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Literature summary for 3.4.14.5 extracted from

  • Wang, L.; Zhang, B.; Ji, J.; Li, B.; Yan, J.; Zhang, W.; Wu, Y.; Wang, X.
    Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors (2009), Eur. J. Med. Chem., 44, 3318-3322.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(S)-1-(2-(2-(2-oxo-3-(3,4,5-trimethoxyphenyl)imidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(2-oxo-3-p-tolylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(2-oxo-3-phenylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(2-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(3,5-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(3-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(3-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(4-chlorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-(4-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-cyclohexyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-isopropyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
(S)-1-(2-(2-(3-tert-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
Homo sapiens
alogliptin SYR-322 Homo sapiens
saxagliptin BMS477118 Homo sapiens
sitagliptin MK-0431 Homo sapiens
vildagliptin LAF-237 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glucagon-like peptide 1 + H2O Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glucagon-like peptide 1 + H2O
-
Homo sapiens ?
-
?
Gly-L-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Gly-L-Pro + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
CD26
-
Homo sapiens
dipeptidyl peptidase IV
-
Homo sapiens
DPP-IV
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000166
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens vildagliptin
0.0000204
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(3,5-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000258
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(4-chlorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000293
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(2-oxo-3-p-tolylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000348
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(2-oxo-3-phenylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000445
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000478
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-isopropyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000535
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000601
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(3-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000651
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(3-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000681
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-tert-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000686
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-cyclohexyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0000824
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(4-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0001336
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(3-(2-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
0.0001656
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C Homo sapiens (S)-1-(2-(2-(2-oxo-3-(3,4,5-trimethoxyphenyl)imidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile