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Assay Detail

CHEMBL3100398

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

Binding
Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction
17
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Trachea
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.
Huang L, Shan W, Zhou Q, Xie J, Lai K, Li X.
Bioorg Med Chem Lett (2014) 24 : 249 -253
PubMed 24300734 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.43 9.90
Activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1363 ARFORMOTEROL 4.0 2 9.90
CHEMBL3099249 3 9.00
CHEMBL3099248 3 8.30
CHEMBL3099250 3 8.00
CHEMBL3099251 3 7.90
CHEMBL434 ISOPROTERENOL 4.0 3 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1363 ARFORMOTEROL EC50 = 0.1259 nM 9.90
CHEMBL1363 ARFORMOTEROL EC50 = 0.13 nM 9.89
CHEMBL3099249 EC50 = 1.0 nM 9.00
CHEMBL3099249 EC50 = 1.05 nM 8.98
CHEMBL3099248 EC50 = 5.02 nM 8.30
CHEMBL3099248 EC50 = 5.012 nM 8.30
CHEMBL3099250 EC50 = 10.0 nM 8.00
CHEMBL3099250 EC50 = 10.32 nM 7.99
CHEMBL3099251 EC50 = 12.59 nM 7.90
CHEMBL3099251 EC50 = 12.59 nM 7.90
CHEMBL434 ISOPROTERENOL EC50 = 31.64 nM 7.50
CHEMBL434 ISOPROTERENOL EC50 = 31.62 nM 7.50
CHEMBL434 ISOPROTERENOL Activity - -
CHEMBL3099250 Activity - -
CHEMBL3099251 Activity - -
CHEMBL3099248 Activity - -
CHEMBL3099249 Activity - -