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Literature summary for 3.4.23.46 extracted from

  • Kimura, T.; Hamada, Y.; Stochaj, M.; Ikari, H.; Nagamine, A.; Abdel-Rahman, H.; Igawa, N.; Hidaka, K.; Nguyen, J.T.; Saito, K.; Hayashi, Y.; Kiso, Y.
    Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1 carboxylic acid bioisosteres (2006), Bioorg. Med. Chem. Lett., 16, 2380-2386.
    View publication on PubMed
Search for more literature for 3.4.23.46

Application

Application Comment Organism
medicine development of beta-secretase inhibitors as anti-Alzheimer's disease drugs Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.0002 mM, complete inhibition, IC50: 1.2 nM Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.0002 mM, 98.1% inhibition, IC50: 3.9 nM Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.0002 mM, 78.1% inhibition Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.002 mM, 87.1% inhibition, IC50: 8.2 nM Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide 0.0002 mM, 98.1% inhibition, IC50: 4.8 nM Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide 0.0002 mM, 94.2% inhibition, IC50: 6.6 nM Homo sapiens
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide 0.0002 mM, 97.2% inhibition, IC50: 6.4 nM Homo sapiens
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.002 mM, 99.7% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.002 mM, 98.3% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.002 mM, 29.2% inhibition; 0.002 mM, 62.1% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide 0.002 mM, 83.7% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-([3-(4-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]amino)-3-oxopropyl]-L-leucinamide 0.002 mM, 74.2% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide 0.002 mM, 92.2% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide 0.002 mM, 94.4% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-thiadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide 0.002 mM, 91.9% inhibition Homo sapiens
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
BACE1
-
 Homo sapiens
beta-secretase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000012
-
 0.0002 mM, complete inhibition, IC50: 1.2 nM Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
0.0000039
-
 0.0002 mM, 98.1% inhibition, IC50: 3.9 nM Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
0.0000048
-
 0.0002 mM, 98.1% inhibition, IC50: 4.8 nM Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
0.0000064
-
 0.0002 mM, 97.2% inhibition, IC50: 6.4 nM Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
0.0000066
-
 0.0002 mM, 94.2% inhibition, IC50: 6.6 nM Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
0.0000082
-
 0.002 mM, 87.1% inhibition, IC50: 8.2 nM Homo sapiens 3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide