Assay Detail
Binding
CHEMBL1909171
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DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.21 | 9.38 |
| Ki | 871 | 6.66 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | 4.0 | 2 | 9.82 |
| CHEMBL517712 | ATROPINE | 4.0 | 2 | 8.88 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 8.44 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | — | 2 | 8.03 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 2 | 8.02 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 7.92 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 7.92 |
| CHEMBL1490 | TRIHEXYPHENIDYL | 4.0 | 2 | 7.92 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 2 | 7.80 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | -1.0 | 2 | 7.72 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 7.54 |
| CHEMBL1200604 | TROPICAMIDE | 4.0 | 2 | 7.43 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 2 | 7.42 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 7.42 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | — | 2 | 7.39 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | -1.0 | 2 | 7.12 |
| CHEMBL58 | MITOXANTRONE | 4.0 | 2 | 7.11 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 7.07 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 7.04 |
| CHEMBL1200623 | ETHYLESTRENOL | 4.0 | 2 | 6.98 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 6.91 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 2 | 6.87 |
| CHEMBL1200406 | DIMENHYDRINATE | 4.0 | 2 | 6.79 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 6.77 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 6.72 |
| CHEMBL395110 | MEPAZINE | 4.0 | 2 | 6.70 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 6.69 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 6.63 |
| CHEMBL936 | DIPHENIDOL | 4.0 | 2 | 6.56 |
| CHEMBL305660 | EBASTINE | 4.0 | 2 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | IC50 | = | 0.422 | nM | 9.38 |
| CHEMBL517712 | ATROPINE | Ki | = | 1.328 | nM | 8.88 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 3.668 | nM | 8.44 |
| CHEMBL517712 | ATROPINE | IC50 | = | 3.735 | nM | 8.43 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | Ki | = | 9.339 | nM | 8.03 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 9.612 | nM | 8.02 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1490 | TRIHEXYPHENIDYL | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1123 | DICYCLOMINE | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1231 | OXYBUTYNIN | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL1490 | TRIHEXYPHENIDYL | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1200604 | TROPICAMIDE | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1172 | DESLORATADINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL1123 | DICYCLOMINE | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL58 | MITOXANTRONE | Ki | = | 77.9 | nM | 7.11 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL1200604 | TROPICAMIDE | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL1200623 | ETHYLESTRENOL | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL1172 | DESLORATADINE | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL900 | ORPHENADRINE | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL1200406 | DIMENHYDRINATE | Ki | = | 164.0 | nM | 6.79 |
| CHEMBL42 | CLOZAPINE | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL490 | PAROXETINE | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL395110 | MEPAZINE | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL58 | MITOXANTRONE | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL936 | DIPHENIDOL | Ki | = | 274.0 | nM | 6.56 |
| CHEMBL305660 | EBASTINE | Ki | = | 279.5 | nM | 6.55 |
| CHEMBL1200623 | ETHYLESTRENOL | IC50 | = | 292.0 | nM | 6.54 |