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Assay Detail

CHEMBL924510

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Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as cAMP level
12
Total Activities
12
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 Intermediate

Target

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

Publication

Potent oxindole based human beta3 adrenergic receptor agonists.
Stevens FC, Bloomquist WE, Borel AG, Cohen ML, Droste CA, Heiman ML, Kriauciunas A, Sall DJ, Tinsley FC, Jesudason CD.
Bioorg Med Chem Lett (2007) 17 : 6270 -6273
PubMed 17911024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.88 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251579 1 8.57
CHEMBL251372 1 8.28
CHEMBL248547 1 8.18
CHEMBL248751 1 8.08
CHEMBL430392 1 7.97
CHEMBL404626 1 7.92
CHEMBL401335 1 7.91
CHEMBL251176 1 7.86
CHEMBL251177 1 7.85
CHEMBL248750 1 7.75
CHEMBL251167 1 7.61
CHEMBL250579 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251579 EC50 = 2.7 nM 8.57
CHEMBL251372 EC50 = 5.2 nM 8.28
CHEMBL248547 EC50 = 6.6 nM 8.18
CHEMBL248751 EC50 = 8.3 nM 8.08
CHEMBL430392 EC50 = 10.6 nM 7.97
CHEMBL404626 EC50 = 12.0 nM 7.92
CHEMBL401335 EC50 = 12.3 nM 7.91
CHEMBL251176 EC50 = 13.9 nM 7.86
CHEMBL251177 EC50 = 14.0 nM 7.85
CHEMBL248750 EC50 = 17.6 nM 7.75
CHEMBL251167 EC50 = 24.4 nM 7.61
CHEMBL250579 EC50 = 268.1 nM 6.57