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Assay Detail

CHEMBL1036710

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

Binding
Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biarylether amide quinolines as liver X receptor agonists.
Bernotas RC, Singhaus RR, Kaufman DH, Ullrich J, Fletcher H, Quinet E, Nambi P, Unwalla R, Wilhelmsson A, Goos-Nilsson A, Farnegardh M, Wrobel J.
Bioorg Med Chem (2009) 17 : 1663 -1670
PubMed 19162487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.45 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214719 1 7.03
CHEMBL502579 1 7.01
CHEMBL450409 1 6.86
CHEMBL505445 1 6.84
CHEMBL454596 1 6.77
CHEMBL460198 1 6.24
CHEMBL461890 1 6.10
CHEMBL518033 1 5.93
CHEMBL461891 1 5.90
CHEMBL480298 1 5.82
CHEMBL541472 1 -
CHEMBL460197 1 -
CHEMBL516464 1 -
CHEMBL459563 1 -
CHEMBL459562 1 -
CHEMBL457037 1 -
CHEMBL471608 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214719 EC50 = 93.0 nM 7.03
CHEMBL502579 EC50 = 98.0 nM 7.01
CHEMBL450409 EC50 = 138.0 nM 6.86
CHEMBL505445 EC50 = 144.0 nM 6.84
CHEMBL454596 EC50 = 170.0 nM 6.77
CHEMBL460198 EC50 = 572.0 nM 6.24
CHEMBL461890 EC50 = 800.0 nM 6.10
CHEMBL518033 EC50 = 1180.0 nM 5.93
CHEMBL461891 EC50 = 1272.0 nM 5.90
CHEMBL480298 EC50 = 1525.0 nM 5.82
CHEMBL541472 EC50 - -
CHEMBL460197 EC50 - -
CHEMBL516464 EC50 - -
CHEMBL459563 EC50 - -
CHEMBL459562 EC50 - -
CHEMBL457037 EC50 - -
CHEMBL471608 EC50 - -