Assay Detail
Binding
CHEMBL4605227
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor transiently expressed in HEK293T cell membranes incubated for 1 hr by scintillation counting method
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| 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 |
|---|---|---|---|
| Ki | 31 | 8.88 | 10.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4636528 | — | — | 1 | 10.16 |
| CHEMBL4633816 | — | — | 1 | 10.15 |
| CHEMBL4647437 | — | — | 1 | 10.14 |
| CHEMBL4640703 | — | — | 1 | 10.08 |
| CHEMBL4644192 | — | — | 1 | 9.77 |
| CHEMBL4639307 | — | — | 1 | 9.64 |
| CHEMBL4649201 | — | — | 1 | 9.60 |
| CHEMBL4645543 | — | — | 1 | 9.47 |
| CHEMBL4640324 | — | — | 1 | 9.46 |
| CHEMBL4644670 | — | — | 1 | 9.44 |
| CHEMBL4648071 | — | — | 1 | 9.41 |
| CHEMBL4636302 | — | — | 1 | 9.33 |
| CHEMBL4643867 | — | — | 1 | 9.28 |
| CHEMBL4644852 | — | — | 1 | 9.20 |
| CHEMBL4639938 | — | — | 1 | 9.19 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 9.13 |
| CHEMBL4640544 | — | — | 1 | 9.05 |
| CHEMBL4648196 | — | — | 1 | 9.00 |
| CHEMBL4643643 | — | — | 1 | 8.96 |
| CHEMBL4644999 | — | — | 1 | 8.82 |
| CHEMBL4645235 | — | — | 1 | 8.77 |
| CHEMBL4632615 | — | — | 1 | 8.64 |
| CHEMBL4636887 | — | — | 1 | 8.57 |
| CHEMBL4637155 | — | — | 1 | 8.18 |
| CHEMBL4633165 | — | — | 1 | 8.15 |
| CHEMBL4635566 | — | — | 1 | 7.96 |
| CHEMBL4632545 | — | — | 1 | 7.85 |
| CHEMBL4637749 | — | — | 1 | 7.72 |
| CHEMBL4646717 | — | — | 1 | 7.52 |
| CHEMBL4641288 | — | — | 1 | 7.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4636528 | — | Ki | = | 0.069 | nM | 10.16 |
| CHEMBL4633816 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4647437 | — | Ki | = | 0.072 | nM | 10.14 |
| CHEMBL4640703 | — | Ki | = | 0.084 | nM | 10.08 |
| CHEMBL4644192 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL4639307 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL4649201 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL4645543 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL4640324 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL4644670 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL4648071 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL4636302 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL4643867 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL4644852 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL4639938 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL1346 | DARIFENACIN | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL4640544 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL4648196 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4643643 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4644999 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4645235 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4632615 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4636887 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4637155 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4633165 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4635566 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4632545 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4637749 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4646717 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4641288 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL4636009 | — | Ki | = | 2000.0 | nM | 5.70 |