Literature summary for 3.4.14.5 extracted from

Ammirati, M.J.; Andrews, K.M.; Boyer, D.D.; Brodeur, A.M.; Danley, D.E.; Doran, S.D.; Hulin, B.; Liu, S.; McPherson, R.K.; Orena, S.J.; Parker, J.C.; Polivkova, J.; Qiu, X.; Soglia, C.B.; Treadway, J.L.; VanVolkenburg, M.A.; Wilder, D.C.; Piotrowski, D.W.
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl)-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor (2009), Bioorg. Med. Chem. Lett., 19, 1991-1995.

Inhibitors

Inhibitors	Comment	Organism
(1S,3S,5S)-2-[(2S)-2-amino-2-[(1R,3S,5S)-3-hydroxytricyclo[3.3.1.13,7]dec-1-yl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile	-	Homo sapiens
(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	-	Homo sapiens
(2S)-1-([[(1R,3S,5S)-3-hydroxytricyclo[3.3.1.13,7]dec-1-yl]amino]acetyl)pyrrolidine-2-carbonitrile	-	Homo sapiens
(2S,3S)-3-methyl-1-oxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine	-	Homo sapiens
(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4R)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin)-2-yl]-methanone	-	Homo sapiens
(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl)-piperazin-1-yl)-pyrrolidin-2-yl]-methanone	PF-00734200, potent, selective, orally active dipeptidyl peptidase IV inhibitor	Homo sapiens
1-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3,4,4-tetrafluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3-difluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrazine	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyridine-3-carbonitrile	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)[1,3]oxazolo[5,4-b]pyridine	-	Homo sapiens
2-(4-[(3R,5S)-5-[(3-fluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine	-	Homo sapiens
2-([6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl)benzonitrile	-	Homo sapiens
2-[4-[(3R,5S)-5-(azetidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine	-	Homo sapiens
2-[4-[(3R,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine	-	Homo sapiens
2-[4-[(3R,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine	-	Homo sapiens
2-[4-[(3R,5S)-5-[[(3R,4R)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine	-	Homo sapiens
2-[4-[(3R,5S)-5-[[(3R,4S)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine	-	Homo sapiens
2-[4-[(3R,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P27487	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
blood plasma	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
Gly-L-Pro-7-amido-4-methylcoumarin + H2O	-	Homo sapiens	Gly-L-Pro + 7-amino-4-methylcoumarin	-	?

Synonyms

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

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.0000048	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyridine-3-carbonitrile
0.0000052	-	-	Homo sapiens	1-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
0.0000052	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)[1,3]oxazolo[5,4-b]pyridine
0.0000056	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrazine
0.0000058	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
0.0000074	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
0.0000082	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
0.0000087	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
0.0000129	-	-	Homo sapiens	(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl)-piperazin-1-yl)-pyrrolidin-2-yl]-methanone
0.000013	-	-	Homo sapiens	2-[4-[(3R,5S)-5-[[(3R,4S)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
0.000025	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3,4,4-tetrafluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
0.000031	-	-	Homo sapiens	2-[4-[(3R,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
0.000031	-	-	Homo sapiens	2-[4-[(3R,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
0.000041	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3-fluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
0.000051	-	-	Homo sapiens	2-[4-[(3R,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
0.000134	-	-	Homo sapiens	2-(4-[(3R,5S)-5-[(3,3-difluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
0.000309	-	-	Homo sapiens	2-[4-[(3R,5S)-5-(azetidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
0.000309	-	-	Homo sapiens	2-[4-[(3R,5S)-5-[[(3R,4R)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
0.000338	-	-	Homo sapiens	(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4R)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin)-2-yl]-methanone