Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.23.46 extracted from

  • Winneroski, L.L.; Schiffler, M.A.; Erickson, J.A.; May, P.C.; Monk, S.A.; Timm, D.E.; Audia, J.E.; Beck, J.P.; Boggs, L.N.; Borders, A.R.; Boyer, R.D.; Brier, R.A.; Hudziak, K.J.; Klimkowski, V.J.; Garcia Losada, P.; Mathes, B.M.; Stout, S.L.; Watson, B.M.; Mergott, D.J.
    Preparation and biological evaluation of conformationally constrained BACE1 inhibitors (2015), Bioorg. Med. Chem., 23, 3260-3268 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(+)-N-((4S,4aS,6S,8aR)-10-amino-4,4a,5,6,7,8-hexahydro-1H,3H-4,8a-(epithiomethenoazeno)isochromen-6-yl)-3-chlorobenzamide
-
Homo sapiens
2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl 3-chlorobenzoate
-
Homo sapiens
4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-2-amine
-
Homo sapiens
LY2811376
-
Homo sapiens
LY2886721
-
Homo sapiens
N-((4aRS,6RS,8aSR)-2-amino-5,6,7,8-tetrahydro-4H-4a,8a-(methanooxymethano)benzo[d][1,3]thiazin-6-yl)-3-chlorobenzamide
-
Homo sapiens
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-3-chlorobenzamide
-
Homo sapiens
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-5-fluoropyridine-2-carboxamide
-
Homo sapiens
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)benzamide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
amyloid-beta precursor protein + H2O Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid-beta precursor protein + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
BACE1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00183
-
pH and temperature not specified in the publication Homo sapiens N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-3-chlorobenzamide
0.00225
-
pH and temperature not specified in the publication Homo sapiens (+)-N-((4S,4aS,6S,8aR)-10-amino-4,4a,5,6,7,8-hexahydro-1H,3H-4,8a-(epithiomethenoazeno)isochromen-6-yl)-3-chlorobenzamide
0.0361
-
pH and temperature not specified in the publication Homo sapiens N-((4aRS,6RS,8aSR)-2-amino-5,6,7,8-tetrahydro-4H-4a,8a-(methanooxymethano)benzo[d][1,3]thiazin-6-yl)-3-chlorobenzamide
4
-
pH and temperature not specified in the publication Homo sapiens 4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-2-amine