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Literature summary for 3.4.23.46 extracted from

  • Steele, T.G.; Hills, I.D.; Nomland, A.A.; de Leon, P.; Allison, T.; McGaughey, G.; Colussi, D.; Tugusheva, K.; Haugabook, S.J.; Espeseth, A.S.; Zuck, P.; Graham, S.L.; Stachel, S.J.
    Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement (2009), Bioorg. Med. Chem. Lett., 19, 17-20.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor N-[2-methyl-5-[(6-phenylpyrimidin-4-yl)amino]phenyl]methanesulfonamide. The catalytic aspartate residues in the acitve site are not engaged in inhibitor binding Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-(2-methyl-5-[(6-phenylpyrimidin-4-yl)amino]phenyl)methanesulfonamide
-
Homo sapiens
N-(5-([6-(4-(N,N-dimethyl)aminophenyl)pyrimidin-4-yl]amino)-2-methylphenyl)-N-methylmethanesulfonamide
-
Homo sapiens
N-(5-[[6-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-4-yl]amino]-2-methylphenyl)-N-methylmethanesulfonamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.015
-
-
Homo sapiens N-(5-([6-(4-(N,N-dimethyl)aminophenyl)pyrimidin-4-yl]amino)-2-methylphenyl)-N-methylmethanesulfonamide
0.021
-
-
Homo sapiens N-(5-[[6-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-4-yl]amino]-2-methylphenyl)-N-methylmethanesulfonamide
0.024
-
-
Homo sapiens N-(2-methyl-5-[(6-phenylpyrimidin-4-yl)amino]phenyl)methanesulfonamide