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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Synonyms | Comment | Organism |
---|---|---|
DPP-4 | - |
Homo sapiens |
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 |