Assay Detail
Binding
CHEMBL861240
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Inhibition of [3H]NMS dissociation from muscarinic M2 receptor in Na,K,Pi buffer
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
6H,13H-Pyrazino[1,2-a;4,5-a']diindole analogs: probing the pharmacophore for allosteric ligands of muscarinic M2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.06 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL607179 | DIMETHYLCARACURIE V | — | 1 | 8.09 |
| CHEMBL607178 | DIALLYLCARACURIE V | — | 1 | 7.95 |
| CHEMBL206666 | — | — | 1 | 6.96 |
| CHEMBL382243 | — | — | 1 | 6.64 |
| CHEMBL380352 | CARACURINE V | — | 1 | 6.36 |
| CHEMBL203627 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL607179 | DIMETHYLCARACURIE V | EC50 | = | 8.128 | nM | 8.09 |
| CHEMBL607178 | DIALLYLCARACURIE V | EC50 | = | 11.22 | nM | 7.95 |
| CHEMBL206666 | — | EC50 | = | 109.65 | nM | 6.96 |
| CHEMBL382243 | — | EC50 | = | 229.09 | nM | 6.64 |
| CHEMBL380352 | CARACURINE V | EC50 | = | 436.52 | nM | 6.36 |
| CHEMBL203627 | — | EC50 | = | 446.68 | nM | 6.35 |