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Literature summary extracted from

  • Toti, K.S.; Verbeke, F.; Risseeuw, M.D.; Frecer, V.; Munier-Lehmann, H.; Van Calenbergh, S.
    Synthesis and evaluation of 5-modified thymidines and 5-hydroxymethyl-2-deoxyuridines as Mycobacterium tuberculosis thymidylate kinase inhibitors (2013), Bioorg. Med. Chem., 21, 257-268.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.4.9 1-((2R,4S,5R)-4-hydroxy-5-(2-(methylsulfonyl)ethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Mycobacterium tuberculosis
2.7.4.9 1-((2R,4S,5R)-5-(2-(1H-tetrazol-5-yl)ethyl)-4-hydroxytetrahydrofuran-2-yl)-5-(hydroxymethyl)pyrimidine-2,4(1H,3H)-dione
-
 Mycobacterium tuberculosis
2.7.4.9 1-((2R,4S,5R)-5-(2-(1H-tetrazol-5-yl)ethyl)-4-hydroxytetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Mycobacterium tuberculosis
2.7.4.9 1-[(4aR,5S,7R,7aR)-5-(hydroxymethyl)-2-thioxohexahydro-2H-furo[3,4-e][1,3]oxazin-7-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
 Mycobacterium tuberculosis
2.7.4.9 1-[5-([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)-2,5-dideoxy-a-D-erythro-pentofuranosyl]-5-methyl-4-thioxo-3,4-dihydropyrimidin-2(1H)-one
-
 Mycobacterium tuberculosis
2.7.4.9 2-((2R,3S,5R)-3-((tert-butyldimethylsilyl)oxy)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)-N-methylethanesulfonamide
-
 Mycobacterium tuberculosis
2.7.4.9 2-[(4aS,5R,7R,7aR)-5-[5-(hydroxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]-2,2-dioxidooctahydrocyclopenta[c][1,2,6]thiadiazin-7-yl]-N-methylethanesulfonamide
-
 Mycobacterium tuberculosis
2.7.4.9 3-((2R,3S,5R)-3-hydroxy-5-(5-(hydroxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)propanenitrile
-
 Mycobacterium tuberculosis
2.7.4.9 3-((2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)propanenitrile
-
 Mycobacterium tuberculosis
2.7.4.9 5-hydroxymethyl-dUMP
-
 Mycobacterium tuberculosis
2.7.4.9 additional information not inhibited by 3-((2R,3S,5R)-3-hydroxy-5-(5-(hydroxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)propanenitrile and 1-((2R,4S,5R)-5-(2-(1H-tetrazol-5-yl)ethyl)-4-hydroxytetrahydrofuran-2-yl)-5-(hydroxymethyl)pyrimidine-2,4(1H,3H)-dione Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
2.7.4.9 Mycobacterium tuberculosis
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.4.9 ATP + TMP
-
 Mycobacterium tuberculosis ADP + TDP
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.4.9 thymidylate kinase
-
 Mycobacterium tuberculosis
2.7.4.9 TMPK
-
 Mycobacterium tuberculosis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.4.9 0.00017
-
 1-[5-([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)-2,5-dideoxy-a-D-erythro-pentofuranosyl]-5-methyl-4-thioxo-3,4-dihydropyrimidin-2(1H)-one pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00029
-
 2-[(4aS,5R,7R,7aR)-5-[5-(hydroxymethyl)-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]-2,2-dioxidooctahydrocyclopenta[c][1,2,6]thiadiazin-7-yl]-N-methylethanesulfonamide pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.0035
-
 1-[(4aR,5S,7R,7aR)-5-(hydroxymethyl)-2-thioxohexahydro-2H-furo[3,4-e][1,3]oxazin-7-yl]-5-methylpyrimidine-2,4(1H,3H)-dione pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.048
-
 3-((2R,3S,5R)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)propanenitrile pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.07
-
 1-((2R,4S,5R)-5-(2-(1H-tetrazol-5-yl)ethyl)-4-hydroxytetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.11
-
 5-hydroxymethyl-dUMP pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.24
-
 2-((2R,3S,5R)-3-((tert-butyldimethylsilyl)oxy)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)-N-methylethanesulfonamide pH and temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.34
-
 1-((2R,4S,5R)-4-hydroxy-5-(2-(methylsulfonyl)ethyl)tetrahydrofuran-2-yl)-5-methylpyrimidine-2,4(1H,3H)-dione pH and temperature not specified in the publication Mycobacterium tuberculosis