Assay Detail
Binding
CHEMBL853693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H](R)-QNB binding to human M2 receptor expressed in A9 L cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A9L |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the binding and activity at muscarinic receptor subtypes and chimeras.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.37 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL386983 | — | — | 1 | 8.60 |
| CHEMBL216927 | — | — | 1 | 8.10 |
| CHEMBL216928 | — | — | 1 | 7.40 |
| CHEMBL218755 | — | — | 1 | 7.40 |
| CHEMBL373888 | — | — | 1 | 7.40 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.30 |
| CHEMBL219118 | — | — | 1 | 7.20 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.00 |
| CHEMBL376295 | — | — | 1 | 6.80 |
| CHEMBL216983 | — | — | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL386983 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL216927 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL216928 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL218755 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL373888 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL21536 | XANOMELINE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL219118 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL14 | CARBACHOL | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL376295 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL216983 | — | Ki | = | 316.23 | nM | 6.50 |