Assay Detail
Binding
CHEMBL909210
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Inhibition of [3H]NMS binding to human cloned M5 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 M5 (CHEMBL2035) ↗| 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 | 5.70 | 6.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214898 | — | — | 1 | 6.03 |
| CHEMBL378859 | — | — | 1 | 6.02 |
| CHEMBL378772 | — | — | 1 | 5.80 |
| CHEMBL214342 | — | — | 1 | 5.80 |
| CHEMBL438822 | — | — | 1 | 5.77 |
| CHEMBL214029 | — | — | 1 | 5.77 |
| CHEMBL378872 | — | — | 1 | 5.60 |
| CHEMBL215894 | — | — | 1 | 5.57 |
| CHEMBL213709 | — | — | 1 | 5.55 |
| CHEMBL215189 | — | — | 1 | 5.51 |
| CHEMBL212645 | — | — | 1 | 5.50 |
| CHEMBL215180 | — | — | 1 | 5.46 |
| CHEMBL212141 | — | — | 1 | - |
| CHEMBL214642 | — | — | 1 | - |
| CHEMBL275914 | — | — | 1 | - |
| CHEMBL378885 | — | — | 1 | - |
| CHEMBL211976 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214898 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL378859 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL378772 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL214342 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL438822 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL214029 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL378872 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL215894 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL213709 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL215189 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL212645 | — | Ki | = | 3200.0 | nM | 5.50 |
| CHEMBL215180 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL212141 | — | Ki | > | 5400.0 | nM | - |
| CHEMBL214642 | — | Ki | > | 5100.0 | nM | - |
| CHEMBL275914 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL378885 | — | Ki | > | 5100.0 | nM | - |
| CHEMBL211976 | — | Ki | > | 5100.0 | nM | - |