Assay Detail
Functional
CHEMBL2343487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Partial agonist activity at human M4 receptor co-expressed with Galpha16 in CHO cells assessed as calcium mobilization after 60 mins by FLIPR assay
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Intrinsic activity | 4 | - | - |
| EC50 | 4 | 7.53 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134641 | SABCOMELINE | 2.0 | 2 | 8.24 |
| CHEMBL2336056 | — | — | 2 | 7.82 |
| CHEMBL2336059 | — | — | 2 | 7.54 |
| CHEMBL2336057 | — | — | 2 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134641 | SABCOMELINE | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL2336056 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2336059 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2336057 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL134641 | SABCOMELINE | Intrinsic activity | = | 28.0 | % | - |
| CHEMBL2336059 | — | Intrinsic activity | = | 42.0 | % | - |
| CHEMBL2336057 | — | Intrinsic activity | = | 45.0 | % | - |
| CHEMBL2336056 | — | Intrinsic activity | = | 65.0 | % | - |