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是一种 NMDAR 共激动剂，作用于甘氨酸结合位点，是甘氨酸合成与降解过程中的中间产物和副产品。

Opiranserin HCl 是一种非阿片类药物和非甾体抗炎止痛药，是 2 型甘氨酸转运蛋白 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂，IC50 分别为 0.86 和 1.3 μM。它对 rP2X3 有拮抗作用 (IC50=0.87 μM)，正在开发为用于治疗术后疼痛的注射剂。

N-Arachidonylglycine 是一种内源性大麻素类 anandamide 的羧基类似物，是一种 GPR18 激动剂 (EC50 = 44.5 nM)。它在 CB1 和 CB2 受体上均无活性，可抑制 GLYT2 (IC50 = 5.1 μM)，并作为子宫内膜细胞迁移的有效激活剂。

NAE-IN-M22 是一种有效、选择性和可逆的 NEDD8 活化酶 (NAE) 抑制剂，效力在微摩尔范围内。它抑制多种癌细胞生长并诱导 A549 细胞凋亡。NAE-IN-M22 还可以在体内抑制肿瘤的生长。

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.