Assay Detail
Binding
CHEMBL872390
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for rat cortex muscarinic acetylcholine receptor M1 using [3H]pirenzepine
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 M1 (CHEMBL276) ↗| 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 | 8.09 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1169543 | — | — | 1 | 9.49 |
| CHEMBL606903 | — | — | 1 | 9.02 |
| CHEMBL439867 | — | — | 1 | 8.85 |
| CHEMBL194628 | — | — | 1 | 8.82 |
| CHEMBL371293 | — | — | 2 | 8.74 |
| CHEMBL197588 | — | — | 2 | 8.51 |
| CHEMBL198065 | — | — | 2 | 8.41 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 1 | 8.23 |
| CHEMBL372983 | — | — | 2 | 8.18 |
| CHEMBL606904 | — | — | 1 | 8.08 |
| CHEMBL198669 | — | — | 1 | 8.08 |
| CHEMBL196481 | — | — | 1 | 8.03 |
| CHEMBL1734 | SOLIFENACIN | 4.0 | 1 | 8.00 |
| CHEMBL606962 | — | — | 1 | 7.96 |
| CHEMBL606963 | — | — | 1 | 7.39 |
| CHEMBL197717 | — | — | 1 | 7.28 |
| CHEMBL606902 | — | — | 1 | 6.64 |
| CHEMBL606901 | — | — | 1 | 6.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1169543 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL606903 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL439867 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL194628 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL371293 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL371293 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL197588 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL198065 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL372983 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL198669 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL606904 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL196481 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL1734 | SOLIFENACIN | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL606962 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL372983 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL198065 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL197588 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL606963 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL197717 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL606902 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL606901 | — | Ki | = | 440.0 | nM | 6.36 |