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

BRENDA support

Literature summary for 3.4.23.46 extracted from

  • Wu, Y.J.; Guernon, J.; Shi, J.; Marcin, L.; Higgins, M.; Rajamani, R.; Muckelbauer, J.; Lewis, H.; Chang, C.; Camac, D.; Toyn, J.H.; Ahlijanian, M.K.; Albright, C.F.; Macor, J.E.; Thompson, L.A.
    Discovery of S3-truncated, C-6 heteroaryl substituted aminothiazine beta-site APP cleaving enzyme-1 (BACE1) inhibitors (2016), J. Med. Chem., 59, 8593-8600 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4S)-4-(2,4-difluorophenyl)-6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
-
Mus musculus
(4S)-4-[2,4-difluoro-5-(pyrimidin-5-yl)phenyl]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
-
Mus musculus
(4S,6R)-4-(2,4-difluorophenyl)-4-methyl-6-(pyrimidin-5-yl)-5,6-dihydro-4H-1,3-thiazin-2-amine
-
Mus musculus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Mus musculus P56818
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Mus musculus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
BACE1
-
Mus musculus
beta-site APP cleaving enzyme-1
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000008
-
pH and temperature not specified in the publication Mus musculus (4S)-4-[2,4-difluoro-5-(pyrimidin-5-yl)phenyl]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
0.00015
-
pH and temperature not specified in the publication Mus musculus (4S)-4-(2,4-difluorophenyl)-6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
0.00031
-
pH and temperature not specified in the publication Mus musculus (4S,6R)-4-(2,4-difluorophenyl)-4-methyl-6-(pyrimidin-5-yl)-5,6-dihydro-4H-1,3-thiazin-2-amine