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Assay Detail

CHEMBL877277

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

Binding
In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological studies of N-[4-[2-hydroxy-3-[[2-[4-(1H-imidazol-1- yl)phenoxy]ethyl]amino]propoxy]phenyl]methanesulfonamide, a novel antiarrhythmic agent with class II and class III activities.
Morgan TK, Lis R, Lumma WC, Wohl RA, Nickisch K, Phillips GB, Lind JM, Lampe JW, Di Meo SV, Reiser HJ.
J Med Chem (1990) 33 : 1087 -1090
PubMed 2319556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.18 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL545363 1 5.77
CHEMBL552615 1 5.62
CHEMBL536800 1 5.58
CHEMBL11629 1 5.55
CHEMBL471 SOTALOL 4.0 1 5.05
CHEMBL11944 1 4.75
CHEMBL542544 1 4.68
CHEMBL543251 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL545363 IC50 = 1700.0 nM 5.77
CHEMBL552615 IC50 = 2400.0 nM 5.62
CHEMBL536800 IC50 = 2600.0 nM 5.58
CHEMBL11629 IC50 = 2800.0 nM 5.55
CHEMBL471 SOTALOL IC50 = 9000.0 nM 5.05
CHEMBL11944 IC50 = 18000.0 nM 4.75
CHEMBL542544 IC50 = 21000.0 nM 4.68
CHEMBL543251 IC50 = 38000.0 nM 4.42