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Assay Detail

CHEMBL653162

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Functional
Agonism of recombinant human beta-3 adrenergic receptor assayed by measuring cAMP accumulation in CHO cells expressing beta3-AR
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.
Harada H, Hirokawa Y, Suzuki K, Hiyama Y, Oue M, Kawashima H, Yoshida N, Furutani Y, Kato S.
Bioorg Med Chem Lett (2003) 13 : 1301 -1305
PubMed 12657269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 8.08 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279260 RAFABEGRON 2.0 1 10.21
CHEMBL282190 1 9.96
CHEMBL26183 1 9.44
CHEMBL416012 1 9.17
CHEMBL283426 1 9.04
CHEMBL286819 1 9.02
CHEMBL25645 1 8.77
CHEMBL25534 1 8.77
CHEMBL24851 1 8.55
CHEMBL26393 1 8.27
CHEMBL24350 1 8.00
CHEMBL24615 1 7.96
CHEMBL25133 1 7.92
CHEMBL25724 1 7.92
CHEMBL24967 1 7.85
CHEMBL284782 1 7.68
CHEMBL429396 1 7.66
CHEMBL24414 1 7.55
CHEMBL24899 1 7.42
CHEMBL24269 1 7.02
CHEMBL286818 1 6.92
CHEMBL279931 1 6.66
CHEMBL25823 1 6.62
CHEMBL282039 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279260 RAFABEGRON EC50 = 0.062 nM 10.21
CHEMBL282190 EC50 = 0.11 nM 9.96
CHEMBL26183 EC50 = 0.36 nM 9.44
CHEMBL416012 EC50 = 0.67 nM 9.17
CHEMBL283426 EC50 = 0.92 nM 9.04
CHEMBL286819 EC50 = 0.96 nM 9.02
CHEMBL25645 EC50 = 1.7 nM 8.77
CHEMBL25534 EC50 = 1.7 nM 8.77
CHEMBL24851 EC50 = 2.8 nM 8.55
CHEMBL26393 EC50 = 5.4 nM 8.27
CHEMBL24350 EC50 = 10.0 nM 8.00
CHEMBL24615 EC50 = 11.0 nM 7.96
CHEMBL25133 EC50 = 12.0 nM 7.92
CHEMBL25724 EC50 = 12.0 nM 7.92
CHEMBL24967 EC50 = 14.0 nM 7.85
CHEMBL284782 EC50 = 21.0 nM 7.68
CHEMBL429396 EC50 = 22.0 nM 7.66
CHEMBL24414 EC50 = 28.0 nM 7.55
CHEMBL24899 EC50 = 38.0 nM 7.42
CHEMBL24269 EC50 = 96.0 nM 7.02
CHEMBL286818 EC50 = 120.0 nM 6.92
CHEMBL279931 EC50 = 220.0 nM 6.66
CHEMBL25823 EC50 = 240.0 nM 6.62
CHEMBL282039 EC50 = 3300.0 nM 5.48