Assay Detail
Binding
CHEMBL1909173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Muscarinic M4 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 |
Target
Muscarinic acetylcholine receptor M4 (CHEMBL1821) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 871 | 6.47 | 9.15 |
| Ki | 871 | 7.32 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | 4.0 | 2 | 10.01 |
| CHEMBL517712 | ATROPINE | 4.0 | 2 | 9.98 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 2 | 9.56 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 9.48 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 2 | 9.39 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 9.13 |
| CHEMBL1490 | TRIHEXYPHENIDYL | 4.0 | 2 | 9.12 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 8.98 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 8.66 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 8.56 |
| CHEMBL1200604 | TROPICAMIDE | 4.0 | 2 | 8.46 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | -1.0 | 2 | 8.44 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 8.23 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 8.20 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | — | 2 | 8.07 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 7.96 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 7.89 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 7.89 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | -1.0 | 2 | 7.85 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | — | 2 | 7.82 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 2 | 7.77 |
| CHEMBL395110 | MEPAZINE | 4.0 | 2 | 7.72 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 7.68 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 7.66 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 7.47 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 7.44 |
| CHEMBL936 | DIPHENIDOL | 4.0 | 2 | 7.42 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 7.38 |
| CHEMBL1172 | DESLORATADINE | 4.0 | 2 | 7.33 |
| CHEMBL657 | DIPHENHYDRAMINE | 4.0 | 2 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | Ki | = | 0.098 | nM | 10.01 |
| CHEMBL517712 | ATROPINE | Ki | = | 0.104 | nM | 9.98 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 0.278 | nM | 9.56 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 0.333 | nM | 9.48 |
| CHEMBL1123 | DICYCLOMINE | Ki | = | 0.411 | nM | 9.39 |
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | IC50 | = | 0.706 | nM | 9.15 |
| CHEMBL517712 | ATROPINE | IC50 | = | 0.744 | nM | 9.13 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 0.739 | nM | 9.13 |
| CHEMBL1490 | TRIHEXYPHENIDYL | Ki | = | 0.764 | nM | 9.12 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 1.057 | nM | 8.98 |
| CHEMBL1231 | OXYBUTYNIN | IC50 | = | 1.994 | nM | 8.70 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 2.186 | nM | 8.66 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 2.385 | nM | 8.62 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 2.773 | nM | 8.56 |
| CHEMBL1123 | DICYCLOMINE | IC50 | = | 2.947 | nM | 8.53 |
| CHEMBL1200604 | TROPICAMIDE | Ki | = | 3.483 | nM | 8.46 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | Ki | = | 3.669 | nM | 8.44 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 5.297 | nM | 8.28 |
| CHEMBL1490 | TRIHEXYPHENIDYL | IC50 | = | 5.478 | nM | 8.26 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 5.842 | nM | 8.23 |
| CHEMBL42 | CLOZAPINE | Ki | = | 6.303 | nM | 8.20 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 7.576 | nM | 8.12 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | Ki | = | 8.584 | nM | 8.07 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL900 | ORPHENADRINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL395110 | MEPAZINE | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL715 | OLANZAPINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1200604 | TROPICAMIDE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL490 | PAROXETINE | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL936 | DIPHENIDOL | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL564 | PROMAZINE | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1172 | DESLORATADINE | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL657 | DIPHENHYDRAMINE | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL21731 | MAPROTILINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1200406 | DIMENHYDRINATE | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL58 | MITOXANTRONE | Ki | = | 89.8 | nM | 7.05 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 91.0 | nM | 7.04 |