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Literature summary for 3.4.14.5 extracted from

  • Sheehan, S.M.; Mest, H.J.; Watson, B.M.; Klimkowski, V.J.; Timm, D.E.; Cauvin, A.; Parsons, S.H.; Shi, Q.; Canada, E.J.; Wiley, M.R.; Ruehter, G.; Evers, B.; Petersen, S.; Blaszczak, L.C.; Pulley, S.R.; Margolis, B.J.; Wishart, G.N.; Renson, B.; Hankotius, D.; Mohr, M.; Zechel, J.C.; Michael Kalbfleisch, J.
    Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site (2007), Bioorg. Med. Chem. Lett., 17, 1765-1768.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-[(1-[[2-oxo-2-(3-thienyl)ethyl]amino]cyclopentyl)methoxy]benzamide
-
Homo sapiens
4-[(3R)-3-[(2-oxo-2-phenylethyl)amino]butyl]benzamide
-
Homo sapiens
4-[(3R)-3-[[2-(2-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
Homo sapiens
4-[(3R)-3-[[2-(3,4-difluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
Homo sapiens
4-[(3R)-3-[[2-(4-chlorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
Homo sapiens
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
Homo sapiens
4-[(3R)-3-[[2-oxo-2-(3-thienyl)ethyl]amino]butyl]benzamide
-
Homo sapiens
4-[[(2R)-2-[[2-oxo-2-(3-thienyl)ethyl]amino]propyl]oxy]benzamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27487 recombinant enzyme
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Homo sapiens
DPP-IV
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
-
Homo sapiens 4-[(1-[[2-oxo-2-(3-thienyl)ethyl]amino]cyclopentyl)methoxy]benzamide
0.000039
-
-
Homo sapiens 4-[(3R)-3-[[2-(3,4-difluorophenyl)-2-oxoethyl]amino]butyl]benzamide
0.000084
-
-
Homo sapiens 4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
0.00011
-
-
Homo sapiens 4-[(3R)-3-[[2-oxo-2-(3-thienyl)ethyl]amino]butyl]benzamide
0.00028
-
-
Homo sapiens 4-[(3R)-3-[(2-oxo-2-phenylethyl)amino]butyl]benzamide
0.00034
-
-
Homo sapiens 4-[[(2R)-2-[[2-oxo-2-(3-thienyl)ethyl]amino]propyl]oxy]benzamide
0.00082
-
-
Homo sapiens 4-[(3R)-3-[[2-(4-chlorophenyl)-2-oxoethyl]amino]butyl]benzamide
0.0038
-
-
Homo sapiens 4-[(3R)-3-[[2-(2-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide