Assay Detail
Binding
CHEMBL3383643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M2 receptor expressed in CHO cells by microplate scintillation counting based radioligand binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.19 | 8.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354068 | — | — | 1 | 8.86 |
| CHEMBL3354069 | — | — | 1 | 8.77 |
| CHEMBL143469 | — | — | 1 | 8.50 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.09 |
| CHEMBL3354067 | — | — | 1 | 7.96 |
| CHEMBL3354066 | — | — | 1 | 7.18 |
| CHEMBL3354078 | — | — | 1 | 7.10 |
| CHEMBL3354071 | — | — | 1 | 7.07 |
| CHEMBL3354070 | — | — | 1 | 7.05 |
| CHEMBL3354065 | — | — | 1 | 6.69 |
| CHEMBL3354074 | — | — | 1 | 6.68 |
| CHEMBL3354075 | — | — | 1 | 6.67 |
| CHEMBL3354076 | — | — | 1 | 6.38 |
| CHEMBL3354077 | — | — | 1 | 6.32 |
| CHEMBL3354073 | — | — | 1 | 6.22 |
| CHEMBL3354072 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354068 | — | Ki | = | 1.38 | nM | 8.86 |
| CHEMBL3354069 | — | Ki | = | 1.698 | nM | 8.77 |
| CHEMBL143469 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL21536 | XANOMELINE | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL3354067 | — | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL3354066 | — | Ki | = | 66.07 | nM | 7.18 |
| CHEMBL3354078 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL3354071 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL3354070 | — | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL3354065 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL3354074 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL3354075 | — | Ki | = | 213.8 | nM | 6.67 |
| CHEMBL3354076 | — | Ki | = | 416.87 | nM | 6.38 |
| CHEMBL3354077 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL3354073 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL3354072 | — | Ki | = | 3235.94 | nM | 5.49 |