Iclepertin是一种选择性 GlyT1 抑制剂，主要用于阿尔茨海默病和精神分裂症的研究，具有显著的口服活性。

Sarcosine is an NMDAR co-agonist at the glycine binding site. It is an intermediate and byproduct in glycine synthesis and degradation.

Amoxapine, a tricyclic dibenzoxazepine antidepressant, inhibits GLYT2a transport activity with IC50 of 92 μM.

Bitopertin is a noncompetitive inhibitor of glycine reuptake with IC50 of 25 nM.

ALX 5407 HCl is a selective non-transportable inhibitor of the glycine transporter GlyT1 with IC50 of 3 nM for human GlyT1c.

LY2365109 is a selective inhibitor of GlyT1 with IC50 of 15.8 nM.

ASP 2535 is a potent and selective GlyT1 inhibitor with IC50 of 92 nM.

NFPS is a selective, non-transportable inhibitor of GlyT1 with IC50s of 2.8 and 9.8 nM for hGlyT1, rGlyT1.

Famitinib, a structural analogue of sunitinib, is a multi-targeted receptor tyrosine kinase inhibitor which is potential for treatment of renal cell carcinoma, gastrointestinal stromal tumours, pancreatic cancer, and nasopharyngeal carcinoma.

PF-03463275 is a centrally penetrant, orally available, selective, and competitive inhibitor of GlyT1 (glycine transporter-1) with Ki of 11.6 nM. 

MPDC is a potent inhibitor of the Na+-dependent high-affinity synaptosomal glutamate transporter.