Assay Detail
Binding
CHEMBL751540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity towards Muscarinic acetylcholine receptor M1 by the displacement of [3H]pirenzepine in rat cerebral cortical membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure activity relationships of alkyl substituted analogues of the functional M1 selective muscarinic receptor agonist xanomeline
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.49 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414874 | — | — | 1 | 8.30 |
| CHEMBL69317 | — | — | 1 | 8.30 |
| CHEMBL68160 | — | — | 1 | 8.30 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.15 |
| CHEMBL70051 | — | — | 1 | 8.15 |
| CHEMBL70670 | — | — | 1 | 8.10 |
| CHEMBL71536 | — | — | 1 | 8.10 |
| CHEMBL305412 | — | — | 1 | 7.82 |
| CHEMBL303922 | — | — | 1 | 7.75 |
| CHEMBL303599 | — | — | 1 | 7.62 |
| CHEMBL68482 | — | — | 1 | 7.32 |
| CHEMBL70160 | — | — | 1 | 6.95 |
| CHEMBL305401 | — | — | 1 | 6.83 |
| CHEMBL302515 | — | — | 1 | 6.24 |
| CHEMBL303732 | — | — | 1 | 6.00 |
| CHEMBL71380 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414874 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL69317 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL68160 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL70051 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL70670 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL71536 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL305412 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL303922 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL303599 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL68482 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL70160 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL305401 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL302515 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL303732 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL71380 | — | IC50 | = | 1230.0 | nM | 5.91 |