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Assay Detail

CHEMBL1033546

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Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Discovery of novel acetanilide derivatives as potent and selective beta3-adrenergic receptor agonists.
Maruyama T, Onda K, Hayakawa M, Matsui T, Takasu T, Ohta M.
Eur J Med Chem (2009) 44 : 2533 -2543
PubMed 19232786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.32 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 7.92
CHEMBL561348 1 7.08
CHEMBL561291 1 6.82
CHEMBL551831 1 6.75
CHEMBL563810 1 6.72
CHEMBL561693 1 6.58
CHEMBL551350 1 6.55
CHEMBL562153 1 6.46
CHEMBL551892 1 6.31
CHEMBL539226 1 6.26
CHEMBL552434 1 6.26
CHEMBL551832 1 6.23
CHEMBL564556 1 6.22
CHEMBL550743 1 6.18
CHEMBL561211 1 6.15
CHEMBL564544 1 6.14
CHEMBL550746 1 6.12
CHEMBL561818 1 6.04
CHEMBL557269 1 6.02
CHEMBL417613 1 5.80
CHEMBL552089 1 5.77
CHEMBL466705 1 5.57
CHEMBL552497 1 5.51
CHEMBL562154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL EC50 = 12.0 nM 7.92
CHEMBL561348 EC50 = 83.0 nM 7.08
CHEMBL561291 EC50 = 150.0 nM 6.82
CHEMBL551831 EC50 = 180.0 nM 6.75
CHEMBL563810 EC50 = 190.0 nM 6.72
CHEMBL561693 EC50 = 260.0 nM 6.58
CHEMBL551350 EC50 = 280.0 nM 6.55
CHEMBL562153 EC50 = 350.0 nM 6.46
CHEMBL551892 EC50 = 490.0 nM 6.31
CHEMBL539226 EC50 = 550.0 nM 6.26
CHEMBL552434 EC50 = 550.0 nM 6.26
CHEMBL551832 EC50 = 590.0 nM 6.23
CHEMBL564556 EC50 = 600.0 nM 6.22
CHEMBL550743 EC50 = 660.0 nM 6.18
CHEMBL561211 EC50 = 710.0 nM 6.15
CHEMBL564544 EC50 = 720.0 nM 6.14
CHEMBL550746 EC50 = 760.0 nM 6.12
CHEMBL561818 EC50 = 910.0 nM 6.04
CHEMBL557269 EC50 = 960.0 nM 6.02
CHEMBL417613 EC50 = 1600.0 nM 5.80
CHEMBL552089 EC50 = 1700.0 nM 5.77
CHEMBL466705 EC50 = 2700.0 nM 5.57
CHEMBL552497 EC50 = 3100.0 nM 5.51
CHEMBL562154 EC50 > 100000.0 nM -