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Assay Detail

CHEMBL1909171

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

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