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1-benzyl-7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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1-[(4-methoxyquinazolin-2-yl)methyl]-3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-7-(3-methylbut-2-en-1-yl)-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-7-(4-methylpent-3-en-1-yl)-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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2-mercaptoethanol
inhibition at 140 mM
3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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3-[[7-(but-2-yn-1-yl)-3-methyl-2,6-dioxo-8-(piperazin-1-yl)-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl]benzonitrile
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4'-[[7-(but-2-yn-1-yl)-3-methyl-2,6-dioxo-8-(piperazin-1-yl)-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl]biphenyl-2-carbonitrile
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4-(2-aminoethyl)-benzenesulfonyl fluoride hydrochloride
AEBSF, inhibition at 5 mM
4-(2-aminoethyl)-benzenesulfonylfluoride
4-amidino phenylsulfonyl fluoride
APSF, inhibition at 0.05 mM
4-amidino-phenylsulfonylfluoride
7-(but-2-yn-1-yl)-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-1-[[2-(hydroxymethyl)-1,3-thiazol-4-yl]methyl]-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-1-(naphthalen-2-ylmethyl)-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(piperidin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-1-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-3-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-4-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinazolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-[4-(1H-pyrazol-1-yl)benzyl]-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-8-ethoxy-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-8-[(3S)-3-(hydroxymethyl)-5-oxopiperazin-1-yl]-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
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7-(but-2-yn-1-yl)-8-[(8aS)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
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7-benzyl-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-(propan-2-yl)-3,7-dihydro-1H-purine-2,6-dione
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acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-D-Ala-L-boroPro
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selectively inhibits antiplasmin-cleaving enzyme vs. plasma dipeptidyl peptidase IV
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-D-Asp-L-boroPro
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acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-Gly-L-boroPro
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acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-Ser-Gly-L-boroPro
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acetyl-Arg-Gly-Gly-L-boroPro
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acetyl-Arg-peg-D-Asp-L-boroPro
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acetyl-Arg-peg-Gly-L-boroPro
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acetyl-Arg-peg-Ser-Gly-L-boroPro
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acetyl-Gly-Pro-boronic acid
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chymostatin
50% inhibition at 0.16 mM
diisopropyl fluorophosphate
0.005 mM
diisopropylfluorophosphate
dimethyl sulfoxide
50% inhibition at 4%
dithiothreitol
inhibition at 10 mM
FRQLTSG-pipecolinyl-NQEQV
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L-Val-aminoacyl-proline boronic acid
PT-100
N-[(3R)-1-[7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]piperidin-3-yl]acetamide
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N-[2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide
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N-[2-([7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]amino)ethyl]acetamide
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N-[2-([7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]amino)ethyl]pyridine-4-carboxamide
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N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-9-N-methyl-5-oxoprolinamide
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N2-[7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]glycinamide
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Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(R)-fluoropyrrolidide
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Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(S)-fluoropyrrolidide
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Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
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Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-piperidide
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Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
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Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
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Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQGQV
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Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
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phenylmethylsulfonyl fluoride
Phenylmethylsulfonylfluoride
ValboroPro
complete inhibition at 0.05 mM
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
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[(2R)-1-(N-acetyl-L-alanyl)pyrrolidin-2-yl]boronic acid
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[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
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[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
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[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl-9]-boronic acid
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[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
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[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
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[(2R)-1-[N-[(2,6-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
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[(2S)-1-(D-valyl)pyrrolidin-2-yl]boronic acid
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4-(2-aminoethyl)-benzenesulfonylfluoride
5 mM
4-(2-aminoethyl)-benzenesulfonylfluoride
5 mM
4-amidino-phenylsulfonylfluoride
0.5 mM
4-amidino-phenylsulfonylfluoride
0.5 mM
diisopropylfluorophosphate
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irreversible inhibition
diisopropylfluorophosphate
inhibition at 0.005 mM
diisopropylfluorophosphate
-
50% inhibition at 0.02 mM
diisopropylfluorophosphate
0.005 mM
HgCl2
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N-ethylmaleimide
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phenylmethylsulfonyl fluoride
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phenylmethylsulfonyl fluoride
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50% inhibition at 0.1 mM
phenylmethylsulfonyl fluoride
more than 50% inhibition at 1 mM
Phenylmethylsulfonylfluoride
1 mM
Phenylmethylsulfonylfluoride
1 mM
Talabostat
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additional information
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not inhibited by JTP-4819, Fmoc-Ala-pyrrCN and N-benzyloxycarbonyl-Phe-Pro-BT
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additional information
no inhibition by Z-Pro-prolinal
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additional information
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no inhibition by Z-Pro-prolinal
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additional information
synthesis and inhibitory potencies of selective enzyme inhibitors from a xanthine scaffold, structure-activity relationship analysis using the crystal structures of enzyme complxed with inhibitors, overview
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