Assay Detail
Binding
CHEMBL3383642
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M1 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 | 7.38 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354068 | — | — | 1 | 9.04 |
| CHEMBL3354069 | — | — | 1 | 8.99 |
| CHEMBL143469 | — | — | 1 | 8.78 |
| CHEMBL3354067 | — | — | 1 | 8.17 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.10 |
| CHEMBL3354070 | — | — | 1 | 7.96 |
| CHEMBL3354078 | — | — | 1 | 7.53 |
| CHEMBL3354071 | — | — | 1 | 7.35 |
| CHEMBL3354066 | — | — | 1 | 7.11 |
| CHEMBL3354076 | — | — | 1 | 6.91 |
| CHEMBL3354077 | — | — | 1 | 6.73 |
| CHEMBL3354075 | — | — | 1 | 6.55 |
| CHEMBL3354065 | — | — | 1 | 6.50 |
| CHEMBL3354074 | — | — | 1 | 6.45 |
| CHEMBL3354073 | — | — | 1 | 6.33 |
| CHEMBL3354072 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354068 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL3354069 | — | Ki | = | 1.023 | nM | 8.99 |
| CHEMBL143469 | — | Ki | = | 1.66 | nM | 8.78 |
| CHEMBL3354067 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL21536 | XANOMELINE | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL3354070 | — | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL3354078 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL3354071 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL3354066 | — | Ki | = | 77.62 | nM | 7.11 |
| CHEMBL3354076 | — | Ki | = | 123.03 | nM | 6.91 |
| CHEMBL3354077 | — | Ki | = | 186.21 | nM | 6.73 |
| CHEMBL3354075 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL3354065 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL3354074 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL3354073 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL3354072 | — | Ki | = | 2511.89 | nM | 5.60 |