Assay Detail
Binding
CHEMBL747450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-OXO-M (oxotremorine-M) from the central muscarinic receptor sites of the rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTP
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.10 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL101054 | — | — | 1 | 8.85 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.01 |
| CHEMBL75907 | — | — | 1 | 7.62 |
| CHEMBL74786 | — | — | 1 | 7.16 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 7.11 |
| CHEMBL74300 | — | — | 1 | 6.45 |
| CHEMBL355465 | — | — | 1 | 6.32 |
| CHEMBL353779 | — | — | 1 | 6.26 |
| CHEMBL167375 | — | — | 1 | 6.12 |
| CHEMBL168581 | — | — | 1 | - |
| CHEMBL166115 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL101054 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL75907 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL74786 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL74300 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL355465 | — | IC50 | = | 477.0 | nM | 6.32 |
| CHEMBL353779 | — | IC50 | = | 544.0 | nM | 6.26 |
| CHEMBL167375 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL168581 | — | IC50 | > | 900.0 | nM | - |
| CHEMBL166115 | — | IC50 | > | 900.0 | nM | - |