Assay Detail
Binding
CHEMBL744024
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M2 in rat brain membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 4.75 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284208 | — | — | 1 | 5.58 |
| CHEMBL28033 | — | — | 1 | 5.32 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 4.96 |
| CHEMBL541666 | — | — | 1 | 4.66 |
| CHEMBL540136 | SULFOARECOLINE IODIDE | — | 1 | 4.47 |
| CHEMBL278618 | — | — | 1 | 4.44 |
| CHEMBL27384 | — | — | 1 | 4.42 |
| CHEMBL25649 | — | — | 1 | 4.13 |
| CHEMBL283834 | — | — | 1 | - |
| CHEMBL418022 | — | — | 1 | - |
| CHEMBL285803 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284208 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL28033 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL541666 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL540136 | SULFOARECOLINE IODIDE | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL278618 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL27384 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL25649 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL283834 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL418022 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL285803 | — | IC50 | = | 110000.0 | nM | - |