Assay Detail
Binding
CHEMBL2045513
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Displacement of [3H]N-methylscopolamine from human muscarinic M5 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 M5 (CHEMBL2035) ↗| 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 | 6.75 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 9.68 |
| CHEMBL2042405 | — | — | 1 | 8.77 |
| CHEMBL2042553 | — | — | 1 | 8.74 |
| CHEMBL2042404 | — | — | 1 | 8.36 |
| CHEMBL2042552 | — | — | 1 | 8.27 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 7.85 |
| CHEMBL2042554 | — | — | 1 | 7.09 |
| CHEMBL2042406 | — | — | 1 | 6.97 |
| CHEMBL2042407 | — | — | 1 | 5.12 |
| CHEMBL390842 | — | — | 1 | 5.11 |
| CHEMBL2042402 | — | — | 1 | 4.99 |
| CHEMBL2042400 | — | — | 1 | 4.58 |
| CHEMBL2042551 | — | — | 1 | 4.50 |
| CHEMBL2042403 | — | — | 1 | 4.48 |
| CHEMBL2042401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 0.2089 | nM | 9.68 |
| CHEMBL2042405 | — | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL2042553 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL2042404 | — | Ki | = | 4.365 | nM | 8.36 |
| CHEMBL2042552 | — | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 14.13 | nM | 7.85 |
| CHEMBL2042554 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL2042406 | — | Ki | = | 107.15 | nM | 6.97 |
| CHEMBL2042407 | — | Ki | = | 7585.78 | nM | 5.12 |
| CHEMBL390842 | — | Ki | = | 7762.47 | nM | 5.11 |
| CHEMBL2042402 | — | Ki | = | 10232.93 | nM | 4.99 |
| CHEMBL2042400 | — | Ki | = | 26302.68 | nM | 4.58 |
| CHEMBL2042551 | — | Ki | = | 31622.78 | nM | 4.50 |
| CHEMBL2042403 | — | Ki | = | 33113.11 | nM | 4.48 |
| CHEMBL2042401 | — | Ki | > | 100000.0 | nM | - |