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Assay Detail

CHEMBL1007108

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 immunoassay
21
Total Activities
17
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 highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.
Hattori K, Toda S, Imanishi M, Itou S, Nakajima Y, Washizuka K, Araki T, Hamashima H, 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.
J Med Chem (2009) 52 : 3063 -3072
PubMed 19366244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 8.76 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469395 2 9.20
CHEMBL470856 1 9.17
CHEMBL469821 1 9.06
CHEMBL452134 1 9.00
CHEMBL515397 2 9.00
CHEMBL471060 1 8.96
CHEMBL271574 1 8.92
CHEMBL446806 2 8.92
CHEMBL488224 2 8.90
CHEMBL445481 1 8.85
CHEMBL270026 1 8.66
CHEMBL492401 1 8.60
CHEMBL469396 1 8.54
CHEMBL271945 1 8.54
CHEMBL473702 1 8.49
CHEMBL470292 1 8.00
CHEMBL491726 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469395 EC50 = 0.631 nM 9.20
CHEMBL470856 EC50 = 0.68 nM 9.17
CHEMBL469395 EC50 = 0.83 nM 9.08
CHEMBL469821 EC50 = 0.88 nM 9.06
CHEMBL452134 EC50 = 1.0 nM 9.00
CHEMBL515397 EC50 = 1.0 nM 9.00
CHEMBL471060 EC50 = 1.1 nM 8.96
CHEMBL271574 EC50 = 1.2 nM 8.92
CHEMBL446806 EC50 = 1.2 nM 8.92
CHEMBL488224 EC50 = 1.259 nM 8.90
CHEMBL446806 EC50 = 1.259 nM 8.90
CHEMBL488224 EC50 = 1.3 nM 8.89
CHEMBL445481 EC50 = 1.4 nM 8.85
CHEMBL270026 EC50 = 2.2 nM 8.66
CHEMBL492401 EC50 = 2.512 nM 8.60
CHEMBL469396 EC50 = 2.9 nM 8.54
CHEMBL271945 EC50 = 2.9 nM 8.54
CHEMBL473702 EC50 = 3.2 nM 8.49
CHEMBL515397 EC50 = 4.9 nM 8.31
CHEMBL470292 EC50 = 10.0 nM 8.00
CHEMBL491726 EC50 = 10.0 nM 8.00