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Literature summary for 3.4.14.5 extracted from

  • Ahn, J.H.; Shin, M.S.; Jun, M.A.; Jung, S.H.; Kang, S.K.; Kim, K.R.; Rhee, S.D.; Kang, N.S.; Kim, S.Y.; Sohn, S.K.; Kim, S.G.; Jin, M.S.; Lee, J.O.; Cheon, H.G.; Kim, S.S.
    Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 2622-2628.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-4-(2-benzoylpyrazolidin-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Homo sapiens
(2R)-4-oxo-4-pyrazolidin-1-yl-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Homo sapiens
(2R)-4-oxo-4-[2-(phenylcarbonyl)-1,2-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine competitive Homo sapiens
(2R)-4-oxo-4-[2-(phenylcarbonyl)tetrahydropyridazin-1(2H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine the inhibitor displays a greater than 1400fold selectivity over all the enzymes tested including DPP-8 and DPP-9 Homo sapiens
(2R)-4-[2-[(4-methylphenyl)sulfonyl]pyrazolidin-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Homo sapiens
2-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-phenylpyrazolidine-1-carboxamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
the inhibitor displays a greater than 1400fold selectivity over all the enzymes tested including DPP-8 and DPP-9 Homo sapiens (2R)-4-oxo-4-[2-(phenylcarbonyl)tetrahydropyridazin-1(2H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00007
-
competitive Homo sapiens (2R)-4-oxo-4-[2-(phenylcarbonyl)-1,2-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00035
-
-
Homo sapiens (2R)-4-(2-benzoylpyrazolidin-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0005
-
-
Homo sapiens (2R)-4-[2-[(4-methylphenyl)sulfonyl]pyrazolidin-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00099
-
-
Homo sapiens 2-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-phenylpyrazolidine-1-carboxamide
0.00385
-
-
Homo sapiens (2R)-4-oxo-4-pyrazolidin-1-yl-1-(2,4,5-trifluorophenyl)butan-2-amine