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Literature summary for 3.4.14.5 extracted from

  • Abe, M.; Akiyama, T.; Umezawa, Y.; Yamamoto, K.; Nagai, M.; Yamazaki, H.; Ichikawa, Y.; Muraoka, Y.
    Synthesis and biological activity of sulphostin analogues, novel dipeptidyl peptidase IV inhibitors (2005), Bioorg. Med. Chem., 13, 785-797.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R)-3-amino-1-diaminophosphinyl-2-piperidinone IC50: 46 nM Rattus norvegicus
(3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone IC50: 130 nM Rattus norvegicus
(3S)-3-amino-1-diaminophosphinyl-2-piperidinone IC50: 94 nM Rattus norvegicus
(3S)-3-amino-1-diaminophosphinyl-2-pyrrolidinone IC50: 11 nM Rattus norvegicus
sulphostin IC50: 21 nM Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gly-Pro-2-naphthylamide + H2O
-
Rattus norvegicus Gly-Pro + 2-naphthylamine
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000011
-
IC50: 11 nM Rattus norvegicus (3S)-3-amino-1-diaminophosphinyl-2-pyrrolidinone
0.000021
-
IC50: 21 nM Rattus norvegicus sulphostin
0.000046
-
IC50: 46 nM Rattus norvegicus (3R)-3-amino-1-diaminophosphinyl-2-piperidinone
0.000094
-
IC50: 94 nM Rattus norvegicus (3S)-3-amino-1-diaminophosphinyl-2-piperidinone
0.00013
-
IC50: 130 nM Rattus norvegicus (3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone