Target Validation Information
TTD ID	T69685
Target Name	Glycine transporter GlyT-1 (SLC6A9)
Type of Target	Clinical trial
Drug Potency against Target	ALX-5407	Drug Info	IC50 = 3 nM	[1]
	R1678	Drug Info	IC50 = 18 nM
	Org-24461	Drug Info	IC50 = 22 nM	[3]
	SSR-504734	Drug Info	IC50 = 18 nM	[2]
Action against Disease Model	ALX-5407	Drug Info	ALX 5407, a potent and selective inhibitor of the hGlyT1 glycine transporter, completely inhibited glycine transport in the GlyT1 cells, with an IC(50) value of 3 nM, but had little or no activity at the h uMan GlyT2 transporter, at other binding sites for glycine, or at other neurotransmitter transporters. The inhibition of glycine transport was essentially irreversible. ALX 5407 represents a novel tool in the investigation of N-methyl-D-aspartate-receptor function. This class of drug may lead to novel therapies in the treatment of schizophrenia	[1]
References
REF 1	ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. Mol Pharmacol. 2001 Dec;60(6):1414-20.
REF 2	Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors. Curr Top Med Chem. 2006;6(17):1883-96.
REF 3	Effects of a neutrophil elastase inhibitor (ONO-5046) on acute pulmonary injury induced by tumor necrosis factor alpha (TNFalpha) and activated neutrophils in isolated perfused rabbit lungs. Am J Respir Crit Care Med. 1998 Jan;157(1):89-94.

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