Assay Detail
Binding
CHEMBL2380040
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Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor after 30 mins by scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.77 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26505 | APROFENE | 2.0 | 1 | 7.58 |
| CHEMBL37372 | — | — | 1 | 7.36 |
| CHEMBL2377383 | — | — | 1 | 7.18 |
| CHEMBL2377385 | — | — | 1 | 6.79 |
| CHEMBL2377384 | — | — | 1 | 6.59 |
| CHEMBL2110892 | BIETAMIVERINE | 2.0 | 1 | 6.29 |
| CHEMBL2377262 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26505 | APROFENE | Ki | = | 26.5 | nM | 7.58 |
| CHEMBL37372 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2377383 | — | Ki | = | 65.5 | nM | 7.18 |
| CHEMBL2377385 | — | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL2377384 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL2110892 | BIETAMIVERINE | Ki | = | 517.0 | nM | 6.29 |
| CHEMBL2377262 | — | Ki | = | 2670.0 | nM | 5.57 |