Assay Detail
Binding
CHEMBL748269
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for Muscarinic acetylcholine receptor M5 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 M5 (CHEMBL2035) ↗| 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 | 5.15 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | — | 1 | 7.47 |
| CHEMBL277642 | HIMBACINE | — | 1 | 6.31 |
| CHEMBL279453 | — | — | 1 | 6.27 |
| CHEMBL22108 | DIMETHINDENE | 3.0 | 1 | 6.10 |
| CHEMBL21716 | — | — | 1 | 6.01 |
| CHEMBL278074 | — | — | 1 | 5.98 |
| CHEMBL21321 | — | — | 1 | 5.91 |
| CHEMBL20732 | — | — | 1 | 4.75 |
| CHEMBL21509 | — | — | 1 | 4.72 |
| CHEMBL21508 | — | — | 1 | 4.57 |
| CHEMBL278129 | — | — | 1 | 4.57 |
| CHEMBL280684 | — | — | 1 | 4.52 |
| CHEMBL279225 | — | — | 1 | 4.28 |
| CHEMBL21328 | — | — | 1 | 4.27 |
| CHEMBL283320 | — | — | 1 | 4.27 |
| CHEMBL424214 | — | — | 1 | 4.26 |
| CHEMBL21937 | — | — | 1 | 4.26 |
| CHEMBL279520 | — | — | 1 | 4.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL265256 | TRIPITRAMINE | Ki | = | 33.88 | nM | 7.47 |
| CHEMBL277642 | HIMBACINE | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL279453 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL22108 | DIMETHINDENE | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL21716 | — | Ki | = | 977.24 | nM | 6.01 |
| CHEMBL278074 | — | Ki | = | 1047.13 | nM | 5.98 |
| CHEMBL21321 | — | Ki | = | 1230.27 | nM | 5.91 |
| CHEMBL20732 | — | Ki | = | 17782.79 | nM | 4.75 |
| CHEMBL21509 | — | Ki | = | 19054.61 | nM | 4.72 |
| CHEMBL21508 | — | Ki | = | 26915.35 | nM | 4.57 |
| CHEMBL278129 | — | Ki | = | 26915.35 | nM | 4.57 |
| CHEMBL280684 | — | Ki | = | 30199.52 | nM | 4.52 |
| CHEMBL279225 | — | Ki | = | 52480.75 | nM | 4.28 |
| CHEMBL21328 | — | Ki | = | 53703.18 | nM | 4.27 |
| CHEMBL283320 | — | Ki | = | 53703.18 | nM | 4.27 |
| CHEMBL424214 | — | Ki | = | 54954.09 | nM | 4.26 |
| CHEMBL21937 | — | Ki | = | 54954.09 | nM | 4.26 |
| CHEMBL279520 | — | Ki | = | 66069.34 | nM | 4.18 |