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Assay Detail

CHEMBL936719

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Functional
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-3 adrenergic receptor (CHEMBL246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Stereospecific synthesis and bio-activity of novel beta(3)-adrenoceptor agonists and inverse agonists.
Perrone MG, Santandrea E, Bleve L, Vitale P, Colabufo NA, Jockers R, Milazzo FM, Sciarroni AF, Scilimati A.
Bioorg Med Chem (2008) 16 : 2473 -2488
PubMed 18083578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.95 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284782 1 8.96
CHEMBL259361 1 8.57
CHEMBL403711 1 8.47
CHEMBL259858 1 8.42
CHEMBL260393 1 8.41
CHEMBL260392 1 8.31
CHEMBL1437 NOREPINEPHRINE 4.0 1 8.26
CHEMBL434 ISOPROTERENOL 4.0 1 8.24
CHEMBL679 EPINEPHRINE 4.0 1 7.51
CHEMBL402462 1 6.87
CHEMBL260018 1 6.74
CHEMBL260996 1 6.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284782 EC50 = 1.1 nM 8.96
CHEMBL259361 EC50 = 2.7 nM 8.57
CHEMBL403711 EC50 = 3.4 nM 8.47
CHEMBL259858 EC50 = 3.8 nM 8.42
CHEMBL260393 EC50 = 3.9 nM 8.41
CHEMBL260392 EC50 = 4.9 nM 8.31
CHEMBL1437 NOREPINEPHRINE EC50 = 5.5 nM 8.26
CHEMBL434 ISOPROTERENOL EC50 = 5.8 nM 8.24
CHEMBL679 EPINEPHRINE EC50 = 31.0 nM 7.51
CHEMBL402462 EC50 = 136.0 nM 6.87
CHEMBL260018 EC50 = 181.0 nM 6.74
CHEMBL260996 EC50 = 235.0 nM 6.63