Assay Detail
Binding
CHEMBL909208
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Inhibition of [3H]NMS binding to human cloned M2 receptor expressed in CHO cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.42 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214898 | — | — | 1 | 7.72 |
| CHEMBL215189 | — | — | 1 | 7.17 |
| CHEMBL378772 | — | — | 1 | 7.14 |
| CHEMBL378859 | — | — | 1 | 7.03 |
| CHEMBL215894 | — | — | 1 | 7.00 |
| CHEMBL212645 | — | — | 1 | 6.96 |
| CHEMBL214029 | — | — | 1 | 6.66 |
| CHEMBL378872 | — | — | 1 | 6.51 |
| CHEMBL438822 | — | — | 1 | 6.35 |
| CHEMBL215180 | — | — | 1 | 6.31 |
| CHEMBL214342 | — | — | 1 | 6.14 |
| CHEMBL211976 | — | — | 1 | 5.92 |
| CHEMBL213709 | — | — | 1 | 5.89 |
| CHEMBL212141 | — | — | 1 | 5.82 |
| CHEMBL214642 | — | — | 1 | 5.52 |
| CHEMBL275914 | — | — | 1 | 5.51 |
| CHEMBL378885 | — | — | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214898 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL215189 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL378772 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL378859 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL215894 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL212645 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL214029 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL378872 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL438822 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL215180 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL214342 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL211976 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL213709 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL212141 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL214642 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL275914 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL378885 | — | Ki | = | 3700.0 | nM | 5.43 |