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Literature summary extracted from

  • Familiar, O.; Munier-Lehmann, H.; Ainsa, J.A.; Camarasa, M.J.; Perez-Perez, M.J.
    Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone (2010), Eur. J. Med. Chem., 45, 5910-5918.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.4.9 (+/-)(Z)-5-acetamido-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one
-
Mycobacterium tuberculosis
2.7.4.9 (+/-)(Z)-5-amino-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one
-
Mycobacterium tuberculosis
2.7.4.9 (Z)-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one
-
Mycobacterium tuberculosis
2.7.4.9 (Z)-8-acetamido-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one
-
Mycobacterium tuberculosis
2.7.4.9 (Z)-8-amino-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one
-
Mycobacterium tuberculosis
2.7.4.9 1-[(2Z)-(4-(5-bromouracil-1-yl)but-2-enyl)]-5,6-dihydro-1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolin-2,2-dioxide
-
Mycobacterium tuberculosis
2.7.4.9 1-[(2Z)-4-(1,1-dioxido-2H-naphtho[1,8-cd][1,2]thiazol-2-yl)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
Mycobacterium tuberculosis
2.7.4.9 1-[(Z)-(4-(thymin-1-yl)but-2-enyl)]-5,6-dihydro-1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolin-2,2-dioxide
-
Mycobacterium tuberculosis
2.7.4.9 5-methyl-1-[(2Z)-4-(2-oxobenzo[cd]indol-1(2H)-yl)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
Mycobacterium tuberculosis

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.4.9 0.0045
-
dTMP in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.4.9 ATP + dTMP Mycobacterium tuberculosis
-
ADP + dTDP
-
?

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 + dTMP
-
Mycobacterium tuberculosis ADP + dTDP
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.4.9 thymidine monophosphate 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 0.00027
-
1-[(2Z)-4-(1,1-dioxido-2H-naphtho[1,8-cd][1,2]thiazol-2-yl)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.0003
-
1-[(2Z)-(4-(5-bromouracil-1-yl)but-2-enyl)]-5,6-dihydro-1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolin-2,2-dioxide in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00042
-
5-methyl-1-[(2Z)-4-(2-oxobenzo[cd]indol-1(2H)-yl)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00057
-
1-[(Z)-(4-(thymin-1-yl)but-2-enyl)]-5,6-dihydro-1H,4H-1,2,5-thiadiazolo[4,3,2-ij]quinolin-2,2-dioxide in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00093
-
(Z)-8-acetamido-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00116
-
(Z)-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00246
-
(Z)-8-amino-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.0058
-
(+/-)(Z)-5-acetamido-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis
2.7.4.9 0.00707
-
(+/-)(Z)-5-amino-1-(4-(thymin-1-yl)but-2-enyl)-5,6-dihydro-1H-imidazo[4,5,1-ij]quinolin-2(4H)-one in 50 mM Tris-HCl pH 7.4, 50 mM KCl, 2 mM MgCl2, temperature not specified in the publication Mycobacterium tuberculosis