Assay Detail
Binding
CHEMBL3383646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M5 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 |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.98 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354068 | — | — | 1 | 8.64 |
| CHEMBL3354069 | — | — | 1 | 8.53 |
| CHEMBL143469 | — | — | 1 | 8.40 |
| CHEMBL3354067 | — | — | 1 | 8.25 |
| CHEMBL3354070 | — | — | 1 | 8.06 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.03 |
| CHEMBL3354071 | — | — | 1 | 7.51 |
| CHEMBL3354078 | — | — | 1 | 7.31 |
| CHEMBL3354066 | — | — | 1 | 6.99 |
| CHEMBL3354077 | — | — | 1 | 6.47 |
| CHEMBL3354076 | — | — | 1 | 6.46 |
| CHEMBL3354075 | — | — | 1 | 6.07 |
| CHEMBL3354074 | — | — | 1 | 5.51 |
| CHEMBL3354073 | — | — | 1 | 5.34 |
| CHEMBL3354065 | — | — | 1 | 5.27 |
| CHEMBL3354072 | — | — | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354068 | — | Ki | = | 2.291 | nM | 8.64 |
| CHEMBL3354069 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL143469 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL3354067 | — | Ki | = | 5.623 | nM | 8.25 |
| CHEMBL3354070 | — | Ki | = | 8.71 | nM | 8.06 |
| CHEMBL21536 | XANOMELINE | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL3354071 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL3354078 | — | Ki | = | 48.98 | nM | 7.31 |
| CHEMBL3354066 | — | Ki | = | 102.33 | nM | 6.99 |
| CHEMBL3354077 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL3354076 | — | Ki | = | 346.74 | nM | 6.46 |
| CHEMBL3354075 | — | Ki | = | 851.14 | nM | 6.07 |
| CHEMBL3354074 | — | Ki | = | 3090.3 | nM | 5.51 |
| CHEMBL3354073 | — | Ki | = | 4570.88 | nM | 5.34 |
| CHEMBL3354065 | — | Ki | = | 5370.32 | nM | 5.27 |
| CHEMBL3354072 | — | Ki | = | 14454.4 | nM | 4.84 |