Assay Detail
Binding
CHEMBL751533
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In vitro binding affinity against muscarinic acetylcholine receptor M1 from rat hippocampus, using [3H]pirenzepine (Pz) as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Hippocampus |
| Confidence | 8 — Homologous 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. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines .
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.36 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306941 | — | — | 1 | 8.89 |
| CHEMBL308772 | — | — | 1 | 8.40 |
| CHEMBL75552 | — | — | 1 | 8.40 |
| CHEMBL420007 | — | — | 1 | 8.30 |
| CHEMBL306395 | — | — | 1 | 8.16 |
| CHEMBL73149 | — | — | 1 | 8.15 |
| CHEMBL308744 | — | — | 1 | 8.08 |
| CHEMBL72430 | — | — | 1 | 8.05 |
| CHEMBL76107 | — | — | 1 | 8.01 |
| CHEMBL73338 | — | — | 1 | 7.92 |
| CHEMBL76161 | — | — | 1 | 7.92 |
| CHEMBL74358 | — | — | 1 | 7.75 |
| CHEMBL308803 | — | — | 1 | 7.75 |
| CHEMBL72384 | — | — | 1 | 7.40 |
| CHEMBL308608 | — | — | 1 | 7.37 |
| CHEMBL442369 | — | — | 1 | 7.32 |
| CHEMBL75704 | — | — | 1 | 7.21 |
| CHEMBL307837 | — | — | 1 | 7.14 |
| CHEMBL308168 | — | — | 1 | 6.98 |
| CHEMBL74301 | — | — | 1 | 6.84 |
| CHEMBL72908 | — | — | 1 | 6.83 |
| CHEMBL74786 | — | — | 1 | 6.56 |
| CHEMBL75907 | — | — | 1 | 6.46 |
| CHEMBL307645 | — | — | 1 | 6.43 |
| CHEMBL76296 | — | — | 1 | 6.07 |
| CHEMBL74300 | — | — | 1 | 6.02 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 5.89 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306941 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL308772 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL75552 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL420007 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL306395 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL73149 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL308744 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL72430 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL76107 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL73338 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL76161 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL74358 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL308803 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL72384 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL308608 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL442369 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL75704 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL307837 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL308168 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL74301 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL72908 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL74786 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL75907 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL307645 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL76296 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL74300 | — | IC50 | = | 955.0 | nM | 6.02 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL14 | CARBACHOL | IC50 | = | 1380.0 | nM | 5.86 |