Assay Detail
Binding
CHEMBL909209
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Inhibition of [3H]NMS binding to human cloned M4 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 |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.22 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214898 | — | — | 1 | 7.96 |
| CHEMBL378772 | — | — | 1 | 7.70 |
| CHEMBL378859 | — | — | 1 | 7.62 |
| CHEMBL214029 | — | — | 1 | 7.54 |
| CHEMBL215189 | — | — | 1 | 7.51 |
| CHEMBL438822 | — | — | 1 | 7.41 |
| CHEMBL214342 | — | — | 1 | 7.39 |
| CHEMBL215180 | — | — | 1 | 7.38 |
| CHEMBL212645 | — | — | 1 | 7.32 |
| CHEMBL378872 | — | — | 1 | 7.28 |
| CHEMBL213709 | — | — | 1 | 7.04 |
| CHEMBL215894 | — | — | 1 | 6.92 |
| CHEMBL211976 | — | — | 1 | 6.82 |
| CHEMBL212141 | — | — | 1 | 6.75 |
| CHEMBL378885 | — | — | 1 | 6.54 |
| CHEMBL214642 | — | — | 1 | 6.32 |
| CHEMBL275914 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214898 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL378772 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL378859 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL214029 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL215189 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL438822 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL214342 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL215180 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL212645 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL378872 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL213709 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL215894 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL211976 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL212141 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL378885 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL214642 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL275914 | — | Ki | > | 1700.0 | nM | - |