Target family: SLC15 family of peptide transporters (type: transporter)
Target: Peptide transporter 1

Ligand: 4-AMBA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 2.299999952316284 pKi
Reference (Journal): 4-aminomethylbenzoic acid is a non-translocated competitive inhibitor of the epithelial peptide transporter PepT1.
Published in: J Physiol (Lond.)

Ligand: (3,5)-[19F]2-Phe-ψ-Ala (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Possible utility of peptide-transporter-targeting [<sup>19</sup>F]dipeptides for visualization of the biodistribution of cancers by nuclear magnetic resonance imaging.
Published in: Int J Pharm

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Recognition and transport characteristics of nonpeptidic compounds by basolateral peptide transporter in Caco-2 cells.
Published in: J Pharmacol Exp Ther

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Transport of angiotensin-converting enzyme inhibitors by H+/peptide transporters revisited.
Published in: J Pharmacol Exp Ther

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): A novel inhibitor of the mammalian peptide transporter PEPT1.
Published in: Biochemistry

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2.
Published in: J Biol Chem

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification of the histidine residues involved in substrate recognition by a rat H+/peptide cotransporter, PEPT1.
Published in: FEBS Lett

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The predominant contribution of oligopeptide transporter PepT1 to intestinal absorption of beta-lactam antibiotics in the rat small intestine.
Published in: J Pharm Pharmacol

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Interaction of anionic cephalosporins with the intestinal and renal peptide transporters PEPT 1 and PEPT 2.
Published in: Biochim Biophys Acta

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Valacyclovir: a substrate for the intestinal and renal peptide transporters PEPT1 and PEPT2.
Published in: Biochem Biophys Res Commun

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Direct evidence for peptide transporter (PepT1)-mediated uptake of a nonpeptide prodrug, valacyclovir.
Published in: Biochem Biophys Res Commun

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Application of Intestinal Epithelial Cells Differentiated from Human Induced Pluripotent Stem Cells for Studies of Prodrug Hydrolysis and Drug Absorption in the Small Intestine.
Published in: Drug Metab Dispos

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Inhibitory effect of novel oral hypoglycemic agent nateglinide (AY4166) on peptide transporters PEPT1 and PEPT2.
Published in: Eur J Pharmacol

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
Published in: J Med Chem

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.
Published in: Eur J Pharm Biopharm

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Circumvention of P-gp and MRP2 mediated efflux of lopinavir by a histidine based dipeptide prodrug.
Published in: Int J Pharm

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2.
Published in: Br J Pharmacol

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): High-affinity interaction of sartans with H+/peptide transporters.
Published in: Drug Metab Dispos

Ligand: [14C]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells.
Published in: Am J Physiol

Ligand: [18F]FEPPG (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The Radiolabeling of a Gly-Sar Dipeptide Derivative with Flourine-18 and Its Use as a Potential Peptide Transporter PET Imaging Agent.
Published in: Molecules

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): PepT1-mediated epithelial transport of dipeptides and cephalexin is enhanced by luminal leptin in the small intestine.
Published in: J Clin Invest

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Interactions of the dipeptide ester prodrugs of acyclovir with the intestinal oligopeptide transporter: competitive inhibition of glycylsarcosine transport in human intestinal cell line-Caco-2.
Published in: J Pharmacol Exp Ther

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): 5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.
Published in: Pharm Res

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells.
Published in: Pharm Res

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Molecular interactions between dipeptides, drugs and the human intestinal H+ -oligopeptide cotransporter hPEPT1.
Published in: J Physiol (Lond.)

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Significance and regional dependency of peptide transporter (PEPT) 1 in the intestinal permeability of glycylsarcosine: in situ single-pass perfusion studies in wild-type and Pept1 knockout mice.
Published in: Drug Metab Dispos

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Correlation between epithelial cell permeability of cephalexin and expression of intestinal oligopeptide transporter.
Published in: J Pharmacol Exp Ther

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Interactions of amoxicillin and cefaclor with human renal organic anion and peptide transporters.
Published in: Drug Metab Dispos

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Effects of frequently used pharmaceutical excipients on the organic cation transporters 1-3 and peptide transporters 1/2 stably expressed in MDCKII cells.
Published in: Eur J Pharm Biopharm

Ligand: [3H]GlySar (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Expression profile and functional activity of peptide transporters in prostate cancer cells.
Published in: Mol Pharm

Ligand: [3H]-IPP (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Sodium caprate enables the blood pressure-lowering effect of Ile-Pro-Pro and Leu-Lys-Pro in spontaneously hypertensive rats by indirectly overcoming PepT1 inhibition.
Published in: Eur J Pharm Biopharm

Ligand: [3H]-IPP (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Evaluation of PepT1 transport of food-derived antihypertensive peptides, Ile-Pro-Pro and Leu-Lys-Pro using in vitro, ex vivo and in vivo transport models.
Published in: Eur J Pharm Biopharm

Ligand: [3H]-LKP (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Evaluation of PepT1 transport of food-derived antihypertensive peptides, Ile-Pro-Pro and Leu-Lys-Pro using in vitro, ex vivo and in vivo transport models.
Published in: Eur J Pharm Biopharm

Ligand: [3H]-LKP (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Sodium caprate enables the blood pressure-lowering effect of Ile-Pro-Pro and Leu-Lys-Pro in spontaneously hypertensive rats by indirectly overcoming PepT1 inhibition.
Published in: Eur J Pharm Biopharm

Ligand: [3H]mirogabalin (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Mirogabalin, a novel &#x3b1;<sub>2</sub>&#x3b4; ligand, is not a substrate of LAT1, but of PEPT1, PEPT2, OAT1, OAT3, OCT2, MATE1 and MATE2-K.
Published in: Xenobiotica