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Assay Detail

CHEMBL907771

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Functional
Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay
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 Expert

Target

Oxysterols receptor LXR-beta (CHEMBL4093)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.
Hu B, Collini M, Unwalla R, Miller C, Singhaus R, Quinet E, Savio D, Halpern A, Basso M, Keith J, Clerin V, Chen L, Resmini C, Liu QY, Feingold I, Huselton C, Azam F, Farnegardh M, Enroth C, Bonn T, Goos-Nilsson A, Wilhelmsson A, Nambi P, Wrobel J.
J Med Chem (2006) 49 : 6151 -6154
PubMed 17034119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.62 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 1 7.80
CHEMBL217118 1 7.48
CHEMBL214719 1 7.15
CHEMBL386772 1 6.84
CHEMBL214074 1 6.73
CHEMBL217704 1 6.53
CHEMBL214324 1 6.43
CHEMBL59030 1 6.39
CHEMBL425099 1 5.85
CHEMBL214465 1 5.82
CHEMBL217376 1 5.82
CHEMBL216645 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 16.0 nM 7.80
CHEMBL217118 EC50 = 33.0 nM 7.48
CHEMBL214719 EC50 = 71.0 nM 7.15
CHEMBL386772 EC50 = 143.0 nM 6.84
CHEMBL214074 EC50 = 186.0 nM 6.73
CHEMBL217704 EC50 = 296.0 nM 6.53
CHEMBL214324 EC50 = 374.0 nM 6.43
CHEMBL59030 EC50 = 410.0 nM 6.39
CHEMBL425099 EC50 = 1400.0 nM 5.85
CHEMBL214465 EC50 = 1500.0 nM 5.82
CHEMBL217376 EC50 = 1500.0 nM 5.82
CHEMBL216645 EC50 - -