Assay Detail
Functional
CHEMBL749229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity against M4 muscarinic receptor expressed in RBL-2H3 Mast cells.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | RBL-2H3 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.61 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143434 | — | — | 1 | 9.22 |
| CHEMBL139603 | — | — | 1 | 9.00 |
| CHEMBL142538 | — | — | 1 | 8.85 |
| CHEMBL143466 | — | — | 1 | 8.33 |
| CHEMBL335542 | — | — | 1 | 8.28 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 6.54 |
| CHEMBL143468 | — | — | 1 | 5.96 |
| CHEMBL143469 | — | — | 1 | 4.70 |
| CHEMBL336478 | — | — | 1 | - |
| CHEMBL142126 | — | — | 1 | - |
| CHEMBL141452 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143434 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL139603 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL142538 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL143466 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL335542 | — | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL14 | CARBACHOL | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL143468 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL143469 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL336478 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL142126 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL141452 | — | EC50 | > | 100000.0 | nM | - |