Assay Detail
Binding
CHEMBL745720
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Inhibition of [3H]quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M2 of rat heart
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 12 | 5.53 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284208 | — | — | 1 | 6.36 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 6.23 |
| CHEMBL278618 | — | — | 1 | 5.80 |
| CHEMBL28033 | — | — | 1 | 5.75 |
| CHEMBL540136 | SULFOARECOLINE IODIDE | — | 1 | 5.60 |
| CHEMBL541666 | — | — | 1 | 5.41 |
| CHEMBL26932 | — | — | 1 | 5.31 |
| CHEMBL25649 | — | — | 1 | 5.02 |
| CHEMBL285803 | — | — | 1 | 5.00 |
| CHEMBL27384 | — | — | 1 | 4.80 |
| CHEMBL283834 | — | — | 1 | - |
| CHEMBL418022 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284208 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL278618 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL28033 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL540136 | SULFOARECOLINE IODIDE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL541666 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL26932 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL25649 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL285803 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL27384 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL283834 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL418022 | — | IC50 | > | 1000000.0 | nM | - |