| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T31391 | ||||
| Target Name | Dipeptidyl peptidase 4 (DPP-4) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Sitagliptin | Drug Info | IC50 = 18 nM | [19] | |
| Vildagliptin | Drug Info | IC50 = 3.5 nM | [18] | ||
| ABT-279 | Drug Info | Ki = 1 nM | [19] | ||
| Alogliptin | Drug Info | IC50 = 7 nM | [19] | ||
| Linagliptin | Drug Info | IC50 = 1 nM | [19] | ||
| Saxagliptin | Drug Info | IC50 = 0.5 nM | [18] | ||
| (+/-)-6-(2-chlorophenyl)cyclohex-3-enamine | Drug Info | Ki = 820 nM | [5] | ||
| (3S,4R)-3-butyl-1-phenylpiperidin-4-amine | Drug Info | IC50 = 3500 nM | [8] | ||
| (5-phenyl-3H-benzo[d]imidazol-4-yl)methanamine | Drug Info | IC50 = 12000 nM | [13] | ||
| (R)-1-(2-aminoacetyl)pyrrolidin-2-ylboronic acid | Drug Info | Ki = 0.4 nM | [15] | ||
| (S)-2-Amino-1-azetidin-1-yl-2-cyclohexyl-ethanone | Drug Info | Ki = 3350 nM | [2] | ||
| (S)-2-Amino-1-thiazolidin-3-yl-propane-1-thione | Drug Info | Ki = 7880 nM | [1] | ||
| (S)-pyrrolidin-1-yl(pyrrolidin-2-yl)methanone | Drug Info | IC50 = 9700 nM | [10] | ||
| (S)-pyrrolidin-2-yl(thiazolidin-3-yl)methanone | Drug Info | IC50 = 607 nM | [7] | ||
| 1-benzhydryl-3-butylpiperidin-4-amine | Drug Info | IC50 = 18600 nM | [8] | ||
| 1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine | Drug Info | Ki = 3400 nM | [6] | ||
| 3-butyl-1-(naphthalen-1-yl)piperidin-4-amine | Drug Info | IC50 = 5300 nM | [8] | ||
| 4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine | Drug Info | Ki = 2800 nM | [6] | ||
| 4-(2,4-dichlorophenyl)-1-tosylpyrrolidin-3-amine | Drug Info | Ki = 13000 nM | [6] | ||
| 4-iodophenyl-alaninyl-(S)-2-cyano-pyrrolidine | Drug Info | Ki = 34 nM | [3] | ||
| Cyclohexylglycine-(2S)-cyanopyrrolidine | Drug Info | IC50 = 12 nM | [4] | ||
| D-Val-L-boroPro | Drug Info | IC50 = 2300 nM | [9] | ||
| DIPROTIN A | Drug Info | IC50 = 14400 nM | [11] | ||
| KR-62436 | Drug Info | IC50 = 490 nM | [16] | ||
| L-Ala-L-boroPro | Drug Info | IC50 = 1400 nM | [9] | ||
| L-Val-L-boroPro | Drug Info | IC50 = 1200 nM | [9] | ||
| Linagliptin | Drug Info | IC50 = 1 nM | [14] | ||
| N-isoleucylthiazolidine | Drug Info | IC50 = 1660 nM | [4] | ||
| NVP-DPP728 | Drug Info | IC50 = 22 nM | [12] | ||
| PF-00734200 | Drug Info | IC50 = 12.8 nM | [17] | ||
| References | |||||
| REF 1 | Development of potent and selective dipeptidyl peptidase II inhibitors. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2825-8. | ||||
| REF 2 | New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4770-3. | ||||
| REF 3 | Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. | ||||
| REF 4 | 2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioava... J Med Chem. 2006 Jan 12;49(1):373-80. | ||||
| REF 5 | 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)... J Med Chem. 2006 Nov 2;49(22):6439-42. | ||||
| REF 6 | Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibito... Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. | ||||
| REF 7 | [(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors. Bioorg Med Chem Lett. 2007 May 1;17(9):2618-21. | ||||
| REF 8 | 1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):2966-70. | ||||
| REF 9 | Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines. J Med Chem. 2007 May 17;50(10):2391-8. | ||||
| REF 10 | Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group. Bioorg Med Chem. 2008 Feb 15;16(4):1613-31. | ||||
| REF 11 | Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin. Bioorg Med Chem Lett. 2008 Jan 15;18(2):479-84. | ||||
| REF 12 | A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors. Eur J Med Chem. 2008 Aug;43(8):1603-11. | ||||
| REF 13 | Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2362-7. | ||||
| REF 14 | 3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3158-62. | ||||
| REF 15 | Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. | ||||
| REF 16 | Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes. Bioorg Med Chem. 2009 Mar 1;17(5):1783-802. | ||||
| REF 17 | (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 dipepti... Bioorg Med Chem Lett. 2009 Apr 1;19(7):1991-5. | ||||
| REF 18 | Inhibitors of dipeptidyl peptidase IV--recent advances and structural views. Curr Top Med Chem. 2005;5(16):1623-37. | ||||
| REF 19 | The prolyl-aminodipeptidases and their inhibitors as therapeutic targets for fibrogenic disorders. Mini Rev Med Chem. 2009 Feb;9(2):215-26. | ||||
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