Assay Detail
Binding
CHEMBL2380041
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Inhibition of muscarinic acetylcholine receptor in rat cortex
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 9 | 8.18 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 9.92 |
| CHEMBL1490 | TRIHEXYPHENIDYL | 4.0 | 1 | 8.82 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 8.70 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 1 | 8.34 |
| CHEMBL61946 | CARAMIPHEN | 2.0 | 1 | 8.14 |
| CHEMBL1192807 | — | — | 1 | 8.07 |
| CHEMBL9967 | PIRENZEPINE | 2.0 | 1 | 7.55 |
| CHEMBL1192187 | — | — | 1 | 7.24 |
| CHEMBL27673 | METHOCTRAMINE | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1490 | TRIHEXYPHENIDYL | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1123 | DICYCLOMINE | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL61946 | CARAMIPHEN | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL1192807 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL9967 | PIRENZEPINE | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL1192187 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL27673 | METHOCTRAMINE | Ki | = | 137.0 | nM | 6.86 |