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Assay Detail

CHEMBL1010737

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

Functional
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
12
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.
Kern C, Meyer T, Droux S, Schollmeyer D, Miculka C.
J Med Chem (2009) 52 : 1773 -1777
PubMed 19245211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.51 8.21
Emax 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL509336 RACTOPAMINE 2.0 2 8.21
CHEMBL2218907 ZILPATEROL 2.0 4 8.06
CHEMBL714 ALBUTEROL 4.0 2 8.04
CHEMBL49080 CLENBUTEROL 2.0 2 7.89
CHEMBL462313 2 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL509336 RACTOPAMINE EC50 = 6.2 nM 8.21
CHEMBL2218907 ZILPATEROL EC50 = 8.7 nM 8.06
CHEMBL714 ALBUTEROL EC50 = 9.1 nM 8.04
CHEMBL49080 CLENBUTEROL EC50 = 13.0 nM 7.89
CHEMBL2218907 ZILPATEROL EC50 = 19.0 nM 7.72
CHEMBL462313 EC50 = 6900.0 nM 5.16
CHEMBL462313 Emax = 105.0 % -
CHEMBL2218907 ZILPATEROL Emax = 102.0 % -
CHEMBL49080 CLENBUTEROL Emax = 100.0 % -
CHEMBL509336 RACTOPAMINE Emax = 105.0 % -
CHEMBL714 ALBUTEROL Emax = 100.0 % -
CHEMBL2218907 ZILPATEROL Emax = 103.0 % -