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Literature summary for 3.4.23.46 extracted from

  • Malamas, M.S.; Barnes, K.; Hui, Y.; Johnson, M.; Lovering, F.; Condon, J.; Fobare, W.; Solvibile, W.; Turner, J.; Hu, Y.; Manas, E.S.; Fan, K.; Olland, A.; Chopra, R.; Bard, J.; Pangalos, M.N.; Reinhart, P.; Robichaud, A.J.
    Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 2068-2073.
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
 Homo sapiens
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol 1.7% inhibition at 0.0125 mM Homo sapiens
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol 8.46% inhibition at 0.0125 mM Homo sapiens
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol 5.43% inhibition at 0.0125 mM Homo sapiens
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]propan-1-ol
-
 Homo sapiens
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]propan-1-ol 47% inhibition at 0.0125 mM Homo sapiens
4-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenoxy)butanenitrile
-
 Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-(prop-2-en-1-yl)benzamide 6.2% inhibition at 0.0125 mM Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-(propan-2-yl)benzamide 6.58% inhibition at 0.0125 mM Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-butylbenzamide 45% inhibition at 0.0125 mM Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-cyclobutylbenzamide 38.4% inhibition at 0.0125 mM Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-cyclopropylbenzamide 10.6% inhibition at 0.0125 mM Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-ethylbenzamide 36% inhibition at 0.0125 mM Homo sapiens
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-propylbenzamide 28% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(1,3-thiazol-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 3.4% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(hexyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 13% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 31% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pyrazin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 46.6% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pyridazin-3-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 10.4% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pyridin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 6.61% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pyridin-3-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 7.1% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pyridin-4-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 7.22% inhibition at 0.0125 mM Homo sapiens
6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine 9.7% inhibition at 0.0125 mM Homo sapiens
6-[(2,5-diphenyl-1H-pyrrol-1-yl)methyl]pyridin-2-amine 15% inhibition at 0.0125 mM Homo sapiens
6-[[2-(2-chlorophenyl)-5-(4-methoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine 30% inhibition at 0.0125 mM Homo sapiens
6-[[2-(2-chlorophenyl)-5-(4-phenoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine 16% inhibition at 0.0125 mM Homo sapiens
6-[[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine 48% inhibition at 0.0125 mM Homo sapiens
6-[[2-(4-butoxyphenyl)-5-(2-chlorophenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine 31% inhibition at 0.0125 mM Homo sapiens
N-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenyl)pyrimidin-5-amine 9.8% inhibition at 0.0125 mM Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
BACE2
-
 Homo sapiens
beta-secretase
-
 Homo sapiens
beta-site APP cleaving enzyme
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00047
-
 pH and temperature not specified in the publication Homo sapiens 3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]propan-1-ol
0.001
-
 pH and temperature not specified in the publication Homo sapiens 2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
0.0071
-
 pH and temperature not specified in the publication Homo sapiens 4-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenoxy)butanenitrile