Assay Detail
Binding
CHEMBL1248511
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BHK-21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M5 (CHEMBL2035) ↗| 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 |
|---|---|---|---|
| Ki | 6 | 6.64 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 9.00 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | 7.29 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 7.10 |
| CHEMBL522460 | — | — | 1 | 6.03 |
| CHEMBL1242950 | — | — | 1 | 5.35 |
| CHEMBL1242923 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL21536 | XANOMELINE | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL522460 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL1242950 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL1242923 | — | Ki | = | 8900.0 | nM | 5.05 |