Assay Detail
Binding
CHEMBL752315
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In vitro Binding affinity was measured on Muscarinic acetylcholine receptor on rat brain membranes using [3H]oxotremorine-M
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.77 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15944 | — | — | 1 | 8.35 |
| CHEMBL275673 | — | — | 1 | 8.12 |
| CHEMBL15675 | — | — | 1 | 7.56 |
| CHEMBL15956 | — | — | 1 | 7.45 |
| CHEMBL15936 | — | — | 1 | 7.35 |
| CHEMBL279105 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15944 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL275673 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL15675 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL15956 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL15936 | — | IC50 | = | 44.5 | nM | 7.35 |
| CHEMBL279105 | — | IC50 | > | 500.0 | nM | - |