMBL1162964 | — | — | 1 | 6.11 |
| CHEMBL248616 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248811 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1346 | DARIFENACIN | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL437781 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL248614 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL249830 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL250834 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL400167 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL249205 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL248809 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL400953 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL249007 | — | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL250030 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL249206 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL401154 | — | Ki | = | 43.6 | nM | 7.36 |
| CHEMBL249204 | — | Ki | = | 43.6 | nM | 7.36 |
| CHEMBL249006 | — | Ki | = | 58.9 | nM | 7.23 |
| CHEMBL250031 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL250203 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL249005 | — | Ki | = | 524.0 | nM | 6.28 |
| CHEMBL1162964 | — | Ki | = | 776.0 | nM | 6.11 |
| CHEMBL248616 | — | Ki | > | 1000.0 | nM | - |