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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