Assay Detail
Binding
CHEMBL3366381
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Displacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation counting
16
Total Activities
16
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.46 | 8.95 |
| pKi | 2 | - | - |
| pKA | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 8.95 |
| CHEMBL569713 | SCOPOLAMINE | 4.0 | 1 | 8.89 |
| CHEMBL2449003 | ENDO-ATROPINE | — | 1 | 8.52 |
| CHEMBL3323284 | — | — | 1 | 8.26 |
| CHEMBL3323280 | — | — | 1 | 7.78 |
| CHEMBL3323283 | — | — | 1 | 7.77 |
| CHEMBL3323281 | — | — | 1 | 7.71 |
| CHEMBL3323282 | — | — | 1 | 7.68 |
| CHEMBL3323279 | — | — | 1 | 7.06 |
| CHEMBL3323286 | — | — | 1 | 6.92 |
| CHEMBL3323288 | — | — | 1 | 5.40 |
| CHEMBL3121474 | — | — | 1 | 4.52 |
| CHEMBL1197177 | — | — | 1 | - |
| CHEMBL3323287 | — | — | 1 | - |
| CHEMBL266295 | — | — | 1 | - |
| CHEMBL274413 | NAPHMETHONIUM | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 1.122 | nM | 8.95 |
| CHEMBL569713 | SCOPOLAMINE | Ki | = | 1.288 | nM | 8.89 |
| CHEMBL2449003 | ENDO-ATROPINE | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL3323284 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL3323280 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL3323283 | — | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL3323281 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL3323282 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL3323279 | — | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL3323286 | — | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL3323288 | — | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL3121474 | — | Ki | = | 30199.52 | nM | 4.52 |
| CHEMBL1197177 | — | pKi | - | — | - | |
| CHEMBL3323287 | — | pKi | - | — | - | |
| CHEMBL266295 | — | pKA | = | 4.37 | — | - |
| CHEMBL274413 | NAPHMETHONIUM | pKA | = | 5.05 | — | - |