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Assay Detail

CHEMBL981733

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Functional
Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation
22
Total Activities
22
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

Discovery of novel series of benzoic acid derivatives containing biphenyl ether moiety as potent and selective human beta(3)-adrenergic receptor agonists: Part IV.
Nakajima Y, Imanishi M, Itou S, Hamashima H, Tomishima Y, Washizuka K, Sakurai M, Matsui S, Imamura E, Ueshima K, Yamamoto T, Yamamoto N, Ishikawa H, Nakano K, Unami N, Hamada K, Hattori K.
Bioorg Med Chem Lett (2008) 18 : 5037 -5040
PubMed 18752946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.00 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 9.01
CHEMBL272584 1 8.96
CHEMBL492006 1 8.72
CHEMBL523265 1 8.47
CHEMBL491645 1 8.34
CHEMBL519985 1 8.19
CHEMBL482627 1 8.18
CHEMBL271576 1 8.17
CHEMBL489200 1 8.14
CHEMBL490222 1 8.07
CHEMBL521611 1 8.03
CHEMBL484265 1 8.02
CHEMBL489199 1 7.96
CHEMBL492005 1 7.92
CHEMBL489201 1 7.89
CHEMBL523817 1 7.85
CHEMBL524145 1 7.68
CHEMBL522641 1 7.51
CHEMBL409828 1 7.41
CHEMBL490415 1 7.25
CHEMBL491634 1 7.22
CHEMBL411234 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL EC50 = 0.97 nM 9.01
CHEMBL272584 EC50 = 1.1 nM 8.96
CHEMBL492006 EC50 = 1.9 nM 8.72
CHEMBL523265 EC50 = 3.4 nM 8.47
CHEMBL491645 EC50 = 4.6 nM 8.34
CHEMBL519985 EC50 = 6.5 nM 8.19
CHEMBL482627 EC50 = 6.6 nM 8.18
CHEMBL271576 EC50 = 6.7 nM 8.17
CHEMBL489200 EC50 = 7.2 nM 8.14
CHEMBL490222 EC50 = 8.6 nM 8.07
CHEMBL521611 EC50 = 9.4 nM 8.03
CHEMBL484265 EC50 = 9.5 nM 8.02
CHEMBL489199 EC50 = 11.0 nM 7.96
CHEMBL492005 EC50 = 12.0 nM 7.92
CHEMBL489201 EC50 = 13.0 nM 7.89
CHEMBL523817 EC50 = 14.0 nM 7.85
CHEMBL524145 EC50 = 21.0 nM 7.68
CHEMBL522641 EC50 = 31.0 nM 7.51
CHEMBL409828 EC50 = 39.0 nM 7.41
CHEMBL490415 EC50 = 56.0 nM 7.25
CHEMBL491634 EC50 = 60.0 nM 7.22
CHEMBL411234 EC50 = 100.0 nM 7.00