Assay Detail
Functional
CHEMBL1248359
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | BHK-21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.28 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.21 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 8.00 |
| CHEMBL1242979 | — | — | 1 | 6.52 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21536 | XANOMELINE | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL667 | ACETYLCHOLINE | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1242979 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | EC50 | = | 400.0 | nM | 6.40 |