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Assay Detail

CHEMBL651141

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Functional
Agonistic activity against human Beta-3 adrenergic receptor as cAMP accumulation in CHO cells expressing beta3-AR
10
Total Activities
10
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 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 10 8.95 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279260 RAFABEGRON 2.0 1 10.80
CHEMBL284782 1 10.02
CHEMBL26183 1 9.82
CHEMBL26393 1 9.44
CHEMBL25133 1 9.01
CHEMBL24350 1 8.92
CHEMBL286818 1 8.19
CHEMBL279931 1 7.96
CHEMBL25823 1 7.89
CHEMBL282039 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279260 RAFABEGRON EC50 = 0.016 nM 10.80
CHEMBL284782 EC50 = 0.095 nM 10.02
CHEMBL26183 EC50 = 0.15 nM 9.82
CHEMBL26393 EC50 = 0.36 nM 9.44
CHEMBL25133 EC50 = 0.97 nM 9.01
CHEMBL24350 EC50 = 1.2 nM 8.92
CHEMBL286818 EC50 = 6.5 nM 8.19
CHEMBL279931 EC50 = 11.0 nM 7.96
CHEMBL25823 EC50 = 13.0 nM 7.89
CHEMBL282039 EC50 = 33.0 nM 7.48