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Literature summary for 3.4.11.18 extracted from

  • Kallander, L.S.; Lu, Q.; Chen, W.; Tomaszek, T.; Yang, G.; Tew, D.; Meek, T.D.; Hofmann, G.A.; Schulz-Pritchard, C.K.; Smith, W.W.; Janson, C.A.; Ryan, M.D.; Zhang, G.F.; Johanson, K.O.; Kirkpatrick, R.B.; Ho, T.F.; Fisher, P.W.; Mattern, M.R.; Johnson, R.K.; Hansbury, M.J.; Winkler, J.D.; Ward, K.W.; Veber, D.F.; Thompson, S.K.
    4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo (2005), J. Med. Chem., 48, 5644-5647.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
2-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value 41 nM Homo sapiens
2-methyl-6-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value 6 nM Homo sapiens
3,8-dihydroindeno(1,2-d)(1,2,3)triazole Co(II)-form, Ki,app-value 52 nM Homo sapiens
3-(1H-1,2,3-triazol-5-yl)aniline Co(II)-form, Ki,app-value 280 nM Homo sapiens
3-(1H-1,2,3-triazol-5-yl)phenol Co(II)-form, Ki,app-value 300 nM Homo sapiens
3-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value 260 nM Homo sapiens
3-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value 52 nM Homo sapiens
4-(1H-1,2,3-triazol-5-yl)aniline Co(II)-form, Ki,app-value 337 nM Homo sapiens
4-(1H-1,2,3-triazol-5-yl)phenol Co(II)-form, Ki,app-value above 1000 nM Homo sapiens
4-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value above 1000 nM Homo sapiens
4-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value 8 nM, Mn(II)-form, 0.014 mM, 50% reduction of viability of human umbilical vein endothelial cell above 0.03 mM Homo sapiens
5-(1-benzofuran-2-yl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 15 nM, Mn(II)-form, 26% inhibition at 0.02 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.006 mM Homo sapiens
5-(2-methoxyphenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 150 nM Homo sapiens
5-(2-methylphenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 112 nM Homo sapiens
5-(3,4-dibromophenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 1 nM, Mn(II)-form, 0.016 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.002 mM Homo sapiens
5-(3-bromophenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 4 nM Homo sapiens
5-(3-iodophenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 16 nM Homo sapiens
5-(3-methylphenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 18 nM Homo sapiens
5-(4-bromophenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 3 nM, Mn(II)-form, 0.011 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.006 mM Homo sapiens
5-(4-chlorophenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 6 nM, Mn(II)-form, 0.011 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.005 mM Homo sapiens
5-(4-ethylphenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 30 nM Homo sapiens
5-(4-iodophenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 1 nM, Mn(II)-form, not inhibitory at 0.02 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.02 mM Homo sapiens
5-(4-methylphenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value 15 nM, Mn(II)-form, 4400 nM, 50% reduction of viability of human umbilical vein endothelial cell at 0.03 mM Homo sapiens
5-(4-propylphenyl)-1H-1,2,3-triazole Co(II)-form, Ki,app-value above 1000 nM Homo sapiens
5-biphenyl-2-yl-1H-1,2,3-triazole Co(II)-form, Ki,app-value above 1000 nM Homo sapiens
5-methyl-2-(1H-1,2,3-triazol-5-yl)pyridine Co(II)-form, Ki,app-value 3 nM, Mn(II)-form, 0.015 mM, 50% reduction of viability of human umbilical vein endothelial cell at 0.002 mM Homo sapiens
5-phenyl-1H-1,2,3-triazole Co(II)-form, Ki,app-value 70 nM Homo sapiens
N-benzyl-3-(1H-1,2,3-triazol-5-yl)aniline Co(II)-form, Ki,app-value 29 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isoform µetAP2
-