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Assay Detail

CHEMBL1036709

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

Binding
Displacement of [3H]T0901317 from human recombinant N-terminal biotinylated tagged LXRalpha ligand binding domain expressed in Escherichia coli
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxysterols receptor LXR-alpha (CHEMBL2808)
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
IC50 17 7.13 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214719 1 8.02
CHEMBL505445 1 7.92
CHEMBL502579 1 7.92
CHEMBL450409 1 7.82
CHEMBL454596 1 7.70
CHEMBL516464 1 7.47
CHEMBL460197 1 7.30
CHEMBL457037 1 7.13
CHEMBL480298 1 7.04
CHEMBL459563 1 6.97
CHEMBL461890 1 6.90
CHEMBL460198 1 6.80
CHEMBL471608 1 6.64
CHEMBL461891 1 6.57
CHEMBL518033 1 6.55
CHEMBL459562 1 6.45
CHEMBL541472 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214719 IC50 = 9.5 nM 8.02
CHEMBL505445 IC50 = 12.0 nM 7.92
CHEMBL502579 IC50 = 12.0 nM 7.92
CHEMBL450409 IC50 = 15.0 nM 7.82
CHEMBL454596 IC50 = 20.0 nM 7.70
CHEMBL516464 IC50 = 34.0 nM 7.47
CHEMBL460197 IC50 = 50.0 nM 7.30
CHEMBL457037 IC50 = 74.0 nM 7.13
CHEMBL480298 IC50 = 91.0 nM 7.04
CHEMBL459563 IC50 = 108.0 nM 6.97
CHEMBL461890 IC50 = 125.0 nM 6.90
CHEMBL460198 IC50 = 158.0 nM 6.80
CHEMBL471608 IC50 = 231.0 nM 6.64
CHEMBL461891 IC50 = 272.0 nM 6.57
CHEMBL518033 IC50 = 280.0 nM 6.55
CHEMBL459562 IC50 = 357.0 nM 6.45
CHEMBL541472 IC50 = 1002.0 nM 6.00