Target family: S9: Prolyl oligopeptidase (type: enzyme)
Target: dipeptidyl peptidase 4

Ligand: ZY15557 (Synthetic organic)
Interaction type: Inhibitor
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 8.260000228881836 pKi
Reference (Journal): ZY15557, a novel, long acting inhibitor of dipeptidyl peptidase-4, for the treatment of Type 2 diabetes mellitus.
Published in: Br J Pharmacol

Ligand: vildagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & UK (2007)
Primary target: yes
Median affinity: 7.800000190734863 pKi
Reference (Journal): Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes.
Published in: Curr Drug Targets

Ligand: vildagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & UK (2007)
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead.
Published in: ChemMedChem

Ligand: teneligliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2012), S Korea (2014)
Primary target: yes
Median affinity: 9.430000305175781 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: 9.739999771118164 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: sitagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2006), EMA (2007)
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Nature of action of Sitagliptin, the dipeptidyl peptidase-IV inhibitor in diabetic animals.
Published in: Indian J Pharmacol

Ligand: saxagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2009)
Primary target: yes
Median affinity: 9.199999809265137 pKi
Reference (Journal): Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes.
Published in: Curr Drug Targets

Ligand: omarigliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pKi
Reference (Journal): Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: compound 9 [PMID: 20718420] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.
Published in: J Med Chem

Ligand: compound 24dd [PMID: 20684603] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.850000381469727 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 1 [Xiao et al. 2014] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold.
Published in: ChinChem Lett

Ligand: begelomab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 10 pKd
Reference (Patent): Anti-CD26 Antibodies and Uses Thereof.

Ligand: anagliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2012)
Primary target: no
Median affinity: 8.420000076293945 pIC50
Reference (Journal): Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.
Published in: Bioorg Med Chem

Ligand: alogliptin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2013)
Primary target: yes
Median affinity: 8.5 pIC50
Reference (Journal): Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.
Published in: Eur J Med Chem