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Literature summary for 3.4.23.46 extracted from

  • Yan, G.; Hao, L.; Niu, Y.; Huang, W.; Wang, W.; Xu, F.; Liang, L.; Wang, C.; Jin, H.; Xu, P.
    2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors Synthesis, biological evaluation and docking studies (2017), Eur. J. Med. Chem., 137, 462-475 .
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
2-((4-amino-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 17.8% inhibition at 0.05 mM Homo sapiens
2-((5-amino-1,3,4-thiadiazol-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 21.8% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide 62.4% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide 77.5% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 25.9% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide 9.4% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide 85.6% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(p-tolyl)thiazol-2-yl)acetamide 11.5% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide 84.5% inhibition at 0.01 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(2-nitrophenyl)thiazol-2-yl)acetamide 6.5% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-(2-fluoropyridin-3-yl)phenyl)thiazol-2-yl)acetamide 88.7% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide 78.5% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide 16.5% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide 83.9% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(p-tolyl)thiazol-2-yl)acetamide 8.1% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide 78.6% inhibition at 0.01 mM Homo sapiens
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 50.7% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide 12.3% inhibition at 0.01 mM Homo sapiens
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide 5.9% inhibition at 0.01 mM Homo sapiens
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 10.7% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 85.8% inhibition at 0.05 mM Homo sapiens
2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 82.5% inhibition at 0.05 mM Homo sapiens
2-((6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide 22.5% inhibition at 0.05 mM Homo sapiens
N-(4-(3-bromophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide 90.4% inhibition at 0.05 mM Homo sapiens
N-(4-(4-acetamido-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide 4.7% inhibition at 0.05 mM Homo sapiens
N-(4-(4-acetamido-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide 1.4% inhibition at 0.05 mM Homo sapiens
N-(4-(4-amino-3,5-dichlorophenyl)-1H-imidazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide 87.7% inhibition at 0.01 mM Homo sapiens
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide 79.9% inhibition at 0.05 mM Homo sapiens
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide 91.8% inhibition at 0.05 mM Homo sapiens
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide 39.6% inhibition at 0.05 mM Homo sapiens
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide 86.1% inhibition at 0.05 mM Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid-beta precursor protein + H2O
-
 Homo sapiens ?
-
 ?
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
BACE1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0032
-
 at pH 4.5 and 25°C Homo sapiens N-(4-(4-amino-3,5-dichlorophenyl)-1H-imidazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
0.0042
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
0.0046
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
0.0077
-
 at pH 4.5 and 25°C Homo sapiens N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
0.0134
-
 at pH 4.5 and 25°C Homo sapiens N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide
0.0135
-
 at pH 4.5 and 25°C Homo sapiens N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
0.015
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
0.015
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-(2-fluoropyridin-3-yl)phenyl)thiazol-2-yl)acetamide
0.0175
-
 at pH 4.5 and 25°C Homo sapiens N-(4-(3-bromophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
0.0191
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
0.0243
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
0.0261
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
0.0276
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
0.0296
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
0.0374
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
0.0386
-
 at pH 4.5 and 25°C Homo sapiens 2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide