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2.7.1.21: thymidine kinase

This is an abbreviated version!
For detailed information about thymidine kinase, go to the full flat file.

Word Map on EC 2.7.1.21

Reaction

ATP
+
thymidine
=
ADP
 +
dTMP

Synonyms

2'-deoxythymidine kinase, ATP-thymidine 5'-phosphotransferase, beta-thymidine kinase-1, beta-thymidine kinase-2, calmodulin-binding protein, CaM-binding protein, CaMBP, CHV-TK, dThd kinase-1, dThd kinase-2, EC 2.7.1.75, EHV4-TK, FHV-TK, HSV-1 TK, HSV1-TK, kinase, deoxythymidine (phosphorylating), kinase, thymidine (phosphorylating), LMJF_21_1210, mitochondrial thymidine kinase, More, Mt-TK, TdR kinase, ThyB, thymidine kinase, thymidine kinase 1, thymidine kinase 2, thymidine kinase 2, mitochondrial, thymidine kinase I, thymidine kinase-1, thymidine kinase-2, thymidylate kinase, TK, TK-1, TK-2, TK1, TK1a, TK1b, TK2, type 1 thymidine kinase, type II thymidine kinase 1, UL23, VVTK

ECTree

     2 Transferases
         2.7 Transferring phosphorus-containing groups
             2.7.1 Phosphotransferases with an alcohol group as acceptor
                2.7.1.21 thymidine kinase

Inhibitors

Inhibitors on EC 2.7.1.21 - thymidine kinase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl 3,3-dimethylbutanoate
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl benzoate
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl diphenylacetate
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl dodecanoate
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl heptanoate
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl pivalate
(4E)-N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
(4E)-N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
(E)-5-(2-bromovinyl)-1-beta-D-(arabinofuranosyl)uracil
-
-
1-(3'-deoxy-5'-O-triphenylmethyl-beta-D-thymidin-3'-yl)-3-(4-chloro-3-(trifluoromethyl)-phenyl)-thiourea
-
-
1-(3,4-dichlorobenzyl)-3-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]thiourea
1-(3,4-dichlorophenyl)-3-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]thiourea
1-benzyl-3-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]thiourea
1-beta-D-(arabinofuranosyl)thymine
-
-
1-[(2Z)-4-(4-benzylpiperazin-1-yl)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[(2Z)-4-(benzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[(2Z)-4-(benzyloxy)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[(2Z)-4-(dibenzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-5,6-dihydrothymine
1-[(2Z)-4-hydroxybut-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine
-
-
1-[2,3-dihydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[3-hydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(2S,5R)-2-(hydroxymethyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-3-yl]thiourea
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(2S,5R)-2-(hydroxymethyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-3-yl]urea
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]thiourea
1-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]-3-phenylthiourea
2'-deoxy-3'-aminothymidine
-
5 mM
2'-exo-methanocarba-thymidine
Herpes simplex virus
-
-
2-(4-chlorophenyl)-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
2-biphenyl-4-yl-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
2-mercaptoethanol
-
5 mM
3'-(1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
-
3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-3'-deoxythymidine
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-3'-deoxythymidine
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
-
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
3'-(4-butyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
-
3'-(4-chlorobenzylamino)-3'-deoxy-beta-D-thymidine
-
-
3'-(4-chlorophenyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridine
-
-
3'-(4-chlorophenyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
-
3'-(4-cyclopentylmethyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
-
3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
3'-(5-(4-chlorophenyl)-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
-
3'-([[(4-chlorophenyl)carbamothioyl]amino]methyl)-3'-deoxythymidine
3'-([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)-2',3'-dideoxy-3,4-dihydrothymidine
-
-
3'-azido-2',3'-dideoxy-3,4-dihydrothymidine
3'-azido-3'-deoxythymidine
3'-benzylamino-3'-deoxy-beta-D-thymidine
-
-
3'-deoxy-3'-(4-(3,4-dichlorophenyl)-1,2,3-triazol-1-yl)-beta-D-thymidine
-
-
3'-deoxy-3'-(4-phenyl-1,2,3-triazol-1-yl)-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridine
-
-
3'-deoxy-3'-(4-phenyl-1,2,3-triazol-1-yl)-beta-D-thymidine
-
-
3'-deoxy-3'-(4-pyridin-2-yl-1,2,3-triazol-1-yl)-beta-D-thymidine
-
-
3'-deoxy-3'-(5-phenyl-1,2,3-triazol-1-yl)-beta-D-thymidine
-
-
3'-deoxy-3'-([[(3,4-dichlorophenyl)carbamothioyl]amino]methyl)thymidine
3'-deoxy-3'-([[(4-methoxyphenyl)carbamothioyl]amino]methyl)thymidine
3'-deoxy-3'-([[(4-methylphenyl)carbamothioyl]amino]methyl)thymidine
3'-deoxy-3'-fluorothymidine
-
inhibits thymidine phosphorylation catalyzed by thymidine kinase 2
3'-ethyl-5-methyl-2'-deoxyuridine
-
3'-fluorothymidine
-
inhibits thymidine phosphorylation catalyzed by thymidine kinase 2
3'-hexanoylamino-3'-deoxythymidine
-
very potent inhibitor of thymidine kinase 2
3'-O-ethyl-2'-deoxyuridine
-
3'-O-methyl-2'-deoxyuridine
-
3'-spiro-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)-5-methyluridine
inhibits phosphorylation of 2'-deoxythymidine, IC50: 0.0046 mM
3'-[(3-trifluoromethyl-4-chloro)-benzylamino]-3'-deoxy-beta-D-thymidine
-
-
3'-[([[4-(benzyloxy)phenyl]carbamothioyl]amino)methyl]-3'-deoxythymidine
3'-[([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)methyl]-3'-deoxythymidine
3-N-methyl-5-iodo-2'-deoxyuridine
-
-
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylbutanamide
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-oxo-2-(tritylamino)ethyl]butanamide
5'-aminothymidine
-
-
5'-deoxy-5'-[(tricyclo[3.3.1.13,7]dec-1-ylcarbamothioyl)amino]thymidine
5'-deoxy-5'-[[(diphenylmethyl)carbamothioyl]amino]thymidine
5'-O-(4,4'-dimethoxytrityl)thymidine
IC50: 0.468 mM
5'-O-[4-(fluorosulfonyl)benzene-1-sulfonyl]thymidine
-
-
5-(3'-amino-3'-deoxy-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridin-3'Nyl)-1-(4-chloro-3-trifluoromethylphenyl)-tetrazole
-
-
5-(3'-amino-3'-deoxy-beta-D-thymidin-3'N-yl)-1-(4-chloro-3-trifluoromethylphenyl)-tetrazole
-
-
5-(3'-amino-3'-deoxy-beta-D-thymidin-3'N-yl)-1-benzyl-tetrazole
-
-
5-(E)-(2-bromovinyl)-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
5-(E)-(2-bromovinyl)uridine
5-azido-2'-deoxyuridine
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type enzyme at 0.003 mM, 50% photoincorporation inhibition of C336Y mutant at 0.05 mM
5-azido-2'-deoxyuridine-5'-monophosphate
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type enzyme at 0.05 mM, 50% photoincorporation inhibition of C336Y mutant at 0.135 mM
5-benzylamino-(3'-deoxy-beta-D-thymidin-3'N-yl)-tetrazole
-
-
5-bromodeoxyuridine
5-bromovinyldeoxyuridine
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type enzyme at 0.0015 mM, 50% photoincorporation inhibition of C336Y mutant above 0.025 mM
5-Chlorodeoxyuridine
-
competitive to thymidine
5-ethyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
5-fluoro-2'-deoxyuridine
concentration dependent reduction of activity
5-fluorodeoxyuridine
5-iodo-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
5-iodo-2'-deoxyuridine
potent inhibitor
5-iododeoxyuridine
5-methyl-1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
5-methyl-1-[(2Z)-4-(4-methylpiperazin-1-yl)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
5-methyl-1-[(2Z)-4-(tritylamino)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-cytosine
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
5-methyl-1-[4-(trityloxy)but-2-yn-1-yl]pyrimidine-2,4(1H,3H)-dione
5-methyl-1-[4-(trityloxy)butyl]pyrimidine-2,4(1H,3H)-dione
5-propyl-2'-deoxyuridine
-
5-trifluoromethyl-2-deoxyuridine
potent inhibitor
5-Trifluoromethyldeoxyuridine
-
competitive to thymidine
5-[(4-chloro-3-trifluoromethylphenyl)amino]-1-(3'-deoxy-beta-D-thymidin-3'N-yl)-tetrazole
-
-
5-[(E)-2-bromoethenyl]-2'-O-decanoyluridine
competitive with respect to 2'-deoxythymidine, IC50: 0.0012 mm
5-[(E)-2-bromoethenyl]-2'-O-octanoyluridine
5-[amino-(4-chloro-3-trifluoromethylphenyl)]-1-(3'-deoxy-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridin-3'N-yl)-tetrazole
-
-
6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylhexanamide
6-methyluridine
-
9-[(2Z)-4-(trityloxy)but-2-en-1-yl]-guanine
aciclovir
Herpes simplex virus
-
competitive inhibitor
acyclovir
acyclovir H-phosphonate
-
-
adenine
-
-
alpha-D-5-ethyl-2'-deoxyuridine
-
alpha-L-thymidine
-
ammoniumsulfate
Herpes simplex virus
-
50% inhibition at 200 mM
beta-D-5-ethyl-2'-deoxyuridine
potent inhibitor
beta-L-thymidine
potent inhibitor
bromo-dUTP
-
-
Caffeine
CH3CO2-
-
-
dATP
-
strong feedback inhibition, tight binding at the active site in stoichiometric amount
deoxcytidine
deoxyuridine
dGDP
-
competitive to ATP
EDTA
-
complete incactivation at 2.5 mM
iododeoxycytidine
Herpes simplex virus
-
-
m-Fluorothymine
-
-
Mg2+
Tequatrovirus T4
-
non-competitive
N-(2-cyanoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
N-(2-cyanoethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
N-(2-[[cyano(phenyl)methyl]amino]-2-oxoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
N-(3'-deoxy-beta-D-thymidin-3'-yl)-N'-(4-chloro-3-trifluoromethylphenyl)-benzylguanidine
-
-
N-(3'-deoxy-beta-D-thymidin-3'-yl)-N'-(4-chloro-3-trifluoromethylphenyl)-guanidine
-
-
N-(3'-deoxy-beta-D-thymidin-3'-yl)-N'-(4-chloro-3-trifluoromethylphenyl)-isopropylguanidine
-
-
N-(cyanomethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
N-(diphenylmethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
N-methyl-4-[[[8-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)octyl]oxy](diphenyl)methyl]benzamide
-
-
N-methyl-4-[{[8-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)octyl]oxy}(diphenyl)methyl]benzamide
-
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-2,2-diphenylacetamide
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-3-(trifluoromethyl)benzamide
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-9H-xanthene-9-carboxamide
N-[2-[(diphenylmethyl)amino]-2-oxoethyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
N-[cyano(phenyl)methyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
N3-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-thymine
P1-(5'-adenosyl)-P5-(5'-thymidyl)pentaphosphate
-
P1-(Adenosine-5')-P3-(thymidine-5')-triphosphate
-
-
P1-(adenosine-5')-P4-(thymidine-5')-tetraphosphate
-
-
P1-(Adenosine-5')-P5-(thymidine-5')-pentaphosphate
-
-
P1-(Adenosine-5')-P6-(thymidine-5')-hexaphosphate
-
-
penciclovir
potassium phosphate
-
80% inhibition at 50 mM
sulfate
-
competitive inhibitor of ATP binding
suramin
theophylline
-
-
thymidine
thymidylate
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type and C336Y mutant enzyme at 0.0125 mM
trifluridine
concentration dependent reduction of activity
W7
slight inhibitory in presence of calmodulin
additional information
-