Assay Detail
Binding
CHEMBL3383644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M3 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 | 7.18 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354068 | — | — | 1 | 9.10 |
| CHEMBL3354069 | — | — | 1 | 8.96 |
| CHEMBL143469 | — | — | 1 | 8.54 |
| CHEMBL3354067 | — | — | 1 | 8.33 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.11 |
| CHEMBL3354070 | — | — | 1 | 8.00 |
| CHEMBL3354071 | — | — | 1 | 7.35 |
| CHEMBL3354078 | — | — | 1 | 7.24 |
| CHEMBL3354066 | — | — | 1 | 7.03 |
| CHEMBL3354075 | — | — | 1 | 6.70 |
| CHEMBL3354077 | — | — | 1 | 6.47 |
| CHEMBL3354076 | — | — | 1 | 6.24 |
| CHEMBL3354074 | — | — | 1 | 6.20 |
| CHEMBL3354065 | — | — | 1 | 5.92 |
| CHEMBL3354073 | — | — | 1 | 5.72 |
| CHEMBL3354072 | — | — | 1 | 4.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354068 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL3354069 | — | Ki | = | 1.096 | nM | 8.96 |
| CHEMBL143469 | — | Ki | = | 2.884 | nM | 8.54 |
| CHEMBL3354067 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL21536 | XANOMELINE | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL3354070 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3354071 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL3354078 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL3354066 | — | Ki | = | 93.33 | nM | 7.03 |
| CHEMBL3354075 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL3354077 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL3354076 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL3354074 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL3354065 | — | Ki | = | 1202.26 | nM | 5.92 |
| CHEMBL3354073 | — | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL3354072 | — | Ki | = | 11748.98 | nM | 4.93 |