Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: dipeptidyl peptidase 8

Ligand: vildagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & UK (2007)
Primary target: no
Median affinity: 5.659999847412109 pIC50
Reference (Journal): Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead.
Published in: ChemMedChem

Ligand: tominostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
Published in: J Med Chem

Ligand: teneligliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2012), S Korea (2014)
Primary target: no
Median affinity: 6.590000152587891 pIC50
Reference (Journal): Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Published in: Bioorg Med Chem

Ligand: talabostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.819999694824219 pKi
Reference (Journal): Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.
Published in: J Med Chem

Ligand: ICeD-2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): A Phenotypic Screen Identifies Potent DPP9 Inhibitors Capable of Killing HIV-1 Infected Cells.
Published in: ACS Chem Biol

Ligand: compound 9 [PMID: 20718420] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.429999828338623 pIC50
Reference (Journal): Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
Published in: J Med Chem

Ligand: compound 42 [PMID: 37721854] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.21999979019165 pIC50
Reference (Journal): Highly Selective Inhibitors of Dipeptidyl Peptidase 9 (DPP9) Derived from the Clinically Used DPP4-Inhibitor Vildagliptin.
Published in: J Med Chem

Ligand: compound 24dd [PMID: 20684603] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.570000171661377 pKi
Reference (Journal): Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.
Published in: J Med Chem

Ligand: compound 18 [PMID: 15664838] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.900000095367432 pIC50
Reference (Journal): Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
Published in: Bioorg Med Chem Lett

Ligand: 1G244 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor.
Published in: Biochem Pharmacol