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Assay Detail

CHEMBL667337

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

Functional
Tested for beta-receptor binding inhibition from canine ventricular tissue, using [3H]dihydroalprenolol as the radioligand in anesthetized dogs
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Tissue Cardiac ventricle
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor beta (CHEMBL2094118)
Type PROTEIN FAMILY
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 6 6.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98975 1 7.40
CHEMBL421005 1 7.05
CHEMBL95457 1 6.57
CHEMBL99718 1 6.52
CHEMBL316868 1 5.44
CHEMBL320445 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98975 IC50 = 40.0 nM 7.40
CHEMBL421005 IC50 = 90.0 nM 7.05
CHEMBL95457 IC50 = 270.0 nM 6.57
CHEMBL99718 IC50 = 300.0 nM 6.52
CHEMBL316868 IC50 = 3600.0 nM 5.44
CHEMBL320445 IC50 = 3700.0 nM 5.43