Target Validation Information
Target ID T31391
Target Name Dipeptidyl peptidase IV
Target Type
Successful
Drug Potency against Target Sitagliptin Drug Info IC50 = 18 nM [552914]
NVP-DPP728 Drug Info IC50 = 22 nM [529262]
(S)-2-Amino-1-azetidin-1-yl-2-cyclohexyl-ethanone Drug Info Ki = 3350 nM [527697]
1-benzhydryl-3-butylpiperidin-4-amine Drug Info IC50 = 18600 nM [528776]
3-butyl-1-(naphthalen-1-yl)piperidin-4-amine Drug Info IC50 = 5300 nM [528776]
D-Val-L-boroPro Drug Info IC50 = 2300 nM [528804]
Linagliptin Drug Info IC50 = 1 nM [529477]
4-iodophenyl-alaninyl-(S)-2-cyano-pyrrolidine Drug Info Ki = 34 nM [527808]
(3S,4R)-3-butyl-1-phenylpiperidin-4-amine Drug Info IC50 = 3500 nM [528776]
1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine Drug Info Ki = 3400 nM [528652]
Linagliptin Drug Info IC50 = 1 nM [552914]
4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine Drug Info Ki = 2800 nM [528652]
L-Val-L-boroPro Drug Info IC50 = 1200 nM [528804]
(+/-)-6-(2-chlorophenyl)cyclohex-3-enamine Drug Info Ki = 820 nM [528488]
(S)-pyrrolidin-2-yl(thiazolidin-3-yl)methanone Drug Info IC50 = 607 nM [528694]
(S)-pyrrolidin-1-yl(pyrrolidin-2-yl)methanone Drug Info IC50 = 9700 nM [529175]
PF-00734200 Drug Info IC50 = 12.8 nM [530008]
L-Ala-L-boroPro Drug Info IC50 = 1400 nM [528804]
4-(2,4-dichlorophenyl)-1-tosylpyrrolidin-3-amine Drug Info Ki = 13000 nM [528652]
Alogliptin Drug Info IC50 = 7 nM [552914]
KR-62436 Drug Info IC50 = 490 nM [529964]
Cyclohexylglycine-(2S)-cyanopyrrolidine Drug Info IC50 = 12 nM [527953]
(R)-1-(2-aminoacetyl)pyrrolidin-2-ylboronic acid Drug Info Ki = 0.4 nM [529685]
(5-phenyl-3H-benzo[d]imidazol-4-yl)methanamine Drug Info IC50 = 12000 nM [529379]
ABT-279 Drug Info Ki = 1 nM [552914]
(S)-2-Amino-1-thiazolidin-3-yl-propane-1-thione Drug Info Ki = 7880 nM [526431]
DIPROTIN A Drug Info IC50 = 14400 nM [529207]
N-isoleucylthiazolidine Drug Info IC50 = 1660 nM [527953]
Saxagliptin Drug Info IC50 = 0.5 nM [552570]
Vildagliptin Drug Info IC50 = 3.5 nM [552570]
References
Ref 552914The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders. Mini Rev Med Chem. 2009 Feb;9(2):215-26.
Ref 529262Eur J Med Chem. 2008 Aug;43(8):1603-11. Epub 2007 Nov 29.A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.
Ref 527697Bioorg Med Chem Lett. 2005 Nov 1;15(21):4770-3.New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors.
Ref 528776Bioorg Med Chem Lett. 2007 Jun 1;17(11):2966-70. Epub 2007 Mar 25.1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
Ref 528776Bioorg Med Chem Lett. 2007 Jun 1;17(11):2966-70. Epub 2007 Mar 25.1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
Ref 528804J Med Chem. 2007 May 17;50(10):2391-8. Epub 2007 Apr 26.Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.
Ref 529477Bioorg Med Chem Lett. 2008 Jun 1;18(11):3158-62. Epub 2008 May 1.3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Ref 527808Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. Epub 2005 Oct 19.Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Ref 528776Bioorg Med Chem Lett. 2007 Jun 1;17(11):2966-70. Epub 2007 Mar 25.1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
Ref 528652Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Ref 552914The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders. Mini Rev Med Chem. 2009 Feb;9(2):215-26.
Ref 528652Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Ref 528804J Med Chem. 2007 May 17;50(10):2391-8. Epub 2007 Apr 26.Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.
Ref 528488J Med Chem. 2006 Nov 2;49(22):6439-42.Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Ref 528694Bioorg Med Chem Lett. 2007 May 1;17(9):2618-21. Epub 2007 Feb 8.[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors.
Ref 529175Bioorg Med Chem. 2008 Feb 15;16(4):1613-31. Epub 2007 Nov 17.Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group.
Ref 530008Bioorg Med Chem Lett. 2009 Apr 1;19(7):1991-5. Epub 2009 Feb 13.(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
Ref 528804J Med Chem. 2007 May 17;50(10):2391-8. Epub 2007 Apr 26.Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.
Ref 528652Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.
Ref 552914The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders. Mini Rev Med Chem. 2009 Feb;9(2):215-26.
Ref 529964Bioorg Med Chem. 2009 Mar 1;17(5):1783-802. Epub 2009 Jan 31.Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.
Ref 527953J Med Chem. 2006 Jan 12;49(1):373-80.2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
Ref 529685J Med Chem. 2008 Oct 9;51(19):6005-13. Epub 2008 Sep 11.Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.
Ref 529379Bioorg Med Chem Lett. 2008 Apr 1;18(7):2362-7. Epub 2008 Mar 4.Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.
Ref 552914The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders. Mini Rev Med Chem. 2009 Feb;9(2):215-26.
Ref 526431Bioorg Med Chem Lett. 2002 Oct 21;12(20):2825-8.Development of potent and selective dipeptidyl peptidase II inhibitors.
Ref 529207Bioorg Med Chem Lett. 2008 Jan 15;18(2):479-84. Epub 2007 Dec 3.Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin.
Ref 527953J Med Chem. 2006 Jan 12;49(1):373-80.2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
Ref 552570Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. Curr Top Med Chem. 2005;5(16):1623-37.
Ref 552570Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. Curr Top Med Chem. 2005;5(16):1623-37.

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