Assay Detail
Binding
CHEMBL751535
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In vitro binding affinity against rat hippocampus M1 receptor using [3H]pirenzepine (Pz) as radioligand
10
Total Activities
10
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 | 10 | 7.25 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL132278 | — | — | 1 | 8.00 |
| CHEMBL335976 | — | — | 1 | 7.80 |
| CHEMBL117903 | — | — | 1 | 7.77 |
| CHEMBL128401 | — | — | 1 | 7.77 |
| CHEMBL131587 | — | — | 1 | 7.55 |
| CHEMBL132272 | — | — | 1 | 7.19 |
| CHEMBL308168 | — | — | 1 | 6.98 |
| CHEMBL336793 | — | — | 1 | 6.76 |
| CHEMBL74786 | — | — | 1 | 6.56 |
| CHEMBL132331 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL132278 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL335976 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL117903 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL128401 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL131587 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL132272 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL308168 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL336793 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL74786 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL132331 | — | IC50 | = | 840.0 | nM | 6.08 |