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Literature summary for 3.4.14.5 extracted from

  • Fukushima, H.; Hiratate, A.; Takahashi, M.; Saito-Hori, M.; Munetomo, E.; Kitano, K.; Saito, H.; Takaoka, Y.; Yamamoto, K.
    Synthesis and structure-activity relationships of potent 1-(2-substituted-aminoacetyl)-4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors (2008), Chem. Pharm. Bull., 56, 1110-1117.
    View publication on PubMed
Search for more literature for 3.4.14.5

Inhibitors

Inhibitors Comment Organism Structure
(2R,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2R,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2R,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2R,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-1-((2S)-2-amino-3-methylpentanoyl)-4-fluoropyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-1-(O-benzyl-L-threonyl)-4-fluoropyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-1-L-alloisoleucyl-4-fluoropyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-1-[(2S)-2-amino-2-cyclohexylacetyl]-4-fluoropyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-1-[O-(tert-butyl)-L-threonyl]-4-fluoropyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-1-[[(3S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]-4-fluoropyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-(N-methyl-L-isoleucyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-(O-methyl-L-threonyl)pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-L-valyl-pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-[(3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-[[(3S)-7-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
 Homo sapiens
(2S,4S)-4-fluoro-1-[[(3S)-7-methoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
 Homo sapiens
2-[[(3S)-3-[[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]carbonyl]-1,2,3,4-tetrahydroisoquinolin-7-yl]oxy]acetamide
-
 Homo sapiens
benzyl 6-([5-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-(4S)-4-amino-5-oxopentanoyl]amino)hexanoate
-
 Homo sapiens
benzyl [(5S)-5-amino-6-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-6-oxohexyl]carbamate
-
 Homo sapiens
NVP-DPP728
-
 Homo sapiens
saxagliptin BMS-477118 Homo sapiens
sitagliptin MK-0431 Homo sapiens
vildagliptin NVP-LAF237 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
0.0000006
-
-
 Homo sapiens (2S,4S)-1-((2S)-2-amino-3-methylpentanoyl)-4-fluoropyrrolidine-2-carbonitrile
0.0000006
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
0.0000007
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-L-valyl-pyrrolidine-2-carbonitrile
0.0000007
-
-
 Homo sapiens benzyl 6-([5-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-(4S)-4-amino-5-oxopentanoyl]amino)hexanoate
0.0000008
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
0.0000011
-
-
 Homo sapiens (2S,4S)-1-[(2S)-2-amino-2-cyclohexylacetyl]-4-fluoropyrrolidine-2-carbonitrile
0.0000012
-
-
 Homo sapiens (2S,4S)-1-L-alloisoleucyl-4-fluoropyrrolidine-2-carbonitrile
0.0000012
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-[[(3S)-7-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
0.0000014
-
-
 Homo sapiens benzyl [(5S)-5-amino-6-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-6-oxohexyl]carbamate
0.0000017
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-[[(3S)-7-methoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
0.0000021
-
-
 Homo sapiens (2S,4S)-1-(O-benzyl-L-threonyl)-4-fluoropyrrolidine-2-carbonitrile
0.0000022
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-[(3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]pyrrolidine-2-carbonitrile
0.0000025
-
-
 Homo sapiens (2S,4S)-1-[[(3S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]-4-fluoropyrrolidine-2-carbonitrile
0.0000033
-
-
 Homo sapiens 2-[[(3S)-3-[[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]carbonyl]-1,2,3,4-tetrahydroisoquinolin-7-yl]oxy]acetamide
0.0000047
-
-
 Homo sapiens (2S,4S)-4-fluoro-1-(O-methyl-L-threonyl)pyrrolidine-2-carbonitrile
0.0000049
-
-
 Homo sapiens (2S,4S)-1-[O-(tert-butyl)-L-threonyl]-4-fluoropyrrolidine-2-carbonitrile
0.000006
-
-
 Homo sapiens (2S,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
0.000042
-
-
 Homo sapiens (2S,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
0.0001
-
 IC50 above 0.0001 mM Homo sapiens (2S,4S)-4-fluoro-1-(N-methyl-L-isoleucyl)pyrrolidine-2-carbonitrile
0.000246
-
-
 Homo sapiens (2R,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
0.0003
-
 IC50 above 0.0003 mM Homo sapiens (2R,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
0.0003
-
 IC50 above 0.0003 mM Homo sapiens (2S,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
0.0003
-
 IC50 above 0.0003 mM Homo sapiens (2R,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
0.0003
-
 IC50 above 0.0003 mM Homo sapiens (2R,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile