Assay Detail
Functional
CHEMBL744227
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonistic activity against M1 muscarinic receptor expressed in A9 L cells.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | A9L |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.33 | 8.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL335542 | — | — | 1 | 8.07 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.24 |
| CHEMBL140746 | — | — | 1 | 7.10 |
| CHEMBL336933 | — | — | 1 | 6.92 |
| CHEMBL140985 | — | — | 1 | 6.75 |
| CHEMBL142538 | — | — | 1 | 6.47 |
| CHEMBL337131 | — | — | 1 | 6.46 |
| CHEMBL343055 | — | — | 1 | 6.36 |
| CHEMBL142184 | — | — | 1 | 6.24 |
| CHEMBL341759 | — | — | 1 | 6.23 |
| CHEMBL143469 | — | — | 1 | 6.14 |
| CHEMBL140789 | — | — | 1 | 6.04 |
| CHEMBL143466 | — | — | 1 | 5.82 |
| CHEMBL143434 | — | — | 1 | 5.68 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 4.89 |
| CHEMBL139603 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL335542 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL21536 | XANOMELINE | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL140746 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL336933 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL140985 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL142538 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL337131 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL343055 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL142184 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL341759 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL143469 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL140789 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL143466 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL143434 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL14 | CARBACHOL | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL139603 | — | EC50 | = | 13000.0 | nM | 4.89 |