Assay Detail
Binding
CHEMBL744147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Muscarinic acetylcholine receptor binding assay was conducted using [3H]cis-methyldioxolane (CMD) to label agonist sites in membrane preparations from rat neocortex
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.68 | 8.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL86903 | — | — | 1 | 8.99 |
| CHEMBL315676 | — | — | 1 | 8.46 |
| CHEMBL87622 | — | — | 1 | 8.37 |
| CHEMBL82378 | — | — | 1 | 8.15 |
| CHEMBL83074 | — | — | 1 | 8.10 |
| CHEMBL84726 | — | — | 1 | 7.91 |
| CHEMBL85264 | — | — | 1 | 7.91 |
| CHEMBL85936 | — | — | 1 | 7.87 |
| CHEMBL85645 | — | — | 1 | 7.78 |
| CHEMBL85678 | — | — | 1 | 7.74 |
| CHEMBL81895 | — | — | 1 | 7.72 |
| CHEMBL313918 | — | — | 1 | 7.66 |
| CHEMBL81878 | — | — | 1 | 7.56 |
| CHEMBL313749 | — | — | 1 | 7.56 |
| CHEMBL86197 | — | — | 1 | 7.55 |
| CHEMBL314420 | — | — | 1 | 7.53 |
| CHEMBL312823 | — | — | 1 | 7.46 |
| CHEMBL85460 | — | — | 1 | 7.43 |
| CHEMBL84893 | — | — | 1 | 7.33 |
| CHEMBL420781 | — | — | 1 | 7.28 |
| CHEMBL87485 | — | — | 1 | 7.28 |
| CHEMBL86288 | — | — | 1 | 7.05 |
| CHEMBL84919 | — | — | 1 | 6.96 |
| CHEMBL86150 | — | — | 1 | 6.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL86903 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL315676 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL87622 | — | IC50 | = | 4.29 | nM | 8.37 |
| CHEMBL82378 | — | IC50 | = | 7.08 | nM | 8.15 |
| CHEMBL83074 | — | IC50 | = | 8.04 | nM | 8.10 |
| CHEMBL84726 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL85264 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL85936 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL85645 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL85678 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL81895 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL313918 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL81878 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL313749 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL86197 | — | IC50 | = | 28.2 | nM | 7.55 |
| CHEMBL314420 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL312823 | — | IC50 | = | 34.7 | nM | 7.46 |
| CHEMBL85460 | — | IC50 | = | 37.2 | nM | 7.43 |
| CHEMBL84893 | — | IC50 | = | 46.4 | nM | 7.33 |
| CHEMBL420781 | — | IC50 | = | 53.1 | nM | 7.28 |
| CHEMBL87485 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL86288 | — | IC50 | = | 88.9 | nM | 7.05 |
| CHEMBL84919 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL86150 | — | IC50 | = | 218.0 | nM | 6.66 |