Target Validation Information
TTD ID	T55285
Target Name	Glycine receptor (GlyR)
Type of Target	Successful
Drug Potency against Target	(12E,20Z,18S)-8-hydroxyvariabilin	Drug Info	IC50 = 7000 nM	[3]
	10-methoxy-ginkgolide C	Drug Info	IC50 = 7800 nM	[2]
	3,14-DIDEHYDROGINKGOLIDE A	Drug Info	IC50 = 9500 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 = 2100 nM	[2]
	Ginkgolide C	Drug Info	IC50 = 8200 nM	[2]
	Ginkgolide J	Drug Info	IC50 = 12000 nM	[2]
	Ginkgolide M	Drug Info	IC50 = 1300 nM	[2]
	GINKOLIDE B	Drug Info	IC50 = 3700 nM	[2]
	THIOCOLCHICOSIDE	Drug Info	IC50 = 1500 nM	[1]
	[3H]strychnine	Drug Info	IC50 = 14 nM	[1]
Action against Disease Model	GW 468816	Drug Info	The effect of bicuculline on the inhibition of the spontaneous firing of two Purkinje cells(A, B) by GABA (solid line, 5 nA).	[4]
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.
REF 3	Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae. Bioorg Med Chem. 2010 Apr 15;18(8):2912-9.
REF 4	Antagonism between bicuculline and GABA in the cat brain. Brain Res. 1971 Oct 8;33(1):57-73.

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