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Literature summary for 3.4.14.5 extracted from

  • Kim, D.; Kowalchick, J.E.; Brockunier, L.L.; Parmee, E.R.; Eiermann, G.J.; Fisher, M.H.; He, H.; Leiting, B.; Lyons, K.; Scapin, G.; Patel, S.B.; Petrov, A.; Pryor, K.D.; Roy, R.S.; Wu, J.K.; Zhang, X.; Wyvratt, M.J.; Zhang, B.B.; Zhu, L.; Thornberry, N.A.; Weber, A.E.
    Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines (2008), J. Med. Chem., 51, 589-602.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-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-(2,4,5-trifluorophenyl)butan-2-amine
-
Rattus norvegicus
(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-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-[(5S)-5-methyl-3-(trifluoromethyl)-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-[(6R)-6-methyl-3-(trifluoromethyl)-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-[(6S)-6-methyl-3-(trifluoromethyl)-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-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-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-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-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-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-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-[(8R)-8-benzyl-3-(trifluoromethyl)-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-[(8R)-8-ethyl-3-(trifluoromethyl)-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-[(8R)-8-methyl-3-(trifluoromethyl)-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-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-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-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-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-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-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-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-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-[(8S)-8-benzyl-3-(trifluoromethyl)-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-[(8S)-8-ethyl-3-(trifluoromethyl)-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-[(8S)-8-methyl-3-(trifluoromethyl)-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-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-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-[5,5-dimethyl-3-(trifluoromethyl)-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-[8,8-dimethyl-3-(trifluoromethyl)-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
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
Rattus norvegicus
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
Rattus norvegicus
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
Rattus norvegicus
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000018
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00000031
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00000032
-
determination of the pharmacokinetic profile Rattus norvegicus (R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
0.0000004
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00000043
-
-
Rattus norvegicus (2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00000046
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00000066
-
-
Rattus norvegicus (2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0000015
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0000028
-
determination of the pharmacokinetic profile Rattus norvegicus 2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
0.0000043
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000005
-
-
Rattus norvegicus (2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0000057
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0000063
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000014
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000018
-
determination of the pharmacokinetic profile Rattus norvegicus (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000023
-
-
Rattus norvegicus (2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000032
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000042
-
-
Rattus norvegicus (2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000088
-
-
Rattus norvegicus (2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000091
-
-
Rattus norvegicus (2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000092
-
-
Rattus norvegicus (2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000113
-
-
Rattus norvegicus (2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000116
-
-
Rattus norvegicus (2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000123
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000131
-
-
Rattus norvegicus (2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000132
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00014
-
-
Rattus norvegicus (2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000175
-
-
Rattus norvegicus (2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00032
-
-
Rattus norvegicus (2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000377
-
-
Rattus norvegicus 2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
0.00043
-
-
Rattus norvegicus (R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
0.000438
-
-
Rattus norvegicus (2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000587
-
-
Rattus norvegicus (2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine