Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T50269 | ||||
Target Name | Strychnine-binding glycine receptor (GLRA1) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | 10-methoxy-ginkgolide C | Drug Info | IC50 = 5200 nM | [2] | |
3,14-DIDEHYDROGINKGOLIDE A | Drug Info | IC50 = 3100 nM | [2] | ||
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine | Drug Info | IC50 = 4100 nM | [1] | ||
3-demethoxy-3-D-mannopyranosylaminothiocolchicine | Drug Info | IC50 = 13100 nM | [1] | ||
3-demethoxy-3-D-xylopyranosylaminothiocolchicine | Drug Info | IC50 = 3300 nM | [1] | ||
3-demethoxy-3-L-fucopyranosylaminothiocolchicine | Drug Info | IC50 = 4200 nM | [1] | ||
3-demethoxy-3D-glucopyranosylaminothiocolchicine | Drug Info | IC50 = 10600 nM | [1] | ||
GINKGOLIDE A | Drug Info | IC50 = 3800 nM | [2] | ||
Ginkgolide C | Drug Info | IC50 = 5900 nM | [2] | ||
Ginkgolide J | Drug Info | IC50 = 6400 nM | [2] | ||
Ginkgolide M | Drug Info | IC50 = 650 nM | [2] | ||
GINKOLIDE B | Drug Info | IC50 = 1700 nM | [2] | ||
THIOCOLCHICOSIDE | Drug Info | IC50 = 1500 nM | [1] | ||
[3H]strychnine | Drug Info | IC50 = 14 nM | [1] | ||
References | |||||
REF 1 | 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7. | ||||
REF 2 | Probing the pharmacophore of ginkgolides as glycine receptor antagonists. J Med Chem. 2007 Apr 5;50(7):1610-7. | ||||
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