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Xaa-Pro aminopeptidase 1 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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ApstatinIC5018000.0 [1], 21000.0 [2]
CID 10336627IC501100.0 [1], 23000.0 [2]
(2S)-1-[(2S,3S)-3-Amino-2-hydroxy-5-methylhexanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC5092000.0 [1], 800000.0 [2]
(2S)-1-[(2S,4R)-1-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-4-hydroxypyrrolidine-2-carbonyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC502000000.0 [1]
2-[(2S)-2-[[(2S)-1-Amino-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-4-phenylbutanoic acidIC505700.0 [1], 720000.0 [2]
(2S)-1-[(2R,3R)-3-Amino-2-hydroxy-5-methylhexanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC501500000.0 [1]
(2S)-1-[(2S,3R)-3-Amino-2-hydroxy-5-methylhexanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC501200.0 [1], 6300.0 [2]
(2S)-1-[(2S)-1-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamideIC5045000.0 [1], 250000.0 [2]
(2S)-1-[(2S)-1-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]pyrrolidine-2-carbonyl]-N-[(2S)-1-[[(2S)-1-[[(2R)-1-amino-1-oxo-3-sulfanylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC502700.0 [1], 6800.0 [2]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;hydrochlorideIC5040000.0 [1]
(R)-3-Amino-1-((R)-2-benzylpiperazin-1-yl)-4-(2-fluorophenyl)butan-1-oneIC5010000.0 [1]
DPPI 1c hydrochlorideIC5030000.0 [1]
Sitagliptin HydrochlorideIC5010000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
(R)-3-Amino-4-(2-fluorophenyl)-1-(piperazin-1-yl)butan-1-oneIC5010000.0 [1]
(2S)-1-[(3R,4S)-4-Amino-3-hydroxy-6-methylheptanoyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC502000000.0 [1]
(2S)-1-[(4R)-3-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-1,3-thiazolidine-4-carbonyl]-N-[(2S)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamideIC5082000.0 [1]
(2R,5S)-1-(2-(1-(Ethoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2R,5S)-1-(2-(1-(Butoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-pyrazolo[1,5-a]pyrimidin-5-ylphenyl)butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
(2S,5R)-1-[2-(1-Adamantylamino)acetyl]pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2R,5S)-1-(2-(1-(Methoxymethyl)cyclopentylamino)acetyl)pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-7-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
(2R,5S)-1-[2-[(3-Hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2S,5R)-1-[2-(3-Tricyclo[3.3.1.03,7]nonanylamino)acetyl]pyrrolidine-2,5-dicarbonitrileIC5030000.0 [1]
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
(2S,3S)-3-Amino-N,N-dimethyl-4-oxo-4-pyrrolidin-1-yl-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamide;2,2,2-trifluoroacetic acidIC5040000.0 [1]
1-Naphthalenecarboxylic acid, 2-[(phenylsulfonyl)amino]-IC50100000.0 [1]
(3R)-3-Amino-1-[5,5-dimethyl-3-(trifluoromethyl)-6,8-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(2S)-N-[(2S)-1-Amino-1-oxopropan-2-yl]-1-[2-(hydroxycarbamoyl)cyclohexanecarbonyl]pyrrolidine-2-carboxamideIC502000000.0 [1]
(2S)-N-[(2S)-1-Amino-1-oxopropan-2-yl]-1-(2-sulfanylcyclopentanecarbonyl)pyrrolidine-2-carboxamideIC5053000.0 [1]
(3R)-3-Amino-1-[5,8-dimethyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[3-(trifluoromethyl)-8-[[2-(trifluoromethyl)phenyl]methyl]-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-[[3,5-bis(trifluoromethyl)phenyl]methyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-[(4-fluorophenyl)-hydroxymethyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[(6S)-6-methyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-prop-2-enyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
2-[7-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-benzyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-[(4-methoxyphenyl)methyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-ethyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[8-[(2-fluorophenyl)methyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(3R)-3-Amino-1-[(6R)-6-methyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;hydrochlorideIC5010000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-2-[4-(8-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]-4-oxobutanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-2-(4-imidazo[1,2-b]pyridazin-6-ylphenyl)-N,N-dimethyl-4-oxobutanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-(3-fluoroazetidin-1-yl)-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]butanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-2-[4-(5-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]-4-oxobutanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-2-[4-(1-methyl-6-oxopyridin-3-yl)phenyl]-4-oxobutanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[4,3-a]pyridin-6-yl)phenyl]butanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-2-(4-imidazo[1,2-a]pyridin-6-ylphenyl)-N,N-dimethyl-4-oxobutanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-(4-pyrazolo[1,5-a]pyrimidin-5-ylphenyl)butanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-2-[4-(2-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)phenyl]-4-oxobutanamideIC5040000.0 [1]
(2S,3S)-3-Amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[4-([1,2,4]triazolo[1,5-a]pyridin-7-yl)phenyl]butanamideIC5040000.0 [1]
(3R)-3-Amino-1-[(8S)-8-[(4-fluorophenyl)methyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(8R)-8-[(4-fluorophenyl)methyl]-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(5S,8S)-5,8-dimethyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(5R,8R)-5,8-dimethyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(8S)-8-methyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(8R)-8-methyl-3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(4R)-4-methyl-6-(trifluoromethyl)-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
(3R)-3-Amino-1-[(4S)-4-methyl-6-(trifluoromethyl)-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]-4-(2,4,5-trifluorophenyl)butan-1-oneIC5010000.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Xaa-Pro aminopeptidase 1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/xaa-pro-aminopeptidase-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 9). Quest Database™ Xaa-Pro aminopeptidase 1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/xaa-pro-aminopeptidase-1-inhibitors-ic50-ki.
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