Assay Detail
Binding
CHEMBL752409
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Affinity for Muscarinic acetylcholine receptor M3 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 | 5.26 | 7.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 7.42 |
| CHEMBL279453 | — | — | 1 | 7.18 |
| CHEMBL277642 | HIMBACINE | — | 1 | 7.03 |
| CHEMBL22108 | DIMETHINDENE | 3.0 | 1 | 6.72 |
| CHEMBL21321 | — | — | 1 | 5.77 |
| CHEMBL21716 | — | — | 1 | 5.76 |
| CHEMBL278074 | — | — | 1 | 5.68 |
| CHEMBL280684 | — | — | 1 | 5.00 |
| CHEMBL20732 | — | — | 1 | 4.85 |
| CHEMBL278129 | — | — | 1 | 4.82 |
| CHEMBL21509 | — | — | 1 | 4.67 |
| CHEMBL21508 | — | — | 1 | 4.56 |
| CHEMBL279520 | — | — | 1 | 4.39 |
| CHEMBL283320 | — | — | 1 | 4.34 |
| CHEMBL21937 | — | — | 1 | 4.21 |
| CHEMBL279225 | — | — | 1 | 4.20 |
| CHEMBL21328 | — | — | 1 | 4.14 |
| CHEMBL424214 | — | — | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 38.02 | nM | 7.42 |
| CHEMBL279453 | — | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL277642 | HIMBACINE | Ki | = | 93.33 | nM | 7.03 |
| CHEMBL22108 | DIMETHINDENE | Ki | = | 190.55 | nM | 6.72 |
| CHEMBL21321 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL21716 | — | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL278074 | — | Ki | = | 2089.3 | nM | 5.68 |
| CHEMBL280684 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL20732 | — | Ki | = | 14125.38 | nM | 4.85 |
| CHEMBL278129 | — | Ki | = | 15135.61 | nM | 4.82 |
| CHEMBL21509 | — | Ki | = | 21379.62 | nM | 4.67 |
| CHEMBL21508 | — | Ki | = | 27542.29 | nM | 4.56 |
| CHEMBL279520 | — | Ki | = | 40738.03 | nM | 4.39 |
| CHEMBL283320 | — | Ki | = | 45708.82 | nM | 4.34 |
| CHEMBL21937 | — | Ki | = | 61659.5 | nM | 4.21 |
| CHEMBL279225 | — | Ki | = | 63095.73 | nM | 4.20 |
| CHEMBL21328 | — | Ki | = | 72443.6 | nM | 4.14 |
| CHEMBL424214 | — | Ki | = | 97723.72 | nM | 4.01 |