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3.4.21.B28: fibroblast activation protein alpha subunit

This is an abbreviated version!
For detailed information about fibroblast activation protein alpha subunit, go to the full flat file.

Word Map on EC 3.4.21.B28

Reaction

fibroblast activation protein requires substrates with Pro at P1 and Gly or D-amino acids at P2. Met-alpha2-antiplasmin is cleaved N-terminally at Pro3-Leu4 and Pro12-Asn13 into Asn-alpha2-antiplasmin that is rapidly cross-linked to fibrin and protects it from digestion by plasmin =

Synonyms

antiplasmin-cleaving enzyme, APCE, FAP, FAP-alpha, FAP-specific protease, FAPalpha, fibroblast activation factor, fibroblast activation protein, fibroblast activation protein alpha, fibroblast activation protein protease, fibroblast activation protein-alpha, fibroblast activation protein-specific protease, gelatinase, S09.007, seprase, surface expressed protease, type II transmembrane serine protease, Z-Pro-prolinal-insensitive peptidase, ZIP

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.21 Serine endopeptidases
                3.4.21.B28 fibroblast activation protein alpha subunit

IC50 Value

IC50 Value on EC 3.4.21.B28 - fibroblast activation protein alpha subunit

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.1
1-benzyl-7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
above, pH and temperature not specified in the publication
0.1
1-[(4-methoxyquinazolin-2-yl)methyl]-3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
above, pH and temperature not specified in the publication
0.05
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
pH and temperature not specified in the publication
0.1
3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
above, pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.0058
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
pH and temperature not specified in the publication
0.0012
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.041
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
pH and temperature not specified in the publication
0.0019
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
pH and temperature not specified in the publication
0.00074
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
pH and temperature not specified in the publication
0.01
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.0125
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
above, pH and temperature not specified in the publication
0.0018
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
pH and temperature not specified in the publication
0.0103
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.05
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.0033
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
pH and temperature not specified in the publication
0.011
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.1
alogliptin
Homo sapiens
above, pH and temperature not specified in the publication
0.00752
dutogliptin
Homo sapiens
pH and temperature not specified in the publication
0.000089 - 0.00037
linagliptin
Homo sapiens
pH and temperature not specified in the publication
0.01
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
pH and temperature not specified in the publication
0.0000033
N-[2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.01
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
pH and temperature not specified in the publication
0.01
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
pH and temperature not specified in the publication
0.1
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
above, pH and temperature not specified in the publication
0.091
Phe-Arg-(8-amino-3,6-dioxaoctanoic acid)-Gly-[R]-fluoropyrrolidide
Homo sapiens
cleavage of Met-alpha2-antiplasmin
0.0026
saxagliptin
Homo sapiens
pH and temperature not specified in the publication
0.1
sitagliptin
Homo sapiens
above, pH and temperature not specified in the publication
0.00004
Talabostat
Homo sapiens
-
0.073
vildagliptin
Homo sapiens
pH and temperature not specified in the publication
0.00007
[(2S)-1-(D-valyl)pyrrolidin-2-yl]boronic acid
Homo sapiens
pH and temperature not specified in the publication