Assay Detail
Binding
CHEMBL3406979
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Displacement of [3H]NMS from human M2 receptor expressed in CHOK1 cell membranes after 4 hrs by scintillation counting method
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.53 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 9.70 |
| CHEMBL3401649 | — | — | 1 | 9.22 |
| CHEMBL3401648 | — | — | 1 | 9.22 |
| CHEMBL3401650 | — | — | 1 | 9.05 |
| CHEMBL3401641 | — | — | 1 | 8.77 |
| CHEMBL1908368 | — | — | 1 | 8.70 |
| CHEMBL3401643 | — | — | 1 | 8.38 |
| CHEMBL3401651 | — | — | 1 | 8.32 |
| CHEMBL3401654 | — | — | 1 | 7.53 |
| CHEMBL3401640 | — | — | 1 | 7.46 |
| CHEMBL3401652 | — | — | 1 | 7.04 |
| CHEMBL3401645 | — | — | 1 | 7.00 |
| CHEMBL3401655 | — | — | 1 | 6.87 |
| CHEMBL3401656 | — | — | 1 | 6.85 |
| CHEMBL3401642 | — | — | 1 | 6.64 |
| CHEMBL3401647 | — | — | 1 | 6.54 |
| CHEMBL3401646 | — | — | 1 | 6.46 |
| CHEMBL3401653 | — | — | 1 | 6.09 |
| CHEMBL3401644 | — | — | 2 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3401649 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3401648 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3401650 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3401641 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1908368 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3401643 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3401651 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3401654 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL3401640 | — | IC50 | = | 35.1 | nM | 7.46 |
| CHEMBL3401652 | — | IC50 | = | 91.5 | nM | 7.04 |
| CHEMBL3401645 | — | IC50 | = | 101.1 | nM | 7.00 |
| CHEMBL3401655 | — | IC50 | = | 136.6 | nM | 6.87 |
| CHEMBL3401656 | — | IC50 | = | 140.2 | nM | 6.85 |
| CHEMBL3401642 | — | IC50 | = | 229.6 | nM | 6.64 |
| CHEMBL3401647 | — | IC50 | = | 285.9 | nM | 6.54 |
| CHEMBL3401646 | — | IC50 | = | 347.6 | nM | 6.46 |
| CHEMBL3401653 | — | IC50 | = | 804.2 | nM | 6.09 |
| CHEMBL3401644 | — | IC50 | = | 2531.4 | nM | 5.60 |
| CHEMBL3401644 | — | IC50 | = | 6455.0 | nM | 5.19 |