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Assay Detail

CHEMBL895338

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Functional
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
16
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Beta-2 adrenergic receptor (CHEMBL5414)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Nitric oxide donor beta2-agonists: furoxan derivatives containing the fenoterol moiety and related furazans.
Buonsanti MF, Bertinaria M, Stilo AD, Cena C, Fruttero R, Gasco A.
J Med Chem (2007) 50 : 5003 -5011
PubMed 17845020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.51 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32800 FENOTEROL 4.0 1 7.75
CHEMBL244687 2 7.75
CHEMBL244321 2 7.54
CHEMBL394600 2 7.41
CHEMBL244906 2 6.96
CHEMBL243266 2 6.96
CHEMBL395082 2 6.66
CHEMBL363325 1 5.64
CHEMBL537445 FENOTEROL HBR 1 5.09
CHEMBL206100 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32800 FENOTEROL EC50 = 18.0 nM 7.75
CHEMBL244687 EC50 = 18.0 nM 7.75
CHEMBL244321 EC50 = 29.0 nM 7.54
CHEMBL394600 EC50 = 39.0 nM 7.41
CHEMBL394600 EC50 = 39.0 nM 7.41
CHEMBL244906 EC50 = 110.0 nM 6.96
CHEMBL243266 EC50 = 110.0 nM 6.96
CHEMBL244321 EC50 = 170.0 nM 6.77
CHEMBL395082 EC50 = 220.0 nM 6.66
CHEMBL244687 EC50 = 250.0 nM 6.60
CHEMBL243266 EC50 = 1000.0 nM 6.00
CHEMBL395082 EC50 = 1300.0 nM 5.89
CHEMBL244906 EC50 = 2200.0 nM 5.66
CHEMBL363325 EC50 = 2300.0 nM 5.64
CHEMBL537445 FENOTEROL HBR EC50 = 8200.0 nM 5.09
CHEMBL206100 EC50 = 86000.0 nM 4.07