Assay Detail
Binding
CHEMBL4051398
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]UR-AP060 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cell homogenate after 3 hrs by liquid scintillation counting assay
10
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.00 | 8.98 |
| Kd | 1 | 6.58 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097258 | — | — | 1 | 8.98 |
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 8.92 |
| CHEMBL4059733 | — | — | 1 | 7.99 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 7.77 |
| CHEMBL4070155 | — | — | 1 | 7.63 |
| CHEMBL266295 | — | — | 2 | 6.58 |
| CHEMBL1200993 | GALLAMINE TRIETHIODIDE | 4.0 | 1 | 5.43 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 5.35 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097258 | — | Ki | = | 1.047 | nM | 8.98 |
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 1.202 | nM | 8.92 |
| CHEMBL4059733 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL517712 | ATROPINE | Ki | = | 16.98 | nM | 7.77 |
| CHEMBL4070155 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL266295 | — | Kd | = | 263.03 | nM | 6.58 |
| CHEMBL266295 | — | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL1200993 | GALLAMINE TRIETHIODIDE | Ki | = | 3715.35 | nM | 5.43 |
| CHEMBL21536 | XANOMELINE | Ki | = | 4466.84 | nM | 5.35 |
| CHEMBL7634 | OXOTREMORINE | Ki | = | 10000.0 | nM | 5.00 |