Assay Detail
Binding
CHEMBL4119545
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Displacement of [3H]NMS from recombinant human muscarinic M2 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
15
Total Activities
15
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
Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.72 | 8.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2078942 | — | — | 1 | 8.01 |
| CHEMBL4128341 | — | — | 1 | 7.48 |
| CHEMBL4129580 | — | — | 1 | 7.24 |
| CHEMBL4126290 | — | — | 1 | 7.21 |
| CHEMBL4126071 | — | — | 1 | 7.02 |
| CHEMBL2078987 | — | — | 1 | 7.02 |
| CHEMBL1734 | SOLIFENACIN | 4.0 | 1 | 6.92 |
| CHEMBL4127373 | — | — | 1 | 6.80 |
| CHEMBL4127428 | — | — | 1 | 6.70 |
| CHEMBL4129723 | — | — | 1 | 6.45 |
| CHEMBL4128497 | — | — | 1 | 6.37 |
| CHEMBL4130037 | — | — | 1 | 6.15 |
| CHEMBL4128667 | — | — | 1 | 5.91 |
| CHEMBL4128764 | — | — | 1 | 5.81 |
| CHEMBL4129382 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2078942 | — | Ki | = | 9.772 | nM | 8.01 |
| CHEMBL4128341 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL4129580 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL4126290 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL4126071 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL2078987 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL1734 | SOLIFENACIN | Ki | = | 120.23 | nM | 6.92 |
| CHEMBL4127373 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL4127428 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL4129723 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL4128497 | — | Ki | = | 426.58 | nM | 6.37 |
| CHEMBL4130037 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL4128667 | — | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL4128764 | — | Ki | = | 1548.82 | nM | 5.81 |
| CHEMBL4129382 | — | Ki | = | 2290.87 | nM | 5.64 |