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Literature summary for 3.4.23.46 extracted from

  • Al-Nadaf, A.; Abu Sheikha, G.; Taha, M.O.
    Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads (2010), Bioorg. Med. Chem., 18, 3088-3115.
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
1-[ (3-benzoylamino-phenylcarbamoyl)-methyl]-pyridinium chloride 51% inhibition at 0.05 mM Homo sapiens
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-carbamoyl-pyridiniumchloride 54% inhibition at 0.05 mM Homo sapiens
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-phenethylcarbamoyl-pyridinium chloride 55% inhibition at 0.05 mM Homo sapiens
1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride 61% inhibition at 0.05 mM Homo sapiens
1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride 42% inhibition at 0.05 mM Homo sapiens
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride 78% inhibition at 0.05 mM Homo sapiens
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride complete inhibition at 0.05 mM Homo sapiens
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride 44% inhibition at 0.05 mM Homo sapiens
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride complete inhibition at 0.05 mM Homo sapiens
1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride 50% inhibition at 0.05 mM Homo sapiens
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride complete inhibition at 0.05 mM Homo sapiens
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
 Homo sapiens
1[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride 68% inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride 44% inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride 69% inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride 64% inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride complete inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride 34% inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride 24% inhibition at 0.05 mM Homo sapiens
3-carbamoyl-1-[[3-(toluene-4-sulfonylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride 4% inhibition at 0.05 mM Homo sapiens
3-phenethylcarbamoyl-1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride 58% inhibition at 0.05 mM Homo sapiens
3-phenethylcarbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride 72% inhibition at 0.05 mM Homo sapiens
3-phenethylcarbamoyl-1-[[3-(toluene-4-sulfonylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride 36% inhibition at 0.05 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
BACE-1
-
 Homo sapiens
beta-secretase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.001
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
0.0019
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 3-carbamoyl-1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
0.0022
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
0.0037
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
0.004
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 3-phenethylcarbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
0.012
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
0.013
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
0.0302
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 3-carbamoyl-1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
0.0447
-
 in 50 mM sodium acetate, pH 4.5, at 37°C Homo sapiens 1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-carbamoyl-pyridiniumchloride