Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T13714 | ||||
Target Name | Oxysterols receptor LXR-beta (NR1H2) | ||||
Type of Target |
Clinical trial |
||||
Drug Potency against Target | Drug Info | IC50 = 24 nM | [3] | ||
12,17-dehydroxyriccardin C | Drug Info | IC50 = 14000 nM | [1] | ||
12-dehydroxyriccardin C | Drug Info | IC50 = 7600 nM | [1] | ||
17-dehydroxyriccardin C | Drug Info | IC50 = 13000 nM | [1] | ||
2-Benzyl-3-phenyl-7-(trifluoromethyl)-2H-indazole | Drug Info | IC50 = 41 nM | [3] | ||
4,17-dehydroxyriccardin C | Drug Info | IC50 = 7300 nM | [1] | ||
4-dehydroxyriccardin C | Drug Info | IC50 = 10000 nM | [1] | ||
GSK-9772 | Drug Info | IC50 = 30 nM | [2] | ||
GW-3965 | Drug Info | IC50 = 12 nM | [3] | ||
Riccardin C | Drug Info | IC50 = 6600 nM | [1] | ||
WAY-214950 | Drug Info | IC50 = 33 nM | [3] | ||
References | |||||
REF 1 | 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 2 | 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 3 | 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. | ||||
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