Assay Detail
Functional
CHEMBL4605230
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 7.91 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4636528 | — | — | 1 | 8.39 |
| CHEMBL4640703 | — | — | 1 | 8.16 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.60 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4636528 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4640703 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL14 | CARBACHOL | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1346 | DARIFENACIN | EC50 | = | 32.0 | nM | 7.50 |