Target Validation Information
Target ID T55285
Target Name Glycine receptor
Target Type
Successful
Drug Potency against Target 3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 13100 nM [528408]
(12E,20Z,18S)-8-hydroxyvariabilin Drug Info IC50 = 7000 nM [530814]
GINKOLIDE B Drug Info IC50 = 3700 nM [528727]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 4100 nM [528408]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 4200 nM [528408]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 3300 nM [528408]
Ginkgolide C Drug Info IC50 = 8200 nM [528727]
10-methoxy-ginkgolide C Drug Info IC50 = 7800 nM [528727]
THIOCOLCHICOSIDE Drug Info IC50 = 1500 nM [528408]
GINKGOLIDE A Drug Info IC50 = 2100 nM [528727]
Ginkgolide M Drug Info IC50 = 1300 nM [528727]
3,14-DIDEHYDROGINKGOLIDE A Drug Info IC50 = 9500 nM [528727]
Ginkgolide J Drug Info IC50 = 12000 nM [528727]
STRYCHNINE Drug Info IC50 = 14 nM [528408]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 10600 nM [528408]
Action against Disease Model GW 468816 The effect of bicuculline on the inhibition of the spontaneous firing of two Purkinje cells(A, B) by GABA (solid line, 5 nA). [553153] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The primary cause of hyperekplexia is missense and non-sense mutations in the glycine receptor (GlyR) alpha1 subunit gene (GLRA1) on chromosome 5q33.1, although we have also discovered rare mutations in the genes encoding the GlyR beta subunit (GLRB) and the GlyR clustering proteins gephyrin (GPNH) and collybistin (ARHGEF9). Recent studies of the Na(+)/Cl(-)-dependent glycine transporters GlyT1 and GlyT2 using mouse knockout models and h uMan genetics have revealed that mutations in GlyT2 are a second major cause of hyperekplexia, while the phenotype of the GlyT1 knockout mouse resembles a devastating neurological disorder known as glycine encephalopathy (OMIM 605899). These findings highlight the importance of these transporters in regulating the levels of synaptic glycine [528408]
References
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 553153Antagonism between bicuculline and GABA in the cat brain. Brain Res. 1971 Oct 8;33(1):57-73.
Ref 530814Bioorg Med Chem. 2010 Apr 15;18(8):2912-9. Epub 2010 Mar 6.Ircinialactams: subunit-selective glycine receptor modulators from Australian sponges of the family Irciniidae.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528727J Med Chem. 2007 Apr 5;50(7):1610-7. Epub 2007 Mar 13.Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.

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