Assay Detail
Binding
CHEMBL857563
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Affinity for Muscarinic acetylcholine receptor M2 expressed in CHO cells by [3H]NMS displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 5.85 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 9.57 |
| CHEMBL279453 | — | — | 1 | 8.22 |
| CHEMBL277642 | HIMBACINE | — | 1 | 8.00 |
| CHEMBL22108 | DIMETHINDENE | 3.0 | 1 | 7.35 |
| CHEMBL21716 | — | — | 1 | 6.49 |
| CHEMBL278074 | — | — | 1 | 6.48 |
| CHEMBL21321 | — | — | 1 | 6.38 |
| CHEMBL280684 | — | — | 1 | 5.13 |
| CHEMBL279225 | — | — | 1 | 5.04 |
| CHEMBL278129 | — | — | 1 | 4.98 |
| CHEMBL20732 | — | — | 1 | 4.92 |
| CHEMBL21509 | — | — | 1 | 4.90 |
| CHEMBL21328 | — | — | 1 | 4.85 |
| CHEMBL21508 | — | — | 1 | 4.82 |
| CHEMBL283320 | — | — | 1 | 4.80 |
| CHEMBL279520 | — | — | 1 | 4.53 |
| CHEMBL424214 | — | — | 1 | 4.41 |
| CHEMBL21937 | — | — | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 0.2692 | nM | 9.57 |
| CHEMBL279453 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL277642 | HIMBACINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL22108 | DIMETHINDENE | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL21716 | — | Ki | = | 323.59 | nM | 6.49 |
| CHEMBL278074 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL21321 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL280684 | — | Ki | = | 7413.1 | nM | 5.13 |
| CHEMBL279225 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL278129 | — | Ki | = | 10471.29 | nM | 4.98 |
| CHEMBL20732 | — | Ki | = | 12022.64 | nM | 4.92 |
| CHEMBL21509 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL21328 | — | Ki | = | 14125.38 | nM | 4.85 |
| CHEMBL21508 | — | Ki | = | 15135.61 | nM | 4.82 |
| CHEMBL283320 | — | Ki | = | 15848.93 | nM | 4.80 |
| CHEMBL279520 | — | Ki | = | 29512.09 | nM | 4.53 |
| CHEMBL424214 | — | Ki | = | 38904.51 | nM | 4.41 |
| CHEMBL21937 | — | Ki | = | 41686.94 | nM | 4.38 |