Target family: Glycine transporter subfamily (type: transporter)
Target: GlyT1

Ligand: ASP2535 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.039999961853027 pIC50
Reference (Journal): A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease.
Published in: Eur J Pharmacol

Ligand: bitopertin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.519999980926514 pEC50
Reference (Journal): Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.
Published in: J Med Chem

Ligand: bitopertin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.329999923706055 pKi
Reference (Journal): Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Published in: J Med Chem

Ligand: GlyT1 inhibitor 27a (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pKi
Reference (Journal): Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Published in: J Med Chem

Ligand: GlyT1 inhibitor 51b (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.739999771118164 pKi
Reference (Journal): Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.
Published in: J Med Chem

Ligand: GSK931145 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.6 pIC50

Ligand: iclepertin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.279999732971191 pIC50
Reference (Journal): Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies.
Published in: Clin Transl Sci

Ligand: iclepertin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Evaluation of Pharmacokinetics and Pharmacodynamics of BI 425809, a Novel GlyT1 Inhibitor: Translational Studies.
Published in: Clin Transl Sci

Ligand: LY2365109 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas.
Published in: Neuropharmacology

Ligand: N-methyl-SSR504734 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.6 pIC50

Ligand: Org 24598 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: PF-03463275 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.940000057220459 pKi
Reference (Journal): The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter.
Published in: Bioorg Med Chem Lett

Ligand: (R)-NFPS (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas.
Published in: Neuropharmacology

Ligand: SSR-103800 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Characterization of SSR103800, a selective inhibitor of the glycine transporter-1 in models predictive of therapeutic activity in schizophrenia.
Published in: Pharmacol Biochem Behav

Ligand: [35S]ACPPB (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): A novel radioligand for glycine transporter 1: characterization and use in autoradiographic and in vivo brain occupancy studies.
Published in: Nucl Med Biol

Ligand: [3H]GSK931145 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Pharmacological characterisation of the GlyT-1 glycine transporter using two novel radioligands.
Published in: Neuropharmacology

Ligand: [3H]NFPS (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  pKd

Ligand: [3H]N-methyl-SSR504734 (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  pKd

Ligand: [3H](R)-NPTS (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): [3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.
Published in: Bioorg Med Chem Lett

Ligand: [3H]SB-733993 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Pharmacological characterisation of the GlyT-1 glycine transporter using two novel radioligands.
Published in: Neuropharmacology