Assay Detail
Binding
CHEMBL891647
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Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M3 receptor expressed in Sf9 cells
26
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.26 | 9.66 |
| IC50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL234440 | — | — | 1 | 9.66 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 9.11 |
| CHEMBL394137 | — | — | 1 | 8.82 |
| CHEMBL234258 | — | — | 1 | 8.68 |
| CHEMBL234438 | — | — | 1 | 8.60 |
| CHEMBL234439 | — | — | 1 | 8.57 |
| CHEMBL391977 | — | — | 1 | 8.54 |
| CHEMBL394254 | — | — | 1 | 8.48 |
| CHEMBL392186 | — | — | 1 | 8.38 |
| CHEMBL234257 | — | — | 1 | 8.31 |
| CHEMBL233202 | — | — | 1 | 8.24 |
| CHEMBL233201 | — | — | 1 | 8.17 |
| CHEMBL435353 | — | — | 1 | 7.96 |
| CHEMBL394255 | — | — | 1 | 7.85 |
| CHEMBL234253 | — | — | 1 | 7.75 |
| CHEMBL233200 | — | — | 1 | 7.72 |
| CHEMBL234254 | — | — | 1 | 7.70 |
| CHEMBL234252 | — | — | 1 | 7.70 |
| CHEMBL233199 | — | — | 1 | 7.64 |
| CHEMBL233198 | — | — | 1 | 7.25 |
| CHEMBL392045 | — | — | 1 | - |
| CHEMBL234260 | — | — | 1 | - |
| CHEMBL234256 | — | — | 1 | - |
| CHEMBL234255 | — | — | 1 | - |
| CHEMBL435158 | — | — | 1 | - |
| CHEMBL429620 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL234440 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL394137 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL234258 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL234438 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL234439 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL391977 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL394254 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL392186 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL234257 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL233202 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL233201 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL435353 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL394255 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL234253 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL233200 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL234254 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL234252 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL233199 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL233198 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL392045 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL234260 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL234256 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL234255 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL435158 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL429620 | — | IC50 | > | 100.0 | nM | - |