Assay Detail
Binding
CHEMBL2380032
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
12
Total Activities
12
Compounds Tested
1
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 M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 12 | 7.27 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.86 |
| CHEMBL2377267 | — | — | 1 | 8.83 |
| CHEMBL2377387 | — | — | 1 | 8.14 |
| CHEMBL2377269 | — | — | 1 | 8.02 |
| CHEMBL2106570 | METHYLBENACTYZIUM BROMIDE | 2.0 | 1 | 7.88 |
| CHEMBL1101 | BIPERIDEN | 4.0 | 1 | 7.49 |
| CHEMBL2377392 | — | — | 1 | 7.05 |
| CHEMBL2377268 | — | — | 1 | 6.54 |
| CHEMBL37372 | — | — | 1 | 6.25 |
| CHEMBL26505 | APROFENE | 2.0 | 1 | 6.20 |
| CHEMBL2377384 | — | — | 1 | 6.17 |
| CHEMBL2377385 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 1.39 | nM | 8.86 |
| CHEMBL2377267 | — | Ki | = | 1.49 | nM | 8.83 |
| CHEMBL2377387 | — | Ki | = | 7.23 | nM | 8.14 |
| CHEMBL2377269 | — | Ki | = | 9.48 | nM | 8.02 |
| CHEMBL2106570 | METHYLBENACTYZIUM BROMIDE | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL1101 | BIPERIDEN | Ki | = | 32.1 | nM | 7.49 |
| CHEMBL2377392 | — | Ki | = | 89.6 | nM | 7.05 |
| CHEMBL2377268 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL37372 | — | Ki | = | 566.0 | nM | 6.25 |
| CHEMBL26505 | APROFENE | Ki | = | 628.0 | nM | 6.20 |
| CHEMBL2377384 | — | Ki | = | 676.0 | nM | 6.17 |
| CHEMBL2377385 | — | Ki | = | 1690.0 | nM | 5.77 |