Assay Detail
Binding
CHEMBL744770
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards M1 muscarinic receptor expressed in A9 L cells by displacing [3H](R)-QNB radioligand.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | L929 |
| 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 |
|---|---|---|---|
| Ki | 21 | 8.59 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL335542 | — | — | 1 | 9.92 |
| CHEMBL141452 | — | — | 1 | 9.72 |
| CHEMBL143468 | — | — | 1 | 9.64 |
| CHEMBL143434 | — | — | 1 | 9.49 |
| CHEMBL143466 | — | — | 1 | 9.24 |
| CHEMBL142126 | — | — | 1 | 9.21 |
| CHEMBL139603 | — | — | 1 | 9.16 |
| CHEMBL143469 | — | — | 1 | 9.08 |
| CHEMBL341759 | — | — | 1 | 9.06 |
| CHEMBL142184 | — | — | 1 | 9.03 |
| CHEMBL337131 | — | — | 1 | 8.92 |
| CHEMBL140142 | — | — | 1 | 8.82 |
| CHEMBL142538 | — | — | 1 | 8.80 |
| CHEMBL139887 | — | — | 1 | 8.72 |
| CHEMBL140789 | — | — | 1 | 8.30 |
| CHEMBL140985 | — | — | 1 | 8.12 |
| CHEMBL140746 | — | — | 1 | 7.85 |
| CHEMBL336933 | — | — | 1 | 7.77 |
| CHEMBL343055 | — | — | 1 | 7.70 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.09 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL335542 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL141452 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL143468 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL143434 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL143466 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL142126 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL139603 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL143469 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL341759 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL142184 | — | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL337131 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL140142 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL142538 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL139887 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL140789 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL140985 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL140746 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL336933 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL343055 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL21536 | XANOMELINE | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL14 | CARBACHOL | Ki | = | 20000.0 | nM | 4.70 |