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Literature summary for 3.4.16.2 extracted from

  • Graham, T.H.; Liu, W.; Verras, A.; Reibarkh, M.; Bleasby, K.; Bhatt, U.R.; Chen, Q.; Garcia-Calvo, M.; Geissler, W.M.; Gorski, J.N.; He, H.; Lassman, M.E.; Lisnock, J.; Li, X.; Shen, Z.; Tong, X.; Tung, E.C.; Wiltsie, J.; Xie, D.; Xu, S.; Xiao, J.; Hale, J.J.; Pinto, S.; Shen, D.M.
    A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes (2012), Bioorg. Med. Chem. Lett., 22, 2818-2822.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
-
 Homo sapiens
[4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone compound has a superior in vivo profile, and also maintains a low brain to plasma ratio Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000003
-
 [4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone pH not specified in the publication, temperature not specified in the publication Mus musculus
0.0000013
-
 [4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone in 100% mouse plasma, pH not specified in the publication, temperature not specified in the publication Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000002
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus [4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone
0.0000003
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens [4-[1-(3-chloro-4-fluorophenyl)-1H-pyrazol-5-yl]piperidin-1-yl][(1R,2R,4S)-2-(2,4-difluorophenyl)-4-(dimethylamino)-4-methylcyclopentyl]methanone