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Assay Detail

CHEMBL1021863

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

Functional
Agonist activity at dog recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
8
Total Activities
8
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 biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.
Imanishi M, Itou S, Washizuka K, Hamashima H, Nakajima Y, Araki T, Tomishima Y, 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 : 4002 -4020
PubMed 18553954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.61 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL486051 1 9.72
CHEMBL507506 1 9.29
CHEMBL488224 1 8.89
CHEMBL271945 1 8.54
CHEMBL487682 1 8.49
CHEMBL453047 1 8.43
CHEMBL470292 1 7.96
CHEMBL59765 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL486051 EC50 = 0.19 nM 9.72
CHEMBL507506 EC50 = 0.51 nM 9.29
CHEMBL488224 EC50 = 1.3 nM 8.89
CHEMBL271945 EC50 = 2.9 nM 8.54
CHEMBL487682 EC50 = 3.2 nM 8.49
CHEMBL453047 EC50 = 3.7 nM 8.43
CHEMBL470292 EC50 = 11.0 nM 7.96
CHEMBL59765 EC50 = 30.0 nM 7.52