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Assay Detail

CHEMBL1687002

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Functional
Agonist activity at human beta3 adrenergic receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β3 adrenergic receptor agonists.
Morriello GJ, Wendt HR, Bansal A, Di Salvo J, Feighner S, He J, Hurley AL, Hreniuk DL, Salituro GM, Reddy MV, Galloway SM, McGettigan KK, Laws G, McKnight C, Doss GA, Tsou NN, Black RM, Morris J, Ball RG, Sanfiz AT, Streckfuss E, Struthers M, Edmondson SD.
Bioorg Med Chem Lett (2011) 21 : 1865 -1870
PubMed 21353541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.49 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1684585 1 9.01
CHEMBL1684583 1 8.39
CHEMBL1684584 1 8.08
CHEMBL1684578 1 7.96
CHEMBL1684577 1 7.82
CHEMBL1684581 1 7.09
CHEMBL1684582 1 5.88
CHEMBL1684580 1 5.69
CHEMBL1684579 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1684585 EC50 = 0.98 nM 9.01
CHEMBL1684583 EC50 = 4.1 nM 8.39
CHEMBL1684584 EC50 = 8.3 nM 8.08
CHEMBL1684578 EC50 = 11.0 nM 7.96
CHEMBL1684577 EC50 = 15.0 nM 7.82
CHEMBL1684581 EC50 = 81.0 nM 7.09
CHEMBL1684582 EC50 = 1307.0 nM 5.88
CHEMBL1684580 EC50 = 2030.0 nM 5.69
CHEMBL1684579 EC50 - -