Compounds > nvp-dpp728
Page last updated: 2024-12-11

nvp-dpp728

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Cross-References

ID SourceID
PubMed CID9796290
CHEMBL ID77538
SCHEMBL ID160102
MeSH IDM0336506

Synonyms (25)

Synonym
bdbm11113
chembl77538 ,
nvp-dpp728
6-{[2-({2-[(2s)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino}pyridine-3-carbonitrile
bmcl15687 compound 2
cyano-(s)-pyrrolidine deriv. 1
cyanopyrrolidine derivative 2
nvp-728
nvp dpp 728 dihydrochloride
247016-69-9
SCHEMBL160102
unii-hcx5m1yiom
nvp-dpp-728
DTXSID70624696
(2s)-1-(2-((2-((5-cyano-2-pyridyl)amino)ethyl)amino)acetyl)pyrrolidine-2-carbonitrile
AKOS030529265
mfcd05260933
6-[[2-[[2-(2s)-2-cyano-1-pyrrolidinyl]-2-oxoethyl]amino]ethyl]amino-3-pyridinecarbononitrile
HCX5M1YIOM ,
3-pyridinecarbonitrile, 6-((2-((2-((2s)-2-cyano-1-pyrrolidinyl)-2-oxoethyl)amino)ethyl)amino)-
6-(2-((2-((2s)-2-cyanopyrrolidin-1-yl)-2-oxo-ethyl)amino)ethylamino)pyridine-3-carbonitrile
1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(s)-pyrroli-dine
HY-14292
CS-0003258
3-pyridinecarbonitrile, 6-[[2-[[2-[(2s)-2-cyano-1-pyrrolidinyl]-2-oxoethyl]amino]ethyl]amino]-

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" One compound, NVP-DPP728 (2), is profiled as a potent, selective, and short-acting DPP-IV inhibitor that has excellent oral bioavailability and potent antihyperglycemic activity."( 1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
Brinkman, JA; Dunning, BE; Hughes, TE; Mangold, BL; Mone, MD; Naderi, GB; Russell, ME; Villhauer, EB; Weldon, SC, 2002)		0.67
" The results suggest that 12j is a potent, stable, selective DPP-IV inhibitor possessing excellent oral bioavailability and potent antihyperglycemic activity with potential for once-a-day administration."( 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
Brinkman, JA; Burkey, BF; Dunning, BE; Hughes, TE; Mangold, BL; Naderi, GB; Prasad, K; Russell, ME; Villhauer, EB, 2003)		0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Heat shock protein HSP 90-betaHomo sapiens (human)IC50 (µMol)4.57300.00100.683610.0000AID258960
Dipeptidyl peptidase 4Rattus norvegicus (Norway rat)IC50 (µMol)2.28760.00231.21555.0000AID240973; AID258960
Dipeptidyl peptidase 4Homo sapiens (human)IC50 (µMol)3.47850.00010.444410.0000AID1127772; AID1796783; AID1796870; AID240687; AID240861; AID241057; AID241330; AID258959; AID349306; AID393688; AID56061; AID56063; AID56215; AID685045
Dipeptidyl peptidase 4Homo sapiens (human)Ki0.02170.00000.34142.2000AID1796607; AID1796753; AID258583
Dipeptidyl peptidase 4Mus musculus (house mouse)IC50 (µMol)0.05300.04600.05000.0530AID258959
Dipeptidyl peptidase 8Homo sapiens (human)IC50 (µMol)8.44570.00192.653210.0000AID1796783; AID1796870; AID240546; AID241294; AID258960
Dipeptidyl peptidase 2Homo sapiens (human)IC50 (µMol)30.74380.00020.93166.6000AID161119; AID163294; AID1796783; AID1796870; AID241293; AID241356; AID258961
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
telomere maintenance via telomeraseHeat shock protein HSP 90-betaHomo sapiens (human)
placenta developmentHeat shock protein HSP 90-betaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-betaHomo sapiens (human)
virion attachment to host cellHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of transforming growth factor beta receptor signaling pathwayHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal ubiquitin-dependent protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of apoptotic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of cell differentiationHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
regulation of cell cycleHeat shock protein HSP 90-betaHomo sapiens (human)
chaperone-mediated protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to interleukin-4Heat shock protein HSP 90-betaHomo sapiens (human)
supramolecular fiber organizationHeat shock protein HSP 90-betaHomo sapiens (human)
negative regulation of proteasomal protein catabolic processHeat shock protein HSP 90-betaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-betaHomo sapiens (human)
positive regulation of protein localization to cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-betaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-betaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-betaHomo sapiens (human)
behavioral fear responseDipeptidyl peptidase 4Homo sapiens (human)
response to hypoxiaDipeptidyl peptidase 4Homo sapiens (human)
proteolysisDipeptidyl peptidase 4Homo sapiens (human)
cell adhesionDipeptidyl peptidase 4Homo sapiens (human)
positive regulation of cell population proliferationDipeptidyl peptidase 4Homo sapiens (human)
negative regulation of extracellular matrix disassemblyDipeptidyl peptidase 4Homo sapiens (human)
peptide hormone processingDipeptidyl peptidase 4Homo sapiens (human)
receptor-mediated endocytosis of virus by host cellDipeptidyl peptidase 4Homo sapiens (human)
T cell costimulationDipeptidyl peptidase 4Homo sapiens (human)
regulation of cell-cell adhesion mediated by integrinDipeptidyl peptidase 4Homo sapiens (human)
locomotory exploration behaviorDipeptidyl peptidase 4Homo sapiens (human)
psychomotor behaviorDipeptidyl peptidase 4Homo sapiens (human)
T cell activationDipeptidyl peptidase 4Homo sapiens (human)
endothelial cell migrationDipeptidyl peptidase 4Homo sapiens (human)
symbiont entry into host cellDipeptidyl peptidase 4Homo sapiens (human)
receptor-mediated virion attachment to host cellDipeptidyl peptidase 4Homo sapiens (human)
negative chemotaxisDipeptidyl peptidase 4Homo sapiens (human)
membrane fusionDipeptidyl peptidase 4Homo sapiens (human)
negative regulation of neutrophil chemotaxisDipeptidyl peptidase 4Homo sapiens (human)
glucagon processingDipeptidyl peptidase 4Homo sapiens (human)
proteolysisDipeptidyl peptidase 8Homo sapiens (human)
apoptotic processDipeptidyl peptidase 8Homo sapiens (human)
immune responseDipeptidyl peptidase 8Homo sapiens (human)
negative regulation of programmed cell deathDipeptidyl peptidase 8Homo sapiens (human)
proteolysisDipeptidyl peptidase 2Homo sapiens (human)
lysosomal protein catabolic processDipeptidyl peptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
double-stranded RNA bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein kinase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-betaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-betaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-betaHomo sapiens (human)
heat shock protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
peptide bindingHeat shock protein HSP 90-betaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
cadherin bindingHeat shock protein HSP 90-betaHomo sapiens (human)
protein dimerization activityHeat shock protein HSP 90-betaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-betaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-betaHomo sapiens (human)
receptor ligand inhibitor activityHeat shock protein HSP 90-betaHomo sapiens (human)
histone methyltransferase bindingHeat shock protein HSP 90-betaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-betaHomo sapiens (human)
virus receptor activityDipeptidyl peptidase 4Homo sapiens (human)
protease bindingDipeptidyl peptidase 4Homo sapiens (human)
aminopeptidase activityDipeptidyl peptidase 4Homo sapiens (human)
serine-type endopeptidase activityDipeptidyl peptidase 4Homo sapiens (human)
signaling receptor bindingDipeptidyl peptidase 4Homo sapiens (human)
protein bindingDipeptidyl peptidase 4Homo sapiens (human)
serine-type peptidase activityDipeptidyl peptidase 4Homo sapiens (human)
dipeptidyl-peptidase activityDipeptidyl peptidase 4Homo sapiens (human)
identical protein bindingDipeptidyl peptidase 4Homo sapiens (human)
protein homodimerization activityDipeptidyl peptidase 4Homo sapiens (human)
chemorepellent activityDipeptidyl peptidase 4Homo sapiens (human)
aminopeptidase activityDipeptidyl peptidase 8Homo sapiens (human)
protein bindingDipeptidyl peptidase 8Homo sapiens (human)
serine-type peptidase activityDipeptidyl peptidase 8Homo sapiens (human)
dipeptidyl-peptidase activityDipeptidyl peptidase 8Homo sapiens (human)
aminopeptidase activityDipeptidyl peptidase 2Homo sapiens (human)
serine-type peptidase activityDipeptidyl peptidase 2Homo sapiens (human)
serine-type exopeptidase activityDipeptidyl peptidase 2Homo sapiens (human)
dipeptidyl-peptidase activityDipeptidyl peptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
COP9 signalosomeHeat shock protein HSP 90-betaHomo sapiens (human)
protein folding chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionHeat shock protein HSP 90-betaHomo sapiens (human)
nucleusHeat shock protein HSP 90-betaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-betaHomo sapiens (human)
membraneHeat shock protein HSP 90-betaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-betaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-betaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-betaHomo sapiens (human)
dynein axonemal particleHeat shock protein HSP 90-betaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-betaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-betaHomo sapiens (human)
aryl hydrocarbon receptor complexHeat shock protein HSP 90-betaHomo sapiens (human)
HSP90-CDC37 chaperone complexHeat shock protein HSP 90-betaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-betaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-betaHomo sapiens (human)
cytosolHeat shock protein HSP 90-betaHomo sapiens (human)
extracellular regionDipeptidyl peptidase 4Homo sapiens (human)
lysosomal membraneDipeptidyl peptidase 4Homo sapiens (human)
plasma membraneDipeptidyl peptidase 4Homo sapiens (human)
focal adhesionDipeptidyl peptidase 4Homo sapiens (human)
cell surfaceDipeptidyl peptidase 4Homo sapiens (human)
membraneDipeptidyl peptidase 4Homo sapiens (human)
apical plasma membraneDipeptidyl peptidase 4Homo sapiens (human)
lamellipodiumDipeptidyl peptidase 4Homo sapiens (human)
endocytic vesicleDipeptidyl peptidase 4Homo sapiens (human)
lamellipodium membraneDipeptidyl peptidase 4Homo sapiens (human)
membrane raftDipeptidyl peptidase 4Homo sapiens (human)
intercellular canaliculusDipeptidyl peptidase 4Homo sapiens (human)
extracellular exosomeDipeptidyl peptidase 4Homo sapiens (human)
plasma membraneDipeptidyl peptidase 4Homo sapiens (human)
cytoplasmDipeptidyl peptidase 8Homo sapiens (human)
cytoplasmDipeptidyl peptidase 8Homo sapiens (human)
cytosolDipeptidyl peptidase 8Homo sapiens (human)
extracellular regionDipeptidyl peptidase 2Homo sapiens (human)
Golgi apparatusDipeptidyl peptidase 2Homo sapiens (human)
azurophil granule lumenDipeptidyl peptidase 2Homo sapiens (human)
intracellular membrane-bounded organelleDipeptidyl peptidase 2Homo sapiens (human)
extracellular exosomeDipeptidyl peptidase 2Homo sapiens (human)
vesicleDipeptidyl peptidase 2Homo sapiens (human)
vesicleDipeptidyl peptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (67)

Assay IDTitleYearJournalArticle
AID16497Cmax after an oral dose of 10 umol/Kg in male Sprague-Dawley rats2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID56059In vitro inhibitory activity against Dipeptidyl peptidase II (DPP II) obtained form bovine kidney homogenate2003Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID17790Absolute bioavailability in maleSprague-Dawley rats2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID393688Inhibition of DPP42009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.
AID15505Clearance from plasma in male cynomolgus monkeys2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID56207In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from rat plasma.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685056Tmax in C57BL/6J mouse at 20 mg/kg, po administered as single dose2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID22409Steady state volume of distribution in male Sprague-Dawley rats2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685050Antidiabetic activity against C57BL/6J mouse assessed as reduction serum glucose AUC levels at 20 mg/kg, po measured up to 30 mins by IPGTT method2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID258583Inhibition of human DPP42006Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
AID685047Selectivity ratio of IC50 for human DPP8 to IC50 for human DPP42012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID241330Inhibitory concentration against dipeptidylpeptidase IV2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID17789Absolute bioavailability in male cynomolgus monkeys2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID127118in vivo ability to inhibit plasma DPP-IV activity throughout OGTT study2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID349306Inhibition of human DPP4 expressed in baculovirus system2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.
AID240546Inhibitory concentration against Dipeptidylpeptidase 82005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
AID241293Inhibitory concentration against dipeptidylpeptidase 2 2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID23793Half-life (t1/2) after an oral dose of 1 uM/Kg in monkey2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685051Antidiabetic activity against C57BL/6J mouse assessed as reduction serum glucose AUC levels at 20 mg/kg, po measured up to 60 mins by IPGTT method2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID56063In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from Caco-2 cells.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685048Selectivity ratio of IC50 for human DPP9 to IC50 for human DPP42012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID386507Inhibition of DPP4 in human plasma by fluorescence assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.
AID56205Inhibition of plasma Dipeptidyl peptidase IV activity for ~4 hours after an oral dosage of 100 mg in human2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID16498Cmax after an oral dose of 10 umol/Kg in male cynomolgus monkeys2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID56219In vitro inhibitory activity against Dipeptidylpeptidase II (DPP-II) extracted from bovine kidney homogenate2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID161119In vitro inhibitory activity against Post-proline cleaving enzyme (PPCE) obtained from human erythrocytes2003Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID240687Inhibitory concentration against Dipeptidylpeptidase IV [DPP-IV]2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
AID56191Inhibitory activity against Dipeptidyl peptidase IV (DPP IV) obtained from human plasma2003Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685046Selectivity ratio of IC50 for human DPP2 to IC50 for human DPP42012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID240861Inhibitory concentration against dipeptidylpeptidase IV2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
AID685045Inhibition of human DPP4 expressed in baculovirus expression system using Gly-Pro-AMC substrate incubated or 30 mins by fluorescence based assay2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID241356Inhibitory concentration against DPP-II [Quiescent cell proline dipeptidase] or DPP-VII2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.
AID1127772Inhibition of DPP4 (unknown origin)2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?
AID685053Antidiabetic activity against C57BL/6J mouse assessed as reduction serum glucose AUC levels at 20 mg/kg, po measured up to 240 mins by IPGTT method2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID56061Inhibition of human dipeptidyl peptidase IV (DPP IV) obtained from human colonic carcinoma cells2003Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685052Antidiabetic activity against C57BL/6J mouse assessed as reduction serum glucose AUC levels at 20 mg/kg, po measured up to 120 mins by IPGTT method2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID258959Inhibitory activity against DPP42006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
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.
AID56208Inhibitory activity against Dipeptidyl peptidase IV (DPP IV) obtained from rat plasma2003Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID241294Inhibitory concentration against dipeptidylpeptidase 82005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID56190In vitro inhibitory activity against Dipeptidyl peptidase IV (DPP-IV) extracted from human plasma.2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID127147In vivo ability to reduce the plasma glucose levels ( in 0-90 minutes glucose AUC) in monkey compared to control during an oral glucose tolerance test (PGTT)2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID127109In vivo ability to inhibit plasma DPP-IV activity 25 minutes post dosing when administered 30 minutes before an OGTT study2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID15504Clearance from plasma in male Sprague-Dawley rats2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685057Cmax in C57BL/6J mouse at 20 mg/kg, po administered as single dose2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID23794Half-life (t1/2) after an oral dose of 100 mg in human2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685059AUC (0 to alpha) in C57BL/6J mouse at 20 mg/kg, po administered as single dose2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID685054Antidiabetic activity in fed db/db mouse assessed as reduction in serum glucose AUC levels at 20 mg/kg, po administered as single dose measured up to 2 hrs2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID163294Inhibitory activity against quiescent cell prolyl peptidase (QPP).2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
AID685058Half life in C57BL/6J mouse at 20 mg/kg, po administered as single dose2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID284824Inhibition of DPP4 in human plasma by fluorescence assay2007Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors.
AID685060Oral bioavailability in C57BL/6J mouse at 20 mg/kg administered as single dose2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID237054Half life was determined2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
AID127146In vivo ability to reduce the peak plasma glucose levels in monkey compared to control ( 88 +/- 3 mg/dL) during an oral glucose tolerance test (OGTT)2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID685055Antidiabetic activity in fed db/db mouse assessed as reduction in serum glucose AUC levels at 20 mg/kg, po administered as single dose measured after 8 hrs2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID685049Antidiabetic activity against C57BL/6J mouse assessed as reduction serum glucose AUC levels at 20 mg/kg, po by IPGTT method2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
Long-acting peptidomimetics based DPP-IV inhibitors.
AID156388In vitro inhibitory activity against post proline-cleaving enzyme (PPCE) extracted from human erythrocytes2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID56215Inhibitory activity against dipeptidylpeptidase IV.2004Bioorganic & medicinal chemistry letters, Jan-05, Volume: 14, Issue:1
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
AID22410Steady state volume of distribution male cynomolgus monkeys2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID56060Inhibition of plasma Dipeptidyl peptidase IV activity for 4 hours after an oral dosage of 1 uM/Kg in monkey2002Journal of medicinal chemistry, Jun-06, Volume: 45, Issue:12
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
AID241057Inhibitory concentration against human dipeptidylpeptidase IV2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
AID240973Inhibitory concentration against rat dipeptidylpeptidase IV2005Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
AID258960Inhibitory activity against DPP82006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
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.
AID258961Inhibitory activity against DPP22006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
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.
AID1796870Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2004.11.023: \\Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.\\2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.
AID1796783Dipeptidyl Peptidase Inhibition Assay from Article 10.1021/jm0507781: \\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 2006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
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.
AID1796753Fluorogenic Assay from Article 10.1016/j.bmcl.2004.01.019: \\Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.\\2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
AID1796607DPPIV Inhibition Assay from Article 10.1016/j.bmcl.2005.09.037: \\Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.\\2006Bioorganic & medicinal chemistry letters, Jan-01, Volume: 16, Issue:1
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (87.50)29.6817
2010's2 (12.50)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.61 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.26 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (18.75%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (81.25%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		3.5720triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
vildagliptin
[no description available]		5.4980amino acid amide
talabostat
talabostat: an antineoplastic agent; structure in first source		3.1210
sulphostin
sulphostin: isolated from Streptomyces; structure in first source		2.0410
linagliptin
Linagliptin: A purine and quinazoline derivative that functions as an INCRETIN and DIPEPTIDYL-PEPTIDASE IV INHIBTOR. It is used as a HYPOGLYCEMIC AGENT in the treatment of TYPE II DIABETES MELLITUS.. linagliptin : A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type II diabetes.		3.1910aminopiperidine;
quinazolines		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
alanylpyrrolidine-boronic acid
[no description available]		3.1410
bms 477118
[no description available]		4.0820adamantanes;
azabicycloalkane;
monocarboxylic acid amide;
nitrile;
tertiary alcohol		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
alogliptin
alogliptin: structure in first source. alogliptin : A piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of type 2 diabetes.		3.1910nitrile;
piperidines;
primary amino compound;
pyrimidines		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus, Adult-Onset
[description not available]		04.6640
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		04.6640