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Assay Detail

CHEMBL1071222

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Functional
Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Huh-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Oxysterols receptor LXR-alpha (CHEMBL2808)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
Singhaus RR, Bernotas RC, Steffan R, Matelan E, Quinet E, Nambi P, Feingold I, Huselton C, Wilhelmsson A, Goos-Nilsson A, Wrobel J.
Bioorg Med Chem Lett (2010) 20 : 521 -525
PubMed 20005711 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 32 6.37 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL611735 1 7.70
CHEMBL595689 1 7.51
CHEMBL612007 1 7.50
CHEMBL594757 1 6.79
CHEMBL62136 T091317 1 6.77
CHEMBL612006 1 6.69
CHEMBL611465 1 6.38
CHEMBL595917 1 6.28
CHEMBL603956 1 6.27
CHEMBL611734 1 6.24
CHEMBL595937 1 6.17
CHEMBL596357 1 6.16
CHEMBL611467 1 6.15
CHEMBL605314 1 6.08
CHEMBL608531 1 6.07
CHEMBL595915 1 6.05
CHEMBL611466 1 6.02
CHEMBL604701 1 5.85
CHEMBL606756 1 5.80
CHEMBL596157 1 5.78
CHEMBL596381 1 5.49
CHEMBL605107 1 -
CHEMBL595007 1 -
CHEMBL595006 1 -
CHEMBL606044 1 -
CHEMBL604905 1 -
CHEMBL604797 1 -
CHEMBL612005 1 -
CHEMBL594545 1 -
CHEMBL596158 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL611735 EC50 = 20.0 nM 7.70
CHEMBL595689 EC50 = 31.0 nM 7.51
CHEMBL612007 EC50 = 32.0 nM 7.50
CHEMBL594757 EC50 = 162.0 nM 6.79
CHEMBL62136 T091317 EC50 = 170.0 nM 6.77
CHEMBL612006 EC50 = 204.0 nM 6.69
CHEMBL611465 EC50 = 420.0 nM 6.38
CHEMBL595917 EC50 = 530.0 nM 6.28
CHEMBL603956 EC50 = 540.0 nM 6.27
CHEMBL611734 EC50 = 570.0 nM 6.24
CHEMBL595937 EC50 = 680.0 nM 6.17
CHEMBL596357 EC50 = 700.0 nM 6.16
CHEMBL611467 EC50 = 710.0 nM 6.15
CHEMBL605314 EC50 = 840.0 nM 6.08
CHEMBL608531 EC50 = 850.0 nM 6.07
CHEMBL595915 EC50 = 890.0 nM 6.05
CHEMBL611466 EC50 = 950.0 nM 6.02
CHEMBL604701 EC50 = 1420.0 nM 5.85
CHEMBL606756 EC50 = 1570.0 nM 5.80
CHEMBL596157 EC50 = 1680.0 nM 5.78
CHEMBL596381 EC50 = 3240.0 nM 5.49
CHEMBL605107 EC50 - -
CHEMBL595007 EC50 - -
CHEMBL595006 EC50 - -
CHEMBL606044 EC50 - -
CHEMBL604905 EC50 - -
CHEMBL604797 EC50 - -
CHEMBL612005 EC50 - -
CHEMBL594545 EC50 - -
CHEMBL596158 EC50 - -
CHEMBL611736 EC50 - -
CHEMBL604703 EC50 - -