Assay Detail
Binding
CHEMBL881234
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Binding affinity for rat heart muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate
22
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M2 (CHEMBL309) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 22 | 6.94 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL194628 | — | — | 1 | 8.17 |
| CHEMBL1169543 | — | — | 1 | 8.06 |
| CHEMBL371293 | — | — | 2 | 7.89 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 7.85 |
| CHEMBL606903 | — | — | 1 | 7.82 |
| CHEMBL372983 | — | — | 2 | 7.66 |
| CHEMBL439867 | — | — | 1 | 7.55 |
| CHEMBL198065 | — | — | 2 | 7.12 |
| CHEMBL606904 | — | — | 1 | 6.96 |
| CHEMBL1734 | SOLIFENACIN | 4.0 | 1 | 6.92 |
| CHEMBL196481 | — | — | 1 | 6.85 |
| CHEMBL198669 | — | — | 1 | 6.36 |
| CHEMBL197588 | — | — | 2 | 6.32 |
| CHEMBL606963 | — | — | 1 | 6.07 |
| CHEMBL606901 | — | — | 1 | 5.80 |
| CHEMBL606962 | — | — | 1 | 5.77 |
| CHEMBL606902 | — | — | 1 | 5.46 |
| CHEMBL197717 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL194628 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL1169543 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL371293 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL606903 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL372983 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL439867 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL372983 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL198065 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL371293 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL606904 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1734 | SOLIFENACIN | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL196481 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL198669 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL197588 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL606963 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL606901 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL606962 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL197588 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL606902 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL197717 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL198065 | — | Ki | > | 1000.0 | nM | - |