Assay Detail
Functional
CHEMBL1248513
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells 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 | 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 |
|---|---|---|---|
| EC50 | 4 | 6.18 | 7.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1242923 | — | — | 1 | 7.01 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | 6.85 |
| CHEMBL1242950 | — | — | 1 | 6.30 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 4.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1242923 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1242950 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL667 | ACETYLCHOLINE | EC50 | = | 27000.0 | nM | 4.57 |