Assay Detail
Binding
CHEMBL2380034
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] N-methylscopolamine from human muscarinic M2 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
17
Total Activities
17
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 |
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 | 17 | 7.46 | 9.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL37372 | — | — | 1 | 9.78 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.84 |
| CHEMBL2106570 | METHYLBENACTYZIUM BROMIDE | 2.0 | 1 | 8.81 |
| CHEMBL2377387 | — | — | 1 | 8.27 |
| CHEMBL2377261 | — | — | 1 | 8.23 |
| CHEMBL2377267 | — | — | 1 | 8.10 |
| CHEMBL1101 | BIPERIDEN | 4.0 | 1 | 7.86 |
| CHEMBL2377269 | — | — | 1 | 7.82 |
| CHEMBL2377268 | — | — | 1 | 7.51 |
| CHEMBL26505 | APROFENE | 2.0 | 1 | 6.97 |
| CHEMBL2377392 | — | — | 1 | 6.94 |
| CHEMBL1191560 | — | — | 1 | 6.61 |
| CHEMBL2377388 | — | — | 1 | 6.55 |
| CHEMBL2377384 | — | — | 1 | 6.46 |
| CHEMBL2377383 | — | — | 1 | 6.13 |
| CHEMBL2110892 | BIETAMIVERINE | 2.0 | 1 | 5.99 |
| CHEMBL2377262 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL37372 | — | Ki | = | 0.165 | nM | 9.78 |
| CHEMBL517712 | ATROPINE | Ki | = | 1.44 | nM | 8.84 |
| CHEMBL2106570 | METHYLBENACTYZIUM BROMIDE | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL2377387 | — | Ki | = | 5.38 | nM | 8.27 |
| CHEMBL2377261 | — | Ki | = | 5.85 | nM | 8.23 |
| CHEMBL2377267 | — | Ki | = | 7.93 | nM | 8.10 |
| CHEMBL1101 | BIPERIDEN | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL2377269 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL2377268 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL26505 | APROFENE | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL2377392 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL1191560 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL2377388 | — | Ki | = | 281.5 | nM | 6.55 |
| CHEMBL2377384 | — | Ki | = | 348.0 | nM | 6.46 |
| CHEMBL2377383 | — | Ki | = | 738.0 | nM | 6.13 |
| CHEMBL2110892 | BIETAMIVERINE | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL2377262 | — | Ki | = | 1340.0 | nM | 5.87 |