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Assay Detail

CHEMBL819219

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

Functional
In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Soleus muscle
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL3252)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent.
Bloom JD, Dutia MD, Johnson BD, Wissner A, Burns MG, Largis EE, Dolan JA, Claus TH.
J Med Chem (1992) 35 : 3081 -3084
PubMed 1354264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.46 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 8.28
CHEMBL284782 1 6.72
CHEMBL38486 1 6.30
CHEMBL32590 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL IC50 = 5.3 nM 8.28
CHEMBL284782 IC50 = 190.0 nM 6.72
CHEMBL38486 IC50 = 500.0 nM 6.30
CHEMBL32590 IC50 = 30000.0 nM 4.52