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Assay Detail

CHEMBL3395623

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

Binding
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
4
Total Activities
3
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

Insights on the role of boron containing moieties in the design of new potent and efficient agonists targeting the β2 adrenoceptor.
Soriano-Ursúa MA, Arias-Montaño JA, Correa-Basurto J, Hernández-Martínez CF, López-Cabrera Y, Castillo-Hernández MC, Padilla-Martínez II, Trujillo-Ferrara JG.
Bioorg Med Chem Lett (2015) 25 : 820 -825
PubMed 25592716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.30 7.75
EC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 7.75
CHEMBL3393402 2 7.55
CHEMBL714 ALBUTEROL 4.0 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL Kd = 17.78 nM 7.75
CHEMBL3393402 Kd = 28.18 nM 7.55
CHEMBL714 ALBUTEROL Kd = 245.47 nM 6.61
CHEMBL3393402 EC50 <= 280.0 nM -