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Assay Detail

CHEMBL977254

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Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-3 adrenergic receptor (CHEMBL4400)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Discovery of a novel series of benzoic acid derivatives as potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. 3. Phenylethanolaminotetraline (PEAT) skeleton containing biphenyl or biphenyl ether moiety.
Imanishi M, Nakajima Y, Tomishima Y, Hamashima H, Washizuka K, Sakurai M, Matsui S, Imamura E, Ueshima K, Yamamoto T, Yamamoto N, Ishikawa H, Nakano K, Unami N, Hamada K, Matsumura Y, Takamura F, Hattori K.
J Med Chem (2008) 51 : 4804 -4822
PubMed 18651730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.49 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL514102 1 7.60
CHEMBL59765 1 7.52
CHEMBL503209 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL514102 EC50 = 25.0 nM 7.60
CHEMBL59765 EC50 = 30.0 nM 7.52
CHEMBL503209 EC50 = 46.0 nM 7.34