Assay Detail
Binding
CHEMBL2380033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis
18
Total Activities
18
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 | 18 | 7.50 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2377383 | — | — | 1 | 9.27 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.66 |
| CHEMBL2377387 | — | — | 1 | 8.51 |
| CHEMBL2106570 | METHYLBENACTYZIUM BROMIDE | 2.0 | 1 | 8.37 |
| CHEMBL1101 | BIPERIDEN | 4.0 | 1 | 8.22 |
| CHEMBL2377392 | — | — | 1 | 8.22 |
| CHEMBL2377267 | — | — | 1 | 8.18 |
| CHEMBL2377269 | — | — | 1 | 8.08 |
| CHEMBL2377268 | — | — | 1 | 7.95 |
| CHEMBL37372 | — | — | 1 | 7.28 |
| CHEMBL2377261 | — | — | 1 | 7.23 |
| CHEMBL2377262 | — | — | 1 | 6.96 |
| CHEMBL2110892 | BIETAMIVERINE | 2.0 | 1 | 6.73 |
| CHEMBL1191560 | — | — | 1 | 6.61 |
| CHEMBL2377388 | — | — | 1 | 6.59 |
| CHEMBL2377385 | — | — | 1 | 6.57 |
| CHEMBL2377384 | — | — | 1 | 6.42 |
| CHEMBL26505 | APROFENE | 2.0 | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2377383 | — | Ki | = | 0.543 | nM | 9.27 |
| CHEMBL517712 | ATROPINE | Ki | = | 2.18 | nM | 8.66 |
| CHEMBL2377387 | — | Ki | = | 3.12 | nM | 8.51 |
| CHEMBL2106570 | METHYLBENACTYZIUM BROMIDE | Ki | = | 4.25 | nM | 8.37 |
| CHEMBL1101 | BIPERIDEN | Ki | = | 5.95 | nM | 8.22 |
| CHEMBL2377392 | — | Ki | = | 5.97 | nM | 8.22 |
| CHEMBL2377267 | — | Ki | = | 6.55 | nM | 8.18 |
| CHEMBL2377269 | — | Ki | = | 8.37 | nM | 8.08 |
| CHEMBL2377268 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL37372 | — | Ki | = | 52.2 | nM | 7.28 |
| CHEMBL2377261 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2377262 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL2110892 | BIETAMIVERINE | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL1191560 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL2377388 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL2377385 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL2377384 | — | Ki | = | 384.0 | nM | 6.42 |
| CHEMBL26505 | APROFENE | Ki | = | 7760.0 | nM | 5.11 |