Assay Detail
Binding
CHEMBL746257
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Affinity for Muscarinic acetylcholine receptor M1 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 | 5.54 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 8.80 |
| CHEMBL279453 | — | — | 1 | 7.51 |
| CHEMBL277642 | HIMBACINE | — | 1 | 6.97 |
| CHEMBL22108 | DIMETHINDENE | 3.0 | 1 | 6.58 |
| CHEMBL21321 | — | — | 1 | 6.05 |
| CHEMBL278074 | — | — | 1 | 5.90 |
| CHEMBL21716 | — | — | 1 | 5.83 |
| CHEMBL20732 | — | — | 1 | 5.15 |
| CHEMBL21509 | — | — | 1 | 5.02 |
| CHEMBL280684 | — | — | 1 | 4.94 |
| CHEMBL278129 | — | — | 1 | 4.92 |
| CHEMBL21508 | — | — | 1 | 4.73 |
| CHEMBL279225 | — | — | 1 | 4.66 |
| CHEMBL283320 | — | — | 1 | 4.62 |
| CHEMBL21937 | — | — | 1 | 4.57 |
| CHEMBL279520 | — | — | 1 | 4.55 |
| CHEMBL424214 | — | — | 1 | 4.53 |
| CHEMBL21328 | — | — | 1 | 4.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL279453 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL277642 | HIMBACINE | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL22108 | DIMETHINDENE | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL21321 | — | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL278074 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL21716 | — | Ki | = | 1479.11 | nM | 5.83 |
| CHEMBL20732 | — | Ki | = | 7079.46 | nM | 5.15 |
| CHEMBL21509 | — | Ki | = | 9549.93 | nM | 5.02 |
| CHEMBL280684 | — | Ki | = | 11481.54 | nM | 4.94 |
| CHEMBL278129 | — | Ki | = | 12022.64 | nM | 4.92 |
| CHEMBL21508 | — | Ki | = | 18620.87 | nM | 4.73 |
| CHEMBL279225 | — | Ki | = | 21877.62 | nM | 4.66 |
| CHEMBL283320 | — | Ki | = | 23988.33 | nM | 4.62 |
| CHEMBL21937 | — | Ki | = | 26915.35 | nM | 4.57 |
| CHEMBL279520 | — | Ki | = | 28183.83 | nM | 4.55 |
| CHEMBL424214 | — | Ki | = | 29512.09 | nM | 4.53 |
| CHEMBL21328 | — | Ki | = | 48977.88 | nM | 4.31 |