Assay Detail
Binding
CHEMBL1067397
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Displacement of [3H]NMS from human muscarinic M4 receptor expressed in CHO cells by microplate scintillation counting
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 | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 4.48 | 5.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.20 |
| CHEMBL74300 | — | — | 1 | 5.04 |
| CHEMBL390842 | — | — | 1 | 4.94 |
| CHEMBL593685 | — | — | 1 | 4.59 |
| CHEMBL593620 | — | — | 1 | 4.52 |
| CHEMBL595265 | — | — | 1 | 4.51 |
| CHEMBL594801 | — | — | 1 | 4.35 |
| CHEMBL593861 | — | — | 1 | 4.27 |
| CHEMBL594803 | — | — | 1 | 4.24 |
| CHEMBL595022 | — | — | 1 | 4.06 |
| CHEMBL404557 | — | — | 1 | 4.06 |
| CHEMBL594376 | — | — | 1 | 4.03 |
| CHEMBL593443 | — | — | 1 | - |
| CHEMBL593871 | — | — | 1 | - |
| CHEMBL593864 | — | — | 1 | - |
| CHEMBL608985 | — | — | 1 | - |
| CHEMBL594802 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14 | CARBACHOL | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL74300 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL390842 | — | Ki | = | 11481.54 | nM | 4.94 |
| CHEMBL593685 | — | Ki | = | 25703.96 | nM | 4.59 |
| CHEMBL593620 | — | Ki | = | 30199.52 | nM | 4.52 |
| CHEMBL595265 | — | Ki | = | 30902.95 | nM | 4.51 |
| CHEMBL594801 | — | Ki | = | 44668.36 | nM | 4.35 |
| CHEMBL593861 | — | Ki | = | 53703.18 | nM | 4.27 |
| CHEMBL594803 | — | Ki | = | 57543.99 | nM | 4.24 |
| CHEMBL595022 | — | Ki | = | 87096.36 | nM | 4.06 |
| CHEMBL404557 | — | Ki | = | 87096.36 | nM | 4.06 |
| CHEMBL594376 | — | Ki | = | 93325.43 | nM | 4.03 |
| CHEMBL593443 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL593871 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL593864 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL608985 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL594802 | — | Ki | > | 100000.0 | nM | - |