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Literature summary for 3.4.23.46 extracted from

  • Malamas, M.S.; Barnes, K.; Johnson, M.; Hui, Y.; Zhou, P.; Turner, J.; Hu, Y.; Wagner, E.; Fan, K.; Chopra, R.; Olland, A.; Bard, J.; Pangalos, M.; Reinhart, P.; Robichaud, A.J.
    Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors (2010), Bioorg. Med. Chem., 18, 630-639.
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
2-amino-3-methyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-3-methyl-5-(pyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one exhibits modest selectivity (about 8fold) against BACE2 Homo sapiens
2-amino-3-methyl-5-phenyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-3-methyl-5-[2-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-3-methyl-5-[2-methyl-6-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one 24% inhibition at 0.0125 mM Homo sapiens
2-amino-5-(2,6-diethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-5-(2,6-dimethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-5-(2-ethyl-6-methylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one 28% inhibition at 0.0125 mM Homo sapiens
2-amino-5-(2-ethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-5-(biphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
 Homo sapiens
8,8-diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Abz-SEVNLDAEFR-Dpa + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
BACE2
-
 Homo sapiens
beta-secretase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00014
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-5-(biphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
0.00048
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-3-methyl-5-(pyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.00077
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-3-methyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
0.00078
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
0.00079
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.00102
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-5-(2-ethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.00117
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.00201
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-3-methyl-5-phenyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
0.0022
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.00613
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-3-methyl-5-[2-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.0236
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-5-(2,6-diethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.0241
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 2-amino-5-(2,6-dimethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
0.0383
-
 temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4 Homo sapiens 8,8-diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine