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Assay Detail

CHEMBL1686738

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

Functional
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.
Hughes AD, Chin KH, Dunham SL, Jasper JR, King KE, Lee TW, Mammen M, Martin J, Steinfeld T.
Bioorg Med Chem Lett (2011) 21 : 1354 -1358
PubMed 21310610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.87 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1256786 FORMOTEROL 4.0 1 9.72
CHEMBL1683933 1 9.49
CHEMBL1263 SALMETEROL 4.0 1 9.48
CHEMBL1683934 1 9.44
CHEMBL1346 DARIFENACIN 4.0 1 9.09
CHEMBL1683942 1 9.05
CHEMBL1683932 1 8.96
CHEMBL1683938 1 8.96
CHEMBL1683931 1 8.89
CHEMBL1683935 1 8.59
CHEMBL1683939 1 8.48
CHEMBL1683940 1 8.08
CHEMBL1683941 1 8.05
CHEMBL1683936 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1256786 FORMOTEROL EC50 = 0.19 nM 9.72
CHEMBL1683933 EC50 = 0.32 nM 9.49
CHEMBL1263 SALMETEROL EC50 = 0.33 nM 9.48
CHEMBL1683934 EC50 = 0.36 nM 9.44
CHEMBL1346 DARIFENACIN EC50 = 0.82 nM 9.09
CHEMBL1683942 EC50 = 0.9 nM 9.05
CHEMBL1683932 EC50 = 1.1 nM 8.96
CHEMBL1683938 EC50 = 1.1 nM 8.96
CHEMBL1683931 EC50 = 1.3 nM 8.89
CHEMBL1683935 EC50 = 2.6 nM 8.59
CHEMBL1683939 EC50 = 3.3 nM 8.48
CHEMBL1683940 EC50 = 8.4 nM 8.08
CHEMBL1683941 EC50 = 8.9 nM 8.05
CHEMBL1683936 EC50 = 14.0 nM 7.85