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Literature summary for 3.4.23.46 extracted from

  • Machauer, R.; Veenstra, S.; Rondeau, J.M.; Tintelnot-Blomley, M.; Betschart, C.; Neumann, U.; Paganetti, P.
    Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 1361-1365.
    View publication on PubMed
Search for more literature for 3.4.23.46

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor (2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R,4S)-N-butyl-4-hydroxy-2-methyl-4-[(2S,5S,7R)-1,2,7-trimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]butanamide 56fold selectivity for beta-secretase over cathepsin D Homo sapiens
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
 Homo sapiens
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00015
-
-
 Homo sapiens (2R,4S)-N-butyl-4-hydroxy-2-methyl-4-[(2S,5S,7R)-1,2,7-trimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]butanamide
0.00025
-
-
 Homo sapiens (2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]-4-hydroxy-2-methylbutanamide
0.00059
-
-
 Homo sapiens (2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide