Assay Detail
Binding
CHEMBL4051397
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]UNSW-MK259 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
12
Total Activities
10
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 | 10 | 7.94 | 10.20 |
| Kd | 2 | 6.13 | 6.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | 4.0 | 1 | 10.20 |
| CHEMBL4097258 | — | — | 1 | 9.97 |
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 9.09 |
| CHEMBL4059733 | — | — | 1 | 8.96 |
| CHEMBL4070155 | — | — | 1 | 8.76 |
| CHEMBL266295 | — | — | 2 | 7.40 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 6.83 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 6.57 |
| CHEMBL1200993 | GALLAMINE TRIETHIODIDE | 4.0 | 1 | 6.33 |
| CHEMBL4089376 | — | — | 2 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL376897 | METHSCOPOLAMINE | Ki | = | 0.0631 | nM | 10.20 |
| CHEMBL4097258 | — | Ki | = | 0.1072 | nM | 9.97 |
| CHEMBL517712 | ATROPINE | Ki | = | 0.8128 | nM | 9.09 |
| CHEMBL4059733 | — | Ki | = | 1.096 | nM | 8.96 |
| CHEMBL4070155 | — | Ki | = | 1.738 | nM | 8.76 |
| CHEMBL266295 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL7634 | OXOTREMORINE | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL266295 | — | Kd | = | 154.88 | nM | 6.81 |
| CHEMBL21536 | XANOMELINE | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL1200993 | GALLAMINE TRIETHIODIDE | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL4089376 | — | Kd | = | 3548.13 | nM | 5.45 |
| CHEMBL4089376 | — | Ki | = | 5495.41 | nM | 5.26 |