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Assay Detail

CHEMBL947299

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

Binding
Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method
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-beta (CHEMBL4093)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
Wrobel J, Steffan R, Bowen SM, Magolda R, Matelan E, Unwalla R, Basso M, Clerin V, Gardell SJ, Nambi P, Quinet E, Reminick JI, Vlasuk GP, Wang S, Feingold I, Huselton C, Bonn T, Farnegardh M, Hansson T, Nilsson AG, Wilhelmsson A, Zamaratski E, Evans MJ.
J Med Chem (2008) 51 : 7161 -7168
PubMed 18973288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.57 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217118 1 8.70
CHEMBL214719 1 8.70
CHEMBL62136 T091317 1 8.05
CHEMBL517015 1 8.00
CHEMBL59030 1 7.92
CHEMBL456237 LXR-623 1.0 1 7.62
CHEMBL521398 1 7.52
CHEMBL514428 1 7.50
CHEMBL457977 1 7.48
CHEMBL488173 1 7.42
CHEMBL520883 1 7.42
CHEMBL488174 1 7.40
CHEMBL464189 1 7.39
CHEMBL486955 1 7.32
CHEMBL515852 1 7.31
CHEMBL458597 1 7.24
CHEMBL488802 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217118 IC50 = 2.0 nM 8.70
CHEMBL214719 IC50 = 2.0 nM 8.70
CHEMBL62136 T091317 IC50 = 9.0 nM 8.05
CHEMBL517015 IC50 = 10.0 nM 8.00
CHEMBL59030 IC50 = 12.0 nM 7.92
CHEMBL456237 LXR-623 IC50 = 24.0 nM 7.62
CHEMBL521398 IC50 = 30.0 nM 7.52
CHEMBL514428 IC50 = 32.0 nM 7.50
CHEMBL457977 IC50 = 33.0 nM 7.48
CHEMBL488173 IC50 = 38.0 nM 7.42
CHEMBL520883 IC50 = 38.0 nM 7.42
CHEMBL488174 IC50 = 40.0 nM 7.40
CHEMBL464189 IC50 = 41.0 nM 7.39
CHEMBL486955 IC50 = 48.0 nM 7.32
CHEMBL515852 IC50 = 49.0 nM 7.31
CHEMBL458597 IC50 = 58.0 nM 7.24
CHEMBL488802 IC50 = 1853.0 nM 5.73