Assay Detail
Binding
CHEMBL1248508
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 6.74 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | 4.0 | 1 | 8.72 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 6.92 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | 6.60 |
| CHEMBL522460 | — | — | 1 | 6.50 |
| CHEMBL1242950 | — | — | 1 | 6.01 |
| CHEMBL1242923 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517712 | ATROPINE | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL21536 | XANOMELINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL522460 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL1242950 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL1242923 | — | Ki | = | 2200.0 | nM | 5.66 |