Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM).

Bitopertin, also known as RG1678, is a potent and selective inhibitor of GlyT1 with an EC50 of 30nM.

Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.

SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.

A potent, specific and mixed glycine transporter subtype 1 (GlyT1) inhibitor (pIC50=7.7) and GPR55 agonist (pEC50=6.5); shows no activity across a set of more than 200 validated molecular target assays from diverse classes, including kinases, proteases and other enzymes, GPCRs.

N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.

GlyT1 inhibitor 46 is a novel potent, selective, orally available inhibitor of glycine transporter-1 (GlyT1) with IC50 of 38 and 21 nM for rat and human GlyT1, respectively.

ALX-1393 (ALX 1393, ALX1393) is a potent, specific GlyT2 inhibitor with Ki of <1 uM.

A potent, selective glycine transporter 1 (GlyT1) inhibitor with IC50 of 100 nM.

A potent, highly selective glycine transporter 1 (GlyT2) inhibitor with IC50 of 16 nM with negligible affinity for GlyT1..