Assay Detail
Binding
CHEMBL2045512
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Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in CHO cells after 120 mins by scintillation counting
15
Total Activities
15
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
1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.81 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 9.85 |
| CHEMBL2042405 | — | — | 1 | 8.83 |
| CHEMBL2042553 | — | — | 1 | 8.63 |
| CHEMBL2042404 | — | — | 1 | 8.58 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 8.44 |
| CHEMBL2042552 | — | — | 1 | 8.31 |
| CHEMBL2042554 | — | — | 1 | 7.15 |
| CHEMBL2042406 | — | — | 1 | 6.82 |
| CHEMBL2042407 | — | — | 1 | 4.95 |
| CHEMBL390842 | — | — | 1 | 4.94 |
| CHEMBL2042402 | — | — | 1 | 4.91 |
| CHEMBL2042551 | — | — | 1 | 4.77 |
| CHEMBL2042400 | — | — | 1 | 4.60 |
| CHEMBL2042403 | — | — | 1 | 4.53 |
| CHEMBL2042401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 0.1413 | nM | 9.85 |
| CHEMBL2042405 | — | Ki | = | 1.479 | nM | 8.83 |
| CHEMBL2042553 | — | Ki | = | 2.344 | nM | 8.63 |
| CHEMBL2042404 | — | Ki | = | 2.63 | nM | 8.58 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL2042552 | — | Ki | = | 4.898 | nM | 8.31 |
| CHEMBL2042554 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL2042406 | — | Ki | = | 151.36 | nM | 6.82 |
| CHEMBL2042407 | — | Ki | = | 11220.18 | nM | 4.95 |
| CHEMBL390842 | — | Ki | = | 11481.54 | nM | 4.94 |
| CHEMBL2042402 | — | Ki | = | 12302.69 | nM | 4.91 |
| CHEMBL2042551 | — | Ki | = | 16982.44 | nM | 4.77 |
| CHEMBL2042400 | — | Ki | = | 25118.86 | nM | 4.60 |
| CHEMBL2042403 | — | Ki | = | 29512.09 | nM | 4.53 |
| CHEMBL2042401 | — | Ki | > | 100000.0 | nM | - |