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Literature summary for 3.4.14.4 extracted from

  • Agic, D.; Hranjec, M.; Jajcanin, N.; Starcevic, K.; Karminski-Zamola, G.; Abramic, M.
    Novel amidino-substituted benzimidazoles: synthesis of compounds and inhibition of dipeptidyl peptidase III (2007), Bioorg. Chem., 35, 153-169.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-furyl)-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutanedihydrochloride
-
Homo sapiens
1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenylcyclobutane dihydrochloride
-
Homo sapiens
1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
Homo sapiens
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-carboxamidine hydrochloride complete inhibition at 0.1 mM Homo sapiens
2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-imidazolinylamidine hydrochloride complete inhibition at 0.1 mM Homo sapiens
2-[(E)-2-phenylethenyl]-1H-benzimidazole
-
Homo sapiens
6-(4,5-dihydro-1H-imidazol-2-yl)-2-[(E)-2-phenylethenyl]-1H-benzimidazole
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
human DPP III is purified from healthy blood donor erythrocytes Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
erythrocyte
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Arg-Arg-2-naphthylamide + H2O
-
Homo sapiens Arg-Arg + 2-naphthylamine
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl aminopeptidase III
-
Homo sapiens
dipeptidyl aminopeptidase III formerly Homo sapiens
dipeptidyl arylamidase III
-
Homo sapiens
dipeptidyl arylamidase III formerly Homo sapiens
dipeptidyl peptidase III
-
Homo sapiens
DPP III
-
Homo sapiens
enkephalinase B
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
activity assay Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
activity assay Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0002
-
1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.001
-
-
Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutane dihydrochloride
0.0017
-
-
Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
0.0017
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
0.0028
-
-
Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
0.0028
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
0.0056
-
-
Homo sapiens 1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
0.0056
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
0.006
-
-
Homo sapiens 1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
0.006
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-o-chlorophenylcyclobutane dihydrochloride
0.007
-
-
Homo sapiens 1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
0.007
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(N-amidino)-2-benzimidazolyl]-2,4-di-o-chlorophenyl-cyclobutane dihydrochloride
0.008
-
-
Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-furyl)-cyclobutane dihydrochloride
0.008
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-furyl)-cyclobutane dihydrochloride
0.01
-
-
Homo sapiens 1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
0.01
-
-
Homo sapiens 6-(4,5-dihydro-1H-imidazol-2-yl)-2-[(E)-2-phenylethenyl]-1H-benzimidazole
0.01
-
at pH 7.4 for 10 min at 25°C Homo sapiens 1,3-di-[5-(2-imidazolinyl)-2-benzoimidazolyl]-2,4-di-(2-thienyl)-cyclobutanedihydrochloride
0.01
-
at pH 7.4 for 10 min at 25°C, IC50 above 0.01 mM Homo sapiens 1,3-di-[5-(N-isopropylamidino)-2-benzimidazolyl]-2,4-di-phenyl-cyclobutane dihydrochloride
0.018
-
-
Homo sapiens 2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-imidazolinylamidine hydrochloride
0.018
-
at pH 7.4 for 10 min at 25°C Homo sapiens 2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-imidazolinylamidine hydrochloride
0.053
-
-
Homo sapiens 2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-carboxamidine hydrochloride
0.053
-
at pH 7.4 for 10 min at 25°C Homo sapiens 2-(3H-imidazol-4-yl)-1H-benzoimidazole-5-carboxamidine hydrochloride
0.1
-
-
Homo sapiens 2-[(E)-2-phenylethenyl]-1H-benzimidazole