Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDR00420
Target NameOxysterols receptor LXR-alpha    
Type of TargetResearch target    
Drug Potency against TargetGW-3965IC50 = 100 nM[1]
WAY-254011IC50 = 10000 nM[2]
2-(2-hexylphenyl)isoindoline-1,3-dioneIC50 = 13000 nM[3]
WAY-252623IC50 = 179 nM[1]
GSK-9772IC50 = 180 nM[4]
WAY-214950IC50 = 248 nM[1]
2-Benzyl-3-phenyl-7-(trifluoromethyl)-2H-indazoleIC50 = 279 nM[1]
4,17-dehydroxyriccardin CIC50 = 3200 nM[3]
Guttiferone IIC50 = 3400 nM[5]
12-dehydroxyriccardin CIC50 = 4400 nM[3]
riccardin CIC50 = 4900 nM[3]
12,17-dehydroxyriccardin CIC50 = 5700 nM[3]
17-dehydroxyriccardin CIC50 = 6600 nM[3]
4,12,17-dehydroxyriccardin CIC50 = 7100 nM[3]
4-dehydroxyriccardin CIC50 = 8400 nM[3]
WAY-254011IC50 = 9.5 nM[6]
2-(2-phenethylphenyl)isoindoline-1,3-dioneIC50 = 9800 nM[7]
Ref 1J 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. To Reference
Ref 2Bioorg Med Chem. 2009 May 15;17(10):3519-27. Epub 2009 Apr 12.Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta. To Reference
Ref 3Bioorg 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. To Reference
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. To Reference
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. To Reference
Ref 6Bioorg Med Chem. 2009 Dec 1;17(23):8086-92. Epub 2009 Oct 4.4-(3-aryloxyaryl)quinoline alcohols are liver X receptor agonists. To Reference
Ref 7Bioorg 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. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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