Assay Detail
Binding
CHEMBL749006
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Binding affinity of [3H]QNB to CHO cells expressing human Muscarinic acetylcholine receptor M2
24
Total Activities
24
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 |
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 | 4.87 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL312823 | — | — | 1 | 6.29 |
| CHEMBL86903 | — | — | 1 | 5.72 |
| CHEMBL83074 | — | — | 1 | 5.66 |
| CHEMBL85264 | — | — | 1 | 5.40 |
| CHEMBL315676 | — | — | 1 | 5.22 |
| CHEMBL87622 | — | — | 1 | 5.22 |
| CHEMBL84726 | — | — | 1 | 5.10 |
| CHEMBL313918 | — | — | 1 | 5.09 |
| CHEMBL85936 | — | — | 1 | 5.05 |
| CHEMBL87485 | — | — | 1 | 4.97 |
| CHEMBL85645 | — | — | 1 | 4.82 |
| CHEMBL85678 | — | — | 1 | 4.78 |
| CHEMBL81895 | — | — | 1 | 4.69 |
| CHEMBL313749 | — | — | 1 | 4.68 |
| CHEMBL420781 | — | — | 1 | 4.61 |
| CHEMBL84893 | — | — | 1 | 4.59 |
| CHEMBL314420 | — | — | 1 | 4.57 |
| CHEMBL86288 | — | — | 1 | 4.41 |
| CHEMBL86197 | — | — | 1 | 4.33 |
| CHEMBL85460 | — | — | 1 | 4.32 |
| CHEMBL81878 | — | — | 1 | 4.28 |
| CHEMBL86150 | — | — | 1 | 4.16 |
| CHEMBL84919 | — | — | 1 | 4.07 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL312823 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL86903 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL83074 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL85264 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL315676 | — | IC50 | = | 6030.0 | nM | 5.22 |
| CHEMBL87622 | — | IC50 | = | 6010.0 | nM | 5.22 |
| CHEMBL84726 | — | IC50 | = | 7930.0 | nM | 5.10 |
| CHEMBL313918 | — | IC50 | = | 8070.0 | nM | 5.09 |
| CHEMBL85936 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL87485 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL85645 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL85678 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL81895 | — | IC50 | = | 20600.0 | nM | 4.69 |
| CHEMBL313749 | — | IC50 | = | 20800.0 | nM | 4.68 |
| CHEMBL420781 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL84893 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL314420 | — | IC50 | = | 27200.0 | nM | 4.57 |
| CHEMBL86288 | — | IC50 | = | 38600.0 | nM | 4.41 |
| CHEMBL86197 | — | IC50 | = | 46600.0 | nM | 4.33 |
| CHEMBL85460 | — | IC50 | = | 47900.0 | nM | 4.32 |
| CHEMBL81878 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL86150 | — | IC50 | = | 69300.0 | nM | 4.16 |
| CHEMBL84919 | — | IC50 | = | 84400.0 | nM | 4.07 |
| CHEMBL14 | CARBACHOL | IC50 | = | 119000.0 | nM | - |