Assay Detail
Binding
CHEMBL752317
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]pirenzepine binding to rat brain membrane Muscarinic acetylcholine receptor M1
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 M1 (CHEMBL276) ↗| 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 | 5.78 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284208 | — | — | 1 | 6.60 |
| CHEMBL541666 | — | — | 1 | 6.40 |
| CHEMBL28033 | — | — | 1 | 6.37 |
| CHEMBL26932 | — | — | 1 | 6.28 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 5.96 |
| CHEMBL540136 | SULFOARECOLINE IODIDE | — | 1 | 5.58 |
| CHEMBL25649 | — | — | 1 | 5.55 |
| CHEMBL278618 | — | — | 1 | 5.39 |
| CHEMBL27384 | — | — | 1 | 5.19 |
| CHEMBL285803 | — | — | 1 | 4.52 |
| CHEMBL283834 | — | — | 1 | - |
| CHEMBL418022 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284208 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL541666 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL28033 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL26932 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL540136 | SULFOARECOLINE IODIDE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL25649 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL278618 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL27384 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL285803 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL283834 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL418022 | — | IC50 | > | 1000000.0 | nM | - |