Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T31391 | Target Info | |||
| Target Name | Dipeptidyl peptidase 4 (DPP-4) | ||||
| Synonyms |
Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP
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| Target Type | Successful Target | ||||
| Gene Name | DPP4 | ||||
| Biochemical Class | Peptidase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Muscarinic acetylcholine receptor M1 (CHRM1) | Successful Target | ||||
| UniProt ID | ACM1_HUMAN | |||||
| Gene Name | CHRM1 | |||||
| Synonyms |
M1 receptor
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| Representative Drug(s) | Linagliptin | Drug Info | IC50 = 295 nM | [1] | ||
| Co-Target Name | Dipeptidyl peptidase 9 (DPP-9) | Clinical trial Target | ||||
| UniProt ID | DPP9_HUMAN | |||||
| Gene Name | DPP9 | |||||
| Synonyms |
Dipeptidyl peptidase-like protein 9; Dipeptidyl peptidase IX; Dipeptidyl peptidase IV-related protein 2; DPRP2; DPRP-2; DPP IX; DPLP9; DP9
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| Representative Drug(s) | Vildagliptin | Drug Info | IC50 = 50 nM | Click to Show More | [2] | |
| 2 | Anagliptin | Drug Info | IC50 = 60 nM | [3] | ||
| 3 | Saxagliptin | Drug Info | Ki = 71 nM | [5] | ||
| 4 | Teneligliptin | Drug Info | IC50 = 540 nM | [6] | ||
| 5 | Dutogliptin | Drug Info | IC50 = 663 nM | [7] | ||
| Co-Target Name | Dipeptidyl peptidase 8 (DPP-8) | Clinical trial Target | ||||
| UniProt ID | DPP8_HUMAN | |||||
| Gene Name | DPP8 | |||||
| Synonyms |
Prolyl dipeptidase DPP8; MSTP141; MSTP135; MSTP097; Dipeptidyl peptidase VIII; Dipeptidyl peptidase IV-related protein 1; DPRP1; DPRP-1; DPP VIII; DP8
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| Representative Drug(s) | Anagliptin | Drug Info | IC50 = 68 nM | Click to Show More | [3] | |
| 2 | Saxagliptin | Drug Info | Ki = 130 nM | [5] | ||
| 3 | Teneligliptin | Drug Info | IC50 = 260 nM | [6] | ||
| 4 | Vildagliptin | Drug Info | Ki = 810 nM | [8] | ||
| Co-Target Name | Prolyl endopeptidase FAP (FAP) | Clinical trial Target | ||||
| UniProt ID | SEPR_HUMAN | |||||
| Gene Name | FAP | |||||
| Synonyms |
Integral membrane serine protease; Fibroblast activation protein alpha; FAP; Antiplasmin-cleaving enzyme; APCE; 170-kDa melanoma membrane-bound gelatinase
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| Representative Drug(s) | Linagliptin | Drug Info | IC50 = 70.8 nM | [4] | ||
| Co-Target Name | Dipeptidyl-peptidase 7 (DPP7) | Patented-recorded Target | ||||
| UniProt ID | DPP2_HUMAN | |||||
| Gene Name | DPP7 | |||||
| Synonyms |
Quiescent cell proline dipeptidase; QPP; Dipeptidyl peptidase II; Dipeptidyl peptidase 7; Dipeptidyl peptidase 2; Dipeptidyl aminopeptidase II; DPP2; DPP II
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| Representative Drug(s) | Dutogliptin | Drug Info | IC50 ~ 400 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1464-8. | ||||
| REF 2 | Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study. Eur J Med Chem. 2019 Oct 15;180:509-523. | ||||
| REF 3 | 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. Bioorg Med Chem. 2011 Dec 1;19(23):7221-7. | ||||
| REF 4 | Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. ACS Med Chem Lett. 2016 Mar 12;7(5):498-501. | ||||
| REF 5 | Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes. J Med Chem. 2006 Oct 19;49(21):6416-20. | ||||
| REF 6 | 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. Bioorg Med Chem. 2012 Oct 1;20(19):5705-19. | ||||
| REF 7 | Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold. Medchemcomm. 2014;5:1700-7. | ||||
| REF 8 | Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Bioorg Med Chem. 2012 Oct 1;20(19):5864-83. | ||||
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