Assay Detail
Binding
CHEMBL931446
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Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHO cells
12
Total Activities
12
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 | Autocuration |
Publication
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.22 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.50 |
| CHEMBL381623 | — | — | 1 | 9.10 |
| CHEMBL1908368 | — | — | 1 | 8.90 |
| CHEMBL428962 | — | — | 1 | 8.80 |
| CHEMBL409151 | — | — | 1 | 8.60 |
| CHEMBL264676 | — | — | 1 | 8.50 |
| CHEMBL258959 | — | — | 1 | 8.20 |
| CHEMBL264414 | — | — | 1 | 7.70 |
| CHEMBL371734 | — | — | 1 | 7.60 |
| CHEMBL260228 | — | — | 1 | 7.50 |
| CHEMBL410061 | — | — | 1 | 7.40 |
| CHEMBL411514 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | Ki | = | 0.3162 | nM | 9.50 |
| CHEMBL381623 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL1908368 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL428962 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL409151 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL264676 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL258959 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL264414 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL371734 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL260228 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL410061 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL411514 | — | Ki | = | 158.49 | nM | 6.80 |