Assay Detail
Binding
CHEMBL746455
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Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 5.48 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 8.19 |
| CHEMBL279453 | — | — | 1 | 8.00 |
| CHEMBL277642 | HIMBACINE | — | 1 | 7.96 |
| CHEMBL22108 | DIMETHINDENE | 3.0 | 1 | 6.39 |
| CHEMBL21321 | — | — | 1 | 5.91 |
| CHEMBL21716 | — | — | 1 | 5.77 |
| CHEMBL278074 | — | — | 1 | 5.74 |
| CHEMBL21509 | — | — | 1 | 4.92 |
| CHEMBL20732 | — | — | 1 | 4.91 |
| CHEMBL280684 | — | — | 1 | 4.90 |
| CHEMBL278129 | — | — | 1 | 4.83 |
| CHEMBL279520 | — | — | 1 | 4.67 |
| CHEMBL21508 | — | — | 1 | 4.65 |
| CHEMBL283320 | — | — | 1 | 4.61 |
| CHEMBL21937 | — | — | 1 | 4.47 |
| CHEMBL279225 | — | — | 1 | 4.33 |
| CHEMBL21328 | — | — | 1 | 4.26 |
| CHEMBL424214 | — | — | 1 | 4.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL279453 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL277642 | HIMBACINE | Ki | = | 10.96 | nM | 7.96 |
| CHEMBL22108 | DIMETHINDENE | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL21321 | — | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL21716 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL278074 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL21509 | — | Ki | = | 12022.64 | nM | 4.92 |
| CHEMBL20732 | — | Ki | = | 12302.69 | nM | 4.91 |
| CHEMBL280684 | — | Ki | = | 12589.25 | nM | 4.90 |
| CHEMBL278129 | — | Ki | = | 14791.08 | nM | 4.83 |
| CHEMBL279520 | — | Ki | = | 21379.62 | nM | 4.67 |
| CHEMBL21508 | — | Ki | = | 22387.21 | nM | 4.65 |
| CHEMBL283320 | — | Ki | = | 24547.09 | nM | 4.61 |
| CHEMBL21937 | — | Ki | = | 33884.42 | nM | 4.47 |
| CHEMBL279225 | — | Ki | = | 46773.51 | nM | 4.33 |
| CHEMBL21328 | — | Ki | = | 54954.09 | nM | 4.26 |
| CHEMBL424214 | — | Ki | = | 89125.09 | nM | 4.05 |