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Literature summary for 3.2.2.1 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

Inhibitors Comment Organism Structure
(+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
(+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
(+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol transition state analogue inhibitor, comparison with inhibition of human and bovine enzyme Plasmodium falciparum
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
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
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
1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol transition state analogue inhibitor, comparison with inhibition of human and Plasmodium falciparum enzyme Bos taurus
1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol transition state analogue inhibitor, comparison with inhibition of bovine and Plasmodium falciparum enzyme Homo sapiens
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
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
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
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
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
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

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Homo sapiens
-
-
-
Plasmodium falciparum
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000229
-
1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol pH 7.0 Homo sapiens
0.00000048
-
1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol pH 7.0 Bos taurus
0.000000665
-
1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-3,3dimethanol pH 7.0 Bos taurus
0.000001
-
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin H pH 7.0 Bos taurus
0.0000011
-
4'-deaza-1'-aza-2'-deoxy-1'-(9-methylene)-immucillin H pH 7.0 Homo sapiens
0.0000018
-
(+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol pH 7.0 Homo sapiens
0.0000018
-
(+-)-1-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2-methanol pH 7.0 Bos taurus
0.0000063
-
1-[(7-benzyloxymethyl-6-tert-butoxy-9-deazapurin-9-yl)methyl] azetidine-3-methanol pH 7.0 Homo sapiens
0.0000129
-
meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride pH 7.0 Homo sapiens
0.000016
-
meso-[(9-deazahypoxanthin-9-yl)methyl]azetidine-2,4-dimethanol hydrochloride pH 7.0 Bos taurus