Assay Detail
Functional
CHEMBL4605232
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Antagonist activity at human muscarinic M3 receptor expressed in HEK293 assessed as inhibition of carbachol-induced IP1 accumulation preincubated for 30 mins followed by carbachol addition and measured after 90 mins by TR-HTRF assay
8
Total Activities
8
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 | 8 | 7.92 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | 4.0 | 1 | 8.24 |
| CHEMBL4647437 | — | — | 1 | 8.20 |
| CHEMBL4633816 | — | — | 1 | 8.17 |
| CHEMBL4636528 | — | — | 1 | 8.03 |
| CHEMBL4640703 | — | — | 1 | 7.85 |
| CHEMBL4648071 | — | — | 1 | 7.77 |
| CHEMBL4640324 | — | — | 1 | 7.72 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545181 | TIOTROPIUM BROMIDE | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4647437 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4633816 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4636528 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4640703 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4648071 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4640324 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1346 | DARIFENACIN | EC50 | = | 45.0 | nM | 7.35 |