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Assay Detail

CHEMBL647668

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

Binding
Tested for Beta adrenergic receptor binding inhibition from canine ventricular tissue, using [3H]dihydroalprenolol as the radioligand in anesthetized dogs
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
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 25 5.24 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95784 1 6.82
CHEMBL317163 1 6.38
CHEMBL98773 1 6.11
CHEMBL95966 1 6.00
CHEMBL95754 1 5.64
CHEMBL98979 1 5.54
CHEMBL95911 1 5.54
CHEMBL318131 1 5.41
CHEMBL471 SOTALOL 4.0 1 5.14
CHEMBL99513 1 5.08
CHEMBL99815 1 4.91
CHEMBL99532 1 4.91
CHEMBL98575 1 4.80
CHEMBL317274 1 4.80
CHEMBL99331 1 4.80
CHEMBL95727 1 4.59
CHEMBL99652 1 4.51
CHEMBL95894 1 4.36
CHEMBL99188 1 4.21
CHEMBL99179 1 -
CHEMBL95985 1 -
CHEMBL99391 1 -
CHEMBL95795 1 -
CHEMBL99814 1 -
CHEMBL95804 SEMATILIDE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95784 IC50 = 150.0 nM 6.82
CHEMBL317163 IC50 = 420.0 nM 6.38
CHEMBL98773 IC50 = 780.0 nM 6.11
CHEMBL95966 IC50 = 990.0 nM 6.00
CHEMBL95754 IC50 = 2300.0 nM 5.64
CHEMBL98979 IC50 = 2900.0 nM 5.54
CHEMBL95911 IC50 = 2900.0 nM 5.54
CHEMBL318131 IC50 = 3900.0 nM 5.41
CHEMBL471 SOTALOL IC50 = 7200.0 nM 5.14
CHEMBL99513 IC50 = 8400.0 nM 5.08
CHEMBL99815 IC50 = 12200.0 nM 4.91
CHEMBL99532 IC50 = 12400.0 nM 4.91
CHEMBL98575 IC50 = 15800.0 nM 4.80
CHEMBL317274 IC50 = 15700.0 nM 4.80
CHEMBL99331 IC50 = 15700.0 nM 4.80
CHEMBL95727 IC50 = 25800.0 nM 4.59
CHEMBL99652 IC50 = 30900.0 nM 4.51
CHEMBL95894 IC50 = 43800.0 nM 4.36
CHEMBL99188 IC50 = 61400.0 nM 4.21
CHEMBL99179 IC50 = 192000.0 nM -
CHEMBL95985 IC50 = 360000.0 nM -
CHEMBL99391 IC50 = 109000.0 nM -
CHEMBL95795 IC50 = 293000.0 nM -
CHEMBL99814 IC50 = 227000.0 nM -
CHEMBL95804 SEMATILIDE IC50 = 7000000.0 nM -