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(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
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(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
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(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
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1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
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1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
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1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
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2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
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Diprotin A
dipeptidyl peptidase IV in soluble and membrane-bound fractions from the hypothalamus and hippocampus areas is distinguished kinetically as insensitive and sensitive to diprotin A, respectively
(1R)-2-[[(3R,4R)-4-amino-1-[1-[4-(1H-1,2,4-triazol-1-yl)phenyl]ethyl]pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
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(1R,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
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(1S,2R)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
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(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
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the inhibitor has similar potency to sitagliptin and excellent pharmacokinetic properties
(1S,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopropyl-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropan-2-aminium
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(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
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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
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid
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i. e. ABT-279, a very potent, selective, effective, and well-tolerated inhibitor useful for the treatment of diabetes
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[1-(2-methylpropyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[3-(2-methylpropyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2,5-difluorophenyl)-4-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
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(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-1-(2,4,5-trifluorophenyl)-4-[1,4,4-trimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
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(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
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(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
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(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
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(2R)-4-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4R)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4R)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4R)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4R)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
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(2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2R,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
-
-
(2R,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([(2S,4S)-4-[(2E)-but-2-en-1-yl]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-L-prolylpyrrolidine-2-carbonitrile
-
IC50: 2.9 nmol/L
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4R)-4-tricyclo[3.3.1.13,7]dec-2-yl-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4S)-4-(azocan-1-ylcarbonyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-ethyl-4-hydroxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,4,6-trimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethoxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-cyclohexylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
in vivo plasma DPP-IV inhibition in Wistar rats
(2S)-1-[[(2S,4S)-4-(azepan-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(azetidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(hydroxymethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-isobutylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(azetidin-1-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(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
(2S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoropropan-2-aminium
-
-
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
-
-
(2S,3R)-1-cyclopentylidene-1-fluoro-3-(3-[4-[(trifluoromethyl)sulfonyl]phenyl]-1,2,4-oxadiazol-5-yl)butan-2-aminium
-
-
(2S,3R)-1-cyclopentylidene-1-fluoro-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-aminium
-
-
(2S,3R)-1-cyclopentylidene-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-(3-[2-chloro-4-[(methylsulfonyl)amino]phenyl]-1,2,4-oxadiazol-5-yl)-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-(4-bromo-2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(ethylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-5-hydroxy-1-oxopentan-2-aminium
-
-
(2S,3S)-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-4-cyclopropyl-3-[3-[2-fluoro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
-
(2S,3S,11bS)-3-(1,1-dioxido-1,2-thiazinan-2-yl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-ethyl-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N,2-dimethylpyrrolidine-3-carboxamide
-
-
(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
(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
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(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
(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
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
-
(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
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(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
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(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
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(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
(2S,4S,5S)-N-(cyanomethyl)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-N-ethyl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-prop-2-yn-1-ylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-propylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-N,5-dimethylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-cyclopropyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-allyl-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N4-benzyl-N2-(cyanomethyl)-N2-ethyl-5-methylpyrrolidine-2,4-dicarboxamide
-
-
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
-
-
(3R)-3-amino-1-diaminophosphinyl-2-piperidinone
-
IC50: 46 nM
(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
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
competitive, reversible inhibitor. Pharmacokinetic parameters
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
pharmacokinetic parameters
(3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone
-
IC50: 130 nM
(3S)-3-amino-1-diaminophosphinyl-2-piperidinone
-
IC50: 94 nM
(3S)-3-amino-1-diaminophosphinyl-2-pyrrolidinone
-
IC50: 11 nM
(3S)-N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-fluoro-3-methylbutanamide
-
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
-
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl benzoate
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-diethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-propylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidine-3-carboxamide
-
-
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
-
-
(4R)-3-([1-[1-(2-phenoxyethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-cyanobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-fluorobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-nitrobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([2-ethyl-1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(2'-cyanobiphenyl-4-yl)methyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-methylphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(1-benzylpiperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(1-[3-[2-(aminooxy)cyclopropyl]propyl]piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
-
-
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
-
-
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-[(3R)-3-aminopiperidin-1-yl]-3-(2-chlorobenzyl)-5-methyl-4-oxo-4,5-dihydro-3H-imidazo[4,5-c]quinoline-8-carboxylate
-
compound shows significantly high oral absorption and potent dipeptidyl peptidase IV inhibition in vivo and decreased Zucker fatty rats glucose levels in the oral glucose tolerance test
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
-
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
-
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-methylpiperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-5-methylpiperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]azepan-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
-
vildagliptin, reversible inhibitor, vildagliptin inhibits DPP4 activity by about 50% at a dosage of 0.3 mg/kg body weight
2-([2-[(3R)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-5-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,7-dimethoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,8-dichloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-fluoro-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3S)-3-aminopiperidin-1-yl]-6-fluoro-7-morpholin-4-yl-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
-
pharmacokinetic data
2-[(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-methylpyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
-
-
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
-
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-fluorobenzyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-methoxyethyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4,5-dimethyl-1,3-thiazol-2-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(pyrimidin-2-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclohexylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[2-(thiophen-2-yl)ethyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[3-(propan-2-yloxy)propyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[4-(trifluoromethyl)phenyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine
-
IC50: 190 nmol/L
3-([2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[3-(trifluoromethyl)phenyl]cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[4-(trifluoromethyl)phenyl]cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(2,4-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,5-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-phenylcyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]-amino)-3-methyl-N-[trans-2-(4-methyl-1,3-thiazol-5-yl)cyclopropyl]butanamide
-
-
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
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
15 nM DPP-IV inhibitor with high selectivity over DPP-II, DPP8 and FAP
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-ethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(4-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-phenylcyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(pyridin-3-yl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
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
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
i.e. E3024, selective, and competitive
3-L-prolyl-1,3-thiazolidine
-
IC50: 607 nmol/L
3-N-[(2S,3S)-2-amino-3-methylpentanoyl]-1,3-thiazolidine
-
in genetically susceptible animals, inhibition of DPP IV increases arterial blood pressure via Y1 receptors when elevated blood pressure is reduced with antihypertensive drugs provided that the sympathetic nervous system is functional
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
-
-
3-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-1,3-oxazinan-2-one
-
-
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 21.8 nmol/L
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 41.3 nmol/L
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 10.8 nmol/L
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 34.5 nmol/L
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 13.0 nmol/L
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 14.8 nmol/L
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 125 nmol/L
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 55.1 nmol/L
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 33.6 nmol/L
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 43.8 nmol/L
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 21.0 nmol/L
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 30.4 nmol/L
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 54.9 nmol/L
3-[(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylpropanamide
-
-
3H-imidazo[4,5-c]quinolin-4(5H)-one
-
inhibitor with potent dipeptidyl peptidase IV inhibitory activity that shows poor oral absorption can be improved by esterification of the carboxylic acid moiety
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
-
-
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
-
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
-
-
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
-
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2-methylbenzonitrile
-
instability in human and dog plasma, but not in rat plasma. Unstable in fresh rat, dog, and human blood
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
-
-
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
in vivo plasma DPP-IV inhibition in Wistar rats
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile
-
IC50: 0.27 nmol/L
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile
-
IC50: 2.3 nmol/L
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile
-
IC50: 500 nmol/L
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
-
i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
-
-
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
inhibition of plasma DPP-4 activity after oral administration
ASP-8497
-
(2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate
-
AB-192, irreversible inhibitor, AB-192 sufficiently inhibits DPP4 only in the higher dosage range of more than 1mg/kg body weight
Ca2+
-
mixed type inhibition, Ca2+ ions preferentially bind to the betA-propeller domain
carmegliptin
-
potent and long-acting dipeptidyl peptidase IV inhibitor
diisopropyl fluorophosphate
-
-
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
-
-
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate
-
-
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
-
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
-
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
-
-
ethyl [(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]carbamate
-
-
H-(S)-alaninyl-(R)-boro-proline
-
-
H-(S)-Glu-(R)-boro-alanine
-
-
H-(S)-glutaminyl-(R)-boro-alanine
-
-
H-(S)-glutamyl-(R)-boro-proline
-
-
H-(S)-valinyl-(R)-boro-alanine
-
-
H-(S)-valinyl-(R)-boro-proline
-
-
H-glycyl-(R)-boro-proline
-
-
hemorphin-4 peptide
-
12% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWT, competitive
hemorphin-5 peptide
-
18% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWTQ, competitive
-
hemorphin-7 peptide
-
30% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWTQRF, selective and competitive
L-Ile-L-Pro-L-Ile
-
the dipeptidyl peptidase IV inhibitor switches the enzyme from hydrolase to synthase functional mode to generate endomorphin 2
L-threo-Ile-thiazolidide
-
-
LVV-hemorphin-7 peptide
-
9% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence LVVYPWTQRF, the additional leucine residue reduces the inhibitory potential
Lys[Z(NO2)]-pyrrolidide
-
inhibition of DPPIV catalytic activity is associated with inhibition of NHE3-mediated NaHCO3 reabsorption in the native renal proximal tubule
methionyl-2(S)-cyanopyrrolidine
-
irreversible noncompetitive inhibitor of DP-IV
N-(1,3-benzothiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(3-chloro-4-fluorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4-chlorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
-
-
N-(4-cyanophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-bromo-1,3-thiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-ethylhydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-hydroperoxyhydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
-
N-acetyl-(S)-valinyl-(R)-boro-proline
-
-
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
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-2-methylbutanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylpentanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]butanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]pentanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]propane-1-sulfonamide
-
-
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
-
N3-[2-[(2S)-2-cyanopyrrolidin-1-yl]-1,1-dimethyl-2-oxoethyl]-N-(2-pyridin-2-ylethyl)-b-alaninamide
-
in vivo efficacy in rat models after oral administration
phenylmethylsulfonyl fluoride
-
slight
Pro-Ala
-
hydrolysis of L-Pro-L-Ala
tert-butyl 2-(1-acetylpiperidin-4-yl)-2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,3-dichlorobenzoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(dimethylcarbamoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(pyridin-3-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-[(4-methylcyclohexyl)carbonyl]piperidin-4-yl]hydrazinecarboxylate
-
-
VV-hemorphin-5 peptide
-
10% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQ
VV-hemorphin-6 peptide
-
15% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQR
VV-hemorphin-7 peptide
-
27% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQRF
[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]acetic acid
-
-
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
-
-
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
in vivo efficacy in rat models after oral administration. The inhibitor has potential for further development as antidiabetic agent
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
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
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
alogliptin
-
-
alogliptin
-
potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV
alogliptin
-
nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, complete inhibition of DPP-4 24 h after treatment with 10 mg/kg alogliptin
BI 1356
-
competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro
BI 1356
-
proposed trade name ONDERO, exhibits a prominent concentration-dependent plasma protein binding due to a saturable high affinity binding to the DPP-4 target in plasma
BI 1356
-
proposed trade name ONDERO, highly potent and selective DPP-4 inhibitor
Cd2+
-
-
Hg2+
-
-
isoleucine thiazolidide
-
-
isoleucine thiazolidide
-
in vivo study
isoleucine thiazolidide
-
i.e. P32/98. Enhancement of incretin with the DPP-4 inhibitor P32/98 has therapeutic effects in hyperinsulinaemia, hyperglycaemia and impaired glucose toleranceIGT in Zucker rats with incipient impaired glucose tolerance and manifest impaired glucose tolerance. Apparently, administration of P32/98 in Zucker rats with incipient impaired glucose tolerance results in more efficient beta-cell function, which is associated with less need for insulin to cope with deterioration of glucose tolerance. P32/98 has a strong effect on dyslipidaemia in manifest impaired glucose tolerance. P32/98 has no side effect on intestinal growth. Daily intake of P32/98 is a promising strategy for treatment of glucose intolerance and has the potential to prevent type 2 diabetes
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
potent inhibitor of DPP IV
sitagliptin
-
-
sitagliptin
-
the systemic clearance of sitagliptin in rats is driven primarily by renal elimination of intact parent drug, with contribution from biliary excretion and metabolism (minor). Active transport mechanisms are probably involved in the renal elimination of sitagliptin
sitagliptin
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
vildagliptin
-
-
vildagliptin
-
liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not
vildagliptin
-
i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
Zn2+
-
-
Zn2+
-
mixed type inhibition
additional information
conformational flexibility of tyr548 is unique among protein family members and may be utilized in drug design to achieve peptidase selectivity
-
additional information
-
inhibitory mechanism, the N-terminus sequence of hemorphins influence the interaction between hemorphins and the enzyme
-
additional information
-
4beta-[4-(hydroxyphenyl)prolyl]prolinenitriles show a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates is found to contribute to their long duration of action
-
additional information
-
in male Zucker diabetic rats, DPP-4 inhibition shows a delay in onset of diabetes and improved glucose tolerance and insulin secretion
-
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0.000017 - 0.000024
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.000002 - 0.0006
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000003 - 0.000007
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
0.00000021
(1R,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.000012
(1S,2R)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.000013
(1S,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopropyl-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropan-2-aminium
Rattus norvegicus
-
-
0.000023
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000082
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00018
(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00013
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-2-amine
Rattus norvegicus
-
-
0.000065
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
Rattus norvegicus
-
-
0.00014
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
Rattus norvegicus
-
-
0.000027
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000065
(2R)-1-(2,5-difluorophenyl)-4-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00019
(2R)-1-(2,5-difluorophenyl)-4-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00022
(2R)-1-(2,5-difluorophenyl)-4-[1-(2-methylpropyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-1-(2,5-difluorophenyl)-4-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00018
(2R)-1-(2,5-difluorophenyl)-4-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00015
(2R)-1-(2,5-difluorophenyl)-4-[1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00028
(2R)-1-(2,5-difluorophenyl)-4-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00003
(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00026
(2R)-1-(2,5-difluorophenyl)-4-[3-(2-methylpropyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00006
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00023
(2R)-1-(2,5-difluorophenyl)-4-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00013
(2R)-1-(2,5-difluorophenyl)-4-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.000084
(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000145
(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000098
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00158
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000128
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000059
(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000135
(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000076
(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000264
(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000272
(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000021
(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00003
(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000037
(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00057
(2R)-4-oxo-1-(2,4,5-trifluorophenyl)-4-[1,4,4-trimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
Rattus norvegicus
-
-
0.001018
(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00000031
(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000057
(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000004
(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000032
(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000438
(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000123
(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000132
(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000015
(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000805
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000151
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000018
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000087
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00486
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.000366
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.000511
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.00005
(2R)-4-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-4-[(4R)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00037
(2R)-4-[(4R)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000058
(2R)-4-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000084
(2R)-4-[(4R)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00011
(2R)-4-[(4R)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00006
(2R)-4-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00038
(2R)-4-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00049
(2R)-4-[(4S)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00063
(2R)-4-[(4S)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00078
(2R)-4-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00057
(2R)-4-[(4S)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00034
(2R)-4-[(4S)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00061
(2R)-4-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000014
(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000023
(2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000042
(2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000091
(2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00000046
(2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00000018
(2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00000043
(2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00000066
(2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000005
(2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000043
(2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.0000063
(2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000131
(2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000116
(2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00032
(2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00014
(2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000113
(2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000088
(2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000587
(2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000045
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000029
(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000092
(2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000175
(2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000093
(2R,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
Rattus norvegicus
-
-
0.000017
(2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000015
(2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000298
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00001
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000031
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000031
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000012
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000013
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000012
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000002
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000016
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000005
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000025
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000006
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00001
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000019
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000006
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000009
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000008
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000005
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000008
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000014
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000022
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00004
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000035
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000021
(2S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.0016
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
Rattus norvegicus
-
-
0.00149
(2S,3R)-1-cyclopentylidene-1-fluoro-3-(3-[4-[(trifluoromethyl)sulfonyl]phenyl]-1,2,4-oxadiazol-5-yl)butan-2-aminium
Rattus norvegicus
-
-
0.00009
(2S,3R)-1-cyclopentylidene-1-fluoro-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-aminium
Rattus norvegicus
-
-
0.001165
(2S,3R)-1-cyclopentylidene-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000057
(2S,3R)-3-(3-[2-chloro-4-[(methylsulfonyl)amino]phenyl]-1,2,4-oxadiazol-5-yl)-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000645
(2S,3R)-3-[3-(4-bromo-2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.00005
(2S,3R)-3-[3-[2-chloro-4-(ethylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.0000032
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
Rattus norvegicus
-
-
0.0000075
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000525
(2S,3R)-3-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000203
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.000017
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.00004
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Rattus norvegicus
-
-
0.00007
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-5-hydroxy-1-oxopentan-2-aminium
Rattus norvegicus
-
-
0.000122
(2S,3S)-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.000019
(2S,3S)-4-cyclopropyl-3-[3-[2-fluoro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Rattus norvegicus
-
-
0.000142
(2S,3S,11bS)-3-(1,1-dioxido-1,2-thiazinan-2-yl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Rattus norvegicus
-
-
0.000121
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
Rattus norvegicus
-
-
0.000046
(3R)-3-amino-1-diaminophosphinyl-2-piperidinone
Rattus norvegicus
-
IC50: 46 nM
0.00013
(3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone
Rattus norvegicus
-
IC50: 130 nM
0.000094
(3S)-3-amino-1-diaminophosphinyl-2-piperidinone
Rattus norvegicus
-
IC50: 94 nM
0.000011
(3S)-3-amino-1-diaminophosphinyl-2-pyrrolidinone
Rattus norvegicus
-
IC50: 11 nM
0.0000036
(3S)-N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-fluoro-3-methylbutanamide
Rattus norvegicus
-
-
0.0000551
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.0000549
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000021
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000171
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.00019
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.0000022
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
Rattus norvegicus
-
-
0.000638
(4R)-3-([1-[1-(2-phenoxyethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.00071
(4R)-3-([1-[1-(4-cyanobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.002228
(4R)-3-([1-[1-(4-fluorobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.000698
(4R)-3-([1-[1-(4-nitrobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001459
(4R)-3-([1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.004767
(4R)-3-([1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.003755
(4R)-3-([2-ethyl-1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001022
(4R)-3-[(1-[1-[(2'-cyanobiphenyl-4-yl)methyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001449
(4R)-3-[(1-[1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.006677
(4R)-3-[(1-[1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.002701
(4R)-3-[(1-[1-[(4-methylphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001631
(4R)-3-[[1-(1-benzylpiperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.00176
(4R)-3-[[1-(1-[3-[2-(aminooxy)cyclopropyl]propyl]piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.012
(4R)-3-[[1-(piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.000037
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
Rattus norvegicus
-
-
0.000011
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
Rattus norvegicus
-
-
0.00000032
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00043
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Rattus norvegicus
-
-
0.0000072
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000072
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000103
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000109
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000175
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000762
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Rattus norvegicus
-
-
0.0000014
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000169
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000176
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000029
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
Rattus norvegicus
-
-
0.000009
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000031
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000011
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000314
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000383
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000811
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000151
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Rattus norvegicus
-
-
0.0000176
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000035
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000039
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000019
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-methylpiperidin-2-one
Rattus norvegicus
-
-
0.0000037
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-5-methylpiperidin-2-one
Rattus norvegicus
-
-
0.00043
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]azepan-2-one
Rattus norvegicus
-
-
0.000022 - 0.0078
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
0.0000998
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
Rattus norvegicus
-
-
0.0000047
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
Rattus norvegicus
-
-
0.0000018
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
Rattus norvegicus
-
-
0.0000744
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.000013
2-([2-[(3R)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-5-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000019
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,7-dimethoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000013
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,8-dichloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000008
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000015
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-fluoro-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000029
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.00003
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000018
2-([2-[(3S)-3-aminopiperidin-1-yl]-6-fluoro-7-morpholin-4-yl-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000195 - 0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000165
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
Rattus norvegicus
-
-
0.0000028
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000377
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
Rattus norvegicus
-
-
0.00051
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-fluorobenzyl)acetamide
Rattus norvegicus
-
-
0.001027
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-methoxyethyl)acetamide
Rattus norvegicus
-
-
0.000185
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4,5-dimethyl-1,3-thiazol-2-yl)acetamide
Rattus norvegicus
-
-
0.00009 - 0.000098
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
0.000143
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(pyrimidin-2-yl)acetamide
Rattus norvegicus
-
-
0.000523
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
Rattus norvegicus
-
-
0.000506
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclohexylacetamide
Rattus norvegicus
-
-
0.000217 - 0.000236
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
0.000415
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[2-(thiophen-2-yl)ethyl]acetamide
Rattus norvegicus
-
-
0.000468
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[3-(propan-2-yloxy)propyl]acetamide
Rattus norvegicus
-
-
0.000308
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[4-(trifluoromethyl)phenyl]acetamide
Rattus norvegicus
-
-
0.000817
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.0000012
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Rattus norvegicus
-
-
0.000026
3-([2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000056
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000047
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00006
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[3-(trifluoromethyl)phenyl]cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000085
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[4-(trifluoromethyl)phenyl]cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000084
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(2,4-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000068
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000063
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000101
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000075
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,5-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000042
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000064
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000073
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000086
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000054
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000085
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-phenylcyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000016
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]-amino)-3-methyl-N-[trans-2-(4-methyl-1,3-thiazol-5-yl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000027
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000015
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000017
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-ethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000021
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000026
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00002
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000022
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(4-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000019
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-phenylcyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000024
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(pyridin-3-yl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000607
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
Rattus norvegicus
-
-
0.000142
3-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-1,3-oxazinan-2-one
Rattus norvegicus
-
-
0.0000093
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
Rattus norvegicus
-
-
0.0000033
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.0000125
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000136
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000343
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.000168
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.0000341
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.0000096
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.0000189
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
Rattus norvegicus
-
-
0.0000018
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
Rattus norvegicus
-
-
0.0000336
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
Rattus norvegicus
-
-
0.0000107
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000134
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000101
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000061
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000103
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000019
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Rattus norvegicus
-
-
0.00078
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
Rattus norvegicus
-
i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
0.000234
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
Rattus norvegicus
-
-
0.00000236
ASP-8497
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000068
carmegliptin
Rattus norvegicus
-
-
0.000031
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
Rattus norvegicus
-
-
0.000219
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
Rattus norvegicus
-
-
0.00019
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
Rattus norvegicus
-
-
0.0000153
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
Rattus norvegicus
-
-
0.00115
ethyl [(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]carbamate
Rattus norvegicus
-
-
0.000134
N-(1,3-benzothiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000119 - 0.000124
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.000359
N-(3-chloro-4-fluorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000258
N-(4-chlorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000023
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
Rattus norvegicus
-
-
0.0002
N-(4-cyanophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000226
N-(5-bromo-1,3-thiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00049
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-ethylhydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.03845
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-hydroperoxyhydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000088 - 0.00012
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.00011 - 0.00013
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000049
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
Rattus norvegicus
-
-
0.000092
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
Rattus norvegicus
-
-
0.000077
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000092
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
Rattus norvegicus
-
-
0.00009
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
Rattus norvegicus
-
-
0.000047
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
Rattus norvegicus
-
-
0.000087
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
Rattus norvegicus
-
-
0.000066
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
Rattus norvegicus
-
-
0.000009
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Rattus norvegicus
-
-
0.000014
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.00000038
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
Rattus norvegicus
-
-
0.000012
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Rattus norvegicus
-
-
0.00003
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Rattus norvegicus
-
-
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
Rattus norvegicus
-
-
0.000024
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
Rattus norvegicus
-
-
0.000053
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.000094
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.00002
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.000034
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
Rattus norvegicus
-
-
0.01
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-2-methylbutanamide
Rattus norvegicus
-
-
0.0000026 - 0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylpentanamide
Rattus norvegicus
-
-
0.00051
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]butanamide
Rattus norvegicus
-
-
0.0022
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]pentanamide
Rattus norvegicus
-
-
0.00133
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]propane-1-sulfonamide
Rattus norvegicus
-
-
0.000236
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.00000171
saxagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000115 - 0.00003
sitagliptin
0.000021
sulphostin
Rattus norvegicus
-
IC50: 21 nM
0.001534
tert-butyl 2-(1-acetylpiperidin-4-yl)-2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.004149
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.001793
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,3-dichlorobenzoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.001228
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(dimethylcarbamoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.00083
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.00079
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.000667
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(pyridin-3-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.000866
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-[(4-methylcyclohexyl)carbonyl]piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
1.2
TLCK
Rattus norvegicus
-
pH 8.0, 37°C
0.00000167 - 0.000051
vildagliptin
0.0000163
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
Rattus norvegicus
-
-
0.000069
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
Rattus norvegicus
-
-
0.000017
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000024
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000002
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.0006
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000003
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000007
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000022
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
Rattus norvegicus
-
-
0.0078
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
Rattus norvegicus
-
-
0.0000195
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.00009
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
Rattus norvegicus
-
-
0.000098
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
Rattus norvegicus
-
-
0.000217
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
Rattus norvegicus
-
-
0.000236
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
Rattus norvegicus
-
-
0.000119
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000124
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000088
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00012
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00011
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00013
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.0000026
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.0000093
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.0000115
sitagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.000018
sitagliptin
Rattus norvegicus
-
-
0.00003
sitagliptin
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00000167
vildagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.000051
vildagliptin
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
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Tiruppathi, C.; Miyamoto, Y.; Ganapathy, V.; Roesel, R.A.; Whitford, G.M.; Leibach, F.H.
Hydrolysis and transport of proline-containing peptides in renal brush-border membrane vesicles from dipeptidyl peptidase IV-positive and dipeptidyl peptidase IV-negative rat strains
J. Biol. Chem.
265
1476-1483
1990
Rattus norvegicus
brenda
Ogata, S.; Misumi, Y.; Ikehara, Y.
Primary structure of rat liver dipeptidyl peptidase IV deduced from its cDNA and identification of the NH2-terminal signal sequence as the membrane-anchoring domain
J. Biol. Chem.
264
3596-3601
1989
Rattus norvegicus
brenda
Reuter, W.; Hartel, S.; Hanski, C.; Huhle, T.; Zimmer, T.; Gossrau, R.
Biochemical properties of dipeptidyl peptidase IV in liver and hepatoma plasma membranes
Adv. Enzyme Regul.
28
253-269
1989
Rattus norvegicus
brenda
Hong, W.; Piazza, G.A.; Hixson, D.C.; Doyle, D.
Expression of enzymatically active rat dipeptidyl peptidase IV in Chinese hamster ovary cells after transfection
Biochemistry
28
8474-8479
1989
Rattus norvegicus
brenda
Piazza, G.A.; Callanan, H.M.; Mowery, J.; Hixson, D.C.
Evidence for a role of dipeptidyl peptidase IV in fibronectin-mediated interactions of hepatocytes with extracellular matrix
Biochem. J.
262
327-334
1989
Rattus norvegicus
brenda
Kikuchi, M.; Fukuyama, K.; Epstein, W.L.
Soluble dipeptidyl peptidase IV from terminal differentiated rat epidermal cells: purification and its activity on synthetic and natural peptides
Arch. Biochem. Biophys.
266
369-376
1988
Rattus norvegicus
brenda
Yamashita, K.; Tachibana, Y.; Matsuda, Y.; Katunuma, N.; Kochibe, N.; Kobata, A.
Comparative studies of the sugar chains of aminopeptidase N and dipeptidylpeptidase IV purified from rat kidney brush-border membrane
Biochemistry
27
5565-5573
1988
Rattus norvegicus
brenda
Hartel, S.; Hanski, C.; Kreisel, W.; Hoffmann, C.; Mauck, J.; Reutter, W.
Rapid purification of dipeptidyl peptidase IV from rat liver plasma membrane
Biochim. Biophys. Acta
924
543-547
1987
Rattus norvegicus
brenda
Hanski, C.; Zimmer, T.; Gossrau, R.; Reutter, W.
Increased activity of dipeptidyl peptidase IV in serum of hepatoma-bearing rats coincides with the loss of the enzyme from the hepatoma plasma membrane
Experientia
42
826-828
1986
Rattus norvegicus
brenda
Bartles, J.R.; Braiterman, L.T.; Hubbard, A.L.
Biochemical characterization of domain-specific glycoproteins of the rat hepatocyte plasma membrane
J. Biol. Chem.
260
12792-12802
1985
Rattus norvegicus
brenda
Umezawa, H.; Aoyagi, T.; Ogawa, K.; Naganawa, H.; Hamada, M.; Takeuchi, T.
Diprotins A and B, inhibitors of dipeptidyl aminopeptidase IV, produced by bacteria
J. Antibiot.
37
422-425
1984
Rattus norvegicus
brenda
Heins, J.; Neubert, K.; Barth, A.; Canizaro, P.C.; Behal, F.J.
Kinetic investigation of the hydrolysis of aminoacyl p-nitroanilides by dipeptidyl peptidase IV from human and pig kidney
Biochim. Biophys. Acta
785
30-35
1984
Homo sapiens, Rattus norvegicus, Sus scrofa
brenda
Miura, S.; Song, I.S.; Morita, A.; Erickson, R.H.; Kim, Y.S.
Distribution and biosynthesis of aminopeptidase N and dipeptidyl aminopeptidase IV in rat small intestine
Biochim. Biophys. Acta
761
66-75
1983
Rattus norvegicus
brenda
Erickson, R.H.; Bella, A.M.; Brophy, E.J.; Kobata, A.; Kim, Y.S.
Purification and molecular characterization of rat intestinal brush border membrane dipeptidyl aminopeptidase IV
Biochim. Biophys. Acta
756
258-265
1983
Rattus norvegicus
brenda
Bella, A.M.; Erickson, R.H.; Kim, Y.S.
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Rattus norvegicus, Homo sapiens (P27487)
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Homo sapiens, Mus musculus, Rattus norvegicus
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Homo sapiens, Rattus norvegicus, Rattus norvegicus Wistar
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Homo sapiens, Rattus norvegicus (P14740)
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3-[2-((2S)-2-Cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes
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Rattus norvegicus
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2005-2012
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Rattus norvegicus (P14740), Homo sapiens (P27487)
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2007
Homo sapiens, Rattus norvegicus
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Kim, D.; Kowalchick, J.E.; Edmondson, S.D.; Mastracchio, A.; Xu, J.; Eiermann, G.J.; Leiting, B.; Wu, J.K.; Pryor, K.D.; Patel, R.A.; He, H.; Lyons, K.A.; Thornberry, N.A.; Weber, A.E.
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate)
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Rattus norvegicus
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Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin
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Canis lupus familiaris, Macaca mulatta, Rattus norvegicus
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Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones
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Canis lupus familiaris, Homo sapiens, Rattus norvegicus
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(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
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Canis lupus familiaris, Mus musculus, Rattus norvegicus
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Chen, P.; Caldwell, C.G.; Mathvink, R.J.; Leiting, B.; Marsilio, F.; Patel, R.A.; Wu, J.K.; He, H.; Lyons, K.A.; Thornberry, N.A.; Weber, A.E.
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes
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2007
Rattus norvegicus
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Corbett, J.W.; Dirico, K.; Song, W.; Boscoe, B.P.; Doran, S.D.; Boyer, D.; Qiu, X.; Ammirati, M.; Vanvolkenburg, M.A.; McPherson, R.K.; Parker, J.C.; Cox, E.D.
Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors
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Rattus norvegicus, Homo sapiens (P27487), Homo sapiens
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Rattus norvegicus
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Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not
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2007
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Dipeptidyl peptidase-4 inhibition and the treatment of type 2 diabetes: preclinical biology and mechanisms of action
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2007
Homo sapiens, Mus musculus, Rattus norvegicus, Sus scrofa
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Augstein, P.; Berg, S.; Heinke, P.; Altmann, S.; Salzsieder, E.; Demuth, H.U.; Freyse, E.J.
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2008
Rattus norvegicus
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Green, B.D.; Flatt, P.R.; Bailey, C.J.
Inhibition of dipeptidylpeptidase IV activity as a therapy of type 2 diabetes
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2006
Homo sapiens, Mus musculus, Rattus norvegicus
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Byrd, J.B.; Shreevatsa, A.; Putlur, P.; Foretia, D.; McAlexander, L.; Sinha, T.; Does, M.D.; Brown, N.J.
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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
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Feng, J.; Zhang, Z.; Wallace, M.B.; Stafford, J.A.; Kaldor, S.W.; Kassel, D.B.; Navre, M.; Shi, L.; Skene, R.J.; Asakawa, T.; Takeuchi, K.; Xu, R.; Webb, D.R.; Gwaltney, S.L.
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8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes
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Ischemia/reperfusion injury: The role of CD26/dipeptidyl-peptidase-IV-inhibition in lung transplantation
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In vivo profiling of DPP4 inhibitors reveals alterations in collagen metabolism and accumulation of an amyloid peptide in rat plasma
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3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors
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Homo sapiens, Rattus norvegicus
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Tsai, T.Y.; Hsu, T.; Chen, C.T.; Cheng, J.H.; Chiou, M.C.; Huang, C.H.; Tseng, Y.J.; Yeh, T.K.; Huang, C.Y.; Yeh, K.C.; Huang, Y.W.; Wu, S.H.; Wang, M.H.; Chen, X.; Chao, Y.S.; Jiaang, W.T.
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors
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Rattus norvegicus
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Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
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Forssmann, U.; Stoetzer, C.; Stephan, M.; Kruschinski, C.; Skripuletz, T.; Schade, J.; Schmiedl, A.; Pabst, R.; Wagner, L.; Hoffmann, T.; Kehlen, A.; Escher, S.E.; Forssmann, W.G.; Elsner, J.; von Hoersten, S.
Inhibition of CD26/dipeptidyl peptidase IV enhances CCL11/eotaxin-mediated recruitment of eosinophils in vivo
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Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety
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Homo sapiens, Mus musculus, Rattus norvegicus
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Homo sapiens, Mus musculus, Rattus norvegicus
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Thomas, L.; Eckhardt, M.; Langkopf, E.; Tadayyon, M.; Himmelsbach, F.; Mark, M.
(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with oth
J. Pharmacol. Exp. Ther.
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Homo sapiens, Mus musculus, Rattus norvegicus
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Michel, M.C.; Fliers, E.; Van Noorden, C.J.
Dipeptidyl peptidase IV inhibitors in diabetes: more than inhibition of glucagon-like peptide-1 metabolism?
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Rattus norvegicus
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Kirino, Y.; Kamimoto, T.; Sato, Y.; Kawazoe, K.; Minakuchi, K.; Nakahori, Y.
Increased plasma dipeptidyl peptidase IV (DPP IV) activity and decreased DPP IV activity of visceral but not subcutaneous adipose tissue in impaired glucose tolerance rats induced by high-fat or high-sucrose diet
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2009
Rattus norvegicus
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Nordhoff, S.; Cerezo-Galvez, S.; Deppe, H.; Hill, O.; Lopez-Canet, M.; Rummey, C.; Thiemann, M.; Matassa, V.G.; Edwards, P.J.; Feurer, A.
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV
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4201-4203
2009
Rattus norvegicus
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Gupta, R.C.; Chhipa, L.; Mandhare, A.B.; Zambad, S.P.; Chauthaiwale, V.; Nadkarni, S.S.; Dutt, C.
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor
Bioorg. Med. Chem. Lett.
19
5021-5025
2009
Rattus norvegicus
brenda
Yeh, T.K.; Tsai, T.Y.; Hsu, T.; Cheng, J.H.; Chen, X.; Song, J.S.; Shy, H.S.; Chiou, M.C.; Chien, C.H.; Tseng, Y.J.; Huang, C.Y.; Yeh, K.C.; Huang, Y.L.; Huang, C.H.; Huang, Y.W.; Wang, M.H.; Tang, H.K.; Chao, Y.S.; Chen, C.T.; Jiaang, W.T.
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
Bioorg. Med. Chem. Lett.
20
3596-3600
2010
Homo sapiens, Rattus norvegicus
brenda
Krupina, N.A.; Kushnareva, E.Y.; Khlebnikova, N.N.; Zolotov, N.N.; Kryzhanovskii, G.N.
Behavioral changes in rats induced by a dipeptidyl peptidase IV inhibitor methionyl-2(S)-cyanopyrrolidine: experimental model of anxiety-depression disorder
Bull. Exp. Biol. Med.
147
285-290
2009
Rattus norvegicus
brenda
Luft, V.C.; Schmidt, M.I.; Pankow, J.S.; Hoogeveen, R.C.; Couper, D.; Heiss, G.; Duncan, B.B.; Duncan, B.B.
Dipeptidyl peptidase IV and incident diabetes: the Atherosclerosis Risk in Communities (ARIC) study
Diabetes Care
33
1109-1111
2010
Rattus norvegicus
brenda
Kiraly, K.; Szalay, B.; Szalai, J.; Barna, I.; Gyires, K.; Verbeken, M.; Ronai, A.Z.
Intrathecally injected Ile-Pro-Ile, an inhibitor of membrane ectoenzyme dipeptidyl peptidase IV, is antihyperalgesic in rats by switching the enzyme from hydrolase to synthase functional mode to generate endomorphin 2
Eur. J. Pharmacol.
620
21-26
2009
Rattus norvegicus
brenda
Hung, T.T.; Wu, J.Y.; Liu, J.F.; Cheng, H.C.
Epitope analysis of the rat dipeptidyl peptidase IV monoclonal antibody 6A3 that blocks pericellular fibronectin-mediated cancer cell adhesion
FEBS J.
276
6548-6559
2009
Rattus norvegicus (P14740)
brenda
Kirino, Y.; Sato, Y.; Kamimoto, T.; Kawazoe, K.; Minakuchi, K.; Nakahori, Y.
Interrelationship of dipeptidyl peptidase IV (DPP4) with the development of diabetes, dyslipidaemia and nephropathy: A streptozotocin-induced model using wild-type and DPP4-deficient rats
J. Endocrinol.
200
53-61
2009
Rattus norvegicus
brenda
Alponti, R.F.; Frezzatti, R.; Barone, J.M.; Alegre, V.D.; Silveira, P.F.
Dipeptidyl peptidase IV in the hypothalamus and hippocampus of monosodium glutamate obese and food-deprived rats
Metab. Clin. Exp.
60
234-242
2011
Rattus norvegicus (P14740)
brenda
Arscott, W.; LaBauve, A.; May, V.; Wesley, U.
Suppression of neuroblastoma growth by dipeptidyl peptidase IV: Relevance of chemokine regulation and caspase activation
Oncogene
28
479-491
2009
Rattus norvegicus
brenda
Ikuma, Y.; Hochigai, H.; Kimura, H.; Nunami, N.; Kobayashi, T.; Uchiyama, K.; Umezome, T.; Sakurai, Y.; Sawada, N.; Tadano, J.; Sugaru, E.; Ono, M.; Hirose, Y.; Nakahira, H.
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors: Use of a carboxylate prodrug to improve bioavailability
Bioorg. Med. Chem.
23
779-790
2015
Rattus norvegicus
brenda
Gomez, H.; Chappe, M.; Valiente, P.A.; Pons, T.; Chavez, M.d.e..L.; Charli, J.L.; Pascual, I.
Effect of zinc and calcium ions on the rat kidney membrane-bound form of dipeptidyl peptidase IV
J. Biosci.
38
461-469
2013
Rattus norvegicus
brenda
Rhnert, P.; Schmidt, W.; Emmerlich, P.; Goihl, A.; Wrenger, S.; Bank, U.; Nordhoff, K.; Tger, M.; Ansorge, S.; Reinhold, D.; Striggow, F.
Dipeptidyl peptidase IV, aminopeptidase N and DPIV/APN-like proteases in cerebral ischemia
J. Neuroinflammation
9
44
2012
Rattus norvegicus
brenda
Neidert, L.; Al-Tarhuni, M.; Goldman, D.; Kluess, H.; Jackson, D.
Endogenous dipeptidyl peptidase IV modulates skeletal muscle arteriolar diameter in rats
Physiol. Rep.
6
e13564
2018
Rattus norvegicus (P14740)
brenda