Assay Detail
Binding
CHEMBL1909174
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DRUGMATRIX: Muscarinic M5 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 M5 (CHEMBL2035) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DrugMatrix in vitro pharmacology data
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 871 | 6.78 | 9.49 |
| IC50 | 871 | 6.64 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | 4.0 | 2 | 9.49 |
| CHEMBL517712 | ATROPINE | 4.0 | 2 | 9.18 |
| CHEMBL1201203 | BENZTROPINE | 4.0 | 2 | 8.84 |
| CHEMBL1123 | DICYCLOMINE | 4.0 | 2 | 8.77 |
| CHEMBL1231 | OXYBUTYNIN | 4.0 | 2 | 8.63 |
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 2 | 8.56 |
| CHEMBL643 | PROMETHAZINE | 4.0 | 2 | 8.48 |
| CHEMBL629 | AMITRIPTYLINE | 4.0 | 2 | 8.24 |
| CHEMBL1626 | CLEMASTINE | 4.0 | 2 | 8.22 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 2 | 8.18 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | — | 2 | 8.14 |
| CHEMBL1490 | TRIHEXYPHENIDYL | 4.0 | 2 | 8.06 |
| CHEMBL42 | CLOZAPINE | 4.0 | 2 | 8.02 |
| CHEMBL71 | CHLORPROMAZINE | 4.0 | 2 | 7.75 |
| CHEMBL1628227 | DOXEPIN | 4.0 | 2 | 7.72 |
| CHEMBL900 | ORPHENADRINE | 4.0 | 2 | 7.70 |
| CHEMBL445 | NORTRIPTYLINE | 4.0 | 2 | 7.70 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | -1.0 | 2 | 7.62 |
| CHEMBL395110 | MEPAZINE | 4.0 | 2 | 7.55 |
| CHEMBL715 | OLANZAPINE | 4.0 | 2 | 7.54 |
| CHEMBL415 | CLOMIPRAMINE | 4.0 | 2 | 7.42 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | -1.0 | 2 | 7.41 |
| CHEMBL564 | PROMAZINE | 4.0 | 2 | 7.34 |
| CHEMBL1200604 | TROPICAMIDE | 4.0 | 2 | 7.19 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | — | 2 | 7.11 |
| CHEMBL490 | PAROXETINE | 4.0 | 2 | 7.05 |
| CHEMBL221753 | BENZETHONIUM CHLORIDE | 2.0 | 2 | 7.02 |
| CHEMBL657 | DIPHENHYDRAMINE | 4.0 | 2 | 6.94 |
| CHEMBL21731 | MAPROTILINE | 4.0 | 2 | 6.94 |
| CHEMBL728 | PROCHLORPERAZINE | 4.0 | 2 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL1354199 | METHSCOPOLAMINE BROMIDE | IC50 | = | 0.446 | nM | 9.35 |
| CHEMBL517712 | ATROPINE | Ki | = | 0.662 | nM | 9.18 |
| CHEMBL517712 | ATROPINE | IC50 | = | 0.922 | nM | 9.04 |
| CHEMBL1201203 | BENZTROPINE | Ki | = | 1.451 | nM | 8.84 |
| CHEMBL1123 | DICYCLOMINE | Ki | = | 1.711 | nM | 8.77 |
| CHEMBL1201203 | BENZTROPINE | IC50 | = | 2.019 | nM | 8.70 |
| CHEMBL1231 | OXYBUTYNIN | Ki | = | 2.315 | nM | 8.63 |
| CHEMBL1123 | DICYCLOMINE | IC50 | = | 2.382 | nM | 8.62 |
| CHEMBL516 | CYPROHEPTADINE | Ki | = | 2.755 | nM | 8.56 |
| CHEMBL1231 | OXYBUTYNIN | IC50 | = | 3.222 | nM | 8.49 |
| CHEMBL643 | PROMETHAZINE | Ki | = | 3.307 | nM | 8.48 |
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 3.835 | nM | 8.42 |
| CHEMBL643 | PROMETHAZINE | IC50 | = | 4.603 | nM | 8.34 |
| CHEMBL629 | AMITRIPTYLINE | Ki | = | 5.762 | nM | 8.24 |
| CHEMBL1626 | CLEMASTINE | Ki | = | 6.016 | nM | 8.22 |
| CHEMBL479 | THIORIDAZINE | Ki | = | 6.643 | nM | 8.18 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | Ki | = | 7.277 | nM | 8.14 |
| CHEMBL629 | AMITRIPTYLINE | IC50 | = | 8.02 | nM | 8.10 |
| CHEMBL1626 | CLEMASTINE | IC50 | = | 8.373 | nM | 8.08 |
| CHEMBL1490 | TRIHEXYPHENIDYL | Ki | = | 8.679 | nM | 8.06 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 9.246 | nM | 8.03 |
| CHEMBL42 | CLOZAPINE | Ki | = | 9.532 | nM | 8.02 |
| CHEMBL334255 | CETYLPYRIDINIUM BROMIDE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1490 | TRIHEXYPHENIDYL | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL42 | CLOZAPINE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL71 | CHLORPROMAZINE | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1628227 | DOXEPIN | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL445 | NORTRIPTYLINE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL900 | ORPHENADRINE | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1628227 | DOXEPIN | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL445 | NORTRIPTYLINE | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL395110 | MEPAZINE | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL900 | ORPHENADRINE | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL715 | OLANZAPINE | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL2107687 | VALETHAMATE BROMIDE | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL415 | CLOMIPRAMINE | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL715 | OLANZAPINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL395110 | MEPAZINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL564 | PROMAZINE | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL415 | CLOMIPRAMINE | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1319362 | HOMATROPINE HYDROBROMIDE | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1200604 | TROPICAMIDE | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL564 | PROMAZINE | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1909073 | PIPERILATE ETHOBROMIDE | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL1200604 | TROPICAMIDE | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL490 | PAROXETINE | Ki | = | 89.0 | nM | 7.05 |