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Assay Detail

CHEMBL654268

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

Binding
Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol
26
Total Activities
26
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, cardiac electrophysiology, and beta-blocking activity of novel arylpiperazines with potential as class II/III antiarrhythmic agents.
Phillips GB, Morgan TK, Lumma WC, Gomez RP, Lind JM, Lis R, Argentieri T, Sullivan ME.
J Med Chem (1992) 35 : 743 -750
PubMed 1347318 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.37 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162513 1 6.80
CHEMBL349978 1 6.64
CHEMBL350847 1 6.27
CHEMBL165901 1 6.17
CHEMBL162200 1 5.96
CHEMBL350432 1 5.96
CHEMBL163587 1 5.77
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 5.70
CHEMBL9666 1 5.70
CHEMBL162182 1 5.64
CHEMBL163153 1 5.52
CHEMBL350581 1 5.48
CHEMBL59597 1 5.10
CHEMBL471 SOTALOL 4.0 1 5.05
CHEMBL9841 1 4.92
CHEMBL165175 1 4.92
CHEMBL165012 1 4.89
CHEMBL9746 1 4.85
CHEMBL114478 1 4.82
CHEMBL9434 PHENYLPIPERAZINE 1 4.72
CHEMBL351183 1 4.58
CHEMBL162095 1 4.51
CHEMBL165462 1 4.42
CHEMBL59517 1 4.42
CHEMBL163363 1 -
CHEMBL166330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162513 IC50 = 160.0 nM 6.80
CHEMBL349978 IC50 = 230.0 nM 6.64
CHEMBL350847 IC50 = 540.0 nM 6.27
CHEMBL165901 IC50 = 680.0 nM 6.17
CHEMBL162200 IC50 = 1100.0 nM 5.96
CHEMBL350432 IC50 = 1100.0 nM 5.96
CHEMBL163587 IC50 = 1700.0 nM 5.77
CHEMBL478 CHLOROPHENYLPIPERAZINE IC50 = 2000.0 nM 5.70
CHEMBL9666 IC50 = 2000.0 nM 5.70
CHEMBL162182 IC50 = 2300.0 nM 5.64
CHEMBL163153 IC50 = 3000.0 nM 5.52
CHEMBL350581 IC50 = 3300.0 nM 5.48
CHEMBL59597 IC50 = 8000.0 nM 5.10
CHEMBL471 SOTALOL IC50 = 9000.0 nM 5.05
CHEMBL9841 IC50 = 12000.0 nM 4.92
CHEMBL165175 IC50 = 12000.0 nM 4.92
CHEMBL165012 IC50 = 13000.0 nM 4.89
CHEMBL9746 IC50 = 14000.0 nM 4.85
CHEMBL114478 IC50 = 15000.0 nM 4.82
CHEMBL9434 PHENYLPIPERAZINE IC50 = 19000.0 nM 4.72
CHEMBL351183 IC50 = 26000.0 nM 4.58
CHEMBL162095 IC50 = 31000.0 nM 4.51
CHEMBL165462 IC50 = 38000.0 nM 4.42
CHEMBL59517 IC50 = 38000.0 nM 4.42
CHEMBL163363 IC50 > 100000.0 nM -
CHEMBL166330 IC50 > 100000.0 nM -