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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