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Assay Detail

CHEMBL1909172

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

Binding
DRUGMATRIX: Muscarinic M3 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 M3 (CHEMBL245)
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 6.33 8.95
Ki 871 7.00 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1354199 METHSCOPOLAMINE BROMIDE 4.0 2 9.62
CHEMBL1201203 BENZTROPINE 4.0 2 9.56
CHEMBL517712 ATROPINE 4.0 2 9.36
CHEMBL1231 OXYBUTYNIN 4.0 2 9.24
CHEMBL1123 DICYCLOMINE 4.0 2 9.03
CHEMBL1490 TRIHEXYPHENIDYL 4.0 2 8.50
CHEMBL643 PROMETHAZINE 4.0 2 8.38
CHEMBL629 AMITRIPTYLINE 4.0 2 8.27
CHEMBL2107687 VALETHAMATE BROMIDE -1.0 2 8.25
CHEMBL334255 CETYLPYRIDINIUM BROMIDE 2 8.14
CHEMBL1626 CLEMASTINE 4.0 2 8.08
CHEMBL516 CYPROHEPTADINE 4.0 2 8.02
CHEMBL1628227 DOXEPIN 4.0 2 7.82
CHEMBL1319362 HOMATROPINE HYDROBROMIDE -1.0 2 7.80
CHEMBL42 CLOZAPINE 4.0 2 7.77
CHEMBL479 THIORIDAZINE 4.0 2 7.72
CHEMBL1200604 TROPICAMIDE 4.0 2 7.52
CHEMBL1909073 PIPERILATE ETHOBROMIDE 2 7.48
CHEMBL415 CLOMIPRAMINE 4.0 2 7.44
CHEMBL445 NORTRIPTYLINE 4.0 2 7.44
CHEMBL900 ORPHENADRINE 4.0 2 7.43
CHEMBL490 PAROXETINE 4.0 2 7.42
CHEMBL395110 MEPAZINE 4.0 2 7.40
CHEMBL71 CHLORPROMAZINE 4.0 2 7.36
CHEMBL936 DIPHENIDOL 4.0 2 7.28
CHEMBL221753 BENZETHONIUM CHLORIDE 2.0 2 7.09
CHEMBL715 OLANZAPINE 4.0 2 7.08
CHEMBL564 PROMAZINE 4.0 2 7.06
CHEMBL1172 DESLORATADINE 4.0 2 7.02
CHEMBL1200406 DIMENHYDRINATE 4.0 2 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1354199 METHSCOPOLAMINE BROMIDE Ki = 0.239 nM 9.62
CHEMBL1201203 BENZTROPINE Ki = 0.272 nM 9.56
CHEMBL517712 ATROPINE Ki = 0.439 nM 9.36
CHEMBL1231 OXYBUTYNIN Ki = 0.574 nM 9.24
CHEMBL1123 DICYCLOMINE Ki = 0.927 nM 9.03
CHEMBL1354199 METHSCOPOLAMINE BROMIDE IC50 = 1.129 nM 8.95
CHEMBL1201203 BENZTROPINE IC50 = 1.285 nM 8.89
CHEMBL517712 ATROPINE IC50 = 2.071 nM 8.68
CHEMBL1231 OXYBUTYNIN IC50 = 2.71 nM 8.57
CHEMBL1490 TRIHEXYPHENIDYL Ki = 3.151 nM 8.50
CHEMBL643 PROMETHAZINE Ki = 4.149 nM 8.38
CHEMBL1123 DICYCLOMINE IC50 = 4.375 nM 8.36
CHEMBL629 AMITRIPTYLINE Ki = 5.436 nM 8.27
CHEMBL2107687 VALETHAMATE BROMIDE Ki = 5.585 nM 8.25
CHEMBL334255 CETYLPYRIDINIUM BROMIDE Ki = 7.297 nM 8.14
CHEMBL1626 CLEMASTINE Ki = 8.253 nM 8.08
CHEMBL516 CYPROHEPTADINE Ki = 9.655 nM 8.02
CHEMBL1628227 DOXEPIN Ki = 15.0 nM 7.82
CHEMBL1490 TRIHEXYPHENIDYL IC50 = 15.0 nM 7.82
CHEMBL1319362 HOMATROPINE HYDROBROMIDE Ki = 16.0 nM 7.80
CHEMBL42 CLOZAPINE Ki = 17.0 nM 7.77
CHEMBL479 THIORIDAZINE Ki = 19.0 nM 7.72
CHEMBL643 PROMETHAZINE IC50 = 20.0 nM 7.70
CHEMBL629 AMITRIPTYLINE IC50 = 26.0 nM 7.58
CHEMBL2107687 VALETHAMATE BROMIDE IC50 = 26.0 nM 7.58
CHEMBL1200604 TROPICAMIDE Ki = 30.0 nM 7.52
CHEMBL1909073 PIPERILATE ETHOBROMIDE Ki = 33.0 nM 7.48
CHEMBL334255 CETYLPYRIDINIUM BROMIDE IC50 = 34.0 nM 7.47
CHEMBL445 NORTRIPTYLINE Ki = 36.0 nM 7.44
CHEMBL415 CLOMIPRAMINE Ki = 36.0 nM 7.44
CHEMBL900 ORPHENADRINE Ki = 37.0 nM 7.43
CHEMBL490 PAROXETINE Ki = 38.0 nM 7.42
CHEMBL1626 CLEMASTINE IC50 = 39.0 nM 7.41
CHEMBL395110 MEPAZINE Ki = 40.0 nM 7.40
CHEMBL71 CHLORPROMAZINE Ki = 44.0 nM 7.36
CHEMBL516 CYPROHEPTADINE IC50 = 46.0 nM 7.34
CHEMBL936 DIPHENIDOL Ki = 52.0 nM 7.28
CHEMBL1628227 DOXEPIN IC50 = 69.0 nM 7.16
CHEMBL1319362 HOMATROPINE HYDROBROMIDE IC50 = 76.0 nM 7.12
CHEMBL42 CLOZAPINE IC50 = 78.0 nM 7.11
CHEMBL221753 BENZETHONIUM CHLORIDE Ki = 81.0 nM 7.09
CHEMBL715 OLANZAPINE Ki = 83.0 nM 7.08
CHEMBL564 PROMAZINE Ki = 88.0 nM 7.06
CHEMBL479 THIORIDAZINE IC50 = 90.0 nM 7.05
CHEMBL1200406 DIMENHYDRINATE Ki = 95.0 nM 7.02
CHEMBL1172 DESLORATADINE Ki = 95.0 nM 7.02
CHEMBL21731 MAPROTILINE Ki = 100.0 nM 7.00
CHEMBL657 DIPHENHYDRAMINE Ki = 137.0 nM 6.86
CHEMBL305660 EBASTINE Ki = 137.2 nM 6.86
CHEMBL1200604 TROPICAMIDE IC50 = 142.0 nM 6.85