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Literature summary for 3.4.22.38 extracted from

  • Isabel, E.; Mellon, C.; Boyd, M.J.; Chauret, N.; Deschenes, D.; Desmarais, S.; Falgueyret, J.P.; Gauthier, J.Y.; Khougaz, K.; Lau, C.K.; Leger, S.; Levorse, D.A.; Li, C.S.; Masse, F.; Percival, M.D.; Roy, B.; Scheigetz, J.; Therien, M.; Truong, V.L.; Wesolowski, G.; Young, R.N.; Zamboni, R.; Black, W.C.
    Difluoroethylamines as an amide isostere in inhibitors of cathepsin K (2011), Bioorg. Med. Chem. Lett., 21, 920-923.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
L-873724
-
Oryctolagus cuniculus
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
Oryctolagus cuniculus
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
Oryctolagus cuniculus
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
Oryctolagus cuniculus
methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
Oryctolagus cuniculus
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
Oryctolagus cuniculus
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
Oryctolagus cuniculus
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
Oryctolagus cuniculus
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
Oryctolagus cuniculus
odanacatib
-
Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus
-
-
-

Synonyms

Synonyms Comment Organism
Cat K
-
Oryctolagus cuniculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000002
-
pH and temperature not specified in the publication Oryctolagus cuniculus odanacatib
0.0000002
-
pH and temperature not specified in the publication Oryctolagus cuniculus L-873724
0.0000003
-
pH and temperature not specified in the publication Oryctolagus cuniculus methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
0.0000003
-
pH and temperature not specified in the publication Oryctolagus cuniculus methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
0.0000003
-
pH and temperature not specified in the publication Oryctolagus cuniculus N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
0.0000003
-
pH and temperature not specified in the publication Oryctolagus cuniculus N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
0.0000008
-
pH and temperature not specified in the publication Oryctolagus cuniculus methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
0.000001
-
pH and temperature not specified in the publication Oryctolagus cuniculus methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
0.0000016
-
pH and temperature not specified in the publication Oryctolagus cuniculus N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
0.0000019
-
pH and temperature not specified in the publication Oryctolagus cuniculus N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide