Information on EC 2.7.1.21 - thymidine kinase

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The enzyme appears in viruses and cellular organisms

EC NUMBER
COMMENTARY
2.7.1.21
-
RECOMMENDED NAME
GeneOntology No.
thymidine kinase
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
ATP + thymidine = ADP + dTMP
show the reaction diagram
mechanism
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
the amino acid residues at positions 51, 83, and 185 are important for enzyme activity
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
molecular docking of substrates and inhibitors, active site structure modeling
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
active site structure, E98 is involved in catalysis
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
active site structure
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
active site structure
P75070
ATP + thymidine = ADP + dTMP
show the reaction diagram
active site structure
O57203
ATP + thymidine = ADP + dTMP
show the reaction diagram
active site structure, substrate binding structures
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
substrate binding and active site structure
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
substrate binding site structures, structural basis for substrate specificity and activity
Herpes simplex virus type 4
-
ATP + thymidine = ADP + dTMP
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
phospho group transfer
-
-
-
-
PATHWAY
KEGG Link
MetaCyc Link
pyrimidine deoxyribonucleosides salvage
-
Pyrimidine metabolism
-
Drug metabolism - other enzymes
-
Metabolic pathways
-
SYSTEMATIC NAME
IUBMB Comments
ATP:thymidine 5'-phosphotransferase
Deoxyuridine can also act as acceptor, and dGTP can act as a donor. The deoxypyrimidine kinase complex induced by Herpes simplex virus catalyses this reaction as well as those of EC 2.7.1.114 (AMP---thymidine kinase), EC 2.7.1.118 (ADP---thymidine kinase) and EC 2.7.4.9 (dTMP-kinase).
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
2'-deoxythymidine kinase
-
-
-
-
2'-deoxythymidine kinase
-
-
ATP-thymidine 5'-phosphotransferase
-
-
-
-
beta-thymidine kinase-1
-
-
beta-thymidine kinase-2
-
-
calmodulin-binding protein
Q27564
-
CaM-binding protein
Q27564
-
dThd kinase-1
-
-
dThd kinase-2
-
-
EC 2.7.1.75
-
-
-
-
EHV4-TK
Herpes simplex virus type 4
-
-
HSV-1 TK
Herpes simplex virus
-
-
HSV1-TK
Herpes simplex virus
-
-
kinase, deoxythymidine (phosphorylating)
-
-
-
-
kinase, thymidine (phosphorylating)
-
-
-
-
Mt-TK
O00142
-
TdR kinase
-
-
-
-
thymidine kinase
-
-
thymidine kinase 1
C3VAL3
-
thymidine kinase 1
Q8LDP6
-
thymidine kinase 1
Q9S750 and Q9FN47
-
thymidine kinase 1
Q0H0H6
-
thymidine kinase 1
-
-
thymidine kinase 1
G5EEZ5
-
thymidine kinase 1
Q803Y1
-
thymidine kinase 1
Q27564
-
thymidine kinase 1
P04047
-
thymidine kinase 1
Herpes simplex virus
-
-
thymidine kinase 1
-
-
thymidine kinase 1
P04183
-
thymidine kinase 1
-
-
thymidine kinase 1
P27158
-
thymidine kinase 1
Q71F77
-
thymidine kinase 1
Q9PPP5
-
thymidine kinase 1
-
-
thymidine kinase 1
Q5I0A2
-
thymidine kinase 2
-
-
thymidine kinase 2
-
-
thymidine kinase 2, mitochondrial
O00142
-
thymidine kinase I
-
-
thymidine kinase I
-
-
-
thymidine kinase I
-
-
thymidine kinase I
-
-
thymidine kinase I
-
-
thymidine kinase I
Pyrobaculum aerophilum IM2
-
-
-
thymidine kinase-1
-
-
thymidine kinase-2
-
-
thymidylate kinase
Herpes simplex virus type 4
-
-
TK-1
-
-
TK-2
O00142
-
TK1
Q9S750 and Q9FN47
-
TK1
Q0H0H6
-
TK1
Q803Y1
-
TK1
P04047
-
TK1
Pyrobaculum aerophilum IM2
-
-
-
TK1
P27158
-
TK1
Q9PPP5
-
TK1
O57203
-
TK1a
Q8LDP6
isoform
TK1b
Q8LDP6
isoform
type 1 thymidine kinase
Herpes simplex virus
-
-
type II thymidine kinase 1
P04183
-
type II thymidine kinase 1
-
-
type II thymidine kinase 1
P75070
-
type II thymidine kinase 1
O57203
-
UL23
-
gene name
UL23
Human herpesvirus 1 L2
-
gene name
-
mitochondrial thymidine kinase
-
-
additional information
-
the enzyme belongs to the thymidine kinase 1, i.e. TK1, family of enzymes
additional information
-
the enzyme belongs to the thymidine kinase 2, i.e. TK2, family of enzymes
additional information
P04183
the enzyme belongs to the thymidine kinase 1, i.e. TK1, family of enzymes
additional information
-
the enzyme belongs to the thymidine kinase 1, i.e. TK1, family of enzymes
CAS REGISTRY NUMBER
COMMENTARY
9002-06-6
-
ORGANISM
COMMENTARY
LITERATURE
SEQUENCE CODE
SEQUENCE DB
SOURCE
duck
-
-
Manually annotated by BRENDA team
ecotype Columbia-0
UniProt
Manually annotated by BRENDA team
ecotype Columbia-0
SwissProt
Manually annotated by BRENDA team
subunits alpha and beta
Q9S750 and Q9FN47
UniProt
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
strain TH20p
-
-
Manually annotated by BRENDA team
Equid herpesvirus 4 TH20p
strain TH20p
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
-
-
Manually annotated by BRENDA team
Herpes simplex virus
type 1; type 2
-
-
Manually annotated by BRENDA team
Herpes simplex virus type 4
type 4
-
-
Manually annotated by BRENDA team
Herpes simplex virus type-1
-
-
-
Manually annotated by BRENDA team
enzyme contains a Val at position 106
-
-
Manually annotated by BRENDA team
i.e. HSV-1, acyclovir-sensitive strain KOS, genetic polymorphism
-
-
Manually annotated by BRENDA team
Human herpesvirus 1 L2
-
-
-
Manually annotated by BRENDA team
i.e. human Herpes virus 3, VZV
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
-
-
Manually annotated by BRENDA team
Murine gammaherpesvirus-68
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
-
SwissProt
Manually annotated by BRENDA team
Pyrobaculum aerophilum IM2
strain IM2
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
blood stream and epimastigote form
-
-
Manually annotated by BRENDA team
Trypanosoma brucei TC221
-
-
-
Manually annotated by BRENDA team
of Amsacta moorei
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
-
-
Manually annotated by BRENDA team
the thymidine kinases from Gram-positive bacteria are more closely related to the eukaryotic thymidine kinase 1 enzymes than are thymidine kinases from Gram-negative bacteria
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
malfunction
-
the thymidine kinase-deletion mutant WA79DELTATK shows more than 20fold increase in sensitivity towards acyclovir and is insensitive to ganciclovir
malfunction
Q8LDP6, Q9FN47
TK1a/TK1b double mutants die at an early stage
malfunction
-
depletion of thymidine kinase 1 decreases the efficiency of DNA repair during recovery from DNA damage and generates more cell death
malfunction
-
isoform TK2-deficient animal show growth retardation and premature death
malfunction
Herpes simplex virus
-
a mutation in the thymidine kinase gene results in a shortened enzyme incapable of E-5-(2-bromovinyl)-2'-deoxyuridine phosphorylating
malfunction
Equid herpesvirus 4 TH20p
-
the thymidine kinase-deletion mutant WA79DELTATK shows more than 20fold increase in sensitivity towards acyclovir and is insensitive to ganciclovir
-
malfunction
Herpes simplex virus type-1
-
a mutation in the thymidine kinase gene results in a shortened enzyme incapable of E-5-(2-bromovinyl)-2'-deoxyuridine phosphorylating
-
physiological function
-
the virus-encoded thymidine kinase is an important determinant of the virus susceptibility to nucleoside analogues
physiological function
-
thymidine kinase 1 Ccontributes to the increase in dTTP pool during recovery from DNA damage and affects the efficiency of DNA repair during recovery for G2/M progression
physiological function
-
thymidine kinase 2 plays an important role in providing precursors for the replication and maintenance of mitochondrial DNA, especially in nonproliferating cells
physiological function
Equid herpesvirus 4 TH20p
-
the virus-encoded thymidine kinase is an important determinant of the virus susceptibility to nucleoside analogues
-
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + (E)-5-(2-bromovinyl)-2'-deoxyuridine
ADP + (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-, drug activation by phosphorylation
-
-
?
ATP + (E)-5-(2-bromovinyl)-2'-deoxyuridine
ADP + (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
about 115% of the activity with 2'-deoxythymidine
-
-
?
ATP + (E)-5-(2-bromovinyl)-2'-deoxyuridine
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + 1-(beta-D-arabinofuranosyl)thymine
ADP + 1-(beta-D-arabinofuranosyl)thymine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 1-beta-D-arabinofuranosylthymine
ADP + 1-beta-D-arabinofuranosylthymine 5'-phosphate
show the reaction diagram
-
as active as with 2'-deoxythymidine
-
-
?
ATP + 2',3'-didehydro-2',3'-dideoxythymidine
ADP + 2',3'-didehydro-2',3'-dideoxythymidine 5-phosphate
show the reaction diagram
-
12% activity compared to thymidine
-
-
?
ATP + 2',3'-dideoxycytidine
ADP + 2',3'-dideoxycytidine 5-phosphate
show the reaction diagram
Human herpesvirus 1, Human herpesvirus 1 L2
-
-
-
-
?
ATP + 2',3'-dideoxydehydrothymidine
ADP + 2',3'-dideoxydehydrothymidine 5-phosphate
show the reaction diagram
Human herpesvirus 1, Human herpesvirus 1 L2
-
-
-
-
?
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
-
-
-
-
-
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
O00142
-
-
-
-
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
Q9R088
-
-
-
?
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
-
induction of conformational changes upon ligand binding, overview
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
P04183
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
P75070
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
O57203
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
induction of conformational changes upon ligand binding, overview
-
-
ir
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
Q9R088
-
-
-
?
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-exo-methanocarba-thymidine
ADP + 2'-exo-methanocarba-thymidine 5'-monophosphate
show the reaction diagram
Herpes simplex virus
-
MCT
-
-
ATP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
ADP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
12.3% activity compared to thymidine
-
-
?
ATP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
ADP + 3'-(4-(2-phenylethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
2.4% activity compared to thymidine
-
-
?
ATP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine
ADP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
3.1% activity compared to thymidine
-
-
?
ATP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine
ADP + 3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
7.1% activity compared to thymidine
-
-
?
ATP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
2.7% activity compared to thymidine
-
-
?
ATP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-(3-chloropropyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
6.5% activity compared to thymidine
-
-
?
ATP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
ADP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
13.7% activity compared to thymidine
-
-
?
ATP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
ADP + 3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
2.6% activity compared to thymidine
-
-
?
ATP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
11.6% activity compared to thymidine
-
-
?
ATP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
4.8% activity compared to thymidine
-
-
?
ATP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
2.9% activity compared to thymidine
-
-
?
ATP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
8.7% activity compared to thymidine
-
-
?
ATP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
2.1% activity compared to thymidine
-
-
?
ATP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
5.5% activity compared to thymidine
-
-
?
ATP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
1.9% activity compared to thymidine
-
-
?
ATP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
7.2% activity compared to thymidine
-
-
?
ATP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
2.2% activity compared to thymidine
-
-
?
ATP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
ADP + 3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
4.7% activity compared to thymidine
-
-
?
ATP + 3'-azido-2',3'-deoxythymidine
ADP + 3'-azido-2',3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 3'-azido-2',3'-dideoxythymidine
ADP + 3'-azido-2',3'-dideoxythymidine 5'-phosphate
show the reaction diagram
-
about 165% of the activity with 2'-deoxythymidine
-
-
?
ATP + 3'-azido-2',3'-dideoxythymidine
ADP + 3'-azido-2',3'-dideoxythymidine 5'-phosphate
show the reaction diagram
-
about 5% of the activity with 2'-deoxythymidine
-
-
?
ATP + 3'-azido-2',3'-dideoxythymidine
ADP + 3'-azido-2',3'-dideoxythymidine 5-phosphate
show the reaction diagram
-
60% activity compared to thymidine
-
-
?
ATP + 3'-azido-3'-deoxythymidine
ADP + 3'-azido-3'-deoxythymidine 5'-phosphate
show the reaction diagram
Q9PPP5, -
27.8% activity compared to thymidine
-
-
?
ATP + 3'-azido-3'-deoxythymidine
ADP + 3'-azido-3'-deoxythymidine 5'-phosphate
show the reaction diagram
-
47.3% activity compared to thymidine
-
-
?
ATP + 3'-azido-3'-deoxythymidine
ADP + 3'-azido-3'-deoxythymidine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 3'-azido-3'-deoxythymidine
ADP + 3'-azido-3'-deoxythymidine 5-phosphate
show the reaction diagram
Q8LDP6, Q9FN47
-
-
-
?
ATP + 3'-azidothymidine
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + 3'-deoxy-2',3'-didehydro-thymidine
ADP + 3'-deoxy-2',3'-didehydro-thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 3'-deoxy-2',3'-didehydrothymidine
ADP + 3'-deoxy-2',3'-didehydrothymidine 5-phosphate
show the reaction diagram
Human herpesvirus 1, Human herpesvirus 1 L2
-
-
-
-
?
ATP + 3'-deoxythymidine
ADP + 3'-deoxythymidine 5-phosphate
show the reaction diagram
Human herpesvirus 1, Human herpesvirus 1 L2
-
-
-
-
?
ATP + 3'-fluoro-3'-deoxythymidine
ADP + 3'-fluoro-3'-deoxythymidine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 3-(benzylcarbamimidoyl)thymidine
ADP + 3-(benzylcarbamimidoyl)thymidine 5-phosphate
show the reaction diagram
-
14.9% activity compared to thymidine
-
-
?
ATP + 3-(butylcarbamimidoyl)thymidine
ADP + 3-(butylcarbamimidoyl)thymidine 5-phosphate
show the reaction diagram
-
1.2% activity compared to thymidine
-
-
?
ATP + 3-(phenylcarbamimidoyl)thymidine
ADP + 3-(phenylcarbamimidoyl)thymidine 5-phosphate
show the reaction diagram
-
1.9% activity compared to thymidine
-
-
?
ATP + 3-(tetrazol-5-ylmethyl)thymidine
ADP + 3-(tetrazol-5-ylmethyl)thymidine 5-phosphate
show the reaction diagram
-
39.5% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine
ADP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine 5'-phosphate
show the reaction diagram
-
63.7% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine
ADP + 3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine 5'-phosphate
show the reaction diagram
-
42.5% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine
ADP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine 5'-phosphate
show the reaction diagram
-
52.4% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine
ADP + 3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine 5'-phosphate
show the reaction diagram
-
55.6% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine
ADP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine 5'-phosphate
show the reaction diagram
-
58.2% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine
ADP + 3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine 5'-phosphate
show the reaction diagram
-
42.9% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-propyltetrazol-5-ylmethyl]thymidine
ADP + 3-[1(2)-propyltetrazol-5-ylmethyl]thymidine 5-phosphate
show the reaction diagram
-
55.7% activity compared to thymidine
-
-
?
ATP + 3-[1(2)-propyltetrazol-5-yl]thymidine
ADP + 3-[1(2)-propyltetrazol-5-yl]thymidine 5-phosphate
show the reaction diagram
-
57.6% activity compared to thymidine
-
-
?
ATP + 3-[2-(chloro-1,7-carboranyl)ethylcarbamimidoyl]thymidine
ADP + 3-[2-(chloro-1,7-carboranyl)ethylcarbamimidoyl]thymidine 5-phosphate
show the reaction diagram
-
16.3% activity compared to thymidine
-
-
?
ATP + 3-[2-imino-2-(benzylamino)ethyl]thymidine
ADP + 3-[2-imino-2-(benzylamino)ethyl]thymidine 5-phosphate
show the reaction diagram
-
16.8% activity compared to thymidine
-
-
?
ATP + 3-[2-imino-2-(butylamino)ethyl]thymidine
ADP + 3-[2-imino-2-(butylamino)ethyl]thymidine 5-phosphate
show the reaction diagram
-
2.3% activity compared to thymidine
-
-
?
ATP + 3-[2-imino-2-(phenylamino)ethyl]thymidine
ADP + 3-[2-imino-2-(phenylamino)ethyl]thymidine 5-phosphate
show the reaction diagram
-
11.3% activity compared to thymidine
-
-
?
ATP + 3-[2-imino-2-(propylamino)ethyl]thymidine
ADP + 3-[2-imino-2-(propylamino)ethyl]thymidine 5-phosphate
show the reaction diagram
-
1.9% activity compared to thymidine
-
-
?
ATP + 3-[2-imino-2-[2-(chloro-1,7-carboranyl)ethylamino]ethyl]thymidine
ADP + 3-[2-imino-2-[2-(chloro-1,7-carboranyl)ethylamino]ethyl]thymidine 5-phosphate
show the reaction diagram
-
3.0% activity compared to thymidine
-
-
?
ATP + 3-[2-imino-2-[2-(chloro-1,7-carboranyl)propylamino]ethyl]thymidine
ADP + 3-[2-imino-2-[2-(chloro-1,7-carboranyl)propylamino]ethyl]thymidine 5-phosphate
show the reaction diagram
-
5.6% activity compared to thymidine
-
-
?
ATP + 3-[3-(chloro-1,7-carboranyl)propylcarbamimidoyl]thymidine
ADP + 3-[3-(chloro-1,7-carboranyl)propylcarbamimidoyl]thymidine 5-phosphate
show the reaction diagram
-
15.5% activity compared to thymidine
-
-
?
ATP + 3-[4-(chloro-1,7-carboranyl)butylcarbamimidoyl]thymidine
ADP + 3-[4-(chloro-1,7-carboranyl)butylcarbamimidoyl]thymidine 5-phosphate
show the reaction diagram
-
27.3% activity compared to thymidine
-
-
?
ATP + 5-azido-3'-azido-2',3'-dideoxyuridine
ADP + 5-azido-3'-azido-2',3'-dideoxyuridine 5'-monophosphate
show the reaction diagram
Herpes simplex virus
-
-
photoaffinity analog of 3'-azidothymidine
?
ATP + 5-bromo-2'-deoxyuridine
ADP + 5-bromo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-bromo-2'-deoxyuridine
ADP + 5-bromo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-bromo-2'-deoxyuridine
ADP + 5-bromo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-bromo-2'-deoxyuridine
ADP + 5-bromo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-bromodeoxyuridine
ADP + 5-bromodeoxyuridine 5-phosphate
show the reaction diagram
-
84% activity compared to thymidine
-
-
?
ATP + 5-chloro-2'-deoxyuridine
ADP + 5-chloro-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-chloro-2'-deoxyuridine
ADP + 5-chloro-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-chlorodeoxyuridine
ADP + 5-chlorodeoxyuridine 5-phosphate
show the reaction diagram
-
110% activity compared to thymidine
-
-
?
ATP + 5-diaza-2'-deoxyuridine
ADP + 5-diaza-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-fluoro-2'-deoxyuridine
ADP + 5-fluoro-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-fluoro-2'-deoxyuridine
ADP + 5-fluoro-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-fluoro-2'-deoxyuridine
ADP + 5-fluoro-2'-deoxyuridine 5-phosphate
show the reaction diagram
-
good substrate, 120% activity compared to thymidine
-
-
?
ATP + 5-fluorodeoxyuridine
ADP + 5-fluorodeoxyuridine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-iodo-2'-deoxyuridine
ADP + 5-iodo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-iodo-2'-deoxyuridine
ADP + 5-iodo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-iodo-2'-deoxyuridine
ADP + 5-iodo-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-iodo-2'-deoxyuridine
?
show the reaction diagram
-, Q6S4W2
5-iodo-2'-deoxyuridine is efficiently phosphorylated by thymidine kinase confirming that these compound enters the active site of the enzyme and acts as alternate substrate
-
-
?
ATP + 5-iododeoxyuridine
ADP + 5-iododeoxyuridine 5-phosphate
show the reaction diagram
-
89% activity compared to thymidine
-
-
?
ATP + 5-mercapto-2'-deoxyuridine
ADP + 5-mercapto-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-trifluoromethyl-2'-deoxyuridine
ADP + 5-trifluoromethyl-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 5-trifluoromethyl-2-deoxyuridine
?
show the reaction diagram
-, Q6S4W2
5-trifluoromethyl-2-deoxyuridine is efficiently phosphorylated by thymidine kinase confirming that these compound enters the active site of the enzyme and acts as alternate substrate
-
-
?
ATP + 6-aza-2'-deoxythymidine
ADP + 6-aza-2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 9-(1,3-dihydroxy-2-propoxymethyl)guanine
ADP + 9-(1,3-dihydroxy-2-propoxymethyl)guanine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 9-[(hydroxyethyl)methyl]guanine
ADP + 9-[(hydroxyethyl)methyl]guanine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + aciclovir
ADP + aciclovir 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + aciclovir monophosphate
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + acyclovir
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + acyclovir
?
show the reaction diagram
Herpes simplex virus
-
poor substrate
-
-
?
ATP + acyclovir
ADP + acyclovir phosphate
show the reaction diagram
-
drug activation by phosphorylation, drug activation by phosphorylation, some naturally occurring mutations lead to inability of acyclovir phosphorylation and thus resistance against the drug
-
-
?
ATP + acyclovir
ADP + acyclovir 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + arabinosyl cytosine
?
show the reaction diagram
-
-
-
-
?
ATP + azidothymidine
?
show the reaction diagram
Q71F77
-
-
-
?
ATP + azidothymidine monophosphate
?
show the reaction diagram
Q71F77
-
-
-
?
ATP + beta-5-ethyl-2'-deoxyuridine
?
show the reaction diagram
-, Q6S4W2
beta-5-ethyl-2'-deoxyuridine is efficiently phosphorylated by thymidine kinase confirming that these compound enters the active site of the enzyme and acts as alternate substrate
-
-
?
ATP + beta-L-2',3'-dideoxy-3'-thiacytidine
ADP + beta-L-2',3'-dideoxy-3'-thiacytidine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + beta-L-thymidine
ADP + beta-L-thymidine 5-phosphate
show the reaction diagram
-
less than 5% activity compared to thymidine
-
-
?
ATP + cytosine arabinoside 5'-triphosphate
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + deoxyadenosine
ADP + dAMP
show the reaction diagram
Trypanosoma brucei, Trypanosoma brucei TC221
-
-
-
-
?
ATP + deoxycytidine
ADP + dCMP
show the reaction diagram
-
-
-
-
?
ATP + deoxycytidine
ADP + dCMP
show the reaction diagram
-
-
-
-
?
ATP + deoxycytidine
ADP + dCMP
show the reaction diagram
-
7% activity compared to thymidine
-
-
?
ATP + deoxycytidine
ADP + dCMP
show the reaction diagram
-
substrate for mutant enzymes M42I and L134A
-
-
?
ATP + deoxycytidine
ADP + dCMP
show the reaction diagram
Trypanosoma brucei TC221
-
-
-
-
?
ATP + deoxyguanosine
ADP + dGMP
show the reaction diagram
-
about 20% activity compared to thymidine
-
-
?
ATP + deoxyguanosine
ADP + dGMP
show the reaction diagram
-
substrate for mutant enzymes S182T and S182A
-
-
?
ATP + deoxyguanosine
ADP + dGMP
show the reaction diagram
Trypanosoma brucei TC221
-
about 20% activity compared to thymidine
-
-
?
ATP + deoxyinosine
ADP + dIMP
show the reaction diagram
Trypanosoma brucei, Trypanosoma brucei TC221
-
about 30% activity compared to thymidine
-
-
?
ATP + deoxyuridine
ADP + dUMP
show the reaction diagram
Q8LDP6, Q9FN47
-
-
-
?
ATP + deoxyuridine
ADP + dUMP
show the reaction diagram
-
69% activity compared to thymidine
-
-
?
ATP + deoxyuridine
ADP + dUMP
show the reaction diagram
-
about 185% activity compared to thymidine
-
-
?
ATP + dideoxyinosine
ADP + dideoxyinosine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + E-5-(2-bromovinyl)-2'-deoxyuridine
ADP + E-5-(2-bromovinyl)-2'-deoxyuridine 5-phosphate
show the reaction diagram
-
-
-
-
?
ATP + ganciclovir
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + ganciclovir
ADP + ganciclovir phosphate
show the reaction diagram
-
-
-
-
?
ATP + ganciclovir monophosphate
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + guanosine
ADP + GMP
show the reaction diagram
-
1% activity compared to thymidine
-
-
?
ATP + iododideoxyuridine
ADP + iododideoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + lobucavir
?
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + methylthymidine
ADP + methylthymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Herpes simplex virus
-
-
-
-
-
ATP + thymidine
ADP + dTMP
show the reaction diagram
Herpes simplex virus
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q9R088
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Murine gammaherpesvirus-68
Q83342
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q71F77
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
P27158
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q0H0H6
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q9S750 and Q9FN47
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
G5EEZ5
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q803Y1
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q5I0A2
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
C3VAL3
-
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q8LDP6, Q9FN47
best substrate
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
100% activity
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
100% activity
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
100% activity
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Q9PPP5, -
100% activity
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by GTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by GTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by GTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by GTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by GTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Herpes simplex virus
-
ATP can be substituted by GTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by GTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Herpes simplex virus
-
ATP can be substituted by dGTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dGTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by ATP-arabinoside, ATP can be substituted by UTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by UTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by UTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by UTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dCTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dCTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dCTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Herpes simplex virus
-
ATP can be substituted by dCTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dCTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
requirement for high levels of ATP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
requirement for high levels of ATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Herpes simplex virus
-
ATP can be substituted by dATP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by dATP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by CTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by CTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by CTP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by CTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by CTP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by ITP
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
ATP can be substituted by ITP
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
-
best substrate combination, 100% activity
-
-
?
ATP + thymidine
ADP + dTMP
show the reaction diagram
Human herpesvirus 1 L2
-
-
-
-
?
ATP + thymidine
?
show the reaction diagram
-
-
-
-
?
ATP + thymidine
?
show the reaction diagram
-
-
-
-
?
ATP + thymidine
?
show the reaction diagram
-
involved in DNA replication
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-, Q27564
-
-
-
ir
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
Herpes simplex virus type 4
-
-
-
-
r
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
enzyme contains the putative thymidine-binding motif FQRK
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-, Q6S4W2
ATP acts as specific phosphate donor
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
Equid herpesvirus 4 TH20p
-
-
-
-
?
ATP + thymidine 5'-phosphate
ADP + thymidine diphosphate
show the reaction diagram
Herpes simplex virus type 4
-
-
-
-
r
ATP + trifluoromethylthymidine
ADP + trifluoromethylthymidine 5-phosphate
show the reaction diagram
-
good substrate, 130% activity compared to thymidine
-
-
-
ATP + uridine
ADP + UMP
show the reaction diagram
-
-
-
-
?
ATP + [methyl-3H]thymidine
ADP + [methyl-3H]thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
CTP + thymidine
CDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
-
CTP + thymidine
CDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
-
CTP + thymidine
CDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
CTP + thymidine
CDP + dTMP
show the reaction diagram
-
-
-
-
?
dGTP + thymidine
dGDP + dTMP
show the reaction diagram
-
99% activity compared to ATP
-
-
?
GTP + thymidine
GDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
-
GTP + thymidine
GDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
-
GTP + thymidine
GDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
GTP + thymidine
GDP + dTMP
show the reaction diagram
-
-
-
-
?
TTP + thymidine
TDP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
UTP + thymidine
UDP + dTMP
show the reaction diagram
-
-
-
-
?
UTP + thymidine
UDP + dTMP
show the reaction diagram
-
17% activity compared to ATP
-
-
?
GTP + thymidine
GDP + dTMP
show the reaction diagram
-
42% activity compared to ATP
-
-
?
additional information
?
-
Q9R088
overview: nucleoside analogs
-
-
-
additional information
?
-
-
5-halogenated cytidines, bromouridine, iodouridine, uridine, 5-fluorodeoxycytidine, purine ribonucleosides
-
-
-
additional information
?
-
-
overview: thymidine analogs
-
-
-
additional information
?
-
-
comparison rat liver, Trypanosoma brucei
-
-
-
additional information
?
-
-
overview thymine nucleosides, 2'-deoxyribonucleosides, arabinosides, ribonucleosides
-
-
-
additional information
?
-
-
no phosphorylation of deoxyuridine, 5-halogenated deoxyuridines
-
-
-
additional information
?
-
-
no substrates: ganciclovir, acyclovir, 2'-deoxycytidine
-
-
-
additional information
?
-
-
overview: phosphoryl donors
-
-
-
additional information
?
-
-
the cell-cycle-regulated enzyme is important in nucleotide metabolism and an activator of antiviral and anticancer drugs
-
-
-
additional information
?
-
-
the enzyme is tightly regulated in the cell cycle by multiple mechanism, e.g. by phosphorylation at Ser13 in mitotic-arrested cells, regulation model
-
-
-
additional information
?
-
-
the viral enzyme shows a broader substrate specificity than the human host cell enzyme
-
-
-
additional information
?
-
-
ligand-induced conformational changes in dimeric and tetrameric forms of the enzyme alter the catalytic activity
-
-
-
additional information
?
-
-
modeling of ganciclovir binding into the enzyme crystal structure, overview
-
-
-
additional information
?
-
P04183
narrow substrate specificity
-
-
-
additional information
?
-
-
substrate specificity of wild-type and mutant enzymes, overview
-
-
-
additional information
?
-
-
Val106 has effects on structure-function relation of the enzyme
-
-
-
additional information
?
-
Herpes simplex virus type 4
-
wide substrate specificity phosphorylating pyrimidine nucleosides, nucleoside monophophates, and several nucleoside analogues
-
-
-
additional information
?
-
-
the type II thymidine kinase ecoded by cowpox virus exhibits a more limited substrate specificity than the type I thymidine kinase encoded by HSV-1
-
-
-
additional information
?
-
-, Q6S4W2
beta-L-thymidine is poorly phosphorylated by the enzyme
-
-
-
additional information
?
-
-, Q6S4W2
does not use UTP, GTP, and TTP as cosubstrates
-
-
-
additional information
?
-
-
CTP, diphosphate, uridine, adenosine, cytosine, deoxyguanosine, deoxyguanosine, dTMP, thymine 1-beta-D-arabinofuranoside, 1-beta-D-arabinofuranosylcytosine, acyclovir, and 5-iodo-2'-deoxycytidine are no substrates
-
-
-
additional information
?
-
-
domain 1 of thymidine kinase is catalytically inactive but improves substrate binding by domain 2. The enzyme shows the following order of catalytic efficiencies: thymidine > deoxyuridine >> deoxyinosine > deoxyguanosine. The enzyme shows no activity with deoxyadenosine and deoxycytidine
-
-
-
additional information
?
-
-
no activity with 3-(propylcarbamimidoyl)thymidine and 3-(tetrazol-5-yl)thymidine
-
-
-
additional information
?
-
-
the wild type enzyme shows no activity with deoxycytidine and deoxyadenosine
-
-
-
additional information
?
-
Trypanosoma brucei TC221
-
domain 1 of thymidine kinase is catalytically inactive but improves substrate binding by domain 2. The enzyme shows the following order of catalytic efficiencies: thymidine > deoxyuridine >> deoxyinosine > deoxyguanosine. The enzyme shows no activity with deoxyadenosine and deoxycytidine
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + (E)-5-(2-bromovinyl)-2'-deoxyuridine
ADP + (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
drug activation by phosphorylation
-
-
?
ATP + 2'-deoxycytidine
ADP + 2'-deoxycytidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
P04183
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
P75070
-
-
-
?
ATP + 2'-deoxythymidine
ADP + 2'-deoxythymidine 5'-phosphate
show the reaction diagram
O57203
-
-
-
?
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
ir
ATP + 2'-deoxyuridine
ADP + 2'-deoxyuridine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + acyclovir
ADP + acyclovir phosphate
show the reaction diagram
-
drug activation by phosphorylation, some naturally occurring mutations lead to inability of acyclovir phosphorylation and thus resistance against the drug
-
-
?
ATP + thymidine
?
show the reaction diagram
-
-
-
-
?
ATP + thymidine
?
show the reaction diagram
-
-
-
-
?
ATP + thymidine
?
show the reaction diagram
-
involved in DNA replication
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-
-
-
-
?
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
-, Q27564
-
-
-
ir
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
Herpes simplex virus type 4
-
-
-
-
r
ATP + thymidine
ADP + thymidine 5'-phosphate
show the reaction diagram
Equid herpesvirus 4, Equid herpesvirus 4 TH20p
-
-
-
-
?
ATP + thymidine 5'-phosphate
ADP + thymidine diphosphate
show the reaction diagram
Herpes simplex virus type 4
-
-
-
-
r
additional information
?
-
-
the cell-cycle-regulated enzyme is important in nucleotide metabolism and an activator of antiviral and anticancer drugs
-
-
-
additional information
?
-
-
the enzyme is tightly regulated in the cell cycle by multiple mechanism, e.g. by phosphorylation at Ser13 in mitotic-arrested cells, regulation model
-
-
-
additional information
?
-
-
the viral enzyme shows a broader substrate specificity than the human host cell enzyme
-
-
-
COFACTOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
ATP
-
binding of ATP induces enzyme tetramerization
ATP
-
P-loop binding site
ATP
-
preferred triphosphate cosubstrate, 3 essential residues T298, K297, and G294 in the conserved ATP-binding region, enzyme binding kinetics
ATP
-
binding of ATP induces reversible transition from a dimer with low catalytic activiy to a tetramer with high catalytic activity
ATP
Herpes simplex virus type 4
-
-
CTP
-
less active than ATP
dATP
-
activation
dGTP
-
activation
GDP
-
activation
GTP
-
less active tahn ATP
TTP
-
low activity with wild-type and mutant enzymes
additional information
-
activity with NTP cofactors in descending order ATP, GTP, CTP, TTP
-
METALS and IONS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
Ca2+
-
can partially substitute for Mg2+
Ca2+
-
can partially substitute for Mg2+
Ca2+
-
can partially substitute for Mg2+
Ca2+
-
calmodulin binding binding is dependent on Ca2+
Co2+
-
can partially substitute for Mg2+
Co2+
-
can partially substitute for Mg2+
Co2+
-
can partially substitute for Mg2+
Cu2+
-
can partially substitute for Mg2+
Fe2+
-
can partially substitute for Mg2+
Mg2+
-
2.9 mM, required
Mg2+
-
Km: 0.8 mM
Mg2+
-
7.5-10 mM, required
Mg2+
-
-
Mg2+
-
required, most efficient metal ion, can be substituted by Mn2+ or Zn2+
Mg2+
O57203
-
Mg2+
Herpes simplex virus
-
required
Mg2+
-, Q6S4W2
MgCl2 is required for activity, reaching its optimal effect at 1.2 mM when ATP is present at 1 mM
Mn2+
-
can partially substitute for Mg2+
Mn2+
-
can partially substitute for Mg2+
Mn2+
-
can partially substitute for Mg2+
Mn2+
-
can partially substitute for Mg2+
Mn2+
-
can partially substitute for Mg2+
Ni2+
-
can partially substitute for Mg2+
Zn2+
-
can partially substitute for Mg2+
Zn2+
-
liver
Zn2+
-
can partially substitute for Mg2+
Zn2+
-
Cys residues C153, C156, C185, and C188 are involved in binding
Zn2+
-
enzyme contains a zinc finger binding motif
Zn2+
P75070
enzyme contains a zinc finger binding motif
Zn2+
O57203
enzyme contains a zinc finger binding motif
Zn2+
-
at a molar ratio of 0.56, connects beta-structures at the root of a ribbon that forms a stem which widens to a lasso-loop
Zn2+
-
at a molar ratio of 0.51, connects beta-structures at the root of a ribbon that forms a stem which widens to a lasso-loop
Mn2+
-, Q6S4W2
MnCl2 can replace MgCl2 in the assay, with optimal activity at 200 mM when ATP is present at 1 mM
additional information
-
inactive with Ba2+ and Ca2+
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl 3,3-dimethylbutanoate
-
IC50: 0.028 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl 3,3-dimethylbutanoate
-
IC50: above 0.5 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl benzoate
-
IC50: 0.03 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl benzoate
-
IC50: above 0.5 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl diphenylacetate
-
IC50: 0.0046 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl diphenylacetate
-
IC50: 0.281 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl dodecanoate
-
IC50: 0.019 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl dodecanoate
-
IC50: above 0.5 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl heptanoate
-
IC50: 0.011 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl heptanoate
-
IC50: 0.42 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl pivalate
-
IC50: 0.04 mM
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl pivalate
-
IC50: above 0.5 mM
(4E)-N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: 0.265 mM
(4E)-N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: above 0.5 mM
(4E)-N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: 0.371 mM
(4E)-N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: above 0.5 mM
(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
-
IC50: 0.18 mM
1-[(2Z)-4-(benzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.057 mM
1-[(2Z)-4-(benzyloxy)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.022 mM
1-[(2Z)-4-(benzyloxy)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: above 0.5 mM
1-[(2Z)-4-(dibenzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0035 mM; IC50: above 0.5 mM
1-[(2Z)-4-(dibenzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0035 mM
1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-5,6-dihydrothymine
-
IC50: 0.01 mM
1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-5,6-dihydrothymine
-
IC50: above 0.5 mM
1-[(2Z)-4-hydroxybut-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.173 mM
1-[(2Z)-4-hydroxybut-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.224 mM
1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine
-
-
-
1-[2,3-dihydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.017 mM
1-[2,3-dihydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.013 mM
1-[3-hydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0036 mM
1-[3-hydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0012 mM
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
-
IC50: 0.023 mM
2-(4-chlorophenyl)-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.198 mM
2-biphenyl-4-yl-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.0041 mM
2-biphenyl-4-yl-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.119 mM
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)-2'-deoxythymidine
-
-
-
3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
Q9PPP5, -
-
-
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine
-
-
-
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine
Q9PPP5, -
-
-
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
-
-
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
-
-
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
-
-
-
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
Q9PPP5, -
-
-
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-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
-
-
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-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
-
-
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
-
-
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
-
-
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
-
-
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
-
-
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
-
-
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
-
-
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-3'-deoxythmidine
-
inhibits thymidine phosphorylation catalyzed by thymidine kinase 2
-
3'-azido-3'-deoxythymidine
-
-
3'-azido-3'-deoxythymidine
Q9PPP5, -
-
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
-, Q6S4W2
-
3'-fluorothymidine
-
inhibits thymidine phosphorylation catalyzed by 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
-
-
3-hexanoylamino-3'-deoxythymidine
-
very potent inhibitor of thymidine kinase 2
-
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylbutanamide
-
IC50: 0.44 mM
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylbutanamide
-
IC50: 0.175 mM
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-oxo-2-(tritylamino)ethyl]butanamide
-
IC50: 0.194 mM
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-oxo-2-(tritylamino)ethyl]butanamide
-
IC50: 0.191 mM
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-(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
-
IC50: 0.0013 mM; IC50: 0.1 mM
5-(E)-(2-bromovinyl)-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: above 0.5 mM
5-(E)-(2-bromovinyl)uridine
-
inhibits phosphorylation of 2'-deoxythymidine
5-(E)-(2-bromovinyl)uridine
-
-
5-aminobenzyl-(3'-deoxy-beta-D-thymidin-3'N-yl)-tetrazole
-
-
-
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-bromodeoxyuridine
-
competitive to thymidine
5-bromodeoxyuridine
-
competitive to thymidine
5-bromodeoxyuridine
-
-
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
-
IC50: 0.02 mM
5-ethyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: above 0.5 mM
5-fluorodeoxyuridine
-
competitive to thymidine
5-fluorodeoxyuridine
-
competitive to thymidine
5-fluorodeoxyuridine
-
-
5-iodo-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.0046 mM
5-iodo-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.048 mM
5-iodo-2'-deoxyuridine
-, Q6S4W2
potent inhibitor
5-iododeoxyuridine
-
competitive to thymidine
5-iododeoxyuridine
-
competitive to thymidine
5-methyl-1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.025 mM
5-methyl-1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.003 mM
5-methyl-1-[(2Z)-4-(4-methylpiperazin-1-yl)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.491 mM
5-methyl-1-[(2Z)-4-(tritylamino)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0023 mM; IC50: above 0.5 mM
5-methyl-1-[(2Z)-4-(tritylamino)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0023 mM
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-cytosine
-
IC50: 0.484 mM
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-cytosine
-
IC50: above 0.5 mM
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0015 mM; IC50: above 0.1 mM
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.045 mM
5-methyl-1-[4-(trityloxy)but-2-yn-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.404 mM
5-methyl-1-[4-(trityloxy)but-2-yn-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0031 mM
5-methyl-1-[4-(trityloxy)butyl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0033 mM
5-methyl-1-[4-(trityloxy)butyl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.01 mM
5-propyl-2'-deoxyuridine
-, Q6S4W2
-
5-trifluoromethyl-2-deoxyuridine
-, Q6S4W2
potent inhibitor
5-Trifluoromethyldeoxyuridine
-
competitive to thymidine
5-[(E)-2-bromoethenyl]-2'-O-decanoyluridine
-
competitive with respect to 2'-deoxythymidine, IC50: 0.0012 mm
5-[(E)-2-bromoethenyl]-2'-O-octanoyluridine
-
IC50: 0.006 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
-
-
-
5-[amino-(4-chloro-3-trifluoromethylphenyl)]-1-(3'-deoxy-beta-D-thymidin-3'N-yl)-tetrazole
-
-
-
6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylhexanamide
-
IC50: 0.019 mM
6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylhexanamide
-
IC50: 0.0034 mM
6-methyluridine
-, Q6S4W2
-
9-[(2Z)-4-(trityloxy)but-2-en-1-yl]-guanine
-
IC50: above 0.5 mM
aciclovir
Herpes simplex virus
-
competitive inhibitor
acyclovir
Herpes simplex virus
-
syn. 9-[(2-hydroxyethoxy)methyl]guanine
acyclovir
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type enzyme at 0.05 mM, 50% photoincorporation inhibition of C336Y mutant above 0.3 mM
acyclovir H-phosphonate
-
-
-
ADP
-
competitive to ATP
ADP
-
competitive to ATP
alpha-D-5-ethyl-2'-deoxyuridine
-, Q6S4W2
-
alpha-L-thymidine
-, Q6S4W2
-
ammoniumsulfate
Herpes simplex virus
-
50% inhibition at 200 mM
ATP
-
non-competitive
ATP
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type enzyme at 0.15 mM, 50% photoincorporation inhibition of C336Y mutant above 1 mM
beta-D-5-ethyl-2'-deoxyuridine
-, Q6S4W2
potent inhibitor
beta-L-thymidine
-, Q6S4W2
potent inhibitor
Caffeine
-
competitive to ATP
Caffeine
-
competitive to ATP, 75% inhibition at 20 mM
dATP
-
strong feedback inhibition, tight binding at the active site in stoichiometric amount
dCTP
-
mitochondrial enzyme
dCTP
-
30-45% inhibition of mitochondrial enzyme at 0.6 or 1 mM, no inhibition of cytosolic enzyme
dCTP
-
80% inhibition of adult enzyme at 1 mM, almost no inhibition of fetal enzyme
dCTP
-
strong feedback inhibition, tight binding at the active site in stoichiometric amount
deoxcytidine
-
-
deoxcytidine
-
poor inhibitor
Deoxyuridine
-
competitive to thymidine
dGDP
-
competitive to ATP
dTDP
-
competitive to ATP
dTDP
-
83% inhibition at 0.1 mM
dTMP
-
competitive to thymidine
dTMP
-
competitive to ATP
dTMP
-
8% inhibition at 0.1 mM
dTTP
-
50-90% inhibition at 0.2-0.8 mM; competitive to thymidine
dTTP
-
non-competitive
dTTP
-
non-competitive with thymidine, competitive to ATP
dTTP
-
inhibition dependent on pH
dTTP
-
84% inhibition at 0.1 mM
dTTP
-
competitive feedback inhibition
dTTP
-
strong feedback inhibition, tight binding at the active site in stoichiometric amount
dTTP
-
feedback inhibitor, binds tightly to the enzyme at the active site
dTTP
-
binds to the active site
dTTP
P75070
binds to the active site
dTTP
O57203
binds to the active site
dTTP
-
competitive feedback inhibition, binding structure analysis
dUTP
-
competitive to ATP
EDTA
-
complete incactivation at 2.5 mM
iododeoxycytidine
Herpes simplex virus
-
-
m-Fluorothymine
-
-
Mg2+
-
non-competitive
N-(2-cyanoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.46 mM
N-(2-cyanoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
N-(2-cyanoethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.353 mM
N-(2-cyanoethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: above 0.5 mM
N-(2-[[cyano(phenyl)methyl]amino]-2-oxoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.318 mM
N-(2-[[cyano(phenyl)methyl]amino]-2-oxoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
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
-
IC50: 0.268 mM
N-(cyanomethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: above 0.5 mM
N-(diphenylmethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.238 mM
N-(diphenylmethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.038 mM
N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.043 mM
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
-
IC50: 0.027 mM
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-2,2-diphenylacetamide
-
IC50: 0.115 mM
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-3-(trifluoromethyl)benzamide
-
IC50: 0.028 mM
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-3-(trifluoromethyl)benzamide
-
IC50: 0.072 mM
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-9H-xanthene-9-carboxamide
-
IC50: 0.033 mM
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-9H-xanthene-9-carboxamide
-
IC50: 0.131 mM
N-[2-[(diphenylmethyl)amino]-2-oxoethyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.287 mM
N-[2-[(diphenylmethyl)amino]-2-oxoethyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
N-[cyano(phenyl)methyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.208 mM
N-[cyano(phenyl)methyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.495 mM
N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.075 mM
N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.275 mM
N3-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-thymine
-
IC50: above 0.5 mM
p-Fluorothymine
-
-
-
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
-
three PCV-resistant FHV-1 variants selected in vitro carry mutations in the TK gene. Penciclovir is a potent selective inhibitor of Feline herpesvirus-1. The virus-encoded thymidine kinase is an important determinant of the virus susceptibility to nucleoside analogues
penciclovir
-, Q6S4W2
-
potassium phosphate
-
80% inhibition at 50 mM
sulfate
-
competitive inhibitor of ATP binding
theophylline
-
-
thymidine
-
-
thymidine
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type enzyme at 0.003 mM, 50% photoincorporation inhibition of C336Y mutant at 0.05 mM
thymidine
-
inhibition of deoxycytidine kinase activity
thymidylate
Herpes simplex virus
-
50% photoincorporation inhibition of wild-type and C336Y mutant enzyme at 0.0125 mM
TTP
-
83% inhibition at 1 mM, 43% inhibition at 0.1 mM, 15% inhibition at 0.01 mM
W7
-
slight inhibitory in presence of calmodulin
Zn2+
-
1.1 mM and 2.9 mM
additional information
-
bisubstrate analogs with adenosine and thymidine joined at their 5' positions by polyphorphoryl linkages of varying lengths can serve as inhibitors
-
additional information
-
overview: purine nucleotides, pyrimidine nucleotides
-
additional information
-
no inhibition: phenylmethylsulfonylfluoride
-
additional information
-
no inhibition: AMP, CMP, GMP, putrescine, spermine, spermidine
-
additional information
-
5'-derivatives of thymidine
-
additional information
-
5'-derivatives of thymidine
-
additional information
-
overview: deoxythymidine analogs
-
additional information
Herpes simplex virus
-
structural requirements of bromine substituted 5-heteroaromatic 2'-deoxyuridines as antiviral agents
-
additional information
-
inhibition potency of dNTPs in descending order: dTTP, dCTP, dATP, inhibitor binding structurally stabilizes the enzyme, induction of conformational changes upon ligand binding, overview
-
additional information
-
structure-aided design of a series of substituted 3'- or 5'-thiourea derivatives of beta- and alpha-thymidine, respectively, as thymidine monophosphate kinase inhibitors
-
additional information
Herpes simplex virus
-
synthesis of tricarbonyl rhenium and technetium complexes of a 5-carboxamide 5-ethyl-2'-deoxyuridine for selective inhibition of herpes simplex virus thymidine kinase
-
additional information
-, Q6S4W2
not inhibited by D-5-(bromovinyl)-2'-deoxyuridine, L-5-(bromovinyl)-2'-deoxyuridine, and 2-phenylamino-9-(4-hydroxybutyl)-6-oxopurine
-
additional information
-
at physiological relevant concentration deoxycytidine phosphorylation is not inhibited by 3-azido-3'-deoxythmidine or 3'-fluorothymidine
-
additional information
-
at physiological relevant concentration deoxycytidine phosphorylation is not inhibited by 3'-azido-3'-deoxythmidine or 3'-fluorothymidine
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
3'-azido-3'-deoxythmidine
-
stimulates deoxycytidine phosphorylation catalyzed by thymidine kinase 2
-
3'-azido-3'-deoxythymidine
-
stimulates deoxycytidine phosphorylation catalyzed by thymidine kinase 2
3'-deoxy-3'-fluorothymidine
-
stimulates deoxycytidine phosphorylation catalyzed by thymidine kinase 2
-
3'-fluorothymidine
-
stimulates deoxycytidine phosphorylation catalyzed by thymidine kinase 2
-
ATP
-
binding of ATP induces enzyme tetramerization, which leads to activation of the enzyme, the dimeric enzyme form is probably less active, 50-100% activation at up to 5 mM
Bovine serum albumin
-
activation at 0.2 mg/ml
-
Calmodulin
-
stimulates the enzyme by 13.8%, might modify the activity, enzyme contains a calmodulin binding domain, Ca2+ is required for binding, compounds W7 and W13 prevent stimulation, overview
dCDP
-
activation
dCDP
-
dCDP activates the enzyme 2.5old
dCTP
-
dCTP is not a phosphate donor, but instead activates the enzyme 7fold
dithiothreitol
-
-
dithiothreitol
-
the enzyme is stimulated by dithiothreitol up to a concentration of 2 mM
GTP
-
activation
Hydroxymethyl-dCDP
-
activation
Hydroxymethyl-dCTP
-
activation
NaCl
-
weak stimulation
potassium acetate
-
weak stimulation
KCl
-
weak stimulation
additional information
-
Km values of allosteric regulators
-
additional information
-
the enzyme is not activated by dATP or dGTP
-
KM VALUE [mM]
KM VALUE [mM] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.05
-
2',3'-didehydro-2',3'-dideoxythymidine
-
at pH 7.8 and 25C
0.004
-
2'-deoxycytidine
-
dNTP-free recombinant dimeric enzyme, pH 7.5, 25C
0.0049
-
2'-deoxycytidine
-
dNTP-free recombinant tetrameric enzyme, pH 7.5, 25C
0.018
-
2'-deoxycytidine
-
tetrameric enzyme, pH 7.5, 25C
0.025
-
2'-deoxycytidine
-
dimeric enzyme, pH 7.5, 25C
0.0058
-
2'-deoxythymidine
-
dNTP-free recombinant dimeric enzyme, pH 7.5, 25C
0.0065
-
2'-deoxythymidine
-
dNTP-free recombinant tetrameric enzyme, pH 7.5, 25C
0.016
-
2'-deoxythymidine
-
37C, pH 7.6
0.025
-
2'-deoxythymidine
-
pH 8.0, 37C
0.041
-
2'-deoxythymidine
-
37C, pH 7.6
0.05
-
2'-deoxythymidine
-
tetrameric enzyme, pH 7.5, 25C
0.054
-
2'-deoxythymidine
-
dimeric enzyme, pH 7.5, 25C
0.33
-
2'-deoxythymidine
-
37C, pH 7.6
0.032
-
3'-azido-2',3'-dideoxythymidine
-
at pH 7.8 and 25C
0.00038
-
3'-azido-3'-deoxythymidine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
0.00043
-
3'-azido-3'-deoxythymidine
-
mutant enzyme T163S, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.00052
-
3'-azido-3'-deoxythymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.0027
-
3'-azido-3'-deoxythymidine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
0.012
-
3'-azido-3'-deoxythymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.015
-
3'-azido-3'-deoxythymidine
-
37C, pH 7.6
0.018
-
3'-azido-3'-deoxythymidine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.033
-
3'-azido-3'-deoxythymidine
-
mutant enzyme L124A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.05
-
3'-azido-3'-deoxythymidine
-
37C, pH 7.6
0.204
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M28A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.254
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M28I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.406
-
3'-azido-3'-deoxythymidine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.6
-
3'-azido-3'-deoxythymidine
-
37C, pH 7.6
2.318
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.0563
-
3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0174
-
3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0318
-
3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0356
-
3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0552
-
3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0799
-
3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0373
-
3-[1(2)-propyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.0552
-
3-[1(2)-propyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.04
-
5-fluoro-2'-deoxyuridine
-
at pH 7.8 and 25C
0.03
-
5-fluorodeoxyuridine
-
full-length enzyme, at pH 7.8 and 37C
0.0012
-
5-iodo-2'-deoxythymidine
-
-
0.011
-
aciclovir monophosphate
Herpes simplex virus
-
-
0.00337
-
acyclovir
Herpes simplex virus
-
37C, mutant SR26
0.0056
-
acyclovir
Herpes simplex virus
-
37C, mutant SR11
0.00979
-
acyclovir
Herpes simplex virus
-
37C, mutant SR39
0.417
-
acyclovir
Herpes simplex virus
-
37C, wild-type
0.0013
-
ATP
Herpes simplex virus
-
pH 7.6, 37C, mutant C336Y
0.0047
-
ATP
-
dimeric enzyme, pH 7.5, 25C
0.0109
-
ATP
-
tetrameric enzyme, pH 7.5, 25C
0.01163
-
ATP
-
37C
0.013
-
ATP
Herpes simplex virus
-
pH 7.6, with deoxycytidine
0.015
-
ATP
-
pH 8.5, 30C
0.021
-
ATP
Herpes simplex virus
-
pH 7.6, with deoxyuridine
0.025
-
ATP
-
wild-type, thymidine as substrate, pH 7.6
0.03
-
ATP
Herpes simplex virus
-
pH 7.6, 37C, wild-type
0.03
-
ATP
-
recombinant wild-type enzyme, pH 7.5, 37C
0.037
-
ATP
-
wild-type, deoxycytidine as substrate, pH 7.6
0.041
-
ATP
-
recombinant mutant T298S, pH 7.5, 37C
0.049
-
ATP
-
recombinant mutant G294A, pH 7.5, 37C
0.05
-
ATP
-
pH 7, 37C
0.059
-
ATP
-
I212 mutant, deoxycytidine as substrate, pH 7.6
0.07
-
ATP
-
cytosolic enzyme, pH 7.5, 37C
0.076
-
ATP
-
pH 8, 25C or 37C
0.08
-
ATP
-
H121N mutant, thymidine as substrate, pH 7.6
0.088
-
ATP
-
recombinant mutant K297R, pH 7.5, 37C
0.09
-
ATP
-
pH 7.4, 37C
0.095
-
ATP
-
I212 mutant, thymidine as substrate, pH 7.6
0.098
-
ATP
-
thymidine kinase domain 2, with 0.05 mM thymidine as cosubstrate, at pH 7.8 and 37C
0.1
-
ATP
-
mitochondrial enzyme, pH 7.5, 37C
0.11
-
ATP
-
mitochondrial enzyme, pH 7.5, 37C
0.118
-
ATP
Herpes simplex virus
-
-
0.14
-
ATP
-
at pH 7.8 and 25C
0.15
-
ATP
-
pH 7.8, 37C
0.162
-
ATP
-
H121N mutant, deoxycytidine as substrate, pH 7.6
0.18
-
ATP
-
full-length enzyme, with 0.0005 mM thymidine as cosubstrate, at pH 7.8 and 37C
0.2
-
ATP
-
pH 8, 37C
0.21
-
ATP
-
full-length enzyme, with 0.05 mM thymidine as cosubstrate, at pH 7.8 and 37C
0.22
-
ATP
-
full-length enzyme, with 0.005 mM thymidine as cosubstrate, at pH 7.8 and 37C
0.3
-
ATP
-
GTP
0.32
-
ATP
-
full-length enzyme, with 0.5 mM deoxyinosine as cosubstrate, at pH 7.8 and 37C
2.6
-
ATP
-
at concentrations above 1 mM, pH 8, 37C
20
-
ATP
-
at concentrations below 1 mM, pH 8, 37C
0.29
-
beta-L-thymidine
-
at pH 7.8 and 25C
0.049
-
CTP
-
recombinant wild-type enzyme, pH 7.5, 37C
0.057
-
CTP
-
about, recombinant mutant T298S, pH 7.5, 37C
0.088
-
CTP
-
recombinant mutant G294A, pH 7.5, 37C
0.108
-
CTP
-
recombinant mutant K297R, pH 7.5, 37C
0.15
-
CTP
-
pH 7.4, 37C
0.15
-
CTP
-
ATP
8.4
-
deoxyadenosine
-
full-length enzyme, at pH 7.8 and 37C
0.003
-
Deoxycytidine
-
mitochondrial enzyme, pH 7.5, 37C
0.0036
-
Deoxycytidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.006
-
Deoxycytidine
-
pH 7.4, 37C
0.011
-
Deoxycytidine
-
wild-type and H121N mutant, pH 7.6
0.0115
-
Deoxycytidine
Q9R088
mTK2-55 pH 7.6
0.0236
-
Deoxycytidine
Q9R088
mTK2-39 pH 7.6
0.0251
-
Deoxycytidine
Q9R088
mTK2 pH 7.6
0.0414
-
Deoxycytidine
-
pH and temperature not specified in the publication
0.106
-
Deoxycytidine
Herpes simplex virus
-
pH 7.6
0.568
-
Deoxycytidine
-
I212 mutant, pH 7.6
2.6
-
deoxyguanosine
-
full-length enzyme, at pH 7.8 and 37C
2.5
-
Deoxyinosine
-
full-length enzyme, at pH 7.8 and 37C
0.0047
-
Deoxyuridine
Herpes simplex virus
-
pH 7.6
0.0066
-
Deoxyuridine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
0.015
-
Deoxyuridine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
0.08
-
Deoxyuridine
-
full-length enzyme, at pH 7.8 and 37C
0.118
-
Deoxyuridine
-
at pH 7.8 and 25C
0.43
-
Deoxyuridine
-
thymidine kinase domain 2, at pH 7.8 and 37C
0.066
-
difluorodeoxycytidine
-
-
0.029
-
difluorodeoxyuridine
-
-
0.00333
-
ganciclovir
Herpes simplex virus
-
37C, mutant SR39
0.00614
-
ganciclovir
Herpes simplex virus
-
37C, mutant SR11
0.01755
-
ganciclovir
Herpes simplex virus
-
37C, mutant SR26
0.0476
-
ganciclovir
Herpes simplex virus
-
37C, wild-type
0.05
-
ganciclovir
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125E
0.069
-
ganciclovir
Herpes simplex virus
-
pH 7.6, 37C, wild-type
0.473
-
ganciclovir
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125N
0.12
-
ganciclovir monophosphate
Herpes simplex virus
-
-
0.041
-
GTP
-
recombinant wild-type enzyme, pH 7.5, 37C
0.043
-
GTP
-
about, recombinant mutant K297R, pH 7.5, 37C
0.045
-
GTP
-
recombinant mutant T298S, pH 7.5, 37C
0.069
-
GTP
-
recombinant mutant G294A, pH 7.5, 37C
0.3
-
GTP
-
pH 7.4, 37C
0.3
-
GTP
-
pH 7.8, 37C
0.0001
-
MgATP2-
-
two active sites for ATP
0.0028
-
MgATP2-
-
dNTP-free recombinant dimeric enzyme, pH 7.5, 25C
0.0059
-
MgATP2-
-
dNTP-free recombinant tetrameric enzyme, pH 7.5, 25C
0.9
-
MgATP2-
-
two active sites for ATP
0.00015
-
thymidine
-
pH 8.5, 30C
0.0002
-
thymidine
Herpes simplex virus
-
pH 7.2, wild-type
0.00023
-
thymidine
-
mutant enzyme P12N/H13I, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.00027
-
thymidine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.0003
-
thymidine
-
37C
0.0003
-
thymidine
-
pH 7.5, recombinant mutants V106A and V106G, in presence of ATP; pH 7.5, recombinant mutant V106H, in absence of ATP
0.0003
-
thymidine
P27158
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.00038
-
thymidine
Herpes simplex virus
-
37C, wild-type
0.0004
-
thymidine
-
pH 7.5, recombinant mutants V106L and V106G, in absence of ATP; pH 7.5, recombinant mutants V106L, V106H and V106T, in presence of ATP
0.00044
-
thymidine
-
wild type enzyme, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.0005
-
thymidine
-
pH 8
0.0005
-
thymidine
-
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.00054
-
thymidine
-
pH 8.0, 37C, recombinant wild-type enzyme
0.0006
-
thymidine
Herpes simplex virus
-
-
0.0006
-
thymidine
-
pH 7.5, recombinant mutant V106M, in absence or presence of ATP; pH 7.5, recombinant wild-type enzyme, in presence of ATP
0.0006
-
thymidine
Q9S750 and Q9FN47
subunit alpha, in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0006
-
thymidine
Q0H0H6
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0006
-
thymidine
G5EEZ5
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0006
-
thymidine
Q803Y1
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.00062
-
thymidine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
0.0007
-
thymidine
-
TK-A, below 0.004 mM deoxythymidine, 25C
0.0007
-
thymidine
-
pH 7.5, recombinant mutant V106K, in absence of ATP
0.0007
-
thymidine
Q9S750 and Q9FN47
subunit alpha, in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0007
-
thymidine
Q0H0H6
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0008
-
thymidine
-
pH 7.5, recombinant mutant V106Q, in absence or presence of ATP
0.0009
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, wild-type
0.0009
-
thymidine
-
pH 7.5, recombinant mutant V106I, in presence of ATP
0.0009
-
thymidine
Q9S750 and Q9FN47
subunit beta, in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication; subunit beta, in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0009
-
thymidine
G5EEZ5
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.00095
-
thymidine
Herpes simplex virus
-
37C, mutant SR11
0.001
-
thymidine
-
TK-C, below 0.004 mM deoxythymidine, 25C
0.0012
-
thymidine
-
pH 7.5, recombinant mutant V106K, in presence of ATP
0.0012
-
thymidine
-
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0013
-
thymidine
Herpes simplex virus
-
37C, mutant SR26
0.0013
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, wild-type
0.0013
-
thymidine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.0014
-
thymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.0014
-
thymidine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
0.0014
-
thymidine
Q803Y1
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0016
-
thymidine
Q5I0A2
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0017
-
thymidine
-
-
0.002
-
thymidine
C3VAL3
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0022
-
thymidine
-
pH 8, 37C
0.0023
-
thymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.0024
-
thymidine
-
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0025
-
thymidine
Herpes simplex virus
-
pH 7.2, Y101F mutant
0.0025
-
thymidine
C3VAL3
in the presence of 2.5 mM ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0026
-
thymidine
-
cytoplasmic enzyme, pH 7.5, 37C
0.0026
-
thymidine
-
mitochondrial enzyme, pH 7.5, 37C
0.00264
-
thymidine
Herpes simplex virus
-
37C, mutant SR39
0.003
-
thymidine
-
pH 7.4
0.003
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125N
0.0032
-
thymidine
-
-
0.0034
-
thymidine
Q9R088
mTK2 pH 7.6
0.0039
-
thymidine
-
-
0.0039
-
thymidine
-
thymidine kinase-2 mutant enzyme I59Y, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.0039
-
thymidine
-
mutant enzyme P12N, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.0041
-
thymidine
-
pH 8, 25C or 37C
0.0043
-
thymidine
-
wild type thymidine kinase-2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.0049
-
thymidine
Q9R088
mTK2-39 pH 7.6
0.0049
-
thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.005
0.0052
thymidine
-
mitochondrial enzyme, pH 7.5, 37C
0.005
-
thymidine
-
pH 7.4, 37C
0.0051
-
thymidine
-
thymidine kinase-2 mutant enzyme I59V, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.0056
-
thymidine
-
pH 8.0, 37C, Km is markedly dependent on pH
0.0056
-
thymidine
-
thymidine kinase-2 mutant enzyme I59L, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.0057
-
thymidine
-
H121N mutant, pH 7.6
0.00596
-
thymidine
-
pH 8.0, 37C, recombinant mutant S13D
0.006
-
thymidine
-
thymidine kinase-2 mutant enzyme I59H, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.007
-
thymidine
-
TK-A, above 0.004 mM deoxythymidine, 25C
0.0073
-
thymidine
Q9R088
mTK2-55 pH 7.6
0.0078
-
thymidine
-
full-length enzyme, at pH 7.8 and 37C
0.008
-
thymidine
-
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.009
-
thymidine
-
pH 7.8, 37C
0.01
-
thymidine
-
cytosolic enzyme, pH 7.5, 37C
0.01
-
thymidine
-
TK-C, above 0.004 mM deoxythymidine, 25C
0.01
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant C336Y
0.012
-
thymidine
-
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.0127
-
thymidine
-
pH 7.5, recombinant mutant V106A, in absence of ATP
0.013
-
thymidine
-
wild-type, pH 7.6
0.016
-
thymidine
-
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.017
-
thymidine
P27158
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.017
-
thymidine
Q5I0A2
in the absence of ATP, in 50 mM Tris/HCl (pH 8.0), 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, temperature not specified in the publication
0.018
-
thymidine
-
I212 mutant, pH 7.6
0.0188
-
thymidine
-
pH and temperature not specified in the publication
0.02
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125E
0.0271
-
thymidine
-
pH 7.5, recombinant wild-type enzyme, in absence of ATP
0.0294
-
thymidine
-
pH 7.5, recombinant mutant V106I, in absence of ATP
0.036
-
thymidine
-
mutant enzyme L124A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.037
-
thymidine
-
mutant enzyme H13I/Y127F, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.043
-
thymidine
-
pH 7.5, recombinant mutant V106T, in absence of ATP
0.046
-
thymidine
-
thymidine kinase domain 2, at pH 7.8 and 37C
0.048
-
thymidine
-
at pH 7.8 and 25C
0.057
-
thymidine
-
pH 7, 37C
0.059
-
thymidine
-
mutant enzyme T163S, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.074
-
thymidine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.263
-
thymidine
-
mutant enzyme P12N/H13I/Y127F, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.317
-
thymidine
-
mutant enzyme M28A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.336
-
thymidine
-
mutant enzyme L134A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.349
-
thymidine
-
mutant enzyme M28I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.565
-
thymidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.59
-
thymidine
-
mutant enzyme P12N/Y127F, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.612
-
thymidine
-
mutant enzyme H13I, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
6
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125D
0.022
-
trifluoromethylthymidine
-
at pH 7.8 and 25C
0.072
-
TTP
-
recombinant wild-type enzyme, pH 7.5, 37C
0.127
-
TTP
-
recombinant mutant T298S, pH 7.5, 37C
7.8
-
uridine
-
full-length enzyme, at pH 7.8 and 37C
0.26
-
UTP
-
pH 7.4, 37C
0.8
-
MgCl2
-
pH 8
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
-
-
additional information
-
additional information
-
kinetics
-
additional information
-
additional information
-
kinetics, ATP-binding kinetics of wild-type and mutant enzymes at room temperature
-
additional information
-
additional information
-
steady-state kinetics, kinetics of conformational changes induced by ligand binding
-
additional information
-
additional information
-
kinetics of wild-type and mutant enzymes in absence or presence of ATP, overview
-
additional information
-
additional information
-
-
-
TURNOVER NUMBER [1/s]
TURNOVER NUMBER MAXIMUM[1/s]
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.0253
-
(E)-5-(2-bromovinyl)-2'-deoxyuridine
Herpes simplex virus
-
determined by capillary electrophoresis method
0.2
-
2'-deoxythymidine
-
pH 8.0, 37C
6.47
-
2'-deoxythymidine
-
37C, pH 7.6
23
-
2'-deoxythymidine
-
37C, pH 7.6
220
-
2'-deoxythymidine
-
37C, pH 7.6
0.17
-
3'-azido-2',3'-dideoxythymidine
-
at pH 7.8 and 25C
0.009
-
3'-azido-3'-deoxythymidine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
0.13
-
3'-azido-3'-deoxythymidine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
0.24
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M28I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.34
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M28A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.53
-
3'-azido-3'-deoxythymidine
-
37C, pH 7.6
0.58
-
3'-azido-3'-deoxythymidine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.81
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.97
-
3'-azido-3'-deoxythymidine
-
37C, pH 7.6
1.3
-
3'-azido-3'-deoxythymidine
-
mutant enzyme T163S, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1.4
-
3'-azido-3'-deoxythymidine
-
mutant enzyme L124A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1.5
-
3'-azido-3'-deoxythymidine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
3.5
-
3'-azido-3'-deoxythymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
9.3
-
3'-azido-3'-deoxythymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
412
-
3'-azido-3'-deoxythymidine
-
37C, pH 7.6
0.47
-
3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.32
-
3-[1(2)-closo-1,7-carboranylbutyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.44
-
3-[1(2)-closo-1,7-carboranylethyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.35
-
3-[1(2)-closo-1,7-carboranylethyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.39
-
3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.37
-
3-[1(2)-closo-1,7-carboranylpropyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.45
-
3-[1(2)-propyltetrazol-5-ylmethyl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.34
-
3-[1(2)-propyltetrazol-5-yl]thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.24
-
5-fluoro-2'-deoxyuridine
-
at pH 7.8 and 25C
3.6
-
5-fluorodeoxyuridine
-
full-length enzyme, at pH 7.8 and 37C
0.238
-
aciclovir monophosphate
Herpes simplex virus
-
determined by capillary electrophoresis method
0.000283
-
acyclovir
Herpes simplex virus
-
37C, mutant SR26
0.000433
-
acyclovir
Herpes simplex virus
-
37C, mutant SR39
0.000467
-
acyclovir
Herpes simplex virus
-
37C, mutant SR11
0.015
-
acyclovir
Herpes simplex virus
-
37C, wild-type
0.28
-
ATP
-
at pH 7.8 and 25C
2
8
ATP
-
recombinant wild-type enzyme, pH 7.5, 37C
3.1
-
ATP
-
full-length enzyme, with 0.05 mM thymidine as cosubstrate, at pH 7.8 and 37C
3.9
-
ATP
-
thymidine kinase domain 2, with 0.05 mM thymidine as cosubstrate, at pH 7.8 and 37C
7
-
ATP
-
recombinant mutant K297R, pH 7.5, 37C
11
-
ATP
-
recombinant mutant G294A, pH 7.5, 37C
24
-
ATP
-
recombinant mutant T298S, pH 7.5, 37C
0.007
-
beta-L-thymidine
-
at pH 7.8 and 25C
9
-
CTP
-
recombinant mutant G294A, pH 7.5, 37C
13.5
-
CTP
-
about, recombinant mutant T298S, pH 7.5, 37C
14
-
CTP
-
recombinant mutant K297R, pH 7.5, 37C
19
-
CTP
-
recombinant wild-type enzyme, pH 7.5, 37C
0.047
-
deoxyadenosine
-
full-length enzyme, at pH 7.8 and 37C
0.17
-
Deoxycytidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1.4
-
Deoxycytidine
Herpes simplex virus
-
pH 7.6
0.34
-
deoxyguanosine
-
full-length enzyme, at pH 7.8 and 37C
0.8
-
Deoxyinosine
-
full-length enzyme, at pH 7.8 and 37C
0.045
-
Deoxyuridine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
0.53
-
Deoxyuridine
-
at pH 7.8 and 25C
1.3
-
Deoxyuridine
Herpes simplex virus
-
pH 7.6
1.5
-
Deoxyuridine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
5.1
-
Deoxyuridine
-
full-length enzyme, at pH 7.8 and 37C
5.3
-
Deoxyuridine
-
thymidine kinase domain 2, at pH 7.8 and 37C
0.0035
-
ganciclovir
Herpes simplex virus
-
37C, mutant SR39
0.0056
-
ganciclovir
Herpes simplex virus
-
37C, mutant SR11
0.0089
-
ganciclovir
Herpes simplex virus
-
37C, mutant SR26
0.04
-
ganciclovir
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125N
0.08
-
ganciclovir
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125E
0.1
-
ganciclovir
Herpes simplex virus
-
37C, wild-type
0.47
-
ganciclovir
Herpes simplex virus
-
pH 7.6, 37C, wild-type
0.0272
-
ganciclovir monophosphate
Herpes simplex virus
-
determined by capillary electrophoresis method
8
-
GTP
-
recombinant mutant G294A, pH 7.5, 37C
17
-
GTP
-
recombinant mutant T298S, pH 7.5, 37C
18.5
-
GTP
-
about, recombinant mutant K297R, pH 7.5, 37C
0.003
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125N
0.0062
-
thymidine
Herpes simplex virus
-
37C, mutant SR26
0.007
-
thymidine
Herpes simplex virus
-
37C, mutant SR11
0.017
-
thymidine
Herpes simplex virus
-
37C, mutant SR39
0.02
-
thymidine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
0.06
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, wild-type
0.11
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125D
0.13
-
thymidine
Herpes simplex virus
-
pH 7.6, 37C, mutant Q125E
0.28
-
thymidine
-
at pH 7.8 and 25C
0.46
-
thymidine
Herpes simplex virus
-
37C, wild-type
0.46
-
thymidine
-
in 25 mM Tris-HCl (pH 7.6), 5 mM MgCl2, 125 mM KCl, 10 mM dithiothreitol, and 0.5 mg/ml bovine serum albumin, at 37C
0.48
-
thymidine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
0.74
-
thymidine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
0.97
-
thymidine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1.4
-
thymidine
-
mutant enzyme M28A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1.5
-
thymidine
-
mutant enzyme M28I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1.8
-
thymidine
-
mutant enzyme L124A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
2.7
-
thymidine
-
mutant enzyme T163S, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
2.8
-
thymidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
3.1
-
thymidine
-
full-length enzyme, at pH 7.8 and 37C
3.5
-
thymidine
-
thymidine kinase domain 2, at pH 7.8 and 37C
4.9
-
thymidine
-
mutant enzyme L134A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
6.4
-
thymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
9.5
-
thymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
265.5
-
thymidine
-
pH 8.0, 37C, recombinant mutant S13D
282
-
thymidine
-
pH 8.0, 37C, recombinant wild-type enzyme
0.36
-
trifluoromethylthymidine
-
at pH 7.8 and 25C
7
-
TTP
-
recombinant mutant T298S, pH 7.5, 37C
11
-
TTP
-
recombinant wild-type enzyme, pH 7.5, 37C
1.5
-
uridine
-
full-length enzyme, at pH 7.8 and 37C
0.03
-
2',3'-didehydro-2',3'-dideoxythymidine
-
at pH 7.8 and 25C
additional information
-
2'-deoxythymidine
-
37C, pH 7.6
21
-
GTP
-
recombinant wild-type enzyme, pH 7.5, 37C
additional information
-
additional information
-
-
-
kcat/KM VALUE [1/mMs-1]
kcat/KM VALUE [1/mMs-1] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.064
-
2',3'-didehydro-2',3'-dideoxythymidine
-
at pH 7.8 and 25C
28913
5
-
3'-azido-2',3'-dideoxythymidine
-
at pH 7.8 and 25C
4954
0.0031
-
3'-azido-3'-deoxythymidine
-
mutant enzyme T163S, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
0.0067
-
3'-azido-3'-deoxythymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
0.078
-
3'-azido-3'-deoxythymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
0.35
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
0.44
-
3'-azido-3'-deoxythymidine
-
mutant enzyme L124A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
0.49
-
3'-azido-3'-deoxythymidine
-
mutant enzyme L134A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
0.94
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M28I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
1.4
-
3'-azido-3'-deoxythymidine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
1.7
-
3'-azido-3'-deoxythymidine
-
mutant enzyme M28A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
22
-
3'-azido-3'-deoxythymidine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
1185
48
-
3'-azido-3'-deoxythymidine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
1185
98
-
3'-azido-3'-deoxythymidine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
1185
5.8
-
5-fluoro-2'-deoxyuridine
-
at pH 7.8 and 25C
3318
120
-
5-fluorodeoxyuridine
-
full-length enzyme, at pH 7.8 and 37C
3977
2.3
-
ATP
-
at pH 7.8 and 25C
4
15
-
ATP
-
full-length enzyme, with 0.05 mM thymidine as cosubstrate, at pH 7.8 and 37C
4
40
-
ATP
-
thymidine kinase domain 2, with 0.05 mM thymidine as cosubstrate, at pH 7.8 and 37C
4
0.0024
-
beta-L-thymidine
-
at pH 7.8 and 25C
14484
0.0056
-
deoxyadenosine
-
full-length enzyme, at pH 7.8 and 37C
601
0.0019
-
Deoxycytidine
-
mutant enzyme L134A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
451
0.048
-
Deoxycytidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
451
0.0066
-
deoxyguanosine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
732
0.13
-
deoxyguanosine
-
full-length enzyme, at pH 7.8 and 37C
732
0.23
-
deoxyguanosine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
732
0.32
-
Deoxyinosine
-
full-length enzyme, at pH 7.8 and 37C
1104
4.5
-
Deoxyuridine
-
at pH 7.8 and 25C
1060
6.8
-
Deoxyuridine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
1060
12
-
Deoxyuridine
-
thymidine kinase domain 2, at pH 7.8 and 37C
1060
63
-
Deoxyuridine
-
full-length enzyme, at pH 7.8 and 37C
1060
150
-
Deoxyuridine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
1060
0.0028
-
thymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
0.0068
-
thymidine
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
0.46
-
thymidine
-
mutant enzyme T163S, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
0.51
-
thymidine
-
mutant enzyme L124A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
4.2
-
thymidine
-
mutant enzyme M28I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
4.5
-
thymidine
-
mutant enzyme M28A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
4.8
-
thymidine
-
at pH 7.8 and 25C
166
5
-
thymidine
-
mutant enzyme M42I, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
10
-
thymidine
-
mutant enzyme S182A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
14
-
thymidine
Q8LDP6, Q9FN47
isoform TK1b, pH and temperature not specified in the publication
166
15
-
thymidine
-
mutant enzyme L134A, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
76
-
thymidine
-
thymidine kinase domain 2, at pH 7.8 and 37C
166
400
-
thymidine
-
full-length enzyme, at pH 7.8 and 37C
166
750
-
thymidine
-
mutant enzyme S182T, in 50 mM Tris-HCl, pH 7.5, 10 mM dithiothreitol, 2.5 mM MgCl2, 0.5 mM CHAPS, 3 mM NaF, 0.5 mg/ml bovine serum albumin and 2.5 mM ATP, temperature not specified in the publication
166
770
-
thymidine
Q8LDP6, Q9FN47
isoform TK1a, pH and temperature not specified in the publication
166
6.4
-
trifluoromethylthymidine
-
at pH 7.8 and 25C
42444
0.19
-
uridine
-
full-length enzyme, at pH 7.8 and 37C
261
Ki VALUE [mM]
Ki VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.003
-
2'-deoxy-3'-aminothymidine
-
pH 7.8, 37C
0.011
-
2'-exo-methanocarba-thymidine
Herpes simplex virus
-
pH 7.2, wild-type
0.0515
-
2'-exo-methanocarba-thymidine
Herpes simplex virus
-
pH 7.2, Y101F mutant
0.0039
-
3'-azido-3'-deoxythmidine
-
pH and temperature not specified in the publication
-
0.0014
-
3'-deoxy-3'-fluorothymidine
-
pH and temperature not specified in the publication
-
0.0014
-
3'-fluorothymidine
-
pH and temperature not specified in the publication
-
1.7
-
3-N-methyl-5-iodo-2'-deoxyuridine
-
pH 7.8, 37C
3
-
5'-aminothymidine
-
pH 7.8, 37C
0.0104
-
5-(E)-(2-bromovinyl)uridine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.00013
-
5-bromodeoxyuridine
-
pH 8.5, 30C
0.0015
0.0055
5-bromodeoxyuridine
-
pH 7.5, 27C
0.00072
-
5-fluorodeoxyuridine
-
pH 8.5, 30C
0.022
-
5-fluorodeoxyuridine
-
pH 8, 37C
0.06
0.096
5-fluorodeoxyuridine
-
pH 7.5, 27C
0.001
0.0045
5-iododeoxyuridine
-
pH 7.5, 27C
0.3
-
acyclovir
Herpes simplex virus
-
pH 7.8, 37C
0.4
-
ADP
-
with ATP as variable substrate, pH 8, 37C
6.5
-
ADP
-
pH 7.4, 37C
3.8
-
ATP
-
pH 7, 37C
0.001
-
Be2+
-
pH 8, 37C
7.5
-
Caffeine
-
pH 7.8, 37C
0.00036
-
dCTP
-
H121N mutant, pH 7.6, competitive with thymidine as substrate
0.00079
-
dCTP
-
wild-type enzyme, pH 7.6, competitive with thymidine as substrate
0.00087
-
dCTP
-
wild-type enzyme, pH 7.6, competitive with deoxycytidine as substrate
0.00089
-
dCTP
-
H121N mutant, pH 7.6, competitive with deoxycytidine as substrate
0.002
-
dCTP
-
pH 7.5, 37C
0.004
-
Deoxycytidine
-
H121N mutant, pH 7.6, non-competitive with thymidine as substrate
0.04
-
Deoxycytidine
-
wild-type enzyme, pH 7.6, non-competitive with thymidine as substrate
0.63
-
Deoxycytidine
-
-
0.00146
-
Deoxyuridine
-
pH 8.5, 30C
0.11
-
Deoxyuridine
-
pH 8, 37C
0.27
1.54
Deoxyuridine
-
pH 7.5, 27C
0.5
0.65
dTDP
-
pH 7.5, 27C
0.65
-
dTMP
-
with ATP or thymidine as variable substrate, pH 8, 37C
3.6
4.7
dTMP
-
pH 7.5, 27C
0.0002
-
dTTP
-
variant TK-A, 25C
0.0006
-
dTTP
-
variant TK-C, 25C
0.00089
-
dTTP
-
H121N mutant, pH 7.6, competitive with thymidine as substrate
0.002
-
dTTP
-
wild-type enzyme, pH 7.6, competitive with thymidine as substrate
0.0025
-
dTTP
-
wild-type and H121N mutant, pH 7.6, non-competitive with deoxycytidine as substrate
0.006
-
dTTP
-
pH 7, 37C
0.01
-
dTTP
-
pH 7.5, 37C
0.014
0.036
dTTP
-
pH 7.5, 27C
0.014
-
iododeoxycytidine
Herpes simplex virus
-
pH 7.8, 37C
0.0036
-
thymidine
-
H121N mutant, pH 7.6, competitive with deoxycytidine as substrate
0.0049
-
thymidine
-
wild-type enzyme, pH 7.6, competitive with deoxycytidine as substrate
0.006
-
thymidine
-
-
0.63
-
TMP
-
pH 7.4, 37C
0.0085
-
TTP
-
competitive to ATP, pH 7.4, 37C
0.0135
-
TTP
-
competitive to thymidine, pH 7.4, 37C
2.5
-
Mg2+
-
pH 7, 37C
additional information
-
additional information
-
bisubstrate analogs with adenosine and thymidine joined at their 5' positions by polyphorphoryl linkages of varying lengths
-
additional information
-
additional information
-
-
-
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.028
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl 3,3-dimethylbutanoate
-
IC50: 0.028 mM
0.5
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl 3,3-dimethylbutanoate
-
IC50: above 0.5 mM
0.03
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl benzoate
-
IC50: 0.03 mM
0.5
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl benzoate
-
IC50: above 0.5 mM
0.0046
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl diphenylacetate
-
IC50: 0.0046 mM
0.281
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl diphenylacetate
-
IC50: 0.281 mM
0.019
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl dodecanoate
-
IC50: 0.019 mM
0.5
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl dodecanoate
-
IC50: above 0.5 mM
0.011
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl heptanoate
-
IC50: 0.011 mM
0.42
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl heptanoate
-
IC50: 0.42 mM
0.04
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl pivalate
-
IC50: 0.04 mM
0.5
-
(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl pivalate
-
IC50: above 0.5 mM
0.265
-
(4E)-N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: 0.265 mM
0.5
-
(4E)-N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: above 0.5 mM
0.371
-
(4E)-N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: 0.371 mM
0.5
-
(4E)-N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hex-4-enamide
-
IC50: above 0.5 mM
0.043
-
(E)-5-(2-bromovinyl)-1-beta-D-(arabinofuranosyl)uracil
-
-
0.5
-
1-(3'-deoxy-5'-O-triphenylmethyl-beta-D-thymidin-3'-yl)-3-(4-chloro-3-(trifluoromethyl)-phenyl)-thiourea
-
IC50 above 0.5 mM, thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.041
-
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
-
-
0.365
-
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
-
-
0.057
-
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
-
-
0.422
-
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
-
-
0.099
-
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
-
-
0.5
-
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
-
IC50 above 0.5 mM
0.285
-
1-beta-D-(arabinofuranosyl)thymine
-
-
0.18
-
1-[(2Z)-4-(4-benzylpiperazin-1-yl)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.18 mM
0.057
-
1-[(2Z)-4-(benzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.057 mM
0.022
-
1-[(2Z)-4-(benzyloxy)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.022 mM
0.5
-
1-[(2Z)-4-(benzyloxy)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: above 0.5 mM
0.0035
-
1-[(2Z)-4-(dibenzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0035 mM
0.5
-
1-[(2Z)-4-(dibenzylamino)but-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: above 0.5 mM
0.01
-
1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-5,6-dihydrothymine
-
IC50: 0.01 mM
0.5
-
1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-5,6-dihydrothymine
-
IC50: above 0.5 mM
0.173
-
1-[(2Z)-4-hydroxybut-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.173 mM
0.224
-
1-[(2Z)-4-hydroxybut-2-en-1-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.224 mM
0.0015
-
1-[(Z)-4-(triphenylmethoxy)-2-butenyl]thymine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.013
-
1-[2,3-dihydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.013 mM
0.017
-
1-[2,3-dihydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.017 mM
0.0012
-
1-[3-hydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0012 mM
0.0036
-
1-[3-hydroxy-4-(trityloxy)butyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0036 mM
0.00015
-
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
-
-
0.195
-
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
-
-
0.00042
-
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
-
-
0.335
-
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
-
-
0.038
-
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
-
-
0.472
-
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
-
-
0.405
-
1-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]-3-phenylthiourea
-
-
0.5
-
1-[[(2R,3S,5S)-3-hydroxy-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl]methyl]-3-phenylthiourea
-
IC50 above 0.5 mM
0.023
-
2-(4-chlorophenyl)-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.023 mM
0.198
-
2-(4-chlorophenyl)-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.198 mM
0.0041
-
2-biphenyl-4-yl-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.0041 mM
0.119
-
2-biphenyl-4-yl-N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]acetamide
-
IC50: 0.119 mM
0.0047
-
3'-(1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.06
-
3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.12
-
3'-(4-(2-phenyl-ethyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.053
-
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.211
-
3'-(4-(2-pyridine)-1,2,3-triazole-1-yl)-2'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.105
-
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.208
-
3'-(4-(3-chloro-propyl)-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.044
-
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.071
-
3'-(4-(4-fluorophenyl)-1,2,3-triazole-1-yl)-2'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.0003
-
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.073
-
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.078
-
3'-(4-benzyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.00023
-
3'-(4-butyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.0033
-
3'-(4-chlorobenzylamino)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.000036
-
3'-(4-chlorophenyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.000046
-
3'-(4-chlorophenyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.00015
-
3'-(4-cyclopentylmethyl-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.086
-
3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.15
-
3'-(4-pentyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.099
-
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.2
-
3'-(4-phenyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.189
-
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.311
-
3'-(4-propyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.114
-
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.318
-
3'-(4-tert-butyl-1,2,3-triazol-1-yl)-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
-
0.004
-
3'-(5-(4-chlorophenyl)-1,2,3-triazol-1-yl)-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.0012
-
3'-([[(4-chlorophenyl)carbamothioyl]amino]methyl)-3'-deoxythymidine
-
-
0.4
-
3'-([[(4-chlorophenyl)carbamothioyl]amino]methyl)-3'-deoxythymidine
-
-
0.000036
-
3'-([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)-2',3'-dideoxy-3,4-dihydrothymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
0.00015
-
3'-([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)-2',3'-dideoxy-3,4-dihydrothymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
0.003
-
3'-azido-3'-deoxythymidine
-
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
0.0125
-
3'-azido-3'-deoxythymidine
Q9PPP5, -
in 50 mM Tris/HCl pH 7.6, 5 mM MgCl2, at 37C
0.0046
-
3'-benzylamino-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.000042
-
3'-deoxy-3'-(4-(3,4-dichlorophenyl)-1,2,3-triazol-1-yl)-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.00025
-
3'-deoxy-3'-(4-phenyl-1,2,3-triazol-1-yl)-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.00032
-
3'-deoxy-3'-(4-phenyl-1,2,3-triazol-1-yl)-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.0013
-
3'-deoxy-3'-(4-pyridin-2-yl-1,2,3-triazol-1-yl)-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.0011
-
3'-deoxy-3'-(5-phenyl-1,2,3-triazol-1-yl)-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml bovine serum albumin, at 37C
-
0.00064
-
3'-deoxy-3'-([[(3,4-dichlorophenyl)carbamothioyl]amino]methyl)thymidine
-
-
0.087
-
3'-deoxy-3'-([[(3,4-dichlorophenyl)carbamothioyl]amino]methyl)thymidine
-
-
0.0031
-
3'-deoxy-3'-([[(4-methoxyphenyl)carbamothioyl]amino]methyl)thymidine
-
-
0.5
-
3'-deoxy-3'-([[(4-methoxyphenyl)carbamothioyl]amino]methyl)thymidine
-
IC50 above 0.5 mM
0.0012
-
3'-deoxy-3'-([[(4-methylphenyl)carbamothioyl]amino]methyl)thymidine
-
-
0.444
-
3'-deoxy-3'-([[(4-methylphenyl)carbamothioyl]amino]methyl)thymidine
-
-
0.018
-
3'-ethyl-5-methyl-2'-deoxyuridine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.0046
-
3'-spiro-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)-5-methyluridine
-
inhibits phosphorylation of 2'-deoxythymidine, IC50: 0.0046 mM
0.00033
-
3'-[(3-trifluoromethyl-4-chloro)-benzylamino]-3'-deoxy-beta-D-thymidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.00043
-
3'-[([[4-(benzyloxy)phenyl]carbamothioyl]amino)methyl]-3'-deoxythymidine
-
-
0.232
-
3'-[([[4-(benzyloxy)phenyl]carbamothioyl]amino)methyl]-3'-deoxythymidine
-
-
0.00047
-
3'-[([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)methyl]-3'-deoxythymidine
-
-
0.046
-
3'-[([[4-chloro-3-(trifluoromethyl)phenyl]carbamothioyl]amino)methyl]-3'-deoxythymidine
-
-
0.175
-
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylbutanamide
-
IC50: 0.175 mM
0.44
-
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylbutanamide
-
IC50: 0.44 mM
0.191
-
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-oxo-2-(tritylamino)ethyl]butanamide
-
IC50: 0.191 mM
0.194
-
4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-[2-oxo-2-(tritylamino)ethyl]butanamide
-
IC50: 0.194 mM
0.031
-
5'-deoxy-5'-[(tricyclo[3.3.1.13,7]dec-1-ylcarbamothioyl)amino]thymidine
-
-
0.392
-
5'-deoxy-5'-[(tricyclo[3.3.1.13,7]dec-1-ylcarbamothioyl)amino]thymidine
-
-
0.11
-
5'-deoxy-5'-[[(diphenylmethyl)carbamothioyl]amino]thymidine
-
-
0.5
-
5'-deoxy-5'-[[(diphenylmethyl)carbamothioyl]amino]thymidine
-
IC50 above 0.5 mM
0.468
-
5'-O-(4,4'-dimethoxytrityl)thymidine
-
IC50: 0.468 mM
0.000014
-
5-(3'-amino-3'-deoxy-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridin-3'Nyl)-1-(4-chloro-3-trifluoromethylphenyl)-tetrazole
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.000035
-
5-(3'-amino-3'-deoxy-beta-D-thymidin-3'N-yl)-1-(4-chloro-3-trifluoromethylphenyl)-tetrazole
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.0009
-
5-(3'-amino-3'-deoxy-beta-D-thymidin-3'N-yl)-1-benzyl-tetrazole
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.0013
-
5-(E)-(2-bromovinyl)-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.0013 mM
0.1
-
5-(E)-(2-bromovinyl)-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.1 mM
0.5
-
5-(E)-(2-bromovinyl)-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: above 0.5 mM
0.0026
-
5-aminobenzyl-(3'-deoxy-beta-D-thymidin-3'N-yl)-tetrazole
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.02
-
5-ethyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.02 mM
0.5
-
5-ethyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: above 0.5 mM
0.0046
-
5-iodo-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.0046 mM
0.048
-
5-iodo-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-uracil
-
IC50: 0.048 mM
0.001
-
5-iodo-2'-deoxyuridine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.003
-
5-methyl-1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.003 mM
0.025
-
5-methyl-1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.025 mM
0.491
-
5-methyl-1-[(2Z)-4-(4-methylpiperazin-1-yl)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.491 mM
0.0023
-
5-methyl-1-[(2Z)-4-(tritylamino)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0023 mM
0.5
-
5-methyl-1-[(2Z)-4-(tritylamino)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: above 0.5 mM
0.484
-
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-cytosine
-
IC50: 0.484 mM
0.5
-
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-cytosine
-
IC50: above 0.5 mM
0.0015
-
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0015 mM
0.045
-
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.045 mM
0.1
-
5-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: above 0.1 mM
0.0031
-
5-methyl-1-[4-(trityloxy)but-2-yn-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0031 mM
0.404
-
5-methyl-1-[4-(trityloxy)but-2-yn-1-yl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.404 mM
0.0033
-
5-methyl-1-[4-(trityloxy)butyl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.0033 mM
0.01
-
5-methyl-1-[4-(trityloxy)butyl]pyrimidine-2,4(1H,3H)-dione
-
IC50: 0.01 mM
0.0444
-
5-propyl-2'-deoxyuridine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.0006
-
5-trifluoromethyl-2-deoxyuridine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.0012
-
5-[(E)-2-bromoethenyl]-2'-O-decanoyluridine
-
competitive with respect to 2'-deoxythymidine, IC50: 0.0012 mM
0.00015
-
5-[(E)-2-bromoethenyl]-2'-O-octanoyluridine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
0.006
-
5-[(E)-2-bromoethenyl]-2'-O-octanoyluridine
-
IC50: 0.006 mM
0.0004
-
5-[amino-(4-chloro-3-trifluoromethylphenyl)]-1-(3'-deoxy-beta-(E)-5-(2-bromovinyl)-2'-deoxyuridin-3'N-yl)-tetrazole
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.00059
-
5-[amino-(4-chloro-3-trifluoromethylphenyl)]-1-(3'-deoxy-beta-D-thymidin-3'N-yl)-tetrazole
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.0034
-
6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylhexanamide
-
IC50: 0.0034 mM
0.019
-
6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-N-tritylhexanamide
-
IC50: 0.019 mM
0.015
-
6-methyluridine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.5
-
9-[(2Z)-4-(trityloxy)but-2-en-1-yl]-guanine
-
IC50: above 0.5 mM
0.017
-
alpha-D-5-ethyl-2'-deoxyuridine
-, Q6S4W2
-
0.035
-
alpha-L-thymidine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.0025
-
beta-D-5-ethyl-2'-deoxyuridine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.005
-
beta-L-thymidine
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
0.46
-
N-(2-cyanoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.46 mM
0.5
-
N-(2-cyanoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
0.353
-
N-(2-cyanoethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.353 mM
0.5
-
N-(2-cyanoethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: above 0.5 mM
0.318
-
N-(2-[[cyano(phenyl)methyl]amino]-2-oxoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.318 mM
0.5
-
N-(2-[[cyano(phenyl)methyl]amino]-2-oxoethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
0.0013
-
N-(3'-deoxy-beta-D-thymidin-3'-yl)-N'-(4-chloro-3-trifluoromethylphenyl)-benzylguanidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.00043
-
N-(3'-deoxy-beta-D-thymidin-3'-yl)-N'-(4-chloro-3-trifluoromethylphenyl)-guanidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.00058
-
N-(3'-deoxy-beta-D-thymidin-3'-yl)-N'-(4-chloro-3-trifluoromethylphenyl)-isopropylguanidine
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
-
0.268
-
N-(cyanomethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.268 mM
0.5
-
N-(cyanomethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: above 0.5 mM
0.238
-
N-(diphenylmethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.238 mM
0.5
-
N-(diphenylmethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
0.038
-
N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.038 mM
0.043
-
N-(diphenylmethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.043 mM
0.000046
-
N-methyl-4-[[[8-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)octyl]oxy](diphenyl)methyl]benzamide
-
thymidine kinase 2, in 50 mM Tris/HCl, pH 8.0, 2.5 mM MgCl2, 10 mM dithiothreitol, 0.5 mM CHAPS, 3 mg/ml obvine serum albumin, at 37C
0.027
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-2,2-diphenylacetamide
-
IC50: 0.027 mM
0.115
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-2,2-diphenylacetamide
-
IC50: 0.115 mM
0.028
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-3-(trifluoromethyl)benzamide
-
IC50: 0.028 mM
0.072
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-3-(trifluoromethyl)benzamide
-
IC50: 0.072 mM
0.033
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-9H-xanthene-9-carboxamide
-
IC50: 0.033 mM
0.131
-
N-[(2Z)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)but-2-en-1-yl]-9H-xanthene-9-carboxamide
-
IC50: 0.131 mM
0.287
-
N-[2-[(diphenylmethyl)amino]-2-oxoethyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.287 mM
0.5
-
N-[2-[(diphenylmethyl)amino]-2-oxoethyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: above 0.5 mM
0.208
-
N-[cyano(phenyl)methyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.208 mM
0.495
-
N-[cyano(phenyl)methyl]-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)butanamide
-
IC50: 0.495 mM
0.075
-
N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.075 mM
0.275
-
N-[cyano(phenyl)methyl]-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)hexanamide
-
IC50: 0.275 mM
0.5
-
N3-methyl-1-[(2Z)-4-(trityloxy)but-2-en-1-yl]-thymine
-
IC50: above 0.5 mM
0.01
-
penciclovir
-, Q6S4W2
at 37C for 20 min in 30 mM potassium phosphate, pH 8.0, 1.2 mM MgCl2
SPECIFIC ACTIVITY [µmol/min/mg]
SPECIFIC ACTIVITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
0.014
-
Herpes simplex virus
-
-
0.031
-
-
liver enzyme
0.053
-
-
-
0.089
-
Herpes simplex virus
-
-
0.094
-
-
placenta enzyme
0.124
0.183
-
-
0.13
-
Herpes simplex virus
-
-
0.46
-
Herpes simplex virus
-
-
3.6
-
-
-
7.5
-
-
-
325
-
-
-
additional information
-
-
-
additional information
-
-
-
additional information
-
-
-
additional information
-
-
-
additional information
-
-
-
additional information
-
-
activities of recombinant wild-type and mutant enzymes in dimeric or tetrameric form, i.e. in absence or presence of ATP, overview
pH OPTIMUM
pH MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
7
7.2
-
fetal liver
7
8.5
-
adult liver
7.4
7.8
-
mitochondrial enzyme
7.4
-
-
-
7.4
-
-
bimodal pH profile with a peak at pH 7.4 and a minor peak at pH 9.0
7.5
8.5
-
for phosphorylation of thymidine
7.5
-
-
TK-A and TK-C
7.5
-
-
assay at
7.5
-
-
assay at
7.5
-
-
assay at
7.5
-
-
assay at
7.5
-
-
assay at
7.6
7.8
-
cytoplasmic enzyme
8
-
-
assay at
8
-
-, Q6S4W2
exhibits best activity at pH 8.0 at an ATP concentration range between 0.2 and 4.0 mM
8.5
-
Herpes simplex virus
-
-
9
-
-
bimodal pH profile with a peak at pH 7.4 and a minor peak at pH 9.0
additional information
-
-
-
pH RANGE
pH RANGE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
5
10.2
-
less than 50% of maximal activity above and below
5
8
-
60% of maximal activity at pH 5.0, 50% of maximal activity at pH 8.0
6
10
Herpes simplex virus
-
enzyme is active between pH 6 and pH 10
7
9.5
-
less than 70% of maximal activity above and below
TEMPERATURE OPTIMUM
TEMPERATURE OPTIMUM MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
25
-
-
assay at
37
-
-
assay at
37
-
-
assay at
37
-
-
-
37
-
-
assay at
TEMPERATURE RANGE
TEMPERATURE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
25
37
-
highest activity within this temperature range at 37C
pI VALUE
pI VALUE MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
5.1
-
-
linear pH gradient
5.6
5.9
-
linear pH gradient in PAGE
6.3
6.8
-
variant TK-C
7.6
-
-
variant TK-B
7.8
-
-
variant TK-A
9.1
-
-
linear pH gradient between pH 7 and pH 11
SOURCE TISSUE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
SOURCE
Q8LDP6, Q9FN47
-
Manually annotated by BRENDA team
-
healthy and leucemic cells
Manually annotated by BRENDA team
additional information
-
enzyme is expressed during growth, but decreases in amount after starvation
Manually annotated by BRENDA team
additional information
-
expression in nonproliferating tissue
Manually annotated by BRENDA team
additional information
-
TK2 is constitutively expressed along the cell cycle and often is virtually the only thymidine kinase that is physiologically active in non-proliferating and resting cells
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
Clostridium acetobutylicum (strain ATCC 824 / DSM 792 / JCM 1419 / LMG 5710 / VKM B-1787)
Equine herpesvirus 4 (strain 1942)
Equine herpesvirus 4 (strain 1942)
Equine herpesvirus 4 (strain 1942)
Equine herpesvirus 4 (strain 1942)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Human herpesvirus 1 (strain 17)
Thermotoga maritima (strain ATCC 43589 / MSB8 / DSM 3109 / JCM 10099)
Thermotoga maritima (strain ATCC 43589 / MSB8 / DSM 3109 / JCM 10099)
Thermotoga maritima (strain ATCC 43589 / MSB8 / DSM 3109 / JCM 10099)
Thermotoga maritima (strain ATCC 43589 / MSB8 / DSM 3109 / JCM 10099)
Ureaplasma parvum serovar 3 (strain ATCC 700970)
Ureaplasma parvum serovar 3 (strain ATCC 700970)
Vaccinia virus (strain Ankara)
Varicella-zoster virus (strain Oka vaccine)
MOLECULAR WEIGHT
MOLECULAR WEIGHT MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
24840
-
-
calculated from amino acid sequence
25500
-
-
calculated from amino acid sequence
30000
-
Q9R088
gel filtration, two enzyme forms of MW 30000 and 60000
32000
-
Q9S750 and Q9FN47
for subunit alpha pre-incubated without ATP, two different peaks at 52000 and 32000 Da are obtained during gel filtration
37000
-
Herpes simplex virus
-
SDS-PAGE
38000
-
Q71F77
thymidine kinase 1 without ATP, gel filtration
43000
-
Q0H0H6
gel filtration
46000
-
-
gel filtration
48800
-
-
recombinant enzyme, gel filtration
49000
-
-
gel filtration
49000
-
Q9S750 and Q9FN47
subunit beta, gel filtration
50000
-
-
rLyTK1Val-106, gel filtration
50000
-
-
gel filtration, two enzyme forms of MW 50000 and 70000
50000
-
-
approximately, dimeric enzyme form
52000
-
Q9S750 and Q9FN47
for subunit alpha pre-incubated without ATP, two different peaks at 52000 and 32000 Da are obtained during gel filtration
54000
-
-
gel filtration
55000
-
P27158
gel filtration
57000
-
C3VAL3
gel filtration
57000
-
-
gel filtration
58000
-
-
gel filtration
59000
-
-
non-denaturing gel electrophoresis, two enzyme forms of MW 59000 and 80000
59000
-
Q71F77
thymidine kinase 1 with ATP, gel filtration
60000
-
Q9R088
gel filtration, two enzyme forms of MW 30000 and 60000
60000
-
-
isoform TK1, gel filtration
64000
-
Q5I0A2
for enzyme pre-incubated without ATP, two different peaks at 98000 and 64000 Da are obtained during gel filtration
68440
-
Murine gammaherpesvirus-68
Q83342
calculated form amino acid sequence
69000
-
-
sucrose density gradient centrifugation
70000
74000
-
mitochondria, glycerol gradient centrifugation
70000
74000
-
gel filtration
70000
74000
-
mitochondria, glycerol gradient centrifugation
70000
80000
Herpes simplex virus
-
gel filtration
70000
-
-
SDS-PAGE
70000
-
-
gel filtration, two enzyme forms of MW 50000 and 70000
70000
-
-
gel filtration
70400
80000
-
gel filtration
77100
80700
-
native PAGE
80000
85000
-
gel filtration
80000
-
-
non-denaturing gel electrophoresis, two enzyme forms of MW 59000 and 80000
80000
-
-
sucrose density gradient centrifugation
81000
-
-
sucrose density gradient centrifugation
82000
-
Q803Y1
gel filtration
84000
98000
-
calculation from Stokes' radius and sedimentation coefficient
84000
98000
-
cytoplasm, glycerol density gradient centrifugation
84000
98000
-
-
84000
98000
-
gel filtration
84000
98000
-
cytoplasm, glycerol density gradient centrifugation
86000
-
-
gel filtration
92000
-
-
gel filtration, sucrose density gradient centrifugation
98000
-
Q5I0A2
for enzyme pre-incubated without ATP, two different peaks at 98000 and 64000 Da are obtained during gel filtration
100000
-
-
rLyTK1Met-106, gel filtration
100000
-
-
recombinant enzyme, gel filtration
100000
-
-
approximately, tetrameric enzyme form
130000
-
G5EEZ5
gel filtration
340000
-
-
oligomeric form, gel filtration
additional information
-
-
oligomeric states have MWs of 152200 and 95900, as determined by gel filtration
SUBUNITS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
?
-
x * 28000, SDS-PAGE
?
-
x * 21200, calculated from sequence of cDNA
?
-
x * 26000, SDS-PAGE
?
-
x * 25494, recombinant enzyme, amino acid sequence calculation
?
-
x * 24000, about, SDS-PAGE
?
Herpes simplex virus type 4
-
x * 38800, about, recombinant full length enzyme, amino acid sequence calculation, x * 36500, about, recombinant truncated enzyme, amino acid sequence calculation
?
Q8LDP6, Q9FN47
x * 26100, isoform TK1a, calculated from amino acid sequence; x * 30700, isoform TK1b, calculated from amino acid sequence
?
-
x * 42192, calculated from amino acid sequence; x * 43000, SDS-PAGE
?
Human herpesvirus 1 L2
-
x * 42192, calculated from amino acid sequence; x * 43000, SDS-PAGE
-
dimer
-
2 * 30000, SDS-PAGE
dimer
-
2 * 26000, SDS-PAGE
dimer
-
2 * 24000, cytosol, SDS-PAGE
dimer
Herpes simplex virus
-
2 * 42000, SDS-PAGE
dimer
-
2 * 44000, SDS-PAGE in presence of 2-mercaptoethanol
dimer
-
2 * 48000, SDS-PAGE
dimer
-
2 * 46000-49000, SDS-PAGE
dimer
-
homodimer
dimer
-
2 * 25000, rLyTK1Val-106
dimer
Q9R088
-
dimer
-
2 * 50000, the enzyme exists as a dimer and as a tetramer
dimer
-
enzyme appears as dimer and tetramer
dimer
-
the most abundant enzyme form, less active than the tetramer
dimer
-
the truncated, dimeric enzyme form is fully active
heterotetramer
Q9S750 and Q9FN47
2 * 26000 + 2 * 30700, calculated from amino acid sequence
homodimer
Q0H0H6
2 * 21700, calculated from amino acid sequence
homodimer
-
2 * 25400, calculated from amino acid sequence
homodimer
-
2 * 25000, isoform TK1, SDS-PAGE; 2 * 25500, isoform TK1, calculated from amino acid sequence
homodimer
Q71F77
2 * 25600, calculated from amino acid sequence
homotetramer
C3VAL3
4 * 25600, calculated from amino acid sequence
homotetramer
G5EEZ5
4 * 29700, calculated from amino acid sequence
homotetramer
Q803Y1
4 * 25600, calculated from amino acid sequence
homotetramer
-
4 * 24800, calculated from amino acid sequence
homotetramer
-
4 * 25400, calculated from amino acid sequence
homotetramer
P27158
4 * 25700, calculated from amino acid sequence
homotetramer
Q5I0A2
4 * 26300, calculated from amino acid sequence
monomer
Trypanosoma brucei TC221
-
-
-
tetramer
-
4 * 25000, rLyTK1Met-106
tetramer
-
4 * 50000, the enzyme exists as a dimer and as a tetramer
tetramer
-
enzyme appears as dimer and tetramer
tetramer
-
less abundant form, more active than the dimer
tetramer
-
subunit arrangement of the tetrameric enzyme, enzyme contains a zinc finger domain at residues 150-191
tetramer
-
each subunit contains an alpha/beta-domain, and a domain with a structural zinc ion
trimer
-
3 * 23300, calculated from amino acid sequence
monomer or dimer
-
isoform TK2
additional information
-
binding of ATP induces enzyme tetramerization, which may lead to activation of the enzyme, the dimeric enzyme form is probably less active
additional information
-
enzyme contains a calmodulin binding domain
additional information
-
structure modeling
additional information
-
ligand-induced conformational changes in dimeric and tetrameric forms of the enzyme
additional information
-
oligomerization patterns of wild-type and mutant enzymes, binding of ATP induces reversible transition from a dimer with low catalytic activity to a tetramer with high catalytic activity, Val106 is involved
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
phosphoprotein
-
phosphorylation at Ser13 has regulatory function
Crystallization/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
-
Herpes simplex virus
-
complexed with acyclovir and pencyclovir
Herpes simplex virus
-
complexed with an adenine analogue
Herpes simplex virus
-
complexed with deoxythymidine and ganciclovir
Herpes simplex virus
-
hanging drop vapor diffusion method
Herpes simplex virus
-
sitting and hanging drop vapor diffusion method
Herpes simplex virus
-
full length and truncated enzyme in complex with thymidine and ADP, or with thymidine, sulfate, and a bisubstrate analogues, or with TP4A, or with TP5A, hanging drop vapour diffusion method, reservoir solution containing 0.1 M MES, pH 6.5, 1.2 M ammonium sulfate, and 3 or 5% dioxane, dependent on the complex ligand, mixed with enzyme solution containing 5.5 mg/ml protein, 1.0 mM TMP, 2.0 mM ADP, 25 mM HEPES, pH 7.0, 5 mM MgSO4, 5 mM DTT, 100 mM KCl, and 5% glycerol, at equal volumes of 0.001 ml on a glass cover slide, X-ray diffraction structure determination and analysis at 2.0-3.0 A resolution, molecular replacement method
Herpes simplex virus type 4
-
mutant enzyme T163S, hanging drop vapor diffusion method, using 0.1 M sodium citrate (pH 5.6), 20% (v/v) 2-propanol and 17% (w/v) polyethylene glycol 4000
-
purified recombinant C-terminally truncated enzyme in complex with inhibitor dTTP, hanging drop vapour diffusion method, 7-13 mg/ml protein in solution with 5 mM dTTP mixed with an equal volume of crystallization solution containing 0.1 M Na-citrate, pH 5.6, 20% 2-propanol, and 14-16% PEG 4000, 15C, X-ray diffraction structure determination and analysis at 2.4-3.5 A resolution
-
purified recombinant truncated enzyme comprising residues 15-194 of the wild-type enzyme without His-tag, hanging drop vapour diffusion method, 7 mg/ml protein in 5 mM Tris-HCl, pH 7.2, 10 mM NaCl, and 10 mM DTT, mixed at equal volumes with crystallization buffer containing 0.095 mM tri-sodium citrate, pH 5.5, 12% PEG 4000, 10% isopropanol, 23C, equilibration against a reservoir of 0.5 ml crystallization buffer, 3 days, X-ray diffraction structure determination and analysis at 1.7 A resolution
-
purified recombinant GST-tagged enzyme complexed with ADP and E-5-(2-bromovinyl)-2'-deoxythymidine, sitting drop vapour diffusion method, 21C, mixing of 0.001 ml of enzyme and reservoir solution, the enzyme solution contains 8 mg/ml protein, 0.4 mM ADP, 0.2 mM E-5-(2-bromovinyl)-2'-deoxythymidine, and 0.6 mM MgCl2, reservoir solution contains 0.1 M sodium acetate, at either pH 4.5 or 5.0, and 6-11% w/v PEG 20000, X-ray diffraction structure determination and analysis at 3.2 A resolution, molecular replacement method
-
purified recombinant wild-type and selenomethionine-labeled enzyme in complex with inhibitor dTTP, hanging drop vapour diffusion method, 8 mg/ml protein in solution with 5 mM dTTp mixed with an equal volume of reservoir solution containing 19% PEG 2000, 0.2 M LiCl, 5 mM DTT, and 0.1 M MES, pH 6.0, 15C, X-ray diffraction structure determination and analysis at 2.5 or 3.0 A resolution, respectively
-
pH STABILITY
pH STABILITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
6.5
-
-
best value for stability
TEMPERATURE STABILITY
TEMPERATURE STABILITY MAXIMUM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
15
-
-
rLyTK1Met-106: 50% loss of activity within 41 min, rLyTK1Val-106: 50% loss of activity after 392 min
20
-
-
deletion of the 20 C-terminal amino acids decreases half-life at 20C from 83 min for wild-type enzyme to 78 min, deletion of the 40 C-terninal amino acids increases half-life to 335 min, deletion of the 44 C-terminal amino acids increases half-life to 500 min
25
40
-
40 min stable
25
-
-
enzyme TK-A and TK-C: half-life 25 h
25
-
-
50% loss of activity within 4 min, rLyTK1Met-106
27
43
Herpes simplex virus
-
stable
37
-
-
20% loss of activity in the presence of bovine serum albumin, thymidine and dithiothreitol after 60 min, almost complete loss of activity witout bovine serum albumin, thymidine and dithiothreitol after 60 min
40
-
Herpes simplex virus
-
the half-life of 3 min increases to 6 min in presence of 2 mM ATP or to 30 min in presence of 0.12 mM thymidine
40
-
-
enzyme TK-A: half-life 8 h, enzyme TK-C: half-life 30 min
40
-
-
no activity after 2,5 h
45
-
Herpes simplex virus
-
half-life 28 min, Herpes simplex virus type 2: half-life 120 min
45
-
-
5 min, fetal liver: 50% loss of activity, adult liver: 10% loss of activity
50
-
-
quick inactivation above, dTTP protects against thermal inactivation
additional information
-
Herpes simplex virus
-
2-mercaptoethanol protects against thermal inactivation
additional information
-
-
ATP, thymidine, Mg2+ protect against thermal inactivation
additional information
-
-
irreversible thermal denaturation following a two-state irrversible denaturation model, study with ligand-bound and free enzyme, respectively, overview
GENERAL STABILITY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
dTTP protects against thermal inactivation
-
2-mercaptoethanol protects against thermal inactivation
Herpes simplex virus
-
ATP or thymidine stabilizes, type I more stable in the presence of MgATP2- than type II
Herpes simplex virus
-
binding of dNTP inhibitors and substrates, i.e. 2'-deoxycytidine, Mg-2'-deoxyCTP, 2'-deoxythymidine, and Mg-2'-deoxyTTP structurally stabilizes the enzyme, ligand-bound enzyme is less susceptible to aggregation, proteolysis by trypsin, and thermal denaturation
-
bovine serum albumin, 0.5 mg/ml stabilizes
-
digitonin stabilizes
-
dithiothreitol essential for stability
-
not stabilized by 10% glycerol, 5 mM 2-mercaptoethanol, 5 mM EDTA, 1 mg/ml bovine serum albumin
-
stable in the presence of ATP, bovine serum albumin and CHAPS
-
dithiothreitol, ATP and other nucleosides stabilize
-
stability decreases with increasing purity, ATP, thymidine, Mg2+ protect
-
dithiothreitol, 5 mM stabilizes
-
STORAGE STABILITY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
-20C, 50 mM Tris-HCl buffer, pH 8.0, 10 mM 2-mercaptoethanol, 20% glycerol, 100 mM KCl, 6 months, 20% loss of activity
-
-70C, 10 mM 2-mercaptoethanol, 0.5 mg/ml bovine serum albumin, several months
-
0C, 2-3 months, change of kinetic properties, larger amount of ATP is required to get the same rate of reaction
-
-70C, 0.2 mM deoxythymidine, 3 mM dithiothreitol, 10% glycerol
Herpes simplex virus
-
-20C, 50% glycerol, relatively stable
-
-20C, or 4C, 24 h, more than 50% loss of activity
-
-80C, 2 weeks, no loss of activity in presence of digitonin
-
-20C, enzyme in buffer containing 250 mM imidazole, several months, without noticeable loss of activity
-
4C, enzyme in buffer containing 250 mM imidazole, 1 week, 50% loss of activity
-
-70C, stable for several months
-
-20C, 0.1 mM thymidine, 1 week, 30% loss of activity
-
4C, MTK1-39 and mTK2-55 are stable for up to 3 weeks, mTK2 is less stable
Q9R088
Purification/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
-
Q8LDP6, Q9FN47
3'-aminothymidine-Sepharose resin column chromatography and HisTrap column chromatography
-
recombinant enzyme partially utilizing calmodulin-agarose-beads
-
Ni-NTA column chromatography
-, Q6S4W2
Escherichia coli infected with bacteriophage
-
partial
-
-
Herpes simplex virus
-
expressed in Escherichia coli
Herpes simplex virus
-
HeLa TK- cells infected with virus
Herpes simplex virus
-
wild-type and 3 mutants, homogeneity
Herpes simplex virus
-
wild-type and A167Y mutant
Herpes simplex virus
-
recombinant His-tagged, thrombin-cleavable full length or truncated enzyme from Escherichia coli strain BL21 C41 (DE3) by nickel affinity chromatography, cleavage by thrombin
Herpes simplex virus type 4
-
glutathione-Sepharose column chromatography
-
GST affinity column chromatography
-
partial; rLyTK1Val-106 and rLyTK1Met-106
-
recombinant enzyme as maltose binding fusion protein from Escherichia coli
-
recombinant GST-tagged wild-type and mutant enzymes from Escherichia coli by GST affinity chromatography, cleaving of the tag
-
recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain B834(DE3) by nickel affinity chromatography
-
Ni-NTA column chromatography and HiTrap Q column chromatography
-
recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography
-
expressed in Escherichia coli, homogeneity
-
recombinant GST-tagged enzyme from Escherichia coli strain BL21 by glutathione affinity chromatography
-
recombinant His-tagged wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) are immobilized on nickel beads and purified
-
wild type and a truncated form missing 243 N-terminal amino acids
-
18000fold, 2 different forms
-
3 forms
Q9R088
3 variants TK-A, TK-B, TK-C
-
DEAE-Sephadex gel filtration
-
homogeneity
-
Ni-NTA agarose column chromatography
-
recombinantly expressed as a His-tag fusion enzyme in Escherichia coli
-
Cloned/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
expressed in Escherichia coli BL21(DE3) cells
C3VAL3
expressed in Escherichia coli BL21(DE3) cells
Q9S750 and Q9FN47
expressed in Escherichia coli KY895 cells
Q8LDP6, Q9FN47
expressed in Escherichia coli BL21(DE3) cells
Q0H0H6
expressed in Escherichia coli BL21 cells
-
expressed in Escherichia coli BL21(DE3) cells
G5EEZ5
expression in Escherichia coli as poly-histidine fusion protein in the pET-16b vector
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli BL21(DE3) cells
Q803Y1
expressed in Escherichia coli BL21(DE3) cells
-
gene thyB, DNA and amino acid sequence determination and analysis, phage display, location on chromosome 5, 3 exons, 2 introns, expression in Escherichia coli strain BL21
-
expressed in Escherichia coli
-, Q6S4W2
expression in Escherichia coli as poly-histidine fusion protein in the pET-16b vector
-
expressed in Escherichia coli BL21(DE3) cells
-
-
Herpes simplex virus
-
glutathione S-transferase fusion protein
Herpes simplex virus
-
expression of the His-tagged, thrombin-cleavable full length or truncated enzyme in Escherichia coli strain BL21 C41 (DE3)
Herpes simplex virus type 4
-
DNA and amino acid sequence determination, expression in Escherichia coli as maltose binding fusion protein in inclusion bodies, coexpression of GroEL/ES molecular chaperone system and 3% v/v ethanol supplementation
-
DNA and amino acid sequence determination, expression in Escherichia coli as maltose binding fusion protein in inclusion bodies, coexpression of GroEL/ES molecular chaperone system improves enzyme solubility only marginally, but ethanol supplementation contributes to enzyme recovery due to activation of heat shock response
-
expressed in Escherichia coli
-
expressed in Escherichia coli BL21 cells
-
expressed in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli BL21(DE3)pLysS cells
-
expressed in Escherichia coli Rosetta(DE3) cells as a fusion protein to glutathione transferase
-
expression in Escherichia coli
-
expression in Escherichia coli; expression in Escherichia coli
-
expression of C-terminally truncated enzyme lacking 41 amino acid residues
-
expression of wild-type and Val106 mutants in an enzyme-deficient Escherichia coli strain as GST-fusion proteins
-
N-terminal thrombin-cleavable His6-tagged enzyme, missing 14 amino acids of the N-terminus and 40 amino acids of the C-terminus, in Escherichia coli
-
overexpression of His-tagged wild-type and mutant enzymes in Escherichia coli strain B834(DE3), transient expression as Flag-tagged enzyme in LM-tk- cells
-
expressed in Escherichia coli ER2566 cells
-
expression in Escherichia coli
-
expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3)
-
expression as GST-tagged enzyme in Escherichia coli strain BL21
-
PreScission-cleavable glutathione S-transferase fusion protein
-
expression of His-tagged wild-type and mutant enzymes in Escherichia coli strain BL21(DE3)
-
glutathione S-transferase fusion protein
-
-
Murine gammaherpesvirus-68
Q83342
expressed in Escherichia coli BL21(DE3) cells
P27158
expressed in Escherichia coli KY895 cells
Q71F77
expressed in Escherichia coli BL21-CodonPlus (DE3) cells
-
gene tdk, expression in Escherichia coli as wild-type and selenomethionine-labeled enzymes
-
expression in Escherichia coli as poly-histidine fusion protein in the pET-16b vector
-
expressed in Escherichia coli BL21(DE3) cells
Q5I0A2
EXPRESSION
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
0.001 mM of the mitogenic extracellular kinase 1/2 inhibitor PD0325901 rapidly decreases thymidine kinase 1 protein levels and mRNA expression in SKMEL-28 human melanoma cells with maximum reduction at 48 h posttreatment
-
DNA damage causes up-regulation of thymidine kinase 1 in tumor cells
-
ENGINEERING
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
L143A
-
the mutant shows reduced catalytic efficiency with thymidine compared to the wild type enzyme and exhibits activity towards deoxyguanosine
M42I
-
the mutation has a negative impact on enzyme activity with thymidine as the substrate, affecting both the Km (250fold increase) and the kcat (2fold increase) values
S182A
-
the mutant shows reduced catalytic efficiency with thymidine compared to the wild type enzyme and exhibits activity towards deoxyguanosine
S182T
-
the mutant shows reduced catalytic efficiency with thymidine compared to the wild type enzyme and exhibits activity towards deoxyguanosine
A167Y
Herpes simplex virus
-
heavily reduced ability to phosphorylate pyrimidine nucleosides, ability to phosphorylate ganciclovir and lobucavir is reduced 2fold
C336Y
Herpes simplex virus
-
acyclovir resistant, mutation affects ATP binding site
Q125D
Herpes simplex virus
-
increased Km for thymidine
Q125E
Herpes simplex virus
-
increased Km for thymidine
Q125N
Herpes simplex virus
-
binding mode of thymidine or polypeptide backbone conformation is not altered
Q125N
Herpes simplex virus
-
increased Km for thymidine and ganciclovir
Y101F
Herpes simplex virus
-
12fold increased Km for thymidine
H121N
-
similar subunit structure to wild-type enzyme, decreased enzyme activity
I212N
-
similar subunit structure to wild-type enzyme, less than 1% activity compared to wild-type
I59H
-
the mutant shows imcreased Km compared to the wild type enzyme
I59L
-
the mutant shows imcreased Km compared to the wild type enzyme
I59V
-
the mutant shows imcreased Km compared to the wild type enzyme
I59Y
-
the mutant shows decreased Km compared to the wild type enzyme
L124A
-
the mutant shows reduced catalytic efficiency compared to the wild type enzyme
M28A
-
the mutant shows reduced catalytic efficiency compared to the wild type enzyme
S13D
-
site-directed mutagenesis, ATP-induced tetramerization is perturbed, mutant is less activated by ATP and shows reduced activity compared to the wild-type enzyme
T163S
-
the mutation results in a kinase with a 140fold lower Km for 3-azido-3-deoxythymidine
V106A
-
site-directed mutagenesis, mutant is similar to the wild-type enzyme in size, conformation and polarity, unaltered activity and oligomerization pattern
V106G
-
site-directed mutagenesis, mutant differs in size, conformation and polarity from the wild-type enzyme, reduced activity, permanent tetrameric form irrespective of the presence of ATP
V106H
-
site-directed mutagenesis, mutant differs in size, conformation and polarity from the wild-type enzyme, reduced activity, permanent tetrameric form irrespective of the presence of ATP
V106I
-
site-directed mutagenesis, mutant is similar to the wild-type enzyme in size, conformation and polarity, unaltered activity and oligomerization pattern
V106K
-
site-directed mutagenesis, mutant differs in size, conformation and polarity from the wild-type enzyme, reduced activity, permanent tetrameric form irrespective of the presence of ATP
V106L
-
site-directed mutagenesis, mutant differs in size, conformation and polarity from the wild-type enzyme, reduced activity, permanent tetrameric form irrespective of the presence of ATP
V106M
-
results in tetrameric structure with high thymidine affinity
V106M
-
site-directed mutagenesis, mutant differs in size, conformation and polarity from the wild-type enzyme, reduced activity, permanent tetrameric form irrespective of the presence of ATP
V106Q
-
site-directed mutagenesis, mutant differs in size, conformation and polarity from the wild-type enzyme, reduced activity, permanent tetrameric form irrespective of the presence of ATP
V106T
-
site-directed mutagenesis, mutant is similar to the wild-type enzyme in size, conformation and polarity, unaltered activity and oligomerization pattern
A175V
-
site-sirected mutagenesis, inactive mutant, mutation of residue 51 might in vivo be involved into generation of acyclovir resistance of HSV
D77N
-
site-sirected mutagenesis, mutant activity is slightly increased compared to the wild-type enzyme
E83K
-
site-sirected mutagenesis, inactive mutant, mutation of residue 51 might in vivo be involved into generation of acyclovir resistance of HSV
H13I
-
the mutant shows strongly increased Km compared to the wild type enzyme
P12N
-
the mutant shows increased Km compared to the wild type enzyme
P12N/H13I
-
the mutant shows decreased Km compared to the wild type enzyme
P12N/H13I/Y127F
-
the mutant shows strongly increased Km compared to the wild type enzyme
P12N/Y127F
-
the mutant shows strongly increased Km compared to the wild type enzyme
R51W
-
site-sirected mutagenesis, inactive mutant, mutation of residue 51 might in vivo be involved into generation of acyclovir resistance of HSV
G294A
-
site-directed mutagenesis, about 80% reduced activity compared to the wild-type enzyme, no activity with TTP as cofactor
G294V
-
site-directed mutagenesis, nearly inactive mutant, no ATP binding
K297E
-
site-directed mutagenesis, nearly inactive mutant, no ATP binding
K297Q
-
site-directed mutagenesis, nearly inactive mutant, no ATP binding
K297R
-
site-directed mutagenesis, about 90% reduced activity compared to the wild-type enzyme, prefers GTP as cofactor, no activity with TTP as cofactor
T298A
-
site-directed mutagenesis, about 90% reduced activity compared to the wild-type enzyme
T298S
-
site-directed mutagenesis, about 20% reduced activity compared to the wild-type enzyme
H121N
-
the mutant has less than 7% kinase activity compared to the wild type enzyme
M28I
-
the mutation has a negative impact on enzyme activity with thymidine as the substrate, affecting both the Km (250fold increase) and the kcat (6fold increase) values. The mutant has no activity with deoxycytidine
additional information
-
deletion of the 20 C-terminal amino acids decreases half-life at 20C from 83 min for wild-type enzyme to 78 min, deletion of the 40 C-terninal amino acids increases half-life to 335 min, deletion of the 44 C-terminal amino acids increases half-life to 500 min
H13I/Y127F
-
the mutant shows increased Km compared to the wild type enzyme
additional information
Q9QNF7
the mutant HSV-1-thymidine kinase with a deletion of the first 45 amino acid residues is phenotypically the same as that of wild-type HSV-1-thymidine kinase in terms of the phosphorylation activity of thymidine kinase-associated anti-herpes virus drugs
Renatured/COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
coexpression of GroEL/ES molecular chaperone system improves recombinant enzyme solubility from inclusion bodies only marginally, but ethanol supplementation contributes to enzyme recovery due to activation of heat shock response
-
APPLICATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
medicine
-
enzyme can be useful in gene therapy
medicine
-
the serum levels of thymidine kinase do not correlate with prognosis in a group of patients during the time of the initial diagnosis of acute leukemia. The entry levels of thymidine kinase are not suitable for stratification of child patients with acute leukemia into risk categories
synthesis
-
enzyme can be useful in drug design
medicine
-
Hsv1-tk mutants are present in multiple ganglia of an immunocompromised patient with a history of chronic Acv(r) skin lesions. Mutations in the thymidine kinase gene of herpes simplex virus type 1 explain in most cases of the virus resistance to acyclvir treatment. Mutants arise independently under drug selection and establish latency in human sensory ganglia alone or together with the wild-type virus
medicine
-
enzyme is a target for antiviral therapy and treatment of EBV-associated malignancies
medicine
-
potential efficacy of the adenovirus-thymidine kinase/ganciclovir gene therapy approach as a viable nonsurgical alternative treatment for uterine leiomyomas
molecular biology
-
a method to distinguish between the de novo induction of thymidine kinase mutants and the selection of pre-existing thymidine kinase mutants in the mouse lymphoma assay
medicine
Q71F77
the thymidine kinase 1 gene from tomato in combination with azidothymidine is a powerful suicide gene for anticancer gene therapy
medicine
-
enzyme can be useful in gene therapy
synthesis
-
enzyme can be useful in drug design