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Literature summary for 3.4.21.B28 extracted from

  • Tran, T.; Quan, C.; Edosada, C.Y.; Mayeda, M.; Wiesmann, C.; Sutherlin, D.; Wolf, B.B.
    Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP (2007), Bioorg. Med. Chem. Lett., 17, 1438-1442.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
L-Val-aminoacyl-proline boronic acid PT-100 Homo sapiens
N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-9-N-methyl-5-oxoprolinamide
-
Homo sapiens
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
-
Homo sapiens
[(2R)-1-(N-acetyl-L-alanyl)pyrrolidin-2-yl]boronic acid
-
Homo sapiens
[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
-
Homo sapiens
[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
-
Homo sapiens
[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl-9]-boronic acid
-
Homo sapiens
[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
Homo sapiens
[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
Homo sapiens
[(2R)-1-[N-[(2,6-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q12884
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens Gly-Pro + 7-amino-4-trifluoromethylcoumarin + H2O
-
?

Synonyms

Synonyms Comment Organism
FAP
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000075
-
[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000012
-
[(2R)-1-[N-[(2,6-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000014
-
[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.00002
-
[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000023
-
[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000029
-
[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000051
-
[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000094
-
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000142
-
[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000146
-
N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-9-N-methyl-5-oxoprolinamide in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000161
-
[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000191
-
[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000246
-
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000265
-
[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.00035
-
[(2R)-1-(N-acetyl-L-alanyl)pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.000751
-
[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
0.0029
-
[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens