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Literature summary for 3.4.14.5 extracted from

  • Cox, J.M.; Harper, B.; Mastracchio, A.; Leiting, B.; Sinha Roy, R.; Patel, R.A.; Wu, J.K.; Lyons, K.A.; He, H.; Xu, S.; Zhu, B.; Thornberry, N.A.; Weber, A.E.; Edmondson, S.D.
    Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 4579-4583.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R,4R)-1-(2-methyl-3-oxo-2,3-dihydro[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-(2-methyl-4-oxo-3,4-dihydropyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-(2-methyl-4-oxo-4H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium pharmacokinetic properties Homo sapiens
(3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium pharmacokinetic properties Homo sapiens
(3R,4R)-1-(3-ethyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium pharmacokinetic properties Homo sapiens
(3R,4R)-1-(4-cyanopyridin-2-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-(4-cyclopropylpyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-isoquinolin-1-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-phenyl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pteridin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pyrazino[2,3-b]pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pyridin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pyridin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pyridin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pyrido[2,3-b]pyrazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-pyrido[2,3-b]pyrazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-quinolin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-quinoxalin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[1,2,4]triazolo[4,3-a]pyrimidin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium pharmacokinetic properties Homo sapiens
(3R,4R)-1-[1,2,4]triazolo[4,3-b]pyridazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[2-(trifluoromethyl)imidazo[1,2-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[2-(trifluoromethyl)[1,2,4]triazolo[1,5-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[3-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[3-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[4-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[5-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3R,4R)-1-[6-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3S,4S)-1-pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3S,4S)-1-pyridazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3S,4S)-1-pyrimidin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
(3S,4S)-1-pyrimidin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
Homo sapiens
additional information substituted 3-aminopiperidines are evaluated as DPP-4 inhibitors. The inhibitors show good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9) Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
DPP-4
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000012
-
pharmacokinetic properties Homo sapiens (3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000002
-
-
Homo sapiens (3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000005
-
-
Homo sapiens (3R,4R)-1-(2-methyl-3-oxo-2,3-dihydro[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000005
-
-
Homo sapiens (3R,4R)-1-[2-(trifluoromethyl)[1,2,4]triazolo[1,5-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000006
-
-
Homo sapiens (3R,4R)-1-(3-ethyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000006
-
pharmacokinetic properties Homo sapiens (3R,4R)-1-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000007
-
-
Homo sapiens (3R,4R)-1-(2-methyl-4-oxo-3,4-dihydropyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000007
-
-
Homo sapiens (3R,4R)-1-pyrido[2,3-b]pyrazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000008
-
-
Homo sapiens (3R,4R)-1-(4-cyclopropylpyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000008
-
pharmacokinetic properties Homo sapiens (3R,4R)-1-(2-methyl-4-oxo-4H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000009
-
-
Homo sapiens (3R,4R)-1-[3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000012
-
-
Homo sapiens (3R,4R)-1-quinoxalin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000013
-
-
Homo sapiens (3R,4R)-1-pyrazino[2,3-b]pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000014
-
-
Homo sapiens (3R,4R)-1-(4-cyanopyridin-2-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000016
-
-
Homo sapiens (3R,4R)-1-[3-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000022
-
-
Homo sapiens (3R,4R)-1-[2-(trifluoromethyl)imidazo[1,2-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000026
-
pharmacokinetic properties Homo sapiens (3R,4R)-1-[1,2,4]triazolo[4,3-a]pyrimidin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000031
-
-
Homo sapiens (3R,4R)-1-[1,2,4]triazolo[4,3-b]pyridazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000037
-
-
Homo sapiens (3S,4S)-1-pyrimidin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000043
-
-
Homo sapiens (3R,4R)-1-pteridin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000054
-
-
Homo sapiens (3R,4R)-1-quinolin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000058
-
-
Homo sapiens (3R,4R)-1-pyridin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000063
-
-
Homo sapiens (3S,4S)-1-pyridazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000067
-
-
Homo sapiens (3R,4R)-1-[4-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000082
-
-
Homo sapiens (3S,4S)-1-pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.00009
-
-
Homo sapiens (3S,4S)-1-pyrimidin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000111
-
-
Homo sapiens (3R,4R)-1-[3-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000125
-
-
Homo sapiens (3R,4R)-1-pyridin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.00013
-
-
Homo sapiens (3R,4R)-1-pyrido[2,3-b]pyrazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000144
-
-
Homo sapiens (3R,4R)-1-pyridin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.00021
-
-
Homo sapiens (3R,4R)-1-phenyl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.000463
-
-
Homo sapiens (3R,4R)-1-[5-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.00065
-
-
Homo sapiens (3R,4R)-1-[6-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.0037
-
-
Homo sapiens (3R,4R)-1-isoquinolin-1-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium