Target Validation Information
TTD ID T52297
Target Name Oxysterols receptor LXR-alpha (NR1H3)
Type of Target
Patented-recorded
Drug Potency against Target Drug Info IC50 = 179 nM [4]
12,17-dehydroxyriccardin C Drug Info IC50 = 5700 nM [2]
12-dehydroxyriccardin C Drug Info IC50 = 4400 nM [2]
17-dehydroxyriccardin C Drug Info IC50 = 6600 nM [2]
2-(2-hexylphenyl)isoindoline-1,3-dione Drug Info IC50 = 13000 nM [2]
2-(2-phenethylphenyl)isoindoline-1,3-dione Drug Info IC50 = 9800 nM [5]
2-Benzyl-3-phenyl-7-(trifluoromethyl)-2H-indazole Drug Info IC50 = 279 nM [4]
4,12,17-dehydroxyriccardin C Drug Info IC50 = 7100 nM [2]
4,17-dehydroxyriccardin C Drug Info IC50 = 3200 nM [2]
4-dehydroxyriccardin C Drug Info IC50 = 8400 nM [2]
GSK-9772 Drug Info IC50 = 180 nM [3]
Guttiferone I Drug Info IC50 = 3400 nM [1]
GW-3965 Drug Info IC50 = 100 nM [4]
Riccardin C Drug Info IC50 = 4900 nM [2]
WAY-214950 Drug Info IC50 = 248 nM [4]
References
REF 1 Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand. J Nat Prod. 2005 Apr;68(4):617-9.
REF 2 Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development. Bioorg Med Chem. 2008 Apr 15;16(8):4272-85.
REF 3 Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. J Med Chem. 2008 Sep 25;51(18):5758-65.
REF 4 Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic tr... J Med Chem. 2008 Nov 27;51(22):7161-8.
REF 5 Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LX... Bioorg Med Chem. 2009 Jul 15;17(14):5001-14.

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