Assay Detail
ADMET
CHEMBL4605226
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]N-methylscopolamine from human muscarinic M2 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 | ADMET |
| 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 | 7.33 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4644192 | — | — | 1 | 8.77 |
| CHEMBL4644670 | — | — | 1 | 8.70 |
| CHEMBL4647437 | — | — | 1 | 8.48 |
| CHEMBL4636528 | — | — | 1 | 8.47 |
| CHEMBL4633816 | — | — | 1 | 8.43 |
| CHEMBL4640703 | — | — | 1 | 8.24 |
| CHEMBL1346 | DARIFENACIN | 4.0 | 1 | 7.92 |
| CHEMBL4643867 | — | — | 1 | 7.89 |
| CHEMBL4639307 | — | — | 1 | 7.85 |
| CHEMBL4640324 | — | — | 1 | 7.85 |
| CHEMBL4649201 | — | — | 1 | 7.77 |
| CHEMBL4636302 | — | — | 1 | 7.77 |
| CHEMBL4640544 | — | — | 1 | 7.55 |
| CHEMBL4643643 | — | — | 1 | 7.52 |
| CHEMBL4648071 | — | — | 1 | 7.51 |
| CHEMBL4645543 | — | — | 1 | 7.51 |
| CHEMBL4645235 | — | — | 1 | 7.41 |
| CHEMBL4639938 | — | — | 1 | 7.33 |
| CHEMBL4644852 | — | — | 1 | 7.28 |
| CHEMBL4644999 | — | — | 1 | 7.16 |
| CHEMBL4636887 | — | — | 1 | 7.09 |
| CHEMBL4648196 | — | — | 1 | 7.01 |
| CHEMBL4635566 | — | — | 1 | 6.92 |
| CHEMBL4632615 | — | — | 1 | 6.89 |
| CHEMBL4632545 | — | — | 1 | 6.50 |
| CHEMBL4633165 | — | — | 1 | 6.47 |
| CHEMBL4637749 | — | — | 1 | 6.43 |
| CHEMBL4637155 | — | — | 1 | 6.28 |
| CHEMBL4646717 | — | — | 1 | 6.01 |
| CHEMBL4641288 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4644192 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4644670 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4647437 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4636528 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4633816 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL4640703 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL1346 | DARIFENACIN | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4643867 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4639307 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4640324 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4649201 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4636302 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4640544 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4643643 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4648071 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4645543 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4645235 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4639938 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL4644852 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4644999 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4636887 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL4648196 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4635566 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4632615 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4632545 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL4633165 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4637749 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL4637155 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL4646717 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL4641288 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL4636009 | — | Ki | = | 28000.0 | nM | 4.55 |