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Assay Detail

CHEMBL744041

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

Binding
Compound was evaluated for blocking activity on Muscarinic acetylcholine receptor in guinea pig atria
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL2094109)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Differential blockade of muscarinic receptor subtypes by polymethylene tetraamines. Novel class of selective antagonists of cardiac M-2 muscarinic receptors.
Melchiorre C, Cassinelli A, Quaglia W.
J Med Chem (1987) 30 : 201 -204
PubMed 3806594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 7.79 8.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 8.69
CHEMBL500996 METHOCTRAMINE HYDROCHLORIDE 1 8.13
CHEMBL1202789 1 7.96
CHEMBL1202787 1 7.80
CHEMBL1202786 1 7.71
CHEMBL541116 1 7.35
CHEMBL1204259 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Kd = 2.042 nM 8.69
CHEMBL500996 METHOCTRAMINE HYDROCHLORIDE Kd = 7.413 nM 8.13
CHEMBL1202789 Kd = 10.96 nM 7.96
CHEMBL1202787 Kd = 15.85 nM 7.80
CHEMBL1202786 Kd = 19.5 nM 7.71
CHEMBL541116 Kd = 44.67 nM 7.35
CHEMBL1204259 Kd = 134.9 nM 6.87