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Assay Detail

CHEMBL1816603

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 inhibition of electrically-stimulated contraction
6
Total Activities
6
Compounds Tested
1
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

The discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating hydantoin or uracil rings.
Procopiou PA, Barrett VJ, Bevan NJ, Butchers PR, Conroy R, Emmons A, Ford AJ, Jeulin S, Looker BE, Lunniss GE, Morrison VS, Mutch PJ, Perciaccante R, Ruston M, Smith CE, Somers G.
Bioorg Med Chem (2011) 19 : 4192 -4201
PubMed 21696967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 9.03 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1814278 1 9.70
CHEMBL1256786 FORMOTEROL 4.0 1 9.50
CHEMBL1814268 1 9.10
CHEMBL1814280 1 9.00
CHEMBL1814272 1 8.60
CHEMBL1263 SALMETEROL 4.0 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1814278 EC50 = 0.1995 nM 9.70
CHEMBL1256786 FORMOTEROL EC50 = 0.3162 nM 9.50
CHEMBL1814268 EC50 = 0.7943 nM 9.10
CHEMBL1814280 EC50 = 1.0 nM 9.00
CHEMBL1814272 EC50 = 2.512 nM 8.60
CHEMBL1263 SALMETEROL EC50 = 5.012 nM 8.30