Assay Detail
Binding
CHEMBL4051384
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Displacement of [3H]NMS from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay
10
Total Activities
10
Compounds Tested
3
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 | 6 | 9.22 | 9.39 |
| IC50 | 3 | 6.22 | 6.32 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097258 | — | — | 1 | 9.39 |
| CHEMBL4089543 | — | — | 1 | 9.39 |
| CHEMBL4079233 | — | — | 1 | 9.15 |
| CHEMBL4068393 | — | — | 1 | 9.15 |
| CHEMBL4059733 | — | — | 1 | 9.12 |
| CHEMBL4066481 | — | — | 1 | 9.12 |
| CHEMBL266295 | — | — | 1 | 6.32 |
| CHEMBL1200993 | GALLAMINE TRIETHIODIDE | 4.0 | 1 | 6.11 |
| CHEMBL4089376 | — | — | 1 | - |
| CHEMBL4092094 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097258 | — | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL4089543 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL4079233 | — | Ki | = | 0.7079 | nM | 9.15 |
| CHEMBL4068393 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL4059733 | — | Ki | = | 0.7586 | nM | 9.12 |
| CHEMBL4066481 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL266295 | — | IC50 | = | 478.63 | nM | 6.32 |
| CHEMBL1200993 | GALLAMINE TRIETHIODIDE | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL4089376 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4092094 | — | Inhibition | - | % | - |