Assay Detail
Binding
CHEMBL917978
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Binding affinity to human cloned muscarinic receptor M2 expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.77 | 9.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 9.75 |
| CHEMBL375969 | — | — | 1 | 9.33 |
| CHEMBL376057 | — | — | 1 | 9.11 |
| CHEMBL222259 | — | — | 1 | 9.08 |
| CHEMBL219786 | — | — | 1 | 9.02 |
| CHEMBL376870 | — | — | 1 | 8.97 |
| CHEMBL220393 | — | — | 1 | 8.83 |
| CHEMBL385328 | — | — | 1 | 8.56 |
| CHEMBL375073 | — | — | 1 | 8.56 |
| CHEMBL375851 | — | — | 1 | 8.47 |
| CHEMBL376255 | — | — | 1 | 8.37 |
| CHEMBL219825 | — | — | 1 | 8.35 |
| CHEMBL373515 | — | — | 1 | 8.31 |
| CHEMBL45454 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 0.1778 | nM | 9.75 |
| CHEMBL375969 | — | Ki | = | 0.4677 | nM | 9.33 |
| CHEMBL376057 | — | Ki | = | 0.7762 | nM | 9.11 |
| CHEMBL222259 | — | Ki | = | 0.8318 | nM | 9.08 |
| CHEMBL219786 | — | Ki | = | 0.955 | nM | 9.02 |
| CHEMBL376870 | — | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL220393 | — | Ki | = | 1.479 | nM | 8.83 |
| CHEMBL385328 | — | Ki | = | 2.754 | nM | 8.56 |
| CHEMBL375073 | — | Ki | = | 2.754 | nM | 8.56 |
| CHEMBL375851 | — | Ki | = | 3.388 | nM | 8.47 |
| CHEMBL376255 | — | Ki | = | 4.266 | nM | 8.37 |
| CHEMBL219825 | — | Ki | = | 4.467 | nM | 8.35 |
| CHEMBL373515 | — | Ki | = | 4.898 | nM | 8.31 |
| CHEMBL45454 | — | Ki | = | 7.586 | nM | 8.12 |