| Sitagliptin | IC50 | 100000.0 [1] |
| Vildagliptin | IC50 | 20000.0 [1] |
| Linagliptin | IC50 | 70.8 [1], 89.0 [2], 370.0 [3] |
| Alogliptin | IC50 | 100000.0 [1] |
| Talabostat | IC50 | 12.0 [1], 24.0 [2], 70.0 [3] |
| N-(1-Napthalenecarbonyl)-Gly-boroPro | IC50 | 2.3 [1], 19.0 [2] |
| N-(1-Napthalenecarbonyl)-Gly-boroPro | Ki | 7.9 [1] |
| (R)-1-(2-(1-Oxoisoindolin-2-yl)acetyl)pyrrolidin-2-ylboronic acid | IC50 | 93.0 [1], 120.0 [2] |
| (R)-1-(2-(1-Oxoisoindolin-2-yl)acetyl)pyrrolidin-2-ylboronic acid | Ki | 7.5 [1] |
| Py(D)AlaboroPro | IC50 | 36.0 [1] |
| Py(D)AlaboroPro | Ki | 9.0 [1] |
| 2-[3-[2-[2-Cyano-(S)-pyrrolidin-1-yl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,3-dihydroisoindole | IC50 | 20000.0 [1], 100000.0 [2] |
| (R)-1-(2-Acetamidoacetyl)pyrrolidin-2-ylboronic acid | Ki | 23.0 [1] |
| 3-[[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-N-(3,4-dimethoxyphenyl)-3-methylbutanamide | IC50 | 20000.0 [1], 50000.0 [2] |
| (R)-1-(2-(2,5-Dichlorobenzamido)acetyl)pyrrolidin-2-ylboronic acid | Ki | 29.0 [1] |
| (R)-1-((R)-2-Acetamidopropanoyl)pyrrolidin-2-ylboronic acid | IC50 | 2900.0 [1] |
| (R)-1-((R)-2-Acetamidopropanoyl)pyrrolidin-2-ylboronic acid | Ki | 350.0 [1] |
| (2S)-1-[(2S,4S)-4-[2-(1,3-Dihydroisoindol-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carbonyl]-4,4-difluoropyrrolidine-2-carbonitrile | IC50 | 22.0 [1] |
| (2S)-1-[(2S,4S)-4-[2-(1,3-Dihydroisoindol-2-yl)-2-oxoethyl]-5-oxopyrrolidine-2-carbonyl]-4,4-difluoropyrrolidine-2-carbonitrile | Ki | 1.3 [1] |
| N-[4-[(1R)-1-Amino-2-(2,5-difluorophenyl)ethyl]cyclohexyl]-N-methylacetamide | IC50 | 35000.0 [1] |
| (1R)-2-(2,5-Difluorophenyl)-1-[4-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]cyclohexyl]ethanamine | IC50 | 35000.0 [1] |
| 1-[4-[(1R)-1-Amino-2-(2,5-difluorophenyl)ethyl]cyclohexyl]piperidine-3-carboxamide | IC50 | 35000.0 [1] |
| (1R)-2-(2,5-Difluorophenyl)-1-[4-(3,3-difluoropyrrolidin-1-yl)cyclohexyl]ethanamine | IC50 | 35000.0 [1] |
| cis-(R)-2-(2,5-Difluorophenyl)-1-(4-(piperidin-1-yl)cyclohexyl)ethanamine | IC50 | 35000.0 [1] |
| Anagliptin | IC50 | 72700.0 [1] |
| Omarigliptin | IC50 | 67000.0 [1] |
| (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;hydrochloride | IC50 | 40000.0 [1] |
| Dutogliptin | IC50 | 7520.0 [1] |
| Gosogliptin | IC50 | 10300.0 [1] |
| Allo-Ile-Isoindoline | IC50 | 100000.0 [1] |
| Abt-279 | Ki | 30000.0 [1] |
| N-[4-((S)-1-Amino-2-oxo-2-thiazolidin-3-yl-ethyl)-cyclohexyl]-4-trifluoromethoxy-benzenesulfonamide | IC50 | 35000.0 [1] |
| (R)-1-(2-Aminoacetyl)pyrrolidin-2-ylboronic acid | IC50 | 52.0 [1] |
| (2S)-1-[(2S)-2-Amino-4-[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl]-4-oxobutanoyl]pyrrolidine-2-carbonitrile | IC50 | 100000.0 [1] |
| Val-boroAla | IC50 | 22000.0 [1] |
| [(2R)-1-[(2R)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid | IC50 | 11.0 [1] |
| (2S)-2-Amino-4-[(2-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one | IC50 | 100000.0 [1] |
| DPPI 1c hydrochloride | IC50 | 30000.0 [1] |
| 3-[[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-N-(2-phenylethyl)propanamide | IC50 | 20000.0 [1] |
| (2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acid | IC50 | 40000.0 [1] |
| 3-[2-(2-Cyanopyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-N-(1-methyl-1-phenylethyl)butyramide | IC50 | 20000.0 [1] |
| N-Benzyl-3-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]propanamide | IC50 | 20000.0 [1] |
| 3-[2-(2-Cyano-(S)-pyrrolidin-1-yl)-2-oxoethylamino]-N-(1-methyl-1-phenylethyl)propionamide | IC50 | 20000.0 [1] |
| N-[2-[(2S)-2-Cyanopyrrolidin-1-yl]-2-oxoethyl]naphthalene-1-carboxamide | IC50 | 610.0 [1] |
| (2S)-2-Cyano-1-(4-phenyl-L-phenylalanyl)pyrrolidine | IC50 | 1410.0 [1] |
| (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-(4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine | IC50 | 22000.0 [1] |
| 2-[[6-[(3R)-3-Amino-3-methylpiperidin-1-yl]-1,3-dimethyl-2,4-dioxopyrrolo[3,2-d]pyrimidin-5-yl]methyl]-4-fluorobenzonitrile | IC50 | 50000.0 [1] |
| N-[4-[(1S)-1-Amino-2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]cyclohexyl]-4-(trifluoromethoxy)benzamide | IC50 | 35000.0 [1] |
| [(2R)-1-[(2R)-2-Aminopropanoyl]pyrrolidin-2-yl]boronic acid | IC50 | 7800.0 [1] |
| (2S)-1-(2-Benzyl-3-oxo-1H-isoindole-4-carbonyl)pyrrolidine-2-carbonitrile | IC50 | 100000.0 [1] |
| (S)-N-(2-(2-Cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)quinoline-4-carboxamide | IC50 | 3.3 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[(4-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[(4-fluorophenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-2-ylmethylsulfanyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 19076.0 [1] |
| (2S,4S)-1-((R)-2-Amino-3-(benzylsulfonyl)-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[(4-methoxyphenyl)methylsulfinyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[(4-cyanophenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 9450.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[(3-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 16980.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-phenylmethoxyphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 20395.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-phenylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 9660.0 [1] |
| (2S,4S)-1-((R)-3-(4-Methoxybenzylthio)-2-amino-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[3-(4-fluorophenyl)propylsulfanyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 15776.0 [1] |
| N-[[(2S,3As,7aS)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-2,3,3a,4,5,6,7,7a-octahydroindol-2-yl]methyl]-1,1,1-trifluoromethanesulfonamide | IC50 | 34180.0 [1] |
| 1-(Quinazoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthine | IC50 | 1800.0 [1] |
| 7-But-2-ynyl-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-piperazin-1-ylpurine-2,6-dione | IC50 | 1200.0 [1] |
| 1-(Quinoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthine | IC50 | 10300.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(3-phenylpropylsulfonyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-[(2-methoxyphenyl)methylsulfonyl]-3-methylbutanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 12380.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[[4-(trifluoromethyl)phenyl]methylsulfanyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-((R)-2-Amino-3-methyl-3-(phenethylthio)butanoyl)-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-4-ylmethylsulfonyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-methylsulfonylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-(pyridin-4-ylmethylsulfanyl)butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 9660.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(4-methylphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 23440.0 [1] |
| (2S,4S)-1-((R)-2-Amino-3-methyl-3-(3-phenylpropylthio)butanoyl)-4-fluoropyrrolidine-2-carbonitrile | Ki | 12176.0 [1] |
| (2S,4S)-1-((R)-3-(3-Phenoxybenzylthio)-2-amino-3-methylbutanoyl)-4-fluoropyrrolidine-2-carbonitrile | Ki | 12845.0 [1] |
| (2S,4S)-1-[(2R)-2-Amino-3-methyl-3-[(3-phenoxyphenyl)methylsulfonyl]butanoyl]-4-fluoropyrrolidine-2-carbonitrile | Ki | 6863.0 [1] |
| [(2S)-1-[(2S)-2-Amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid | IC50 | 11.0 [1] |
| 6-Chloro-5-[[(2R,5S)-5-[(2S)-2-cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]pyridine-3-carboxylic acid | Ki | 2200.0 [1] |
| (2S)-1-{[(2S,5R)-5-(2-Chlorophenoxymethyl)pyrrolidin-2-yl]carbonyl}pyrrolidine-2-carbonitrile | Ki | 479.0 [1] |
| 3-Chloro-4-{[(2R,5S)-5-{[(2S)-2-cyanopyrrolidin-1-yl]carbonyl}pyrrolidin-2-yl]methoxy}benzoic acid | Ki | 536.0 [1] |
| 4-[[(2R,5S)-5-[(2S)-2-Cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]naphthalene-1-carboxylic acid | Ki | 240.0 [1] |
| (2S)-1-[(2S,5R)-5-[(2-Chloro-4-cyanophenoxy)methyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrile | Ki | 505.0 [1] |
| 1-(4-Methylquinazoline-2-ylmethyl)-3-methyl-7-(2-butynyl)-8-piperazinoxanthine | IC50 | 740.0 [1] |
| 4-[[(2R,5S)-5-[(2S)-2-Cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]-3-propan-2-ylbenzoic acid | Ki | 888.0 [1] |
| 4-Chloro-3-{[(2R,5S)-5-{[(2S)-2-cyanopyrrolidin-1-yl]carbonyl}pyrrolidin-2-yl]methoxy}benzoic acid | Ki | 1770.0 [1] |
| (2S)-1-[(2S,5R)-5-[(2-Chloro-4-methylsulfonylphenoxy)methyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrile | Ki | 394.0 [1] |
| 6-Chloro-5-[[(2R,5S)-5-[(2S)-2-cyanopyrrolidine-1-carbonyl]pyrrolidin-2-yl]methoxy]-1-oxidopyridin-1-ium-3-carboxylic acid | Ki | 1527.0 [1] |
| (2R,5S)-1-(2-(1-(Ethoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrile | IC50 | 30000.0 [1] |
| (2R,5S)-1-(2-(1-(Butoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrile | IC50 | 30000.0 [1] |
| (1S,2R,5S)-5-(Isoindolin-2-yl)-2-(2,4,5-trifluorophenyl)cyclohexanamine | IC50 | 7000.0 [1] |
| (1S,2R,5S)-5-[3-(Trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-2-(2,4,5-trifluorophenyl)cyclohexan-1-amine | IC50 | 60000.0 [1] |
| (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-pyrazolo[1,5-a]pyrimidin-5-ylphenyl)butanamide;2,2,2-trifluoroacetic acid | IC50 | 40000.0 [1] |
| (2S,5R)-1-[2-(1-Adamantylamino)acetyl]pyrrolidine-2,5-dicarbonitrile | IC50 | 30000.0 [1] |
| (2R,5S)-1-(2-(1-(Methoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrile | IC50 | 30000.0 [1] |
| (R)-1-((S)-2,4-Diaminobutanamido)pentylboronic acid | IC50 | 33000.0 [1] |
| (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-7-yl)phenyl]butanamide;2,2,2-trifluoroacetic acid | IC50 | 40000.0 [1] |
| (2R,5S)-1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2,5-dicarbonitrile | IC50 | 30000.0 [1] |
| (2S,5R)-1-[2-(3-Tricyclo[3.3.1.03,7]nonanylamino)acetyl]pyrrolidine-2,5-dicarbonitrile | IC50 | 30000.0 [1] |
| (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acid | IC50 | 40000.0 [1] |