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Literature summary for 3.4.23.46 extracted from

  • Barrow, J.C.; Stauffer, S.R.; Rittle, K.E.; Ngo, P.L.; Yang, Z.; Selnick, H.G.; Graham, S.L.; Munshi, S.; McGaughey, G.B.; Holloway, M.K.; Simon, A.J.; Price, E.A.; Sankaranarayanan, S.; Colussi, D.; Tugusheva, K.; Lai, M.T.; Espeseth, A.S.; Xu, M.; Huang, Q.; Wolfe, A.; Pietrak, B.; Zuck, P.; Levorse, D.A.; Haz, H.a.z.u.
    Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase (2008), J. Med. Chem., 51, 6259-6262.
    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-(4-([4-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-8-yl]methyl)phenyl)acetamide. Inhibitor interacts with the catalytic residues via bridging water molecules Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-(cyclohexylamino)-1-(4-fluorobenzyl)-8-[(2'-methylbiphenyl-4-yl)methyl]-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
Homo sapiens
4-[8-benzyl-4-(cyclohexylamino)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-1-yl]benzamide
-
Homo sapiens
8-(biphenyl-4-ylmethyl)-4-(cyclohexylamino)-1-(4-fluorobenzyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
Homo sapiens
8-benzyl-4-(cyclohexylamino)-1-(3-fluorophenyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
Homo sapiens
N-(4-([4-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-8-yl]methyl)phenyl)acetamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00011
-
-
Homo sapiens 4-(cyclohexylamino)-1-(4-fluorobenzyl)-8-[(2'-methylbiphenyl-4-yl)methyl]-1,3,8-triazaspiro[4.5]dec-3-en-2-one
0.0028
-
-
Homo sapiens N-(4-([4-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-8-yl]methyl)phenyl)acetamide
0.0046
-
-
Homo sapiens 8-(biphenyl-4-ylmethyl)-4-(cyclohexylamino)-1-(4-fluorobenzyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
0.008
-
-
Homo sapiens 4-[8-benzyl-4-(cyclohexylamino)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-1-yl]benzamide
0.011
-
-
Homo sapiens 8-benzyl-4-(cyclohexylamino)-1-(3-fluorophenyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one