Target Validation Information
Target ID T52297
Target Name Oxysterols receptor LXR-alpha
Target Type
Research
Drug Potency against Target 12-dehydroxyriccardin C Drug Info IC50 = 4400 nM [1]
2-(2-phenethylphenyl)isoindoline-1,3-dione Drug Info IC50 = 9800 nM [2]
GW-3965 Drug Info IC50 = 100 nM [3]
WAY-252623 Drug Info IC50 = 179 nM [3]
12,17-dehydroxyriccardin C Drug Info IC50 = 5700 nM [1]
2-(2-hexylphenyl)isoindoline-1,3-dione Drug Info IC50 = 13000 nM [1]
4,17-dehydroxyriccardin C Drug Info IC50 = 3200 nM [1]
4,12,17-dehydroxyriccardin C Drug Info IC50 = 7100 nM [1]
GSK-9772 Drug Info IC50 = 180 nM [4]
WAY-214950 Drug Info IC50 = 248 nM [3]
2-Benzyl-3-phenyl-7-(trifluoromethyl)-2H-indazole Drug Info IC50 = 279 nM [3]
Guttiferone I Drug Info IC50 = 3400 nM [5]
4-dehydroxyriccardin C Drug Info IC50 = 8400 nM [1]
17-dehydroxyriccardin C Drug Info IC50 = 6600 nM [1]
Riccardin C Drug Info IC50 = 4900 nM [1]
References
REF 1Bioorg Med Chem. 2008 Apr 15;16(8):4272-85. Epub 2008 Feb 29.Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
REF 2Bioorg Med Chem. 2009 Jul 15;17(14):5001-14. Epub 2009 Jun 2.Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.
REF 3J Med Chem. 2008 Nov 27;51(22):7161-8.Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.
REF 4J Med Chem. 2008 Sep 25;51(18):5758-65.Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.
REF 5J Nat Prod. 2005 Apr;68(4):617-9.Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.

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