Assay Detail
Binding
CHEMBL751538
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Displacement of [3H]pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Novel functional M1 selective muscarinic agonists. 2. Synthesis and structure-activity relationships of 3-pyrazinyl-1,2,5,6-tetrahydro-1-methylpyridines. Construction of a molecular model for the M1 pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.57 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130715 | — | — | 1 | 8.62 |
| CHEMBL327754 | — | — | 1 | 8.40 |
| CHEMBL131819 | TAZOMELINE | 2.0 | 1 | 8.30 |
| CHEMBL101054 | — | — | 1 | 8.30 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.15 |
| CHEMBL327289 | — | — | 1 | 7.92 |
| CHEMBL130807 | — | — | 1 | 7.57 |
| CHEMBL99476 | — | — | 1 | 7.32 |
| CHEMBL120399 | — | — | 1 | 7.14 |
| CHEMBL305401 | — | — | 1 | 6.83 |
| CHEMBL307645 | — | — | 1 | 6.43 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 5.89 |
| CHEMBL131840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130715 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL327754 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL131819 | TAZOMELINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL101054 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL327289 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL130807 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL99476 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL120399 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL305401 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL307645 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL131840 | — | IC50 | > | 1000.0 | nM | - |