Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.14.5 extracted from

  • Duffy, J.L.; Kirk, B.A.; Wang, L.; Eiermann, G.J.; He, H.; Leiting, B.; Lyons, K.A.; Patel, R.A.; Patel, S.B.; Petrov, A.; Scapin, G.; Wu, J.K.; Thornberry, N.A.; Weber, A.E.
    4-Aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV (2007), Bioorg. Med. Chem. Lett., 17, 2879-2885.
    View publication on PubMed
Search for more literature for 3.4.14.5

Crystallization (Commentary)

Crystallization (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1S)-1-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethanaminium
-
 Homo sapiens
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
-
 Homo sapiens
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-[4-(acetylamino)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-[(phenylsulfonyl)amino]phenyl]butan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)carbonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)sulfonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(2S,3S)-4-(dimethylamino)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
 Homo sapiens
(3S,4S)-5-(dimethylamino)-2-[(3S)-3-fluoropyrrolidin-1-yl]-5-oxo-4-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)pent-1-en-3-aminium
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27487
-
-

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
 Homo sapiens
DPP-4
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
-
 Homo sapiens (3S,4S)-5-(dimethylamino)-2-[(3S)-3-fluoropyrrolidin-1-yl]-5-oxo-4-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)pent-1-en-3-aminium
0.000012
-
-
 Homo sapiens (2S,3S)-4-(dimethylamino)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.000016
-
 0% human serum Homo sapiens (2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000022
-
 0% human serum Homo sapiens (2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.000022
-
 0% human serum Homo sapiens (2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000024
-
 0% human serum Homo sapiens (2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.000025
-
-
 Homo sapiens (2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)carbonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
0.000027
-
 0% human serum Homo sapiens (2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
0.000028
-
-
 Homo sapiens (2S,3S)-4-(dimethylamino)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.000029
-
 0% human serum Homo sapiens (2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.00004
-
 50% human serum Homo sapiens (2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000047
-
 50% human serum Homo sapiens (2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000048
-
 0% human serum Homo sapiens (1S)-1-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethanaminium
0.000064
-
-
 Homo sapiens (2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000074
-
 0% human serum Homo sapiens (2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
0.000092
-
 50% human serum Homo sapiens (2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.000097
-
 50% human serum Homo sapiens (2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
0.00015
-
-
 Homo sapiens (2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.00016
-
-
 Homo sapiens (2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00019
-
 50% human serum Homo sapiens (2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.0002
-
 50% human serum Homo sapiens (2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.00021
-
-
 Homo sapiens (2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00021
-
 50% human serum Homo sapiens (2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
0.0003
-
-
 Homo sapiens (2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00033
-
 0% human serum Homo sapiens (2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.00036
-
 0% human serum Homo sapiens (2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
0.00043
-
-
 Homo sapiens (2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)sulfonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
0.00044
-
 0% human serum Homo sapiens (2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
0.00046
-
 0% human serum Homo sapiens (2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00051
-
 50% human serum Homo sapiens (2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.0006
-
-
 Homo sapiens (2S,3S)-3-[4-(acetylamino)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00087
-
-
 Homo sapiens (2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-[(phenylsulfonyl)amino]phenyl]butan-2-aminium
0.00128
-
 50% human serum Homo sapiens (2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
0.00149
-
 50% human serum Homo sapiens (2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00347
-
 50% human serum Homo sapiens (2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium