Assay Detail
Functional
CHEMBL1248351
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
36
Total Activities
36
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 | 36 | 7.22 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 8.96 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.80 |
| CHEMBL522460 | — | — | 1 | 8.19 |
| CHEMBL1243357 | — | — | 1 | 8.05 |
| CHEMBL1242925 | — | — | 1 | 8.00 |
| CHEMBL1242979 | — | — | 1 | 7.89 |
| CHEMBL1242951 | — | — | 1 | 7.82 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | — | 1 | 7.75 |
| CHEMBL1243328 | — | — | 1 | 7.72 |
| CHEMBL1243358 | — | — | 1 | 7.70 |
| CHEMBL1243387 | — | — | 1 | 7.70 |
| CHEMBL1243232 | — | — | 1 | 7.57 |
| CHEMBL1243233 | — | — | 1 | 7.34 |
| CHEMBL1243110 | — | — | 1 | 7.32 |
| CHEMBL1243043 | — | — | 1 | 7.31 |
| CHEMBL1243044 | — | — | 1 | 7.29 |
| CHEMBL1242923 | — | — | 1 | 7.21 |
| CHEMBL1242924 | — | — | 1 | 7.07 |
| CHEMBL1243138 | — | — | 1 | 7.00 |
| CHEMBL1243267 | — | — | 1 | 6.96 |
| CHEMBL1243109 | — | — | 1 | 6.92 |
| CHEMBL1243010 | — | — | 1 | 6.89 |
| CHEMBL1242950 | — | — | 1 | 6.82 |
| CHEMBL1243011 | — | — | 1 | 6.82 |
| CHEMBL1243295 | — | — | 1 | 6.80 |
| CHEMBL1243202 | — | — | 1 | 6.75 |
| CHEMBL1243074 | — | — | 1 | 6.54 |
| CHEMBL1243386 | — | — | 1 | 6.51 |
| CHEMBL1243296 | — | — | 1 | 6.46 |
| CHEMBL1243075 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL667 | ACETYLCHOLINE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL21536 | XANOMELINE | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL522460 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1243357 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1242925 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1242979 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1242951 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL845 | N-DESMETHYLCLOZAPINE | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1243328 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1243387 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1243358 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1243232 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1243233 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1243110 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL1243043 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1243044 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1242923 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1242924 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1243138 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1243267 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1243109 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1243010 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1242950 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1243011 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1243295 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1243202 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1243074 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1243386 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL1243296 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1243075 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL1243168 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL1243201 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL1243139 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1243266 | — | EC50 | - | — | - | |
| CHEMBL1243327 | — | EC50 | - | — | - | |
| CHEMBL1243169 | — | EC50 | - | — | - |