Assay Detail
Binding
CHEMBL3383645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]NMS from human M4 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 M4 (CHEMBL1821) ↗| 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 | 7.55 | 9.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143469 | — | — | 1 | 9.11 |
| CHEMBL3354068 | — | — | 1 | 9.05 |
| CHEMBL3354069 | — | — | 1 | 8.97 |
| CHEMBL3354070 | — | — | 1 | 8.18 |
| CHEMBL3354067 | — | — | 1 | 8.10 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.95 |
| CHEMBL3354071 | — | — | 1 | 7.84 |
| CHEMBL3354066 | — | — | 1 | 7.58 |
| CHEMBL3354078 | — | — | 1 | 7.49 |
| CHEMBL3354077 | — | — | 1 | 7.02 |
| CHEMBL3354076 | — | — | 1 | 6.95 |
| CHEMBL3354075 | — | — | 1 | 6.81 |
| CHEMBL3354065 | — | — | 1 | 6.68 |
| CHEMBL3354074 | — | — | 1 | 6.41 |
| CHEMBL3354073 | — | — | 1 | 6.35 |
| CHEMBL3354072 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143469 | — | Ki | = | 0.7762 | nM | 9.11 |
| CHEMBL3354068 | — | Ki | = | 0.8913 | nM | 9.05 |
| CHEMBL3354069 | — | Ki | = | 1.072 | nM | 8.97 |
| CHEMBL3354070 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL3354067 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL21536 | XANOMELINE | Ki | = | 11.22 | nM | 7.95 |
| CHEMBL3354071 | — | Ki | = | 14.45 | nM | 7.84 |
| CHEMBL3354066 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL3354078 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL3354077 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL3354076 | — | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL3354075 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL3354065 | — | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL3354074 | — | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL3354073 | — | Ki | = | 446.68 | nM | 6.35 |
| CHEMBL3354072 | — | Ki | = | 588.84 | nM | 6.23 |