Assay Detail
Binding
CHEMBL862220
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Binding affinity to cloned human muscarinic M2 receptor expressed in CHO cells
19
Total Activities
17
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
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 4.86 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL128365 | ARECAIDINE PROPARGYL ESTER | — | 1 | 7.06 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.91 |
| CHEMBL380759 | — | — | 1 | 5.49 |
| CHEMBL2092820 | — | — | 1 | 5.03 |
| CHEMBL2093084 | — | — | 1 | 4.81 |
| CHEMBL2093082 | — | — | 3 | 4.54 |
| CHEMBL2092736 | — | — | 1 | 4.29 |
| CHEMBL2092735 | — | — | 1 | 4.11 |
| CHEMBL2092737 | — | — | 1 | 4.06 |
| CHEMBL3351105 | — | — | 1 | 4.05 |
| CHEMBL2093081 | — | — | 1 | - |
| CHEMBL3351104 | — | — | 1 | - |
| CHEMBL3350063 | — | — | 1 | - |
| CHEMBL3351103 | — | — | 1 | - |
| CHEMBL2093083 | — | — | 1 | - |
| CHEMBL3350064 | — | — | 1 | - |
| CHEMBL3350062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL128365 | ARECAIDINE PROPARGYL ESTER | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL14 | CARBACHOL | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL380759 | — | Ki | = | 3235.94 | nM | 5.49 |
| CHEMBL2092820 | — | Ki | = | 9332.54 | nM | 5.03 |
| CHEMBL2093084 | — | Ki | = | 15488.17 | nM | 4.81 |
| CHEMBL2093082 | — | Ki | = | 28840.32 | nM | 4.54 |
| CHEMBL2092736 | — | Ki | = | 51286.14 | nM | 4.29 |
| CHEMBL2092735 | — | Ki | = | 77624.71 | nM | 4.11 |
| CHEMBL2093082 | — | Ki | = | 81283.05 | nM | 4.09 |
| CHEMBL2092737 | — | Ki | = | 87096.36 | nM | 4.06 |
| CHEMBL3351105 | — | Ki | = | 89125.09 | nM | 4.05 |
| CHEMBL2093081 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL3351104 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL3350063 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL3351103 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL2093082 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL2093083 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL3350064 | — | Ki | < | 100000.0 | nM | - |
| CHEMBL3350062 | — | Ki | < | 100000.0 | nM | - |