BRENDA - Enzyme Database show

Novel potent inhibitors of deoxycytidine kinase identified and compared by multiple assays

Yu, X.C.; Miranda, M.; Liu, Z.; Patel, S.; Nguyen, N.; Carson, K.; Liu, Q.; Swaffield, J.C.; J. Biomol. Screen. 15, 72-79 (2010)

Data extracted from this reference:

Cloned(Commentary)
EC Number
Commentary
Organism
2.7.1.74
expressed in Escherichia coli BL21(DE3) cells
Homo sapiens
Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.1.74
LP-375752
i.e. 2-[4-(6-benzo[b]thiophen-2-yl-pyrimidin-4-yl)-piperazin-1-yl]-1-pyrrolidin-1-yl-ethanone
Homo sapiens
2.7.1.74
LP-503392
i.e. 2-thio-2'-deoxycytidine
Homo sapiens
KM Value [mM]
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.1.74
0.001
-
2'-deoxycytidine
-
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.7.1.74
additional information
Homo sapiens
dCK phosphorylates all three natural deoxyribonucleosides, exhibiting the highest affinity for 2'-deoxycytidine
?
-
-
-
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
2.7.1.74
Homo sapiens
-
-
-
Purification (Commentary)
EC Number
Commentary
Organism
2.7.1.74
-
Homo sapiens
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.1.74
ATP + 1-beta-D-arabinosylcytosine
-
704730
Homo sapiens
ADP + 1-beta-D-arabinosylcytosine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + 2'-deoxyadenosine
-
704730
Homo sapiens
ADP + 2'-deoxyadenosine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + 2'-deoxycytidine
-
704730
Homo sapiens
ADP + 2'-deoxycytidine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + 2'-deoxyguanosine
-
704730
Homo sapiens
ADP + 2'-deoxyguanosine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + cladribine
-
704730
Homo sapiens
ADP + cladribine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + fludarabine
-
704730
Homo sapiens
ADP + fludarabine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + gemcitabine
-
704730
Homo sapiens
ADP + gemcitabine 5'-phosphate
-
-
-
?
2.7.1.74
additional information
dCK phosphorylates all three natural deoxyribonucleosides, exhibiting the highest affinity for 2'-deoxycytidine
704730
Homo sapiens
?
-
-
-
-
Cofactor
EC Number
Cofactor
Commentary
Organism
Structure
2.7.1.74
ATP
-
Homo sapiens
IC50 Value
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.7.1.74
0.00091
-
in 50 mM Tris (pH 7.6)
Homo sapiens
LP-503392
2.7.1.74
0.0138
-
in 50 mM Tris (pH 7.6)
Homo sapiens
LP-375752
Cloned(Commentary) (protein specific)
EC Number
Commentary
Organism
2.7.1.74
expressed in Escherichia coli BL21(DE3) cells
Homo sapiens
Cofactor (protein specific)
EC Number
Cofactor
Commentary
Organism
Structure
2.7.1.74
ATP
-
Homo sapiens
IC50 Value (protein specific)
EC Number
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
2.7.1.74
0.00091
-
in 50 mM Tris (pH 7.6)
Homo sapiens
LP-503392
2.7.1.74
0.0138
-
in 50 mM Tris (pH 7.6)
Homo sapiens
LP-375752
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
2.7.1.74
LP-375752
i.e. 2-[4-(6-benzo[b]thiophen-2-yl-pyrimidin-4-yl)-piperazin-1-yl]-1-pyrrolidin-1-yl-ethanone
Homo sapiens
2.7.1.74
LP-503392
i.e. 2-thio-2'-deoxycytidine
Homo sapiens
KM Value [mM] (protein specific)
EC Number
KM Value [mM]
KM Value Maximum [mM]
Substrate
Commentary
Organism
Structure
2.7.1.74
0.001
-
2'-deoxycytidine
-
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
2.7.1.74
additional information
Homo sapiens
dCK phosphorylates all three natural deoxyribonucleosides, exhibiting the highest affinity for 2'-deoxycytidine
?
-
-
-
Purification (Commentary) (protein specific)
EC Number
Commentary
Organism
2.7.1.74
-
Homo sapiens
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
2.7.1.74
ATP + 1-beta-D-arabinosylcytosine
-
704730
Homo sapiens
ADP + 1-beta-D-arabinosylcytosine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + 2'-deoxyadenosine
-
704730
Homo sapiens
ADP + 2'-deoxyadenosine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + 2'-deoxycytidine
-
704730
Homo sapiens
ADP + 2'-deoxycytidine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + 2'-deoxyguanosine
-
704730
Homo sapiens
ADP + 2'-deoxyguanosine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + cladribine
-
704730
Homo sapiens
ADP + cladribine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + fludarabine
-
704730
Homo sapiens
ADP + fludarabine 5'-phosphate
-
-
-
?
2.7.1.74
ATP + gemcitabine
-
704730
Homo sapiens
ADP + gemcitabine 5'-phosphate
-
-
-
?
2.7.1.74
additional information
dCK phosphorylates all three natural deoxyribonucleosides, exhibiting the highest affinity for 2'-deoxycytidine
704730
Homo sapiens
?
-
-
-
-
General Information
EC Number
General Information
Commentary
Organism
2.7.1.74
metabolism
dCK plays an important role in the salvage pathway of nucleoside metabolism
Homo sapiens
General Information (protein specific)
EC Number
General Information
Commentary
Organism
2.7.1.74
metabolism
dCK plays an important role in the salvage pathway of nucleoside metabolism
Homo sapiens