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Literature summary extracted from

  • Jansen, K.; De Winter, H.; Heirbaut, L.; Cheng, J.; Joossens, J.; Lambeir, A.; De Meester, I.; Augustyns, K.; Van Der Veken, P.
    Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold (2013), MedChemComm, 5, 1700-1707.
No PubMed abstract available

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.B28 1-benzyl-7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 1-[(4-methoxyquinazolin-2-yl)methyl]-3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 7-(but-2-yn-1-yl)-3-methyl-1-(naphthalen-2-ylmethyl)-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinazolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 7-(but-2-yn-1-yl)-8-ethoxy-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 7-benzyl-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 alogliptin
-
 Homo sapiens
3.4.21.B28 dutogliptin
-
 Homo sapiens
3.4.21.B28 linagliptin
-
 Homo sapiens
3.4.21.B28 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 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 N-[2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 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
-
 Homo sapiens
3.4.21.B28 saxagliptin
-
 Homo sapiens
3.4.21.B28 sitagliptin
-
 Homo sapiens
3.4.21.B28 vildagliptin
-
 Homo sapiens
3.4.21.B28 [(2S)-1-(D-valyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.B28 Homo sapiens Q12844
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.B28 fibroblast
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.B28 additional information the enzyme is a is a prolyl specific serine protease Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.B28 FAP
-
 Homo sapiens
3.4.21.B28 FAP-alpha
-
 Homo sapiens
3.4.21.B28 fibroblast activation protein
-
 Homo sapiens
3.4.21.B28 seprase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.B28 0.0000033
-
 pH and temperature not specified in the publication Homo sapiens N-[2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide
3.4.21.B28 0.00007
-
 pH and temperature not specified in the publication Homo sapiens [(2S)-1-(D-valyl)pyrrolidin-2-yl]boronic acid
3.4.21.B28 0.000089 0.00037 pH and temperature not specified in the publication Homo sapiens linagliptin
3.4.21.B28 0.00074
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.0012
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.0018
-
 pH and temperature not specified in the publication Homo sapiens 7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinazolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.0019
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.0026
-
 pH and temperature not specified in the publication Homo sapiens saxagliptin
3.4.21.B28 0.0033
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.0058
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.00752
-
 pH and temperature not specified in the publication Homo sapiens dutogliptin
3.4.21.B28 0.01
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.01
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.01
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.01
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.0103
-
 pH and temperature not specified in the publication Homo sapiens 7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.011
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.0125
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.041
-
 pH and temperature not specified in the publication Homo sapiens 7-(but-2-yn-1-yl)-3-methyl-1-(naphthalen-2-ylmethyl)-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.05
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.05
-
 pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.073
-
 pH and temperature not specified in the publication Homo sapiens vildagliptin
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens sitagliptin
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens alogliptin
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 7-(but-2-yn-1-yl)-8-ethoxy-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 1-benzyl-7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 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
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
3.4.21.B28 0.1
-
 above, pH and temperature not specified in the publication Homo sapiens 1-[(4-methoxyquinazolin-2-yl)methyl]-3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione