Assay Detail
Binding
CHEMBL746566
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Muscarinic acetylcholine receptor binding assay was conducted using [3H]quinuclidinyl benzilate (QNB) to label antagonist sites in membrane preparations from rat neocortex
25
Total Activities
25
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 | 25 | 5.32 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL86903 | — | — | 1 | 6.09 |
| CHEMBL83074 | — | — | 1 | 6.02 |
| CHEMBL82378 | — | — | 1 | 5.90 |
| CHEMBL85264 | — | — | 1 | 5.89 |
| CHEMBL84726 | — | — | 1 | 5.80 |
| CHEMBL87622 | — | — | 1 | 5.69 |
| CHEMBL85936 | — | — | 1 | 5.63 |
| CHEMBL85645 | — | — | 1 | 5.57 |
| CHEMBL81895 | — | — | 1 | 5.41 |
| CHEMBL315676 | — | — | 1 | 5.36 |
| CHEMBL313749 | — | — | 1 | 5.35 |
| CHEMBL87485 | — | — | 1 | 5.32 |
| CHEMBL85460 | — | — | 1 | 5.31 |
| CHEMBL84893 | — | — | 1 | 5.30 |
| CHEMBL314420 | — | — | 1 | 5.21 |
| CHEMBL420781 | — | — | 1 | 5.20 |
| CHEMBL86197 | — | — | 1 | 5.19 |
| CHEMBL81878 | — | — | 1 | 5.16 |
| CHEMBL313918 | — | — | 1 | 5.05 |
| CHEMBL86288 | — | — | 1 | 4.96 |
| CHEMBL84919 | — | — | 1 | 4.88 |
| CHEMBL312823 | — | — | 1 | 4.86 |
| CHEMBL86150 | — | — | 1 | 4.75 |
| CHEMBL85678 | — | — | 1 | 4.62 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL86903 | — | IC50 | = | 806.0 | nM | 6.09 |
| CHEMBL83074 | — | IC50 | = | 958.0 | nM | 6.02 |
| CHEMBL82378 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL85264 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL84726 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL87622 | — | IC50 | = | 2060.0 | nM | 5.69 |
| CHEMBL85936 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL85645 | — | IC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL81895 | — | IC50 | = | 3880.0 | nM | 5.41 |
| CHEMBL315676 | — | IC50 | = | 4350.0 | nM | 5.36 |
| CHEMBL313749 | — | IC50 | = | 4440.0 | nM | 5.35 |
| CHEMBL87485 | — | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL85460 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL84893 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL314420 | — | IC50 | = | 6090.0 | nM | 5.21 |
| CHEMBL420781 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL86197 | — | IC50 | = | 6390.0 | nM | 5.19 |
| CHEMBL81878 | — | IC50 | = | 6920.0 | nM | 5.16 |
| CHEMBL313918 | — | IC50 | = | 8834.0 | nM | 5.05 |
| CHEMBL86288 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL84919 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL312823 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL86150 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL85678 | — | IC50 | = | 24200.0 | nM | 4.62 |
| CHEMBL14 | CARBACHOL | IC50 | = | 33000.0 | nM | 4.48 |