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Literature summary for 2.3.1.97 extracted from

  • Goncalves, V.; Brannigan, J.A.; Whalley, D.; Ansell, K.H.; Saxty, B.; Holder, A.A.; Wilkinson, A.J.; Tate, E.W.; Leatherbarrow, R.J.
    Discovery of Plasmodium vivax N-myristoyltransferase inhibitors: screening, synthesis, and structural characterization of their binding mode (2012), J. Med. Chem., 55, 3578-3582.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1-[(diethylamino)methyl]naphthalen-2-ol
-
Plasmodium vivax
2-[(4-methoxybenzyl)amino]-5,5-dimethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carbonitrile
-
Plasmodium vivax
3-butyl-4-(but-3-yn-1-ylsulfanyl)-6-methoxy-2-methylquinoline
-
Plasmodium vivax
3-butyl-6-methoxy-2-methyl-4-[(2-phenylethyl)sulfanyl]quinoline
-
Plasmodium vivax
3-[(2-bromo-3-butyl-6-methoxyquinolin-4-yl)sulfanyl]propanenitrile
-
Plasmodium vivax
3-[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]propan-1-ol
-
Plasmodium vivax
3-[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]propanenitrile
-
Plasmodium vivax
3-[(3-butyl-6-methoxyquinolin-4-yl)sulfanyl]propanenitrile
-
Plasmodium vivax
3-[(3-ethyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]propanenitrile
-
Plasmodium vivax
3-[(6-methoxy-2-methylquinolin-4-yl)sulfanyl]propanenitrile
-
Plasmodium vivax
4-[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]butanenitrile
-
Plasmodium vivax
6-ethyl-3-(trifluoromethyl)-2,3-dihydro-1,4-benzoxathiine 4,4-dioxide
-
Plasmodium vivax
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-(1-hydroxyethyl)quinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-chloroquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-fluoroquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-methylquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-[(2-cyanoethyl)amino]quinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-[(2-cyanoethyl)sulfanyl]-2-ethylquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-[(2-cyanoethyl)sulfanyl]-2-methylquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-[(2-cyanoethyl)sulfanyl]-2-propylquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-[(2-cyanoethyl)sulfanyl]-6-methoxyquinoline-3-carboxylate
-
Plasmodium vivax
ethyl 4-[(2-cyanoethyl)sulfanyl]quinoline-3-carboxylate
-
Plasmodium vivax
ethyl 6-acetyl-4-(but-3-yn-1-ylsulfanyl)quinoline-3-carboxylate
-
Plasmodium vivax
additional information NMT inhibitors: screening, synthesis, and structural characterization of their binding mode, overview Plasmodium vivax
[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]acetonitrile
-
Plasmodium vivax

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00571
-
peptide pp60src(2-16) pH and temperature not specified in the publication Plasmodium vivax

Organism

Organism UniProt Comment Textmining
Plasmodium vivax
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
myristoyl-CoA + peptide pp60src(2-16) sequence GSNKSKPKDASQRRR-NH2 Plasmodium vivax CoA + N-myristoyl-peptideHs pp60src(2-16)
-
?

Synonyms

Synonyms Comment Organism
N-myristoyltransferase
-
Plasmodium vivax

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00246
-
3-[(3-butyl-6-methoxyquinolin-4-yl)sulfanyl]propanenitrile pH and temperature not specified in the publication Plasmodium vivax
0.0029
-
3-[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]propanenitrile pH and temperature not specified in the publication Plasmodium vivax
0.00323
-
3-[(3-ethyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]propanenitrile pH and temperature not specified in the publication Plasmodium vivax
0.00697
-
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-methylquinoline-3-carboxylate pH and temperature not specified in the publication Plasmodium vivax
0.00777
-
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-fluoroquinoline-3-carboxylate pH and temperature not specified in the publication Plasmodium vivax
0.0109
-
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-chloroquinoline-3-carboxylate pH and temperature not specified in the publication Plasmodium vivax
0.0114
-
6-ethyl-3-(trifluoromethyl)-2,3-dihydro-1,4-benzoxathiine 4,4-dioxide pH and temperature not specified in the publication Plasmodium vivax
0.0116
-
3-butyl-4-(but-3-yn-1-ylsulfanyl)-6-methoxy-2-methylquinoline pH and temperature not specified in the publication Plasmodium vivax
0.0174
-
3-[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]propan-1-ol pH and temperature not specified in the publication Plasmodium vivax
0.0216
-
3-[(2-bromo-3-butyl-6-methoxyquinolin-4-yl)sulfanyl]propanenitrile pH and temperature not specified in the publication Plasmodium vivax
0.02437
-
ethyl 4-[(2-cyanoethyl)sulfanyl]-2-methylquinoline-3-carboxylate above, pH and temperature not specified in the publication Plasmodium vivax
0.02442
-
ethyl 4-[(2-cyanoethyl)sulfanyl]quinoline-3-carboxylate pH and temperature not specified in the publication Plasmodium vivax
0.0263
-
1-[(diethylamino)methyl]naphthalen-2-ol pH and temperature not specified in the publication Plasmodium vivax
0.0264
-
2-[(4-methoxybenzyl)amino]-5,5-dimethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-3-carbonitrile pH and temperature not specified in the publication Plasmodium vivax
0.0352
-
4-[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]butanenitrile pH and temperature not specified in the publication Plasmodium vivax
0.0424
-
ethyl 4-[(2-cyanoethyl)sulfanyl]-6-methoxyquinoline-3-carboxylate pH and temperature not specified in the publication Plasmodium vivax
0.0606
-
ethyl 4-[(2-cyanoethyl)sulfanyl]-2-ethylquinoline-3-carboxylate pH and temperature not specified in the publication Plasmodium vivax
0.1
-
3-[(6-methoxy-2-methylquinolin-4-yl)sulfanyl]propanenitrile above, pH and temperature not specified in the publication Plasmodium vivax
0.1
-
ethyl 4-[(2-cyanoethyl)sulfanyl]-2-propylquinoline-3-carboxylate above, pH and temperature not specified in the publication Plasmodium vivax
0.1
-
[(3-butyl-6-methoxy-2-methylquinolin-4-yl)sulfanyl]acetonitrile above, pH and temperature not specified in the publication Plasmodium vivax
0.1
-
3-butyl-6-methoxy-2-methyl-4-[(2-phenylethyl)sulfanyl]quinoline above, pH and temperature not specified in the publication Plasmodium vivax
0.1
-
ethyl 4-[(2-cyanoethyl)amino]quinoline-3-carboxylate above, pH and temperature not specified in the publication Plasmodium vivax
0.1
-
ethyl 6-acetyl-4-(but-3-yn-1-ylsulfanyl)quinoline-3-carboxylate above, pH and temperature not specified in the publication Plasmodium vivax
0.1
-
ethyl 4-(but-3-yn-1-ylsulfanyl)-6-(1-hydroxyethyl)quinoline-3-carboxylate above, pH and temperature not specified in the publication Plasmodium vivax