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Literature summary extracted from

  • Evans, G.B.; Furneaux, R.H.; Greatrex, B.; Murkin, A.S.; Schramm, V.L.; Tyler, P.C.
    Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases (2008), J. Med. Chem., 51, 948-956.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.2.2.1 (+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
3.2.2.1 (+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
3.2.2.1 (+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol transition state analogue inhibitor, comparison with inhibition of human and bovine enzyme Plasmodium falciparum
3.2.2.1 1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
3.2.2.1 1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
3.2.2.1 1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol transition state analogue inhibitor, comparison with inhibition of human and bovine enzyme. Ki value above 10 microM Plasmodium falciparum
3.2.2.1 1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
3.2.2.1 1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
3.2.2.1 1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol transition state analogue inhibitor, comparison with inhibition of human and bovine enzyme, Ki value above 10 microM Plasmodium falciparum
3.2.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin H i.e. DADMe-ImmH, transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
3.2.2.1 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin H i.e. DADMe-ImmH, transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
3.2.2.1 meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
3.2.2.1 meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
3.2.2.1 meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride transition state analogue inhibitor, comparison with inhibition of human and bovine enzyme Plasmodium falciparum
3.2.2.16 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine transition state analogue inhibitor, comparison with inhibition of Streptococcus pneumoniae enzyme and several methylthioadenosine phosphorylases Escherichia coli
3.2.2.16 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine transition state analogue inhibitor, comparison with inhibition of Escherichia coli enzyme and several methylthioadenosine phosphorylases Streptococcus pneumoniae
3.2.2.16 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine-3-methanol transition state analogue inhibitor, comparison with inhibition of Streptococcus pneumoniae enzyme and several methylthioadenosine phosphorylases Escherichia coli
3.2.2.16 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine-3-methanol transition state analogue inhibitor, comparison with inhibition of Escherichia coli enzyme and several methylthioadenosine phosphorylases Streptococcus pneumoniae
3.2.2.16 methylthio-4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A i.e. MT-DADMe-ImmA, transition state analogue inhibitor, comparison with inhibition of Streptococcus pneumoniae enzyme and several methylthioadenosine phosphorylases Escherichia coli
3.2.2.16 methylthio-4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A i.e. MT-DADMe-ImmA, transition state analogue inhibitor, comparison with inhibition of Escherichia coli enzyme and several methylthioadenosine phosphorylases Streptococcus pneumoniae

Organism

EC Number Organism UniProt Comment Textmining
3.2.2.1 Bos taurus
-
-
-
3.2.2.1 Homo sapiens
-
-
-
3.2.2.1 Plasmodium falciparum
-
-
-
3.2.2.16 Escherichia coli
-
-
-
3.2.2.16 Streptococcus pneumoniae
-
-
-

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.2.2.1 0.000000229
-
 1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol pH 7.0 Homo sapiens
3.2.2.1 0.00000048
-
 1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol pH 7.0 Bos taurus
3.2.2.1 0.000000665
-
 1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol pH 7.0 Bos taurus
3.2.2.1 0.000001
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin H pH 7.0 Bos taurus
3.2.2.1 0.0000011
-
 4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin H pH 7.0 Homo sapiens
3.2.2.1 0.0000018
-
 (+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol pH 7.0 Homo sapiens
3.2.2.1 0.0000018
-
 (+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol pH 7.0 Bos taurus
3.2.2.1 0.0000063
-
 1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol pH 7.0 Homo sapiens
3.2.2.1 0.0000129
-
 meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride pH 7.0 Homo sapiens
3.2.2.1 0.000016
-
 meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride pH 7.0 Bos taurus
3.2.2.16 0.000000048
-
 methylthio-4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin-A
-
 Escherichia coli
3.2.2.16 0.00000045
-
 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine
-
 Escherichia coli
3.2.2.16 0.00000084
-
 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine-3-methanol
-
 Escherichia coli
3.2.2.16 0.000084
-
 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine
-
 Streptococcus pneumoniae
3.2.2.16 0.00015
-
 1-[(9-deazaadenin-9-yl)methyl]-3-methylthiomethylazetidine-3-methanol
-
 Streptococcus pneumoniae