Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile | - |
Homo sapiens | |
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile | 66% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 30% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile | 84% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 73% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile | potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV | Homo sapiens | |
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile | potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV, 82% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 70% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | 85% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 70% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | 75% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 48% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | 64% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 7% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile | 77% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 56% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | 63% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 15% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | 89% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 59% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Rattus norvegicus | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile | - |
Homo sapiens | |
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile | 86% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 74% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one | - |
Homo sapiens | |
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one | 30% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 20% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | - |
Homo sapiens | |
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | - |
Rattus norvegicus | |
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide | - |
Homo sapiens | |
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide | 87% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 31% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | - |
Homo sapiens | |
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | 86% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 18% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose; 88% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 41% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide | - |
Homo sapiens | |
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide | 81% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 60% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus | |
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate | - |
Homo sapiens | |
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate | - |
Rattus norvegicus | |
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide | - |
Homo sapiens | |
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide | 66% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 30% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
blood plasma | - |
Homo sapiens | - |
blood plasma | - |
Rattus norvegicus | - |
Synonyms | Comment | Organism |
---|---|---|
CD26 | - |
Homo sapiens |
CD26 | - |
Rattus norvegicus |
dipeptidyl peptidase IV | - |
Homo sapiens |
dipeptidyl peptidase IV | - |
Rattus norvegicus |
DPP-IV | - |
Homo sapiens |
DPP-IV | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000034 | - |
- |
Homo sapiens | (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile | |
0.000015 | - |
- |
Homo sapiens | (2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile | |
0.000015 | - |
- |
Homo sapiens | (2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | |
0.000015 | - |
- |
Homo sapiens | N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide | |
0.000018 | - |
- |
Homo sapiens | (2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | |
0.000018 | - |
- |
Homo sapiens | (2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | |
0.000019 | - |
- |
Homo sapiens | 3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | |
0.000019 | - |
- |
Homo sapiens | 3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide | |
0.00002 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | |
0.000024 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | |
0.000024 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | |
0.000026 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile | |
0.000027 | - |
- |
Homo sapiens | 3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | |
0.000027 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile | |
0.000027 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile | |
0.000029 | - |
- |
Homo sapiens | 3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide | |
0.00003 | - |
- |
Homo sapiens | (3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one | |
0.00003 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | |
0.000032 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile | |
0.000039 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | |
0.00005 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile | |
0.000051 | - |
- |
Homo sapiens | (2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile | |
0.000063 | - |
- |
Homo sapiens | ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate | |
0.000066 | - |
- |
Homo sapiens | (2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile | |
0.000071 | - |
- |
Homo sapiens | (2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile | |
0.000093 | - |
- |
Homo sapiens | (2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile | |
0.000116 | - |
- |
Homo sapiens | 3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | |
0.00016 | - |
- |
Homo sapiens | (2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile |