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Assay Detail

CHEMBL4049685

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators.
Heitel P, Achenbach J, Moser D, Proschak E, Merk D.
Bioorg Med Chem Lett (2017) 27 : 1193 -1198
PubMed 28169169 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.14 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1023 BEXAROTENE 4.0 1 6.71
CHEMBL62136 T091317 1 6.03
CHEMBL705 ALITRETINOIN 4.0 1 5.96
CHEMBL456237 LXR-623 1.0 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1023 BEXAROTENE EC50 = 196.0 nM 6.71
CHEMBL62136 T091317 EC50 = 940.0 nM 6.03
CHEMBL705 ALITRETINOIN EC50 = 1090.0 nM 5.96
CHEMBL456237 LXR-623 EC50 = 1440.0 nM 5.84