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Assay Detail

CHEMBL650688

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

Binding
Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs
11
Total Activities
10
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 Expert

Target

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

Publication

Synthesis of novel (aryloxy)propanolamines and related compounds possessing both class II and class III antiarrhythmic activity.
Lis R, Morgan TK, Marisca AJ, Gomez RP, Lind JM, Davey DD, Phillips GB, Sullivan ME.
J Med Chem (1990) 33 : 2883 -2891
PubMed 1976812 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.47 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 7.75
CHEMBL98773 1 6.10
CHEMBL1193886 ERSENTILIDE 2.0 2 5.80
CHEMBL95966 1 5.62
CHEMBL95754 1 5.48
CHEMBL95727 1 5.14
CHEMBL471 SOTALOL 4.0 1 5.05
CHEMBL99331 1 4.72
CHEMBL100624 1 4.48
CHEMBL1192069 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL IC50 = 18.0 nM 7.75
CHEMBL98773 IC50 = 800.0 nM 6.10
CHEMBL1193886 ERSENTILIDE IC50 = 1600.0 nM 5.80
CHEMBL95966 IC50 = 2400.0 nM 5.62
CHEMBL1193886 ERSENTILIDE IC50 = 2400.0 nM 5.62
CHEMBL95754 IC50 = 3300.0 nM 5.48
CHEMBL95727 IC50 = 7300.0 nM 5.14
CHEMBL471 SOTALOL IC50 = 8900.0 nM 5.05
CHEMBL99331 IC50 = 19200.0 nM 4.72
CHEMBL100624 IC50 = 33100.0 nM 4.48
CHEMBL1192069 IC50 = 37500.0 nM 4.43