Assay Detail
Binding
CHEMBL752914
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity against muscarinic acetylcholine receptor M1 from rat hippocampus, using [3H]oxotremorine-M (Oxo-M) 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 | 7.96 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308772 | — | — | 1 | 9.05 |
| CHEMBL420007 | — | — | 1 | 8.85 |
| CHEMBL308803 | — | — | 1 | 8.80 |
| CHEMBL306941 | — | — | 1 | 8.77 |
| CHEMBL74358 | — | — | 1 | 8.72 |
| CHEMBL75552 | — | — | 1 | 8.70 |
| CHEMBL74301 | — | — | 1 | 8.70 |
| CHEMBL308608 | — | — | 1 | 8.64 |
| CHEMBL73338 | — | — | 1 | 8.52 |
| CHEMBL442369 | — | — | 1 | 8.24 |
| CHEMBL76161 | — | — | 1 | 8.21 |
| CHEMBL306395 | — | — | 1 | 8.15 |
| CHEMBL76107 | — | — | 1 | 8.10 |
| CHEMBL73149 | — | — | 1 | 8.01 |
| CHEMBL308744 | — | — | 1 | 8.00 |
| CHEMBL307645 | — | — | 1 | 7.97 |
| CHEMBL72430 | — | — | 1 | 7.89 |
| CHEMBL72908 | — | — | 1 | 7.66 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.64 |
| CHEMBL75907 | — | — | 1 | 7.62 |
| CHEMBL75704 | — | — | 1 | 7.54 |
| CHEMBL72384 | — | — | 1 | 7.52 |
| CHEMBL308168 | — | — | 1 | 7.22 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 7.11 |
| CHEMBL74786 | — | — | 1 | 7.08 |
| CHEMBL76296 | — | — | 1 | 6.96 |
| CHEMBL307837 | — | — | 1 | 6.73 |
| CHEMBL74300 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308772 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL420007 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL308803 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL306941 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL74358 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL75552 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL74301 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL308608 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL73338 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL442369 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL76161 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL306395 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL76107 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL73149 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL308744 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL307645 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL72430 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL72908 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL14 | CARBACHOL | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL75907 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL75704 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL72384 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL308168 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL74786 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL76296 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL307837 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL74300 | — | IC50 | = | 355.0 | nM | 6.45 |