Assay Detail
Functional
CHEMBL746418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | Fibroblast |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 7.09 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293982 | — | — | 1 | 8.60 |
| CHEMBL418491 | — | — | 1 | 8.35 |
| CHEMBL64029 | — | — | 1 | 8.12 |
| CHEMBL303360 | — | — | 1 | 8.05 |
| CHEMBL60833 | — | — | 1 | 7.98 |
| CHEMBL291872 | — | — | 1 | 7.70 |
| CHEMBL60331 | — | — | 1 | 7.34 |
| CHEMBL417560 | — | — | 1 | 7.21 |
| CHEMBL294082 | — | — | 1 | 7.15 |
| CHEMBL60419 | — | — | 1 | 7.15 |
| CHEMBL60374 | — | — | 1 | 6.97 |
| CHEMBL60777 | — | — | 1 | 6.96 |
| CHEMBL291351 | — | — | 1 | 6.96 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 6.87 |
| CHEMBL59862 | — | — | 1 | 5.92 |
| CHEMBL60479 | — | — | 1 | 5.74 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.34 |
| CHEMBL81878 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293982 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL418491 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL64029 | — | EC50 | = | 7.6 | nM | 8.12 |
| CHEMBL303360 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL60833 | — | EC50 | = | 10.5 | nM | 7.98 |
| CHEMBL291872 | — | EC50 | = | 20.2 | nM | 7.70 |
| CHEMBL60331 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL417560 | — | EC50 | = | 61.9 | nM | 7.21 |
| CHEMBL294082 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL60419 | — | EC50 | = | 70.5 | nM | 7.15 |
| CHEMBL60374 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL60777 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL291351 | — | EC50 | = | 110.9 | nM | 6.96 |
| CHEMBL21536 | XANOMELINE | EC50 | = | 134.5 | nM | 6.87 |
| CHEMBL59862 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL60479 | — | EC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL14 | CARBACHOL | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL81878 | — | EC50 | = | 7121.0 | nM | 5.15 |