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Literature summary for 3.4.14.5 extracted from

  • Kim, D.; Kowalchick, J.E.; Edmondson, S.D.; Mastracchio, A.; Xu, J.; Eiermann, G.J.; Leiting, B.; Wu, J.K.; Pryor, K.D.; Patel, R.A.; He, H.; Lyons, K.A.; Thornberry, N.A.; Weber, A.E.
    Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate) (2007), Bioorg. Med. Chem. Lett., 17, 3373-3377.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
-
Rattus norvegicus
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
-
Rattus norvegicus
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
-
Rattus norvegicus
(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
-
Rattus norvegicus
(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
-
Rattus norvegicus
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
Rattus norvegicus
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
Rattus norvegicus
sitagliptin
-
Rattus norvegicus
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
DPP-4
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000018
-
-
Rattus norvegicus sitagliptin
0.000021
-
-
Rattus norvegicus (2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000023
-
-
Rattus norvegicus (2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000027
-
-
Rattus norvegicus (2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000029
-
-
Rattus norvegicus (2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00003
-
-
Rattus norvegicus (2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
0.00003
-
-
Rattus norvegicus (2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000037
-
-
Rattus norvegicus (2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000059
-
-
Rattus norvegicus (2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.00006
-
-
Rattus norvegicus (2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
0.000065
-
-
Rattus norvegicus (2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
0.000069
-
-
Rattus norvegicus [7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
0.000076
-
-
Rattus norvegicus (2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000082
-
-
Rattus norvegicus (2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000084
-
-
Rattus norvegicus (2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000087
-
-
Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
0.000098
-
-
Rattus norvegicus (2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000128
-
-
Rattus norvegicus (2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000135
-
-
Rattus norvegicus (2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000145
-
-
Rattus norvegicus (2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000151
-
-
Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
0.00018
-
-
Rattus norvegicus (2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.00019
-
-
Rattus norvegicus ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
0.000219
-
-
Rattus norvegicus ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
0.000234
-
-
Rattus norvegicus 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
0.000264
-
-
Rattus norvegicus (2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000272
-
-
Rattus norvegicus (2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.000366
-
-
Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
0.000511
-
-
Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
0.000805
-
-
Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
0.001018
-
-
Rattus norvegicus (2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.00158
-
-
Rattus norvegicus (2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.00486
-
-
Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine