Assay Detail
Binding
CHEMBL3366379
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-NMS from human muscarinic M2 Y177Q/T423H mutant expressed in Flp-In-CHO 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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.13 | 9.48 |
| pKi | 2 | - | - |
| pKA | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 9.48 |
| CHEMBL3323286 | — | — | 1 | 8.66 |
| CHEMBL3323281 | — | — | 1 | 8.55 |
| CHEMBL3323284 | — | — | 1 | 8.48 |
| CHEMBL569713 | SCOPOLAMINE | 4.0 | 1 | 8.45 |
| CHEMBL2449003 | ENDO-ATROPINE | — | 1 | 8.34 |
| CHEMBL3323280 | — | — | 1 | 8.27 |
| CHEMBL3323283 | — | — | 1 | 8.15 |
| CHEMBL3323279 | — | — | 1 | 7.74 |
| CHEMBL3323287 | — | — | 1 | 7.57 |
| CHEMBL3323288 | — | — | 1 | 7.19 |
| CHEMBL3121474 | — | — | 1 | 6.70 |
| CHEMBL1197177 | — | — | 1 | - |
| CHEMBL3323282 | — | — | 1 | - |
| CHEMBL266295 | — | — | 1 | - |
| CHEMBL274413 | NAPHMETHONIUM | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 0.3311 | nM | 9.48 |
| CHEMBL3323286 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL3323281 | — | Ki | = | 2.818 | nM | 8.55 |
| CHEMBL3323284 | — | Ki | = | 3.311 | nM | 8.48 |
| CHEMBL569713 | SCOPOLAMINE | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL2449003 | ENDO-ATROPINE | Ki | = | 4.571 | nM | 8.34 |
| CHEMBL3323280 | — | Ki | = | 5.37 | nM | 8.27 |
| CHEMBL3323283 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL3323279 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL3323287 | — | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL3323288 | — | Ki | = | 64.57 | nM | 7.19 |
| CHEMBL3121474 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL1197177 | — | pKi | - | — | - | |
| CHEMBL3323282 | — | pKi | - | — | - | |
| CHEMBL266295 | — | pKA | = | 5.47 | — | - |
| CHEMBL274413 | NAPHMETHONIUM | pKA | = | 5.82 | — | - |