Assay Detail
Binding
CHEMBL748895
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Binding affinity for human Muscarinic acetylcholine receptor M2
13
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.29 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL74141 | — | — | 1 | 9.29 |
| CHEMBL418446 | — | — | 3 | 9.05 |
| CHEMBL276239 | — | — | 1 | 9.05 |
| CHEMBL12098 | SCH-211803 | — | 1 | 9.05 |
| CHEMBL150624 | — | — | 3 | 8.89 |
| CHEMBL150845 | — | — | 1 | 8.02 |
| CHEMBL150707 | — | — | 1 | 7.50 |
| CHEMBL412421 | — | — | 1 | 6.98 |
| CHEMBL52203 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL74141 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL276239 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL12098 | SCH-211803 | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL418446 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL150624 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL150624 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL150624 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL418446 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL150845 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL418446 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL150707 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL412421 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL52203 | — | Ki | = | 221.0 | nM | 6.66 |