Assay Detail
Functional
CHEMBL4306810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulatory activity at human Muscarinic acetylcholine receptor M4 expressed in HEK cells co-expressing Glosensor construct assessed as as increase in acteylcholine-induced cAMP accumulation incubated for 7 mins in presence of isoproterenol/acetylcholine by Glosensor cAMP reagent/plate reader based luminescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.93 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.22 |
| CHEMBL7634 | OXOTREMORINE | — | 1 | 8.05 |
| CHEMBL4455058 | — | — | 1 | 7.60 |
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 7.24 |
| CHEMBL4449608 | — | — | 1 | 5.47 |
| CHEMBL4446144 | — | — | 1 | 5.00 |
| CHEMBL4584879 | — | — | 1 | - |
| CHEMBL4436552 | — | — | 1 | - |
| CHEMBL4448257 | — | — | 1 | - |
| CHEMBL4567275 | — | — | 1 | - |
| CHEMBL4576299 | — | — | 1 | - |
| CHEMBL4447576 | — | — | 1 | - |
| CHEMBL4559190 | — | — | 1 | - |
| CHEMBL4593680 | — | — | 1 | - |
| CHEMBL4449297 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL21536 | XANOMELINE | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL7634 | OXOTREMORINE | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4455058 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL667 | ACETYLCHOLINE | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4449608 | — | EC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL4446144 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4584879 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4436552 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4448257 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4567275 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4576299 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4447576 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4559190 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4593680 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4449297 | — | EC50 | > | 10000.0 | nM | - |