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Information on EC 2.4.2.4 - thymidine phosphorylase
for references in articles please use BRENDA:EC2.4.2.4
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EC Tree 2 Transferases
2.4 Glycosyltransferases
2.4.2 Pentosyltransferases
2.4.2.4 thymidine phosphorylase
IUBMB Comments
The enzyme in some tissues also catalyses deoxyribosyltransferase reactions of the type catalysed by EC 2.4.2.6, nucleoside deoxyribosyltransferase.
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria
- 2.4.2.4
- 5-fluorouracil
-
angiogenic
- colorectal
- thymidylate
- dihydropyrimidine
- capecitabine
-
microvessels
- metastasis
-
clinicopathological
- uridine
-
mngie
-
neurogastrointestinal
- tumour
- 5'-deoxy-5-fluorouridine
-
fluoropyrimidine
- thymine
-
5\'-dfur
-
resect
-
encephalomyopathy
-
prodrugs
- lymph
-
intratumoral
- deoxyuridine
- uracil
- orotate
-
phosphorolysis
-
dysmotility
- tpi
-
cachexia
- phosphorylases
- leukoencephalopathy
- ophthalmoplegia
- medicine
-
5-fu-based
-
ptosis
-
taxanes
- pseudo-obstruction
-
tegafur
- deoxyribose
- 5-fluoro-2'-deoxyuridine
-
viii-related
-
hand-foot
- fdump
- ophthalmoparesis
- trifluorothymidine
- analysis
- 5-fluorouridine
-
anti-cd34
-
5-fluorouracil-based
-
tp-induced
- 2'-deoxyuridine
- synthesis
-
fluoropyrimidine-based
showSynonyms
thymidine phosphorylase, pd-ecgf, dthdpase, platelet-derived endothelial cell growth factor, pynpase, pd-ecgf/tp, pyrimidine nucleoside phosphorylase, pdecgf, platelet-derived endothelial cell growth factor/thymidine phosphorylase, gliostatin, more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
angiogenic factor platelet-derived endothelial cell growth factor/thymidine phosphorylase
-
animal growth regulators, blood platelet-derived endothelial cell growth factors
-
-
-
-
blood platelet-derived endothelial cell growth factor
-
-
-
-
deoA
deoxythymidine phosphorylase
-
-
-
-
dthdpase
EC 2.4.2.23
-
-
formerly, part transferred
-
gliostatin
gliostatins
-
-
-
-
PD-ECGF
PD-ECGF/TP
PD-ECGF/TP platelet-derived endothelial cell growth factor
-
-
-
-
PDECGF
phosphorylase, thymidine
-
-
-
-
platelet derived-endothelial cell growth factor
platelet-derived endothelial cell growth factor
platelet-derived endotherial cell growth factor
pyrimidine deoxynucleoside phosphorylase
-
-
-
-
pyrimidine phosphorylase
-
-
-
-
TDRPASE
-
-
-
-
ThdPase
thymidine phosphorylase
thymidine-orthophosphate deoxyribosyltransferase
-
-
-
-
thymidine:orthophosphate deoxy-D-ribosyltransferase
-
-
-
-
Tpase
TYMP
additional information
the enzyme belongs to the pyrimidine nucleoside phosphorylase family
dthdpase
-
-
-
-
gliostatin
-
-
-
-
PD-ECGF
-
-
-
-
PD-ECGF
-
-
platelet-derived endothelial cell growth factor
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
rapid equilibrium random bi-bi mechanism with an enzyme-phosphate-thymine dead-end complex
-
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
mechanism
-
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
mechanism
-
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
ordered sequential reaction mechanism, phosphate is the first substrate to bind to and deoxyribose the last product to dissociate from the enzyme
-
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
ordered bi bi mechanism with the nucleoside the first substrate to add, and the pyrimidine base the last product to leave
-
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
SN2-type catalytic mechanism
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
SN2-type catalytic mechanism
-
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
sequential random bi-bi mechanism
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
sequential random bi-bi mechanism
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
SN1- and SN2-like transition states are proposed for the hTP-catalyzed reaction, overview
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
pentosyl group transfer
pentosyl group transfer
-
-
-
-
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PATHWAY SOURCE
PATHWAYS
BRENDA
MetaCyc
pyrimidine deoxyribonucleosides degradation
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SYSTEMATIC NAME
IUBMB Comments
thymidine:phosphate deoxy-alpha-D-ribosyltransferase
The enzyme in some tissues also catalyses deoxyribosyltransferase reactions of the type catalysed by EC 2.4.2.6, nucleoside deoxyribosyltransferase.
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CAS REGISTRY NUMBER
COMMENTARY
9030-23-3
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
1-(2',6'-dideoxy-alpha-L-lyxo-hexafuranosyl)thymine + phosphate
?
Substrates: -
Products: -
Products: -
?
1-(2',6'-dideoxy-alpha-L-lyxohexafuranosyl)thymine + phosphate
thymine + 2,6-dideoxy-L-lyxohexafuranose 1-phosphate
Substrates: -
Products: -
Products: -
?
1-(2',6'-dideoxy-beta-D-ribo-hexafuranosyl)thymine + phosphate
?
Substrates: -
Products: -
Products: -
?
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine + phosphate
?
Substrates: -
Products: -
Products: -
?
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine + phosphate
thymine + 2,6-dideoxy-D-ribohexafuranose 1-phosphate
Substrates: -
Products: -
Products: -
?
1-(tetrahydro-2-furanyl)-5-fluorouracil + phosphate
?
-
Substrates: i.e. Tegafur
Products: -
Products: -
?
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione + phosphate
?
-
Substrates: 56% conversion after one h
Products: -
Products: -
?
1-[(2R,4S,5R)-5-(aminomethyl)-4-hydroxytetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
-
Substrates: 11% conversion after one h
Products: -
Products: -
?
1-[(2R,4S,5R)-5-(hydroxymethyl)-4-sulfanyltetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
-
Substrates: 0.76% conversion after one h
Products: -
Products: -
?
1-[(2R,4S,5S)-4-hydroxy-5-(sulfanylmethyl)tetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
-
Substrates: 39% conversion after one h
Products: -
Products: -
?
1-[(2R,4S,5S)-5-(chloromethyl)-4-hydroxytetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
-
Substrates: 24% conversion after one h
Products: -
Products: -
?
2'-deoxy-5-nitrouridine + phosphate
5-nitrouracil + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
2'-deoxyuridine + phosphate
uracil + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
2'-deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
3'-deoxy-2',3'-didehydrothymidine + phosphate
?
Substrates: -
Products: -
Products: -
?
3'-deoxy-2',3'-didehydrothymidine + phosphate
thymine + 2,3-dideoxy-2,3-didehydro-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
3'-deoxythymidine + phosphate
thymine + 2,3-dideoxy-D-ribose 1-phosphate
-
Substrates: 3.2% conversion after one h
Products: -
Products: -
?
3'-thiothymidine + phosphate
thymine + 3-thio-2,3-dideoxy-D-ribose 1-phosphate
-
Substrates: 0.76% conversion after 1 h
Products: -
Products: -
?
3-fluorothymidine + phosphate
3-fluorothymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
4'-thiothymidine + phosphate
?
-
Substrates: 3.8% conversion after one h
Products: -
Products: -
?
5'-amino-5'-deoxythymidine + phosphate
thymine + 2,5-dideoxy-5-amino-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
5'-amino-5'-deoxythymidine + phosphate
thymine + 5-amino-2,5-dideoxy-D-ribose 1-phosphate
-
Substrates: 11% conversion after 1 h
Products: -
Products: -
?
5'-chloro-5'-deoxythymidine + phosphate
?
Substrates: -
Products: -
Products: -
?
5'-chloro-5'-deoxythymidine + phosphate
thymine + 5-chloro-2,5-dideoxy-D-ribose 1-phosphate
-
Substrates: 24% conversion after 1 h
Products: -
Products: -
?
5'-deoxy-5'-fluorothymidine + phosphate
thymine + 5-fluoro-2,5-dideoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5'-deoxy-5-fluorouridine + phosphate
5-fluorouracil + 5-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
5'-deoxy-5-fluorouridine + phosphate
5-fluorouracil + 5-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5'-deoxyuridine + phosphate
uracil + 5-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5'-thiothymidine + phosphate
thymine + 5-thio-2,5-dideoxy-D-ribose 1-phosphate
-
Substrates: 39% conversion after 1 h
Products: -
Products: -
?
5-deoxythymidine + phosphate
thymine + 2,5-dideoxyribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5-fluoro-2'-deoxyuridine + phosphate
5-fluorouracil + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
5-fluoro-2'-deoxyuridine + phosphate
5-fluorouracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5-fluorouridine + phosphate
5-fluorouracil + alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
5-fluorouridine + phosphate
5-fluorouracil + D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
6-azathymidine + phosphate
uracil + deoxyribose-1-phosphate
-
Substrates: 5.4% conversion after one h
Products: -
Products: -
?
fluorodeoxyuridine + phosphate
fluorouracil + 2-deoxy-D-ribose
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + alpha-D-deoxyribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymine arabinoside + phosphate
thymine + arabinose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
uracil + 2-deoxy-alpha-D-ribose 1-phosphate
2'-deoxyuridine + phosphate
Substrates: -
Products: -
Products: -
r
uracil + phosphate
uracil + ribose 1-phosphate
-
Substrates: 88% conversion after one h
Products: -
Products: -
?
uridine + phosphate
uracil + alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
2'-deoxythymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
2'-deoxythymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
3'-amino-3'-deoxythymidine + phosphate
?
Substrates: at pH 8.0
Products: -
Products: -
?
4-thiothymidine + phosphate
4-thiothymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
4-thiothymidine + phosphate
4-thiothymine + 2-deoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
5'-deoxy-5-fluorouridine + phosphate
5-fluorouracil + 5-deoxyribose-1-phosphate
-
Substrates: -
Products: -
Products: -
?
5'-deoxy-5-fluorouridine + phosphate
5-fluorouracil + 5-deoxyribose-1-phosphate
-
Substrates: 5'-DFUR
Products: -
Products: -
?
5'-deoxy-5-fluorouridine + phosphate
5-fluorouracil + 5-deoxyribose-1-phosphate
-
Substrates: -
Products: -
Products: -
?
5'-deoxythymidine + phosphate
thymine + 2,5-dideoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
5'-deoxythymidine + phosphate
thymine + 2,5-dideoxy-D-ribose 1-phosphate
-
Substrates: 68% conversion after one h
Products: -
Products: -
?
5-fluoro-2'-deoxyuridine + phosphate
5-fluorouracil + 2-deoxyribose-1-phosphate
-
Substrates: -
Products: -
Products: -
?
5-fluoro-2'-deoxyuridine + phosphate
5-fluorouracil + 2-deoxyribose-1-phosphate
-
Substrates: -
Products: -
Products: -
r
5-fluorouracil + 2-deoxy-alpha-D-ribose 1-phosphate
5-fluoro-2'-deoxyuridine + phosphate
Substrates: -
Products: -
Products: -
?
5-fluorouracil + 2-deoxy-alpha-D-ribose 1-phosphate
5-fluoro-2'-deoxyuridine + phosphate
-
Substrates: the enzyme converts 5-fluorouracil to 5-fluoro-2'-deoxyuridine, activating the prodrug, overview. This action can only take place if there is enough co-substrate. 5-Fluorouracil prodrugs and metabolism, detailed overview
Products: 5-fluoro-2'-deoxyuridine is further converted by thymidine kinase to 5-fluoro-2'-deoxyuridine 5'-monophosphate
Products: 5-fluoro-2'-deoxyuridine is further converted by thymidine kinase to 5-fluoro-2'-deoxyuridine 5'-monophosphate
?
5-fluorouracil + 2-deoxy-alpha-D-ribose 1-phosphate
5-fluoro-2'-deoxyuridine + phosphate
-
Substrates: the enzyme converts 5-fluorouracil to 5-fluoro-2'-deoxyuridine, activating the prodrug, overview. This action can only take place if there is enough co-substrate
Products: -
Products: -
?
5-fluorouridine + phosphate
5-fluorouracil + ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5-fluorouridine + phosphate
5-fluorouracil + ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5-nitro-2'-deoxyuridine + phosphate
5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
5-nitro-2'-deoxyuridine + phosphate
5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
5-nitro-2'-deoxyuridine + phosphate
5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
bromodeoxyuridine + phosphate
bromouracil + 2-deoxy-D-ribose
-
Substrates: -
Products: -
Products: -
?
bromodeoxyuridine + phosphate
bromouracil + 2-deoxy-D-ribose
-
Substrates: -
Products: -
Products: -
?
bromodeoxyuridine + phosphate
bromouracil + 2-deoxy-D-ribose
-
Substrates: at 40% the rate of thymidine
Products: -
Products: -
?
deoxythymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
deoxythymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: 1.2-1.4 times the rate of thymidine at pH 5.7
Products: -
Products: -
?
deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
iododeoxyuridine + phosphate
iodouracil + 2-deoxy-D-ribose
-
Substrates: -
Products: -
Products: -
?
iododeoxyuridine + phosphate
iodouracil + 2-deoxy-D-ribose
-
Substrates: -
Products: -
Products: -
?
thymidine + arsenate
?
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: substrate binding induces domain movement, which leads to the closed conformation of the active site and initiates phosphorylation, molecular dynamic simulation, overview
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: 2-deoxy-alpha-D-ribose 1-phosphate strongly promoted neovascularization
Products: 2-deoxy-alpha-D-ribose 1-phosphate strongly promoted neovascularization
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: the enzyme catalyzes the reversible cleavage of the glycosidic bond of pyrimidine 2'-deoxynucleotides, most likely through SN2-like transition state involving nucleobase, 2'-deoxyribose and phosphate. The active site consists of residues His116, Ser117, Leu148, Arg202, Val208, Ile214, Lys221 and Val241
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: Asp203 plays an important role to afford the substrate-binding site loop stabilization that is required for efficient enzyme catalysis
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: Asp203 plays an important role for loop stabilization required for efficient enzyme catalysis
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: in the reverse reaction only alpha-D-2-deoxyribose 1-phosphate is accepted as substrate
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
Substrates: SN1 mechanism for the phosphorolysis reaction, relevant interaction between the His85 imidazole ring and the O2 of thymidine suggesting that this highly conserved residue could play an important role in the catalytic mechanism of TPase
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: 86% conversion after one h
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
Escherichia coli B / ATCC 11303
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: enzyme is enantioselective, acts only on the naturally occurring D-thymidine and some D-thymidine analogs, but not on their L-counterparts
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
ir
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: intact platelets degrade thymidine but are not able to synthesize thymidine from thymine
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: the enzyme confers resistance to apoptosis induced by hypoxia. The enzymatic degradation of thymidine by thymidine phosphorylase is required for the inhibition of hypoxia-induced apoptosis. The enzyme can confer resistance to apoptosis in addition to its angiogenic activity. The enzyme must play some role in the development or malignancy of tumors. Involved in invasion and metastasis of some solid tumors
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: the enzyme plays a crucial role in intratumoral angiogenesis, which occurs in the early phase of ovarian cancer, or influences angiogenesis indirectly
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
Products: -
Products: -
r
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
Escherichia coli B / ATCC 11303
-
Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: degradation of uridine in tumor specimen
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: enzyme is enantioselective, acts only on the naturally occurring D-thymidine and some D-thymidine analogs, but not on their L-counterparts
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
Products: -
Products: -
?
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: in Escherichia coli and Salmonella typhimurium thymidine phosphorylase plays an important role in metabolism of thymine auxotrophs and is necessary for the conversion of exogenous thymine to thymidine
Products: -
Products: -
?
uridine + phosphate
uracil + D-ribose 1-phosphate
-
Substrates: 56% conversion after 1 h
Products: -
Products: -
?
uridine + phosphate
uracil + D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
uridine + phosphate
uracil + ribose 1-phosphate
-
Substrates: the activities of uridine, deoxyuridine and thymidine phosphorylases from Giardia lamblia remain associated throughout purification, suggesting that a single enzyme is responsible for the 3 activities
Products: -
Products: -
?
uridine + phosphate
uracil + ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
uridine + phosphate
uracil + ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: no substrate: deoxycytidine
Products: -
Products: -
?
additional information
?
-
-
Substrates: specific for deoxyribonucleosides
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: purine deoxyribonucleosides and ribonucleosides are not cleaved
Products: -
Products: -
?
additional information
?
-
-
Substrates: 3'-amino-3'-deoxythymidine is not a thymidine phosphorylase substrate at pH 6.5, no activity with uridine and methyluridine
Products: -
Products: -
?
additional information
?
-
Substrates: 3'-amino-3'-deoxythymidine is not a thymidine phosphorylase substrate at pH 6.5, no activity with uridine and methyluridine
Products: -
Products: -
?
additional information
?
-
-
Substrates: no activity with 3'beta-thymidine, 4'-thio-1'-alpha-thymidine, 1-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]thymine, 5-methyl-2-pyrimidinone nucleoside, and deoxycytidine
Products: -
Products: -
?
additional information
?
-
-
Substrates: the 3'-OH group is important for nucleotide binding, substrate analogues and substrate specificity, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: no activity with arabinosyluracil and 2',3'-dideoxyuridine
Products: -
Products: -
?
additional information
?
-
Substrates: the pyrimidine moiety of thymidine is involved in making hydrogen bonds with the side chains of residues Arg171, Ser186, Lys190, while the deoxyribose moiety form hydrogen bond with a co-crystallized water molecule. The phosphate ion shows hydrogen bonding with Lys84, Ser95, Ser113, and a water molecule
Products: -
Products: -
?
additional information
?
-
Escherichia coli B / ATCC 11303
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: closing/opening motion in the presence of substrate, product, and transition state, molecular dynamic simulation
Products: -
Products: -
?
additional information
?
-
-
Substrates: no substrate: deoxycytidine
Products: -
Products: -
?
additional information
?
-
-
Substrates: the phosphorolytic acitvities towards thymidine, 5'-deoxy-5-fluorouridine and 1-(tetrahydro-2-furanyl)-5-fluorouracil remain closely parallel during purification
Products: -
Products: -
?
additional information
?
-
-
Substrates: purine deoxyribonucleosides are no substrates
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: role in thymidine metabolism, homeostasis, development and regeneration of central nervous system and formation of blood/brain barrier
Products: -
Products: -
?
additional information
?
-
-
Substrates: formation of blood/brain barrier and repair following brain injury
Products: -
Products: -
?
additional information
?
-
-
Substrates: identical to platelet-derived endothelial cell growth factor
Products: -
Products: -
?
additional information
?
-
-
Substrates: identical to platelet-derived endothelial cell growth factor
Products: -
Products: -
?
additional information
?
-
-
Substrates: mitogenic effect, promotes endothelial cell proliferation
Products: -
Products: -
?
additional information
?
-
Substrates: important role in nucleoside metabolism, implicated in angiogenesis and apoptosis
Products: -
Products: -
?
additional information
?
-
-
Substrates: important role in nucleoside metabolism, implicated in angiogenesis and apoptosis
Products: -
Products: -
?
additional information
?
-
Substrates: expression of PD-ECGF/TP may play an important role in the progression of solid tumors
Products: -
Products: -
?
additional information
?
-
Substrates: thymidine phosphorylase and uridine phosphorylase contribute in the conversion of 5'-deoxy-5-fluorouridine into 5-fluorouracil and the conversion of 5-fluorouracil into its active metabolites in peripheral blood mononuclear cell, but thymidine phosphorylase seems to be the most important enzyme for these reactions in PBMC
Products: -
Products: -
?
additional information
?
-
Substrates: molecular modeling based on an X-ray structure of human TP indicates that TP is likely to be mechanistically similar to all other natural members of the class in proceeding through a a oxacarbenium-like transition state or states
Products: -
Products: -
?
additional information
?
-
-
Substrates: molecular modeling based on an X-ray structure of human TP indicates that TP is likely to be mechanistically similar to all other natural members of the class in proceeding through a a oxacarbenium-like transition state or states
Products: -
Products: -
?
additional information
?
-
-
Substrates: thymidine phosphorylase is identical with platelet-derived endothelial cell growth factor, PD-ECGF, which promotes angiogenesis. The mechanism of endometrial angiogenesis involves thymidine phosphorylase and stimulation by ovarian steroids of production of angiogenic regulators by endometrial epithelium and stroma which then act on the endothelium
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme stimulates formation of focal adhesions and the phosphorylation of Tyr397 of focal adhesion kinase, and it induces the expression and/or secretion of other angiogenic factors, overview. Thymidine phosphorylase promotes tumor growth and metastasis by preventing apoptosis and inducing angiogenesis, detailed overview. As gliostatin from fibroma cells, the enzyme inhibits the growth of both astrocytes and glial tumor cells
Products: -
Products: -
?
additional information
?
-
Substrates: initial velocity studies showed an intersecting pattern, consistent with substrate-enzyme-co-substrate complex formation, and a binding pattern indicating that the binding of the substrate interferes with the binding of the co-substrate and vice versa
Products: -
Products: -
?
additional information
?
-
-
Substrates: initial velocity studies showed an intersecting pattern, consistent with substrate-enzyme-co-substrate complex formation, and a binding pattern indicating that the binding of the substrate interferes with the binding of the co-substrate and vice versa
Products: -
Products: -
?
additional information
?
-
Substrates: substrate specificity, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: substrate specificity, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: specificity towards the deoxyribosyl moiety of the substrate
Products: -
Products: -
?
additional information
?
-
-
Substrates: nonsubstituted pyrimidine moiety or one which is substituted in position 5 required
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme in some tissues also catalyzes deoxyribonucleosyltransferase reaction of the type catalyzed by EC 2.4.2.6: 2-deoxy-D-ribosyl-base1 + base2 = 2-deoxy-D-ribosyl-base2 + base1
Products: -
Products: -
?
additional information
?
-
-
Substrates: no substrate: deoxycytidine
Products: -
Products: -
?
additional information
?
-
-
Substrates: no substrate: deoxycytidine
Products: -
Products: -
?
additional information
?
-
-
Substrates: no substrates: deoxyadenosine, deoxyguanosine
Products: -
Products: -
?
additional information
?
-
-
Substrates: no substrates: deoxyadenosine, deoxyguanosine
Products: -
Products: -
?
additional information
?
-
-
Substrates: specific for deoxyribonucleosides
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
5-fluorouracil + 2-deoxy-alpha-D-ribose 1-phosphate
5-fluoro-2'-deoxyuridine + phosphate
-
Substrates: the enzyme converts 5-fluorouracil to 5-fluoro-2'-deoxyuridine, activating the prodrug, overview. This action can only take place if there is enough co-substrate. 5-Fluorouracil prodrugs and metabolism, detailed overview
Products: 5-fluoro-2'-deoxyuridine is further converted by thymidine kinase to 5-fluoro-2'-deoxyuridine 5'-monophosphate
Products: 5-fluoro-2'-deoxyuridine is further converted by thymidine kinase to 5-fluoro-2'-deoxyuridine 5'-monophosphate
?
uracil + 2-deoxy-alpha-D-ribose 1-phosphate
2'-deoxyuridine + phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: 2-deoxy-alpha-D-ribose 1-phosphate strongly promoted neovascularization
Products: 2-deoxy-alpha-D-ribose 1-phosphate strongly promoted neovascularization
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Substrates: -
Products: -
Products: -
r
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
Products: -
Products: -
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
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thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
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Substrates: -
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thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
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Substrates: -
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thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
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Substrates: -
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thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
Substrates: -
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thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
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Substrates: intact platelets degrade thymidine but are not able to synthesize thymidine from thymine
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thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
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Substrates: the enzyme confers resistance to apoptosis induced by hypoxia. The enzymatic degradation of thymidine by thymidine phosphorylase is required for the inhibition of hypoxia-induced apoptosis. The enzyme can confer resistance to apoptosis in addition to its angiogenic activity. The enzyme must play some role in the development or malignancy of tumors. Involved in invasion and metastasis of some solid tumors
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thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
-
Substrates: the enzyme plays a crucial role in intratumoral angiogenesis, which occurs in the early phase of ovarian cancer, or influences angiogenesis indirectly
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thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
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thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
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thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
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thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
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thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
Substrates: -
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
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Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
Escherichia coli B / ATCC 11303
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Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: -
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
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Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: degradation of uridine in tumor specimen
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: enzyme is enantioselective, acts only on the naturally occurring D-thymidine and some D-thymidine analogs, but not on their L-counterparts
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
-
Substrates: enzyme also catalyzes the nucleoside deoxyribosyltransferase reaction with pyrimidine deoxyribonucleosides, ec2.4.2.6
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thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
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Substrates: in Escherichia coli and Salmonella typhimurium thymidine phosphorylase plays an important role in metabolism of thymine auxotrophs and is necessary for the conversion of exogenous thymine to thymidine
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additional information
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Substrates: role in thymidine metabolism, homeostasis, development and regeneration of central nervous system and formation of blood/brain barrier
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Substrates: formation of blood/brain barrier and repair following brain injury
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Substrates: identical to platelet-derived endothelial cell growth factor
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Substrates: identical to platelet-derived endothelial cell growth factor
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Substrates: mitogenic effect, promotes endothelial cell proliferation
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Substrates: important role in nucleoside metabolism, implicated in angiogenesis and apoptosis
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Substrates: important role in nucleoside metabolism, implicated in angiogenesis and apoptosis
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additional information
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Substrates: expression of PD-ECGF/TP may play an important role in the progression of solid tumors
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Substrates: thymidine phosphorylase and uridine phosphorylase contribute in the conversion of 5'-deoxy-5-fluorouridine into 5-fluorouracil and the conversion of 5-fluorouracil into its active metabolites in peripheral blood mononuclear cell, but thymidine phosphorylase seems to be the most important enzyme for these reactions in PBMC
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Substrates: thymidine phosphorylase is identical with platelet-derived endothelial cell growth factor, PD-ECGF, which promotes angiogenesis. The mechanism of endometrial angiogenesis involves thymidine phosphorylase and stimulation by ovarian steroids of production of angiogenic regulators by endometrial epithelium and stroma which then act on the endothelium
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Substrates: the enzyme stimulates formation of focal adhesions and the phosphorylation of Tyr397 of focal adhesion kinase, and it induces the expression and/or secretion of other angiogenic factors, overview. Thymidine phosphorylase promotes tumor growth and metastasis by preventing apoptosis and inducing angiogenesis, detailed overview. As gliostatin from fibroma cells, the enzyme inhibits the growth of both astrocytes and glial tumor cells
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one
(6aS)-1,2,9,10-tetramethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline
uncompetitive inhibition
(E)-1-((2-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-1-((4-chlorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-1-((4-ethylphenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-1-((4-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-1-((hydroxyimino)(p-tolyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
-
(E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
-
(R)-(1-fluoro-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)propan-2-yloxy)methylphosphonic phosphoric anhydride
-
strong inhibitory effect
(S)-(1-fluoro-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)propan-2-yloxy)methylphosphonic phosphoric anhydride
-
strong inhibitory effect
(Z)-1-((2-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((3,4-dichlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((3-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((4-bromophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((4-chlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((4-ethylphenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((4-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((hydroxyimino)(m-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((hydroxyimino)(p-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((hydroxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-1-((hydroxyimino)(thiophen-2-yl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
-
(Z)-N'-((4-chloro-2-oxo-4a,8a-dihydro-2H-chromen-3-yl)methylene)-2-oxo-1,2,4a,8a-tetrahydroquinoline-6-carbohydrazide
-
(Z)-N'-(3-chloro-4-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
(Z)-N'-(4-hydroxy-3,5-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
-
([(1R)-2-fluoro-1-[(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([(1R)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([(1R)-2-fluoro-1-[(5-methyl-2,6-dioxotetrahydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
low inhibitory effect
([(1R)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([(1S)-2-fluoro-1-[(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([(1S)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([(1S)-2-fluoro-1-[(5-methyl-2,6-dioxotetrahydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
low inhibitory effect
([(1S)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([2,2,2-trifluoro-1-[(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
([[(2R,3S,5R)-2-(hydroxymethyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-3-yl]oxy]methyl)phosphonic acid
-
-
1-[2-(3-amino-5-methyl-2,4-dioxo-3,4-dihydropyridin-1(2H)-yl)ethyl]-4-[4-(dimethylamino)phenyl]pyridin-1-ium bromide
the compound, which is used as sensor for the detection of the enzyme, gives a fluorescent signal due to twisted intramolecular charge transfer process induced by binding with the active site of the enzyme
1-[2-deoxy-3,5-O-[phenyl(phosphono)methylidene]-b-L-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
53% inhibition at 0.01 mM; 96% inhibition at 0.01 mM
1-[3,5-O-(2-bromo-1-phosphonoethylidene)-2-deoxy-b-L-erythro-pentofuranosyl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
74% inhibition at 0.01 mM; 80% inhibition at 0.01 mM
1-[3-(3-amino-5-methyl-2,4-dioxo-3,4-dihydropyridin-1(2H)-yl)propyl]-4-[4-(dimethylamino)phenyl]pyridin-1-ium bromide
-
1-[4-(3-amino-5-methyl-2,4-dioxo-3,4-dihydropyridin-1(2H)-yl)butyl]-4-[4-(dimethylamino)phenyl]pyridin-1-ium bromide
-
2-(2-methyl-1H-indol-3-yl)-N'-(2,4,6-trihydroxybenzylidene)acetohydrazide
-
2-(3,4-dichlorophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
2-(3-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(4-bromo-3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(4-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(4-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(benzylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(diphenylmethyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
2-(furan-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(methylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-(methylsulfanyl)-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
-
2-(pyridin-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-11 methyl 4-(4-ethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
2-[(2-phenylethyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-[(3,4-dichlorophenyl)methyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
2-[(3-phenylpropyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-[(5-(4-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
the angiogenic response of 4d is estimated using the chick chorionic allantoic membrane (CAM) assay
2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-7-phenyl-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
-
3-(((4-chlorophenyl)amino)(phenyl)methyl)-5-(2,6-dimethylphenyl)1,3,4-oxadiazole-2(3H)-thione
-
3-(((4-chlorophenyl)amino)methyl)-5-(2-iodophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
3-((4-benzylpiperazin-1-yl)methyl)-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
3-((5-(4-chlorophenyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl)methyl)thiazolidine-2,4-dione
-
3-((benzylamino)methyl)-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
3-(3-(quinoxalin-2-yl)thiazolo[2,3-c][1,2,4]triazol-5-yl)benzene-1,2-diol
-
3-([(2-([-(4-oxo-4H-chromen-3-yl)methylidene]amino)ethyl)imino] methyl)-4H-chromen-4-one
-
-
3-[(2,3-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(2-chloroanilino)methyl]-5-(2-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(2-chloroanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(2-methoxy-6-nitroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
3-[(2-methylanilino)methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(3,4-dichloroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(3,4-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(3-methoxyanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(4-bromoanilino)methyl]-5-(2-bromophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(4-bromoanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(4-methylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]propanamide
-
3-[[(2-phenylethyl)amino]methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[[(4-methoxy-3'-nitro[1,1'-biphenyl]-3-yl)amino]methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
4,4'-[(2R,3S)-2,3-dimethylbutane-1,4-diyl]di(benzene-1,2-diol)
competitive inhibition
4-(2,5-difluorobenzyl)-N-(2-fluorophenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(2-methoxyphenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(3-fluorophenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(3-methoxyphenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(3-nitrophenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(4-fluorophenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(4-methoxyphenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(4-nitrophenyl)piperazine-1-carbothioamide
-
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(1-(4-nitrophenyl)ethylidene)benzohydrazide
-
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trihydroxybenzylidene)benzohydrazide
-
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trimethoxybenzylidene)benzohydrazide
-
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2-nitrobenzylidene)benzohydrazide
-
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(3,4,5-trimethoxybenzylidene)benzohydrazide
-
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(4-(phenoxymethyl)benzylidene)benzohydrazide
-
4-hydroxyl-N'-[(E)-(2,3,4-trihydroxylphenyl)methylidene]benzohydrazide
26% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-(2,4,5-trihydroxylphenyl)methylidene]benzohydrazide
99% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-(2,4,6-trihydroxylphenyl)methylidene]benzohydrazide
8% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-(2-methylphenyl)methylidene]benzohydrazide
99% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-(3-hydroxylphenyl)methylidene]benzohydrazide
99% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-(4-hydroxylphenyl)methylidene]benzohydrazide
99% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-1-(2-hydroxylphenyl)ethylidene]benzohydrazide
25% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-[2-(methoxy)phenyl]methylidene]benzohydrazide
99% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-[2-hydroxyl-5-(methoxy)phenyl]methylidene]benzo-hydrazide
99.9% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-[4-(methoxy)phenyl]methylidene]benzohydrazide
99.8% inhibition at 0.5 mM
4-hydroxyl-N'-[(E)-[4-(methylsulfanyl)phenyl]methylidene]benzohydrazide
23% inhibition at 0.5 mM
4-hydroxyl-N-[(E)-(2-hydroxyl-3-methoxyphenyl)methylidene]benzohydrazide
86.9% inhibition at 0.5 mM
4-hydroxyl-N-[(E)-(2-hydroxylphenyl)methylidene]benzohydrazide
99.6% inhibition at 0.5 mM
4-[(Z)-[(3-hydroxynaphthalen-2-yl)methylidene]amino]-1,5-dimethyl-2-phenylpyrazolidin-3-one
-
5'-O-(2'',4''-dichlorobenzoyl)-thymidine-3'-O-2'',4''-dichlorobenzoate
-
5'-O-(4''-bromobenzoyl)-thymidine-3'-O-4''-bromobenzoate
noncompetitive inhibition
5,5'-butane-1,4-diylbis(4-(4-nitrophenyl)-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
-
5,5'-butane-1,4-diylbis(4-heptyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
-
5,5'-butane-1,4-diylbis(4-hexyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
most potent inhibitor
5,5'-butane-1,4-diylbis(4-methyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
-
5,5'-butane-1,4-diylbis(4-octyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
-
5,5'-butane-1,4-diylbis(4-phenyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
-
5-(2-bromophenyl)-3-[(2-chloroanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-(2-bromophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-(2-chlorophenyl)-3-(((4-chlorophenyl)amino)(phenyl)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(2-chlorophenyl)-3-((thiazol-2-ylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-(((2-nitrophenyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-(((3,3-diphenylpropyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-(((4-fluorophenyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-(((4-hydroxyphenyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((2-methyl-1H-imidazol-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((4-cyclohexylpiperazin-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((cyclohexylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((dicyclohexylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((naphthalen-1-ylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((phenylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-((thiazol-2-ylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
-
5-(4-chlorophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-(4-chlorophenyl)-3-[(2-methylanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
-
5-(4-pyridyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
binding mode, modeling
5-(benzylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
5-(methylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
5-bromo-6-(2-imino-pyrrolidin-1-yl)methyl-uracil
-
tightbinding stoichiometric inhibitor of recombinant Escherichia coli thymidine phosphorylase, can be used as active-site titrants for it using either thymidine or 5-nitro-2'-deoxyuridine as substrate
5-bromo-6-amino-uracil
-
enzyme inhibition results in a significant increase in basal and oxidative stress-induced apoptosis, the effect is abrogated by supplementation with 2-deoxy-D-ribose-1-phosphate
5-bromo-6-[[(1,3-dihydroxypropan-2-yl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
-
5-bromo-6-[[(2,3-dihydroxypropyl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
-
5-chloro-6-(2-imino-pyrrolidin-1-yl)methyluracil
-
tightbinding stoichiometric inhibitor of recombinant Escherichia coli thymidine phosphorylase, can be used as active-site titrants for it using either thymidine or 5-nitro-2'-deoxyuridine as substrate
5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride
-
-
5-chloro-6-[([4-oxo-8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-2-yl]sulfanyl)methyl]pyrimidine-2,4(1H,3H)-dione
-
5-chloro-6-[[(1,3-dihydroxypropan-2-yl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
-
5-fluoro-1-(3,6,9,12,15,18,21,24-octaoxahexatriacontan-1-yl)pyrimidine-2,4(1H,3H)-dione
43% competitive inhibition at 0.04 mM
5-fluoro-1-(3,6,9,12,15,18,21-heptaoxatritriacontan-1-yl)pyrimidine-2,4(1H,3H)-dione
40% competitive inhibition at 0.04 mM
5-fluoro-1-(3,6,9,12,15,18-hexaoxatriacontan-1-yl)pyrimidine-2,4(1H,3H)-dione
38% competitive inhibition at 0.04 mM
5-fluoro-6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
5-fluoro-6-[(4H-1,2,4-triazol-4-ylamino)methyl]pyrimidine-2,4(1H,3H)-dione
-
-
5-Hydroxymethyluracil
-
35% inactivation at 2 mM
5-Iodouracil
His116 directly interacts with the inhibitor via its NE2 group, enzyme binding structure, overview
5-sulfanylidene-2-(thiophen-2-yl)-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
6-(((1,3-dihydroxypropan-2-yl)amino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
the inhibitor shows a noncompetitive inhibition mode with both thymidine and inorganic phosphate substrates. Effect of 8g on cell viabilities of different cancer cell lines, overview
6-(2-amino-imidazol-1-yl)methyl-5-bromouracil
-
tightbinding stoichiometric inhibitor of recombinant Escherichia coli thymidine phosphorylase, can be used as active-site titrants for it using either thymidine or 5-nitro-2'-deoxyuridine as substrate
6-(2-amino-imidazol-1-yl)methyl-5-chlorouracil
-
tightbinding stoichiometric inhibitor of recombinant Escherichia coli thymidine phosphorylase, can be used as active-site titrants for it using either thymidine or 5-nitro-2'-deoxyuridine as substrate
6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
6-methoxy-2-oxo-2H-1-benzopyran-7-yl 6-O-[(2R,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxolan-2-yl]-beta-D-glucopyranoside
uncompetitive inhibition
6-Methyluracil
-
competitive, 86% inhibition at 10 mM and 36% inhibition at 1 mM
6-[[(2,3-dihydroxypropyl)(methyl)amino]methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
-
7-(4-tert-butylphenyl)-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
-
7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
-
7-(methylsulfanyl)-2-phenyl-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
7-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
-
7-[4-(4-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
7-[4-(benzenesulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b']dipyran-2-one
uncompetitive inhibition
8-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
-
8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
-
aurothioglucose
-
the expression of tyhmidine phosphorylase mRNA is significantly decreased by stimulation with aurothioglucose
Bromouracil
-
100% inactivation at 1 mM
deoxyadenosine
-
20% inactivation at 1 mM
dexamethasone
-
the expression of tyhmidine phosphorylase mRNA is significantly decreased by stimulation with dexamethasone
diethyl ((2-[(3,4-dihydro-5-methyl-2,4-dioxopyrimidin-1(2H)-yl)methyl]cyclopent-1-en-1-yl)(difluoro)methyl)phosphonate
-
-
diethyl ((2-[(3,4-dihydro-5-methyl-2,4-dioxopyrimidin-1(2H)-yl)methyl]cyclopent-1-en-1-yl)methyl)phosphonate
-
-
diethyl ((2-[(5-chloro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)methyl]cyclopent-1-en-1-yl)methyl)phosphonate
-
-
diethyl (2-[(5-chloro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)methyl]benzyl)phosphonate
-
-
diethyl [(Z)-4-(5-chloro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)but-2-en-1-yl]phosphonate
-
-
disodium ((2-[(3,4-dihydro-5-methyl-2,4-dioxopyrimidin-1(2H)-yl)methyl]cyclopent-1-en-1-yl)(difluoro)methyl)phosphonate
-
-
disodium ((2-[(3,4-dihydro-5-methyl-2,4-dioxopyrimidin-1(2H)-yl)methyl]cyclopent-1-en-1-yl)methyl)phosphonate
-
-
disodium ((2-[(5-chloro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)methyl]cyclopent-1-en-1-yl)methyl)phosphonate
-
-
disodium (2-[(5-chloro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)methyl]benzyl)phosphonate
-
-
disodium [(Z)-4-(5-chloro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)but-2-en-1-yl]phosphonate
-
-
ethyl 4-(4-chlorophenyl)-2-oxo-6-([(pyridin-4-yl)formohydrazido]methyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-2-oxo-6-([[(5-phenyl-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl)methyl]amino]methyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-2-oxo-6-[[(E)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]methyl]-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-((3-methyl-5-oxo-2H-pyrazol-1(5H)-yl)methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-([(E)-[(4-chlorophenyl)methylidene]amino]methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-([(E)-[(4-methoxyphenyl)methylidene]amino]methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-[([[5-(4-chlorophenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-[([[5-(4-methoxyphenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 4-(4-chlorophenyl)-6-[([[5-(4-methylphenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 6-((1H-imidazol-1-yl)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
-
ethyl 6-((2-aminobenzoyloxy)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetra-hydropyrimidine-5-carboxylate
-
ethyl 6-((benzylamino)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
-
ethyl 6-(benzoyloxymethyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
-
ethyl 6-([(E)-[(4-bromophenyl)methylidene]amino]methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl 6-[([[5-(4-bromophenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
ethyl [3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetate
-
hydrogen [[(1R,2S,4S)-2-(hydroxymethyl)-4-(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)pyrrolidinium-1-yl]methyl]phosphonate
-
-
methyl 1-cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylate
-
methyl 1-cyclopropyl-6-fluoro-4-oxo-7-[4-(phenylacetyl)piperazin-1-yl]-1,4-dihydroquinoline-3-carboxylate
most potent inhibitor
methyl 1-cyclopropyl-6-fluoro-7-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 1-cyclopropyl-6-fluoro-7-[4-(4-nitrobenzene-1-sulfonyl)piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 1-cyclopropyl-6-fluoro-7-[4-(morpholine-4-carbonyl)piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 1-cyclopropyl-6-fluoro-7-[4-[2-(4-methylanilino)-2-oxoethyl]piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 4-(2,3-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2,5-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2,6-dichlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2-(benzyloxy)phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2-fluoro-4-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2-fluorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(2-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(3,4-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(3-(benzyloxy)-4-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(3-(benzyloxy)phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(3-bromo-4,5-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(3-chloro-4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(3-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-(benzyloxy)phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-(dimethylamino) phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-acetoxy-3-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-bromophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-fluoro-3-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-hydroxy-3,5-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-isopropylphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(4-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-(furan-2-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-butyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-ethyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 4-isobutyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 6-methyl-2-oxo-4-(4-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
non-competitive inhibition
methyl 6-methyl-2-oxo-4-(thiophen-2-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 6-methyl-2-oxo-4-(thiophen-3-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate
non-competitive inhibition
methyl 6-methyl-4-(3-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 6-methyl-4-(4-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
non-competitive inhibition
methyl 6-methyl-4-(5-methylfuran-2-yl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 6-methyl-4-(5-methylthiophen-2-yl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 6-methyl-4-(naphthalen-2-yl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
-
methyl 7-(4-acetylpiperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 7-[4-(4-chlorobenzene-1-sulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 7-[4-(4-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl 7-[4-(bromoacetyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
methyl-4-((2-(2-(2-methyl-1H-indol-3-yl)acetyl)hydrazono)methyl)benzoate
-
N'-(2,3-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(2,4-dichlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(2,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(2,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(2-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(2-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(3,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3,5-dichloro-2-hydroxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3-aminobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(3-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3-hydroxy-4-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(4-(dimethylamino)benzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(4-(dimethylamino)benzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(4-chlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(4-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(4-hydroxy-3,5-dimethoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(4-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(5-bromo-2-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-(anthracen-9-ylmethylene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
N'-[(E)-(5-chloro-2-hydroxyphenyl)methylidene]-4-hydroxybenzohydrazide
12.4% inhibition at 0.5 mM
N'-[(E)-[4-(dimethylamino)phenyl]methylidene]4-hydroxylbenzohydrazide
20% inhibition at 0.5 mM
N-((5-(4-chlorophenyl)-2-thioxo-1,3,4-oxadiazole-3(2H)-yl)methyl)3(trifluoromethyl) benzamide
-
N-(2-bromophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
N-(2-chlorophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
N-(3,4-dichlorophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
N-(3-bromophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
N-(4-bromophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
N-(4-oxo-2-sulfanylidene-8-[[4-(trifluoromethyl)phenyl]methyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea
-
N-(8-benzyl-4-oxo-2-sulfanylidene-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea
-
N-(adamantan-1-yl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
N-[(E)-(2,3-dihydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
99.9% inhibition at 0.5 mM
N-[(E)-(2,4-dichlorophenyl)methylidene]-4-hydroxylbenzohydrazide
20% inhibition at 0.5 mM
N-[(E)-(3,4-dihydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
uncompetitive inhibition, 99.3% inhibition at 0.5 mM
N-[(E)-(3,5-dibromo-2-hydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
non-competitive inhibition, 99.9% inhibition at 0.5 mM
N-[(E)-(3-chlorophenyl)methylidene]-4-hydroxylbenzohydrazide
99% inhibition at 0.5 mM
N-[(E)-(4-bromophenyl)methylidene]-4-hydroxylbenzohydrazide
uncompetitive inhibition, 96.6% inhibition at 0.5 mM
N-[(E)-(4-chlorophenyl)methylidene]-4-hydroxylbenzohydrazide
uncompetitive inhibition, 99% inhibition at 0.5 mM
N-[(E)-(5-bromo-2-hydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
38.6% inhibition at 0.5 mM
N-[(E)-1-(2,4-dihydroxylphenyl)ethylidene]-4-hydroxylbenzohydrazide
30% inhibition at 0.5 mM
N-[(E)-1-(2,5-dihydroxylphenyl)ethylidene]-4-hydroxylbenzohydrazide
99.3% inhibition at 0.5 mM
N-[(E)-1-(2,5-dihydroxylphenyl)propylidene]-4-hydroxylbenzohydrazide
uncompetitive inhibition, 99% inhibition at 0.5 mM
N-[(E)-1-(2,6-dihydroxylphenyl)ethylidene]-4-hydroxylbenzohydrazide
uncompetitive inhibition, 93% inhibition at 0.5 mM
N-[(E)-[3,4-bis(methoxy)phenyl]methylidene]-4-hydroxylbenzohydrazide
99% inhibition at 0.5 mM
N-[(E)-[3-ethoxy-2-hydroxylphenyl]methylidene]-4-hydroxylbenzohydrazide
82.4% inhibition at 0.5 mM
TAS-102
is a combination of trifluridine (FTD, a fluorinated thymidine analogue) and tipiracil hydrochloride (TPI, a TP inhibitor) at a 1:0.5 molar ratio. The FTD monophosphate metabolite trifluoromethyl deoxyuridine 5'-monophosphate inhibits TS by binding to its active site, but the inhibition is rapidly reversible. Phosphorylation of trifluoromethyl deoxyuridine 5'-monophosphate results in the formation of trifluoromethyl deoxyuridine 5'-triphosphate that is misincorporated into DNA. Importantly, the concentration of FTD incorporated into DNA is approximately 300fold higher than that of 5FU. FTD is rapidly degraded by TP to its inactive metabolite (5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione). Thus, the main mechanism of action of TAS-102 is its misincorporation into DNA. Tipiracil inhibits the main catabolic pathway of the drug, thus enhancing its half-life and cytotoxicity
trifluridine
FTD, is rapidly degraded by TP to its inactive metabolite, 5-trifluoromethyl-2,4(1H,3H)-pyrimidinedione
[(2S,3aR,4R,6R,6aR)-4-(5-chloro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-6-(hydroxymethyl)tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]phosphonic acid
-
-
[(2S,4R,5S)-5-(2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxy-1,3-oxazolidin-2-yl]phosphonic acid
-
-
[(3aR,4R,6R,6aR)-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-6-(hydroxymethyl)tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]phosphonic acid
-
-
[(3aR,4R,6R,6aR)-4-(hydroxymethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]phosphonic acid
-
-
[2-[(3S)-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]-2-oxoethyl]phosphonic acid
-
41% inhibition at 0.01 mM
[5-[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethoxy]pentyl]phosphonic acid
-
86% inhibition at 0.01 mM
[6-[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethoxy]hexyl]phosphonic acid
-
79% inhibition at 0.01 mM
[[(1R)-2-(5-ethyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-(fluoromethyl)ethoxy]methyl]phosphonic acid
[[(2R,3aR,6aR)-6-(4-amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-4-(hydroxymethyl)hexahydrofuro[3,4-b]furan-2-yl]methyl]phosphonic acid
-
[[(2R,4R)-2-(hydroxymethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]methyl]phosphonic acid
-
83% inhibition at 0.01 mM
[[(2R,4S)-2-(hydroxymethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
-
98% inhibition at 0.01 mM
[[(2R,4S)-2-(hydroxymethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]methyl]phosphonic acid
-
complete inhibition at 0.01 mM
[[(2S,3aR,6aR)-6-(4-amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-4-(hydroxymethyl)hexahydrofuro[3,4-b]furan-2-yl]methyl]phosphonic acid
-
[[(2S,3aR,6aS)-4-(4-amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-6-(hydroxymethyl)hexahydrofuro[3,4-b]furan-2-yl]methyl]phosphonic acid
-
[[(2S,4S)-2-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonothioyl]phosphonic acid
-
complete inhibition at 0.01 mM
[[(2S,4S)-2-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
-
complete inhibition at 0.01 mM
[[(3R,4R)-3-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
-
96% inhibition at 0.01 mM
[[(3R,4R)-3-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]methyl]phosphonic acid
-
99% inhibition at 0.01 mM
[[(3S)-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonothioyl]phosphonic acid
-
91% inhibition at 0.01 mM
[[(3S)-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
-
97% inhibition at 0.01 mM
[[(3S)-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]methyl]phosphonic acid
-
71% inhibition at 0.01 mM
[[(3S,4R)-3-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
-
-
[[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-(prop-2-en-1-yloxy)ethoxy]methyl]phosphonic acid
-
90% inhibition at 0.01 mM
[[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-phenoxyethoxy]methyl]phosphonic acid
-
99% inhibition at 0.01 mM
[[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethoxy](phenyl)methyl]phosphonic acid
-
91% inhibition at 0.01 mM
(2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one
KIN59
(2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one
KIN59
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
93% inhibition at 0.01 mM
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
at 0.01 mM, 82% inhibition of V79 cell-expressed thymidine phosphorylase, 56% inhibition of thymidine phosphorylase from placenta
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
98% inhibition at 0.01 mM
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
at 0.01 mM, 84% inhibition of V79 cell-expressed thymidine phosphorylase, 84% inhibition of thymidine phosphorylase from placenta
([(1R)-2-fluoro-1-[(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
-
([(1R)-2-fluoro-1-[(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
-
([(1R)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
98% inhibition at 0.01 mM
([(1R)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase
([(1R)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
complete inhibition at 0.01 mM
([(1R)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
at 0.01 mM, 91% inhibition of V79 cell-expressed thymidine phosphorylase, 79% inhibition of thymidine phosphorylase from placenta
([(1S)-2-fluoro-1-[(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
-
([(1S)-2-fluoro-1-[(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
-
([(1S)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
93% inhibition at 0.01 mM
([(1S)-2-fluoro-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase
([(1S)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
94% inhibition at 0.01 mM
([(1S)-2-hydroxy-1-[(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
at 0.01 mM, complete of V79 cell-expressed thymidine phosphorylase, 95% inhibition of thymidine phosphorylase from placenta
([2,2,2-trifluoro-1-[(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
-
([2,2,2-trifluoro-1-[(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl]ethoxy]methyl)phosphonic acid
-
-
1-[2-(phosphonomethoxy)ethyl]thymine
-
at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase, 85% inhibition of thymidine phosphorylase from placenta
2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
2-deoxy-alpha-D-ribose 1-phosphate
dRib-1-P , a non-competitive product inhibitor of the forward reaction, in the reverse reaction, dRib-1-P enhanced the binding of thymine
2-deoxy-alpha-D-ribose 1-phosphate
dRib-1-P is a competitive product inhibitor of the forward reaction, in the reverse reaction, dRib-1-P enhances the binding of thymine
2-deoxy-D-ribose
-
product inhibition
2-mercapto-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one
-
25% inhibition at 0.045 mM
2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
-
2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
-
2-phenyl-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
-
2-phenyl-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
-
4-(2,5-difluorobenzyl)-N-(4-(trifluoromethyl)phenyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(4-(trifluoromethyl)phenyl)piperazine-1-carbothioamide
-
5'-O-trityl-inosine
-
i.e. KIN59, IC50: 0.044 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
5'-O-trityl-inosine
-
IC50: 0.044 mM, reversible, noncompetitive inhibition with respect to thymidine and phosphate
5'-O-trityl-inosine
-
i.e. KIN59, IC50: 0.067 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
5'-O-tritylinosine
i.e. KIN59, noncompetitive. Inhibitor docking and conformational changes, molecular modeling using the crystal structure of the enzyme, molecular dynamics simulations, binding site and mode, overview
5'-O-tritylinosine
-
i.e. KIN59, a small-molecule inhibitor. KIN59 not only prevents the formation of new blood vessels but also promotes the degradation of small pre-existing immature blood vessels, not due to unspecific cell toxicity
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride
TPI
5-chloro-6-[1-(imminopyrrolidinyl)methyl]uracil hydrochloride
-
i.e. TPI, competitive
5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil
-
i.e. AIFU, synthesis, overview, uncompetitive with respect to phosphate, acts as transition state analogs, mimicking the anionic thymine leaving group anchored by their protonated side chains to the enzyme-bound phosphate by electrostatic and H-bonding interactions, modeling of ligand binding at the active site, overview
5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil
i.e. AIFU, synthesis, overview, uncompetitive with respect to phosphate, acts as transition state analogs, mimicking the anionic thymine leaving group anchored by their protonated side chains to the enzyme-bound phosphate by electrostatic and H-bonding interactions, modeling of ligand binding at the active site, overview
5-fluorouracil
5-FU, is an anticancer drug, which inhibits human thymidine phosphorylase (hTP) and plays a key role in maintaining the process of DNA replication and repair. It is involved in regulating pyrimidine nucleotide production, by which it inhibits the mechanism of cell proliferation and cancerous tumor growth. In the cell, 80% of 5-FU is metabolized by dihydropyrimidine dehydrogenase (DPD)
5-fluorouracil
5FU, 5-fluorouracil pharmacodynamics, overview. 5FU catabolism is driven by the activity of dihydropyrimidine dehydrogenase (DPD). The expression of the enzymes orotate phosphoribosyl transferase (OPRT), TK, TP, TS and DPD has been demonstrated to influence 5FU activity both in in vitro and in vivo models. 5-Fluoro-2'-deoxyuridine (FUdR), an active antiblastic drug as it can be converted to FdUMP by thymidine kinase (TK), resulting in thymidylate synthase (TS) blockade. FUdR can be hydrolyzed by TP completing the three-step process from capecitabine to 5FU
6-[(2'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
-
IC50: below 0.0000206 mM
6-[(2'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
IC50: below 0.000049 mM
7-deazaxanthine
-
docking conformation of the standard inhibitor in the active site of thymidine phosphorylase, modeling, overview. Modeling of the three-dimensional structures of piperazine derivatives
ribose 1-phosphate
-
20% inactivation at 1.5 mM
thymidine
yields a non-competitive inhibition pattern in agreement with a random mechanism
thymine
thymine is a product activator, but becomes a substrate inhibitor at concentrations eight times higher than its Km. Thymine is an effector rather than a product inhibitor
thymine
thymine is a product activator, but becomes a competitive inhibitor at concentrations eight times higher than its Km
uridine
-
competitive 27% inactivation at 1 mM
[8-(2,4-dioxo-2,3,4,6-tetrahydro-1H-pyrrolo[3,4-d]pyrimidin-1-yl)octyl]phosphonic acid
-
-
[8-(2,4-dioxo-2,3,4,6-tetrahydro-1H-pyrrolo[3,4-d]pyrimidin-1-yl)octyl]phosphonic acid
-
no antitumor activity found with CCRF-CEM T-lymphoblastoid cells, human promyelocytic leukemia HL-60 cells, human cervix carcinoma HeLa S3 cells
[8-(2,4-dioxo-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]phosphonic acid
-
-
[8-(2,4-dioxo-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]phosphonic acid
-
no antitumor activity found with CCRF-CEM T-lymphoblastoid cells, human promyelocytic leukemia HL-60 cells, human cervix carcinoma HeLa S3 cells
[[(1R)-2-(5-ethyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-(fluoromethyl)ethoxy]methyl]phosphonic acid
-
-
[[(1R)-2-(5-ethyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-(fluoromethyl)ethoxy]methyl]phosphonic acid
-
-
[[2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid
-
-
[[2-(5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid
-
-
[[2-(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid
-
complete inhibition at 0.01 mM
[[2-(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid
-
at 0.01 mM, complete inhibition of V79 cell-expressed thymidine phosphorylase, 82% inhibition of thymidine phosphorylase from placenta
additional information
-
photoinactivation in presence of thymine, thymidine and some halogenated analogs
-
additional information
-
not inhibited by 5-chloro-6-methyl-3H-pyrimidin-4-one, 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]-3H-pyrimidin-4-one, 6H-imidazo[1,2-c]pyrimidin-5-one, 7H-pyrrolo[2,3-d]pyrimidin-2(1H)-one, and 7H-pyrrolo[2,3-d]pyrimidine
-
additional information
-
Schiff bases of 3-formylchromone as thymidine phosphorylase inhibitors, no inhibition by 3-formylchromone and 3-methyl-7-hydroxychromone, and by derivatives 3-[(4-pyridinylimino) methyl]-4H-chromen-4-one, 3-[(3-pyridinylimino) methyl]-4H-chromen-4-one, 3-([(3-methoxyphenyl)imino]methyl)-4H-chromen-4-one, 3-([(2-methoxy-4-nitrophenyl) imino] methyl)-4Hchromen-4-one, 2-([-(4-oxo-4H-chromen-3-yl) methylidene]amino)benzoic acid, 3-([(4-methylphenyl)imino]methyl)-4H-chromen-4-one, 3-([(2,6-dimethylphenyl)imino]methyl)-4H-chromen-4-one, and 3-[bis(tert-butylamino)methyl]-4H-chromen-4-one, overview
-
additional information
-
design of benzopyrazine analogues as potent inhibitors of thymidine phosphorylase, synthesis of quinoxaline derivatives, overview. No inhibition by (E)-2-(2-(2-nitrobenzylidene)hydrazinyl)quinoxaline, (E)-2-(2-(4-nitrobenzylidene)hydrazinyl)quinoxaline, (E)-2-(2-(2-methylbenzylidene)hydrazinyl)quinoxaline, (E)-2-(2-(3-methylbenzylidene)hydrazinyl)quinoxaline, (E)-2-(2-(4-methylbenzylidene)hydrazinyl)quinoxaline, (E)-5-methoxy-2-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol, (E)-2-methoxy-5-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol, (E)-2-(2-(3-methoxybenzylidene)hydrazinyl)quinoxaline, (E)-2-(2-(4-methoxybenzylidene)hydrazinyl)quinoxaline, (E)-2-(2-(pyridin-3-ylmethylene)hydrazinyl)quinoxaline, (E)-2-(2-(pyridin-4-ylmethylene)hydrazinyl)quinoxaline, (E)-2-(2-((1H-indol-3-yl)methylene)hydrazinyl)quinoxaline, and (E)-2-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
-
additional information
thymidine esters as substrate analogue inhibitors of angiogenic enzyme thymidine phosphorylase (TP) in vitro, molecular docking studies, erview. Thymidine is functionalized to develop TP inhibitors, derivatization of thymidine at C-5'/3' hydroxyl groups by reacting with different substituted benzoyl chlorides to produce corresponding esters for biological evaluation against TP activity. The pyrimidine moiety makes hydrogen bonds with Thr123, Gln156 and the bound water molecule while one of the bromobenzyl substitutions shows Pi-cation interaction with Arg171. No inhibition by 5'-O-(benzoyl)-thymidine-3'-O-benzoate, 5'-O-(4''-methyl-3''-nitrobenzoyl)-thymidine-3'-O-4''-methyl-3''-nitrobenzoate, 5'-O-(4''-methylbenzoyl)-thymidine-3'-O-4''-methylbenzoate, 5'-O-(3''-methylbenzoyl)-thymidine-3'-O-3''-methylbenzoate, 5'-O-(2''-methylbenzoyl)-thymidine-3'-O-2''-methylbenzoate, 5'-O-(3''-methoxybenzoyl)-thymidine-3'-O-3''-methoxybenzoate, 5'-O-(4''-fluorobenzoyl)-thymidine-3'-O-3''-fluorobenzoate, 5'-O-(4''-nitrobenzoyl)-thymidine-3'-O-4''-nitrobenzoate
-
additional information
synthesis and molecular docking study of piperazine derivatives as potent inhibitor of thymidine phosphorylase, overview
-
additional information
design, synthesis, in-vitro thymidine phosphorylase inhibition, in-vivo antiangiogenic and in-silico studies of C-6 substituted dihydropyrimidines, molecular docking study, overview. No inhibition by ethyl 4-(4-chlorophenyl)-6-((4-nitrobenzoyloxy)methyl)-2-oxo-1,2,3,4-tetra-hydropyrimidine-5-carboxylate, ethyl 4-(4-chlorophenyl)-6-([(E)-[(4-nitrophenyl)methylidene]amino]methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate, 5-acetyl-4-(4-chlorophenyl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one, ethyl 4-(3,4-dihydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate, 5-acetyl-1,6-dimethyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one, 5-acetyl-1,6-dimethyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one, ethyl 1-benzyl-6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate, ethyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate, 5-acetyl-6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one, ethyl 4-(3-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate, and 5-acetyl-4-(3-hydroxyphenyl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one
-
additional information
synthesis of 1,2,4-triazoles as thymidine phosphorylase inhibitors and possible future anti-tumor drugs for treatment of human disease. Molecular docking study. Cytoxicity study. No inhibition by 5-(4-methylphenyl)-4H-1,2,4-triazole-3-thiol, 5-(4-nitrophenyl)- 4H-1,2,4-triazole-3-thiol, 5-(4-methylphenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione, 5-(3,4,5-trimethoxyphenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione, 5-(3-chlorophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione, 5-(4-chlorophenyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione, and 2-[(5-phenyl-4H-1,2,4-triazol-3-yl)thio]acetic acid
-
additional information
in vitro study of thymidine phosphorylase inhibition, overview. Sixteen analogs of N-benzyliden-isoquinoline-3-carbohydrazide are synthesized and evaluated their inhibitory activity against thymidine phosphorylase enzyme, molecular docking study using structure with PDB ID 4EAD as template. No inhibition by (Z)-N'-(3-methoxy-4-(phenoxymethyl)benzylidene)isoquinoline-3-carbohydrazide
-
additional information
-
in vitro study of thymidine phosphorylase inhibition, overview. Sixteen analogs of N-benzyliden-isoquinoline-3-carbohydrazide are synthesized and evaluated their inhibitory activity against thymidine phosphorylase enzyme, molecular docking study using structure with PDB ID 4EAD as template. No inhibition by (Z)-N'-(3-methoxy-4-(phenoxymethyl)benzylidene)isoquinoline-3-carbohydrazide
-
additional information
synthesis of indole-based acetohydrazide derivatives as inhibitors and molecular docking study using structure with PDB ID 4EAD as template, re-docking of the original ligand 3'-azido-2'-fluoro-dideoxyuridine into the active site. No inhibition by N'-(2,4-dimethoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
additional information
an array of structurally diverse non-nucleobase derivatives has beens designed, synthesized and established as promising TP inhibitors, structure-function analysis, overview
-
additional information
natural compounds as angiogenic enzyme thymidine phosphorylase inhibitors, in vitro biochemical inhibition, mechanistic, and in silico modeling and molecular docking studies, enzyme-bound structure modelling, overview. No inhibition by 4',5,7-trihydroxyflavone, 5,7-dihydroxyflavone, 9,10-dimethoxy-5,6,9,12-tetrahydro-2H-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-7-ium, [(1R,9aR)-octahydro-2H-quinolizin-1-yl]methanol, 3,4,5-trihydroxybenzoic acid, and 4-hydroxy-3-methoxybenzoic acid. Cytotoxicity MTT assay on 3T3 cell line
-
additional information
-
a specific thymidine phosphorylase inhibitor TPI completely inhibits
-
additional information
-
iodination reduces activity, 63% inactivation after 5 min and complete inactivation after 20 min
-
additional information
-
thymidine phosphorylase and its degradation product 2-deoxy-D-ribose suppress hypoxia-induced apoptosis, the upregulation of hypoxia-inducible factor 1alpha and the proapoptotic factor, BNIP3, and caspase 3 activation induced by hypoxia
-
additional information
-
thymidine phosphorylase promoter methylation is a mechanism for down-regulation of enzyme expression in cancer cells
-
additional information
-
not inhibited by 1-[(4S,5R)-4-hydroxyisoxazolidin-5-yl]-5-methylpyrimidine-2,4(1H,3H)-dione
-
additional information
-
capecitabine does not affect enzyme activity and expression
-
additional information
-
synthesis of 5-alkyl, 5-aryl, or 5-fluoro derivatives of 1-[2-(phosphonomethoxy)-ethyl]thymine inhibitors that mimic the interatomic distance between the incoming phosphate and leaving pyrimidine groups at the transition state for the putative SN2 mechanism of thymidine phosphorylase, structures, the inhibitors are not effective compared to (phosphonomethoxy)-alkyl-pyrimidine inhibitors, overview. Switching the N1-linked side chains found in 1-[2-(phosphonomethoxy)-ethyl]thymine, 1-[(R)-3-hydroxy-2-(phosphonomethoxy)propyl]thymine and 1-[(R)-3-fluoro-2-(phosphonomethoxy)propyl]thymine to the N3-position of the nucleobases resulted in significant loss of activity. Replacement of the iminopyrrolidine ring found in 5-ethyl-1-[(R)-3-hydroxy-2-(phosphonomethoxy)propyl]uracil with a 3-methylimidazol-3-ium ring leads to a series of less active 5-halo-6-[(3-methylimidazol-3-ium-1-yl)methyl]-uracil chlorides. On the other hand, replacement with a 2-aminoimidazole ring, leads to a number of 6-[(2-aminoimidazol-1-yl)methyl]-5-chloro-(and 5-bromo)uracil hydrochlorides with similar inhibitory strength compared to 5-ethyl-1-[(R)-3-hydroxy-2-(phosphonomethoxy)propyl]uracil, computer-modeling simulations, overview
-
additional information
-
enzyme inhibitors can abrogate the tumorigenic and metastatic properties of the enzyme, e.g. 2-deoxy-L-ribose, which does not inhibit the enzyme but affects its biological functions
-
additional information
comparison of binding structures of 5-FU and its derivatives to human thymidine phosphorylase and dihydropyrimidine dehydrogenase (DPD), analysis of strategies to reduce drug binding to DPD to decrease the required dose of 5-FU. hTP can still undergo open-closed conformations in the absence of the ligand, but the presence of a positively charged ligand better stabilizes the closed conformation and rigidifies the core region of the protein more than unliganded or neutral liganded system. Molecular dynamics simulations, overview. One of the three hinge segments linking the two major alpha and alpha/beta domains of the hTP is an important contributing factor to the enzyme's open-close conformational twist during its inactivation-activation process. In addition, the angle between the alpha/beta-domain and the alpha-domain has shown to undergo wide rotations over the course of MD simulation in the absence of a phosphate, suggesting that it contributes to the stabilization of the closed conformation of the hTP
-
additional information
-
comparison of binding structures of 5-FU and its derivatives to human thymidine phosphorylase and dihydropyrimidine dehydrogenase (DPD), analysis of strategies to reduce drug binding to DPD to decrease the required dose of 5-FU. hTP can still undergo open-closed conformations in the absence of the ligand, but the presence of a positively charged ligand better stabilizes the closed conformation and rigidifies the core region of the protein more than unliganded or neutral liganded system. Molecular dynamics simulations, overview. One of the three hinge segments linking the two major alpha and alpha/beta domains of the hTP is an important contributing factor to the enzyme's open-close conformational twist during its inactivation-activation process. In addition, the angle between the alpha/beta-domain and the alpha-domain has shown to undergo wide rotations over the course of MD simulation in the absence of a phosphate, suggesting that it contributes to the stabilization of the closed conformation of the hTP
-
additional information
synthesis, thymidine phosphorylase inhibitory and computational study of 1,3,4-oxadiazole-2-thione derivatives as potential anticancer agents. Determination of growth inhibition of MCF-7 cells, and analysis of toxicity and pharmacokinetics in the human body. Docking study using the ligand-bound TP structure (PDB ID 1UOU). Structure-function analysis. Electron withdrawing groups at R1 position of phenyl ring and less bulky amines group at R2 position have better anticancer activity. Amine groups at R2 position play an important role in binding to the active site residues of enzyme TP
-
additional information
an array of structurally diverse non-nucleobase derivatives has been designed, synthesized, and established as promising TP inhibitors, structure-function analysis, docking studies, overview. Analysis of oxadiazole and imidazolidine derivatives, pyrazolone and pyrazolo [1,5-a] [1,3,5]triazine analogues, 1,2,4-triazolo [1,5-a] [1,3,5]triazine analogues, quinazoline and quinoxaline derivatives, chromone and isocoumarin derivatives, and plant glycosides
-
additional information
synthesis and biological evaluation of 1-(aryl-aldehyde-oxime)uracil derivatives as a class of thymidine phosphorylase inhibitors, molecular docking and binding energies, overview. The crystal structure of thymidine phosphorylase (PDB ID 1UOU) is used as protein receptor in molecular docking
-
additional information
designed as transition-state analogues by mimicking the oxacarbenium ion, the pyrimidine-2,4-diones are synthesized and evaluated as inhibitors of hTP activity, kinetic mechanisms for the most potent molecule and evaluation of the interaction mode using molecular docking, overview
-
additional information
-
designed as transition-state analogues by mimicking the oxacarbenium ion, the pyrimidine-2,4-diones are synthesized and evaluated as inhibitors of hTP activity, kinetic mechanisms for the most potent molecule and evaluation of the interaction mode using molecular docking, overview
-
additional information
synthesis of isoquinoline-base-oxadiazole derivatives as potent inhibitors of thymidine phosphorylase and molecular docking study, overview. Twenty derivatives of isoquinoline bearing oxadiazole are characterized through different spectroscopic techniques such as HREI-MS, 1H-NMR and 13C-NMR and evaluated for thymidine phosphorylase inhibition, structure-activity relationships study
-
additional information
not inhibited by pyrimethamine, fludarabine phosphate, lamivudine, adefovir depivoxil, 5-azacytidine, azathioprine, arabinosyl adenine, zalcitabine, caffeine, 7-(2,3-dihydroxypropyl)theophylline, theophylline, allopurinol, 6-mercaptopurine, and valacyclovir
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
2-deoxy-alpha-D-ribose 1-phosphate
dRib-1-P , a noncompetitive product inhibitor of the forward reaction, in the reverse reaction, dRib-1-P enhanced the binding of thymine
doxorubicin
thymidine phosphorylase expression is upregulated after treatment with 60 mg/m2 doxorubicin
epirubicin
thymidine phosphorylase expression is upregulated after treatment with 75 mg/m2 epirubicin
interferon alpha2b
-
induces thymidine phosphorylase mRNA and protein expression in a dose-dependent manner
-
interferon beta
-
causes a rapid and transient increase of thymidine phosphorylase expression
-
interferon gamma
-
causes a rapid and transient increase of thymidine phosphorylase expression
-
interleukin-1beta
-
the expression of tyhmidine phosphorylase mRNA is significantly increased by stimulation with interleukin-1beta
-
thymine
thymine is a product activator, but becomes a substrate inhibitor at concentrations eight times higher than its Km. Competitive substrate inhibition at high concentration for the human liver TP
cyclophosphamide
thymidine phosphorylase expression is upregulated after treatment with 600 mg/m2 cyclophosphamide
interferon alpha
-
causes a rapid and transient increase of thymidine phosphorylase expression
-
paclitaxel
-
the expression of thymidine phosphorylase mRNA is up-regulated by the administration of paclitaxel (20 mg/kg)
paclitaxel
the expression of thymidine phosphorylase mRNA is up-regulated by the administration of paclitaxel (20 mg/kg)
Tumor necrosis factor alpha
-
causes a rapid and transient increase of thymidine phosphorylase expression
-
Urea
-
stimulates at low concentration, inhibits at high concentration, 4 M
additional information
-
the enzymatic activity of thymidine phosphorylase is required for the activation of 5-fluorouracil prodrugs, the enzyme induces the expression of several matrix metalloproteinases, increases the levels of hypoxia-inducible factor 1alpha during in vitro hypoxia
-
additional information
-
no activation of protein expression by paclitaxel, therefore no increased haematotoxicity due to thymidine phosphorylase upregulation is expected from the combination of taxanes and capecitabine
-
additional information
-
heterogeneous ribonucleoprotein K regulates thymidine phosphorylase mRNA stability
-
additional information
-
thymidine phosphorylase expression is not up-regulated after docetaxel treatment
-
additional information
-
50.4 Gy radiation in combination with capecitabine leads to elevated thymidine phosphorylase activity
-
additional information
-
preoperative radiotherapy (cumulative dose of 45 Gy) and concomitant capecitabine (825 mg/m2) treatment induce 2.3fold increase of thymidine phosphorylase mRNA levels
-
additional information
-
gliostatin has a role in regulating vascular endothelial growth factor
-
additional information
-
thymidine phosphorylase demonstrates differential expression depending on age, there is no remarkable difference in the mRNA and protein expression of thymidine phosphorylase due to the response in chemotherapy with TS-1
-
additional information
-
capecitabine does not affect enzyme activity and expression
-
additional information
-
the enzyme is activated in several diseases, detailed overview
-
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.35
1-(2',6'-dideoxy-alpha-L-lyxo-hexafuranosyl)thymine
25°C, pH 6.5
0.35
1-(2',6'-dideoxy-alpha-L-lyxohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.3
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.33
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.4
3'-amino-3'-deoxythymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.35
3'-deoxy-2',3'-didehydrothymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.28
4-thiothymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.4
5'-amino-5'-deoxythymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.4
5'-Deoxythymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.16
5-nitro-2'-deoxyuridine
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.23
5-nitro-2'-deoxyuridine
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
additional information
additional information
kinetic mechanism and regulation of native human hepatic thymidine phosphorylase (TP), kinetics
-
additional information
additional information
-
kinetic mechanism and regulation of native human hepatic thymidine phosphorylase (TP), kinetics
-
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.45
1-(2',6'-dideoxy-alpha-L-lyxo-hexafuranosyl)thymine
25°C, pH 6.5
0.45
1-(2',6'-dideoxy-alpha-L-lyxohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.1
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.6
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
1.1
3'-amino-3'-deoxythymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.4
3'-deoxy-2',3'-didehydrothymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
63
4-thiothymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.58
5'-amino-5'-deoxythymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
260
5'-Deoxythymidine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
20
5-nitro-2'-deoxyuridine
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
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kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.2385
(6aS)-1,2,9,10-tetramethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline
pH 7.0, 30°C
0.45
1-(2'-deoxy-beta-D-threo-pentafuranosyl)thymine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
1.5
1-(2-hydroxyethoxymethyl)thymine
-
pH 7.5, 25°C, activity with 4-thiothymidine
0.044
4,4'-[(2R,3S)-2,3-dimethylbutane-1,4-diyl]di(benzene-1,2-diol)
pH 7.0, 30°C
0.0114
5'-O-(3''-bromobenzoyl)-thymidine
pH not specified in the publication, 30°C
0.0078
5'-O-(4''-bromobenzoyl)-thymidine-3'-O-4''-bromobenzoate
pH not specified in the publication, 30°C
0.0128
5'-O-(4''-methoxybenzoyl)-thymidine
pH not specified in the publication, 30°C
0.0125
5'-O-(4''-methylbenzoyl)-thymidine
pH not specified in the publication, 30°C
0.017
5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride
-
in 50 mM Tris, 1 mM EDTA, pH 7.4, at 37°C
0.001
5-fluoro-6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
0.00037
5-fluoro-6-[(4H-1,2,4-triazol-4-ylamino)methyl]pyrimidine-2,4(1H,3H)-dione
-
-
0.0088
6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
0.2952
6-methoxy-2-oxo-2H-1-benzopyran-7-yl 6-O-[(2R,3R,4R)-3,4-dihydroxy-4-(hydroxymethyl)oxolan-2-yl]-beta-D-glucopyranoside
pH 7.0, 30°C
0.1811
8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b']dipyran-2-one
pH 7.0, 30°C
0.005
hydrogen [[(1R,2S,4S)-2-(hydroxymethyl)-4-(5-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)pyrrolidinium-1-yl]methyl]phosphonate
-
-
0.17665
N-[(E)-(3,4-dihydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
at pH 7.0 and 30°C
0.00175
N-[(E)-(3,5-dibromo-2-hydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
at pH 7.0 and 30°C
0.0805
N-[(E)-(4-bromophenyl)methylidene]-4-hydroxylbenzohydrazide
at pH 7.0 and 30°C
0.138
N-[(E)-(4-chlorophenyl)methylidene]-4-hydroxylbenzohydrazide
at pH 7.0 and 30°C
0.15905
N-[(E)-1-(2,5-dihydroxylphenyl)propylidene]-4-hydroxylbenzohydrazide
at pH 7.0 and 30°C
0.168
N-[(E)-1-(2,6-dihydroxylphenyl)ethylidene]-4-hydroxylbenzohydrazide
at pH 7.0 and 30°C
0.00077
[(2S,3aR,4R,6R,6aR)-4-(5-chloro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-6-(hydroxymethyl)tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]phosphonic acid
-
-
0.004
[(2S,4R,5S)-5-(2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)-3,4-dihydroxy-1,3-oxazolidin-2-yl]phosphonic acid
-
-
0.005
[(3aR,4R,6R,6aR)-4-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-6-(hydroxymethyl)tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]phosphonic acid
-
-
0.01
[(3aR,4R,6R,6aR)-4-(hydroxymethyl)-6-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuro[3,4-d][1,3]dioxol-2-yl]phosphonic acid
-
-
0.0334
[[(2R,3aR,6aR)-6-(4-amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-4-(hydroxymethyl)hexahydrofuro[3,4-b]furan-2-yl]methyl]phosphonic acid
-
0.00105
[[(2S,3aR,6aR)-6-(4-amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-4-(hydroxymethyl)hexahydrofuro[3,4-b]furan-2-yl]methyl]phosphonic acid
-
0.00803
[[(2S,3aR,6aS)-4-(4-amino-5-methyl-2-oxopyrimidin-1(2H)-yl)-6-(hydroxymethyl)hexahydrofuro[3,4-b]furan-2-yl]methyl]phosphonic acid
-
0.01
[[(3S,4R)-3-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
-
-
0.0019
(R)-1-[2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.00396
(R)-1-[2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.00022
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.00034
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.00255
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
enzyme from liver, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.00344
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
enzyme from liver, pH 6.4, 37°C, substrate: phosphate
0.00037
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.00078
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.00232
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
enzyme from liver, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.0027
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
enzyme from liver, pH 6.4, 37°C, substrate: phosphate
0.00068
(S)-1-[2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.001
(S)-1-[2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.0004
(S)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.00064
(S)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.00093
(S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.0013
(S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.00146
1-[2-(phosphono-methoxy)ethyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: 2'-deoxythymidine
0.00173
1-[2-(phosphono-methoxy)ethyl]thymine
-
enzyme from SD-lymphoma, pH 6.4, 37°C, substrate: phosphate
0.6
3'-amino-3'-deoxythymidine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.85
3'-Deoxythymidine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.4
5'-bromo-5'-deoxythymidine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.4
5'-iodo-5'-deoxythymidine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.0002
5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00455
5-benzyl-6-chloropyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00103
5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00165
5-butyl-6-chloropyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0000013
5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4-(1H,3H)-pyrimidine
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0000021
5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4-(1H,3H)-pyrimidine
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00002
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride
pH and temperature not specified in the publication
0.4
5-fluoro-1-(tetrahydrofur-2-yl)uracil
-
pH 7.5, 25°C, activity with thymidine
0.45
5-fluoro-1-(tetrahydrofur-2-yl)uracil
-
pH 7.5, 25°C, activity with 4-thiothymidine
0.02
5-phenyl-6-pyrrolidin-1-ylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
5-phenyl-6-pyrrolidin-1-ylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00063
5-[(1E)-but-1-en-1-yl]-6-chloropyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00092
5-[(1E)-but-1-en-1-yl]-6-chloropyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00121
6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00121
6-bromo-5-phenylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00334
6-chloro-5-(1-methylethenyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0051
6-chloro-5-(1-methylethenyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00394
6-chloro-5-(2-naphthyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00459
6-chloro-5-(2-naphthyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00028
6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00054
6-chloro-5-(2-thienyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00127
6-chloro-5-(3,5-dimethylphenyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00174
6-chloro-5-(3,5-dimethylphenyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00071
6-chloro-5-(4-fluorophenyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00097
6-chloro-5-(4-fluorophenyl)pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00042
6-chloro-5-cyclohex-1-en-1-ylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00075
6-chloro-5-cyclohex-1-en-1-ylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0002
6-chloro-5-cyclopent-1-en-1-yluracil
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00029
6-chloro-5-cyclopent-1-en-1-yluracil
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
6-chloro-5-ethylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
6-chloro-5-ethylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0016
6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00465
6-chloro-5-heptylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00106
6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00179
6-chloro-5-hexylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00309
6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00367
6-chloro-5-pentylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0004
6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00043
6-chloro-5-phenylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00402
6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00581
6-chloro-5-propylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00301
6-chloro-5-pyridin-3-ylpyrimidine-2,4(1H,3H)-dione hydrochloride
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00399
6-chloro-5-pyridin-3-ylpyrimidine-2,4(1H,3H)-dione hydrochloride
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00049
6-chloro-5-[(1E)-1-ethylprop-1-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00091
6-chloro-5-[(1E)-1-ethylprop-1-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00041
6-chloro-5-[(1E)-pent-1-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00091
6-chloro-5-[(1E)-pent-1-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00117
6-chloro-5-[(1E)-prop-1-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00121
6-chloro-5-[(1E)-prop-1-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.00047
6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.0005
6-fluoro-5-phenylpyrimidine-2,4(1H,3H)-dione
-
enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
6-methyl-5-phenylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
6-methyl-5-phenylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
6-[(2-aminoethyl)amino]-5-phenylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from V79 cells, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
0.02
6-[(2-aminoethyl)amino]-5-phenylpyrimidine-2,4(1H,3H)-dione
-
Km above 0.02 mM, enzyme purified from placenta, in 20 mM Bis-Tris-HCl (pH 6.4), at 37°C
additional information
additional information
inhibition kinetics, overview
-
additional information
additional information
-
inhibition kinetics, overview
-
additional information
additional information
inhibition kinetics, Lineweaver-Burk plots
-
additional information
additional information
inhibition kinetics, Lineweaver-Burk plots
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.085
(2,4,5-trioxo-3-phenethyl-imidazolidin-1-yl)ethanoic acid
Escherichia coli
-
pH 7.4, 25°C
0.044
(2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one
Homo sapiens
pH and temperature not specified in the publication
0.264
(3-benzyl-2,4,5-trioxoimidazolidin-1-yl)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.0537
(E)-1-((2-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0156
(E)-1-((4-chlorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0107
(E)-1-((4-ethylphenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0413
(E)-1-((4-fluorophenyl)(hydroxyimino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0334
(E)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0252
(E)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0225
(E)-1-((hydroxyimino)(p-tolyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0373
(E)-1-((hydroxyimino)(phenyl)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0032
(E)-2-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,4-diol
Escherichia coli
-
pH 7.4, 25°C
0.03648
(E)-2-(2-chlorophenyl)-5-styryl-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.05822
(E)-2-(4-chlorophenyl)-5-styryl-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.0355
(E)-3-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2-diol
Escherichia coli
-
pH 7.4, 25°C
0.0091
(E)-4-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2-diol
Escherichia coli
-
pH 7.4, 25°C
0.0086
(E)-4-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,3-diol
Escherichia coli
-
pH 7.4, 25°C
0.0363
(E)-4-methoxy-2-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
Escherichia coli
-
pH 7.4, 25°C
0.0344
(E)-5-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2,4-triol
Escherichia coli
-
pH 7.4, 25°C
0.0469
(E)-5-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-2,4,6-triol
Escherichia coli
-
pH 7.4, 25°C
0.0394
(E)-N'-(2,3-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0086
(E)-N'-(2,4-dichlorobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0184
(E)-N'-(2-cyanobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0113
(E)-N'-(2-nitrobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0081
(E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0361
(E)-N'-(3-cyanobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0161
(E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0184
(E)-N'-(4-chlorobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0222
(E)-N'-(4-cyanobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0214
(E)-N'-(4-nitrobenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0447
(E)-N'-(5-bromo-2-methoxybenzlidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0693
(E)-N'-(anthracen-9-ylmethylen)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0493
(Z)-1-((2-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.00012
(Z)-1-((3,4-dichlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0412
(Z)-1-((3-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0027
(Z)-1-((4-bromophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0014
(Z)-1-((4-chlorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0034
(Z)-1-((4-ethylphenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0441
(Z)-1-((4-fluorophenyl)(hydroxyimino)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0251
(Z)-1-((hydroxyimino)(3-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0165
(Z)-1-((hydroxyimino)(4-methoxyphenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0159
(Z)-1-((hydroxyimino)(m-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0072
(Z)-1-((hydroxyimino)(p-tolyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0214
(Z)-1-((hydroxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0399
(Z)-1-((hydroxyimino)(thiophen-2-yl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.0276
(Z)-N'-(1-(4-nitrophenyl)ethylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0081
(Z)-N'-(3-chloro-4-hydroxybenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0044
(Z)-N'-(4-hydroxy-3,5-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
Escherichia coli
pH 7.4, 25°C
0.0856
1-((methoxyimino)(phenyl)methyl)-6-methylpyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH 8.4, 30°C
0.103
1-(2-phenylethyl)imidazolidine-2,4,5-trione
Homo sapiens
pH and temperature not specified in the publication
0.115
1-benzylimidazolidine-2,4,5-trione
Homo sapiens
pH and temperature not specified in the publication
0.128
1-[(2-methylphenyl)methyl]imidazolidine-2,4,5-trione
Homo sapiens
pH and temperature not specified in the publication
0.04
1H-pyrrolo[2,3-d]pyrimidine-2,4(3H,7H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.1
2,7-bis(methylsulfanyl)[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
Homo sapiens
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.02527
2-(2-chlorophenyl)-5-(2-fluorophenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.02403
2-(2-chlorophenyl)-5-(2-methoxyphenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.02891
2-(2-chlorophenyl)-5-(4-chlorophenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.03449
2-(2-chlorophenyl)-5-(4-nitrophenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.0011
2-(2-methyl-1H-indol-3-yl)-N'-(2,4,6-trihydroxybenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0222
2-(2-methyl-1H-indol-3-yl)-N'-(2-methylbenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0158
2-(2-methyl-1H-indol-3-yl)-N'-(2-nitrobenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0411
2-(2-methyl-1H-indol-3-yl)-N'-(3-methylbenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0222
2-(2-methyl-1H-indol-3-yl)-N'-(3-nitrobenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0381
2-(2-methyl-1H-indol-3-yl)-N'-(4-methylbenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0132
2-(2-methyl-1H-indol-3-yl)-N'-(4-nitrobenzylidene)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.256
2-(3'-ethoxy-4'-hydroxyphenyl)quinazolin-4(3H)-one
Escherichia coli
-
at pH 7.0 and 30°C
0.1688
2-(3'-hydroxy-4'-methoxyphenyl)quinazolin-4(3H)-one
Escherichia coli
-
at pH 7.0 and 30°C
0.01084
2-(3,4-dichlorophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0429
2-(3,4-dihydroxyphenyl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.03178
2-(3-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.03442
2-(3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.01309
2-(4-bromo-3-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.02206
2-(4-bromophenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.03271
2-(4-chlorophenyl)-5-(2-fluorophenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.05249
2-(4-chlorophenyl)-5-(2-methoxyphenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.05047
2-(4-chlorophenyl)-5-(4-nitrophenyl)-1,3,4-oxadiazole
Homo sapiens
at pH 7.4 and 25°C
0.03158
2-(4-methylphenyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.05538
2-(benzylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.03637
2-(diphenylmethyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.03154
2-(furan-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.05167
2-(methylsulfanyl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.1
2-(methylsulfanyl)-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
Homo sapiens
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.1
2-(methylsulfanyl)[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione
Homo sapiens
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.02453
2-(pyridin-2-yl)-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.3892
2-11 methyl 4-(4-ethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.013 - 0.04332
2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
0.03956
2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
0.1
2-phenyl-7-sulfanylidene-6,7-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
Homo sapiens
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.0462
2-phenylquinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.1
2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazine-5,7(4H,6H)-dione
Homo sapiens
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.05988
2-[(2-phenylethyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.013
2-[(3,4-dichlorophenyl)methyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.05925
2-[(3-phenylpropyl)sulfanyl]-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.1634
2-[(5-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
Escherichia coli
pH 7.4, 25°C
0.0946
2-[(5-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]propanoic acid
Escherichia coli
pH 7.4, 25°C
0.0439
2-[(5-(4-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
Escherichia coli
pH 7.4, 25°C
0.2206
2-[(5-(4-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]propanoic acid
Escherichia coli
pH 7.4, 25°C
0.1438
2-[(5-(4-methylphenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
Escherichia coli
pH 7.4, 25°C
0.0645
2-[(5-(4-nitrophenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
Escherichia coli
pH 7.4, 25°C
0.013
2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-7-phenyl-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.037
3,3'-(1,3,4-oxadiazole-2,5-diyl)dipyridine
Homo sapiens
pH and temperature not specified in the publication
0.0446
3-(((4-chlorophenyl)amino)methyl)-5-(2-iodophenyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.1833
3-((4-benzylpiperazin-1-yl)methyl)-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0547
3-((5-(4-chlorophenyl)-2-thioxo-1,3,4-oxadiazol-3(2H)-yl)methyl)thiazolidine-2,4-dione
Homo sapiens
pH 7.4, 25°C
0.0303
3-((benzylamino)methyl)-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.04
3-(2,4,5-trioxo-3-phenethyl-imidazolidin-1-yl)-propionamide
Escherichia coli
-
pH 7.4, 25°C
0.106
3-(3-benzyl-2,4,5-trioxoimidazolidin-1-yl)propanamide
Homo sapiens
pH and temperature not specified in the publication
0.1041
3-(anilinomethyl)-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.15
3-([(2-([-(4-oxo-4H-chromen-3-yl)methylidene]amino)ethyl)imino] methyl)-4H-chromen-4-one
Escherichia coli
-
pH 7.6
0.0237
3-[(2,3-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.1305
3-[(2-chloroanilino)methyl]-5-(2-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.04638
3-[(2-chloroanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.1177
3-[(2-chloroanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.0144
3-[(2-methoxy-6-nitroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH and temperature not specified in the publication
0.08724
3-[(2-methoxyanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.1172
3-[(2-methylanilino)methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.061
3-[(2-methylphenyl)methyl]-1H-2-benzopyran-1-one
Homo sapiens
pH and temperature not specified in the publication
0.1338
3-[(3,4-dichloroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.08319
3-[(3,4-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.0844
3-[(3-methoxyanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.04064
3-[(3-methoxyanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.02633
3-[(4-bromoanilino)methyl]-5-(2-bromophenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.1732
3-[(4-bromoanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.05472
3-[(4-methylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.04029
3-[(E)-[(2,4-dichlorophenyl)imino]methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH and temperature not specified in the publication
0.01977
3-[(E)-[(3-methoxy-4-methylphenyl)imino]methyl]-4H-1-benzopyran-4-one
Homo sapiens
pH and temperature not specified in the publication
0.04
3-[2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]propanamide
Homo sapiens
pH and temperature not specified in the publication
0.066
3-[3-(3-chlorobenzyl)-2,4,5-trioxo-imidazolidin-1-yl]-propionamide
Escherichia coli
-
pH 7.4, 25°C
0.088
3-[3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]propanamide
Homo sapiens
pH and temperature not specified in the publication
0.06932
3-[[(2-phenylethyl)amino]methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.0144
3-[[(4-methoxy-3'-nitro[1,1'-biphenyl]-3-yl)amino]methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.2734
4,5-diphenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
Escherichia coli
pH 7.4, 25°C
0.003
4-(2,5-difluorobenzyl)-N-(2-fluorophenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0025
4-(2,5-difluorobenzyl)-N-(2-methoxyphenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0012
4-(2,5-difluorobenzyl)-N-(3-fluorophenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0122
4-(2,5-difluorobenzyl)-N-(3-methoxyphenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0323
4-(2,5-difluorobenzyl)-N-(3-nitrophenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.002
4-(2,5-difluorobenzyl)-N-(4-(trifluoromethyl)phenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.6
4-(2,5-difluorobenzyl)-N-(4-fluorophenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0116
4-(2,5-difluorobenzyl)-N-(4-methoxyphenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0081
4-(2,5-difluorobenzyl)-N-(4-nitrophenyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0223
4-(2,5-difluorobenzyl)-N-(m-tolyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0143
4-(2,5-difluorobenzyl)-N-(o-tolyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0173
4-(2,5-difluorobenzyl)-N-(p-tolyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.02628
4-(5-(2-chlorophenyl)-1,3,4-oxadiazol-2-yl)aniline
Homo sapiens
at pH 7.4 and 25°C
0.02596
4-(5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl)aniline
Homo sapiens
at pH 7.4 and 25°C
0.0146
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(1-(4-nitrophenyl)ethylidene)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0011
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trihydroxybenzylidene)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0546
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trimethoxybenzylidene)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0063
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2-nitrobenzylidene)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0473
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(3,4,5-trimethoxybenzylidene)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0283
4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(4-(phenoxymethyl)benzylidene)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.208
4-hydroxyl-N'-[(E)-(2,4,5-trihydroxylphenyl)methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1772
4-hydroxyl-N'-[(E)-(2-methylphenyl)methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.18
4-hydroxyl-N'-[(E)-(3-hydroxylphenyl)methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1994
4-hydroxyl-N'-[(E)-(4-hydroxylphenyl)methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1837
4-hydroxyl-N'-[(E)-[2-(methoxy)phenyl]methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.172
4-hydroxyl-N'-[(E)-[2-hydroxyl-5-(methoxy)phenyl]methylidene]benzo-hydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1855
4-hydroxyl-N'-[(E)-[4-(methoxy)phenyl]methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1815
4-hydroxyl-N-[(E)-(2-hydroxyl-3-methoxyphenyl)methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1891
4-hydroxyl-N-[(E)-(2-hydroxylphenyl)methylidene]benzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.022
4-[(Z)-[(3-hydroxynaphthalen-2-yl)methylidene]amino]-1,5-dimethyl-2-phenylpyrazolidin-3-one
Homo sapiens
pH and temperature not specified in the publication
0.146
5'-O-(2'',4''-dichlorobenzoyl)-thymidine-3'-O-2'',4''-dichlorobenzoate
Escherichia coli
pH not specified in the publication, 30°C
0.09
5'-O-(2''-methoxybenzoyl)-thymidine
Escherichia coli
pH not specified in the publication, 30°C
0.0333
5'-O-(3''-bromobenzoyl)-thymidine
Escherichia coli
pH not specified in the publication, 30°C
0.0075
5'-O-(4''-bromobenzoyl)-thymidine-3'-O-4''-bromobenzoate
Escherichia coli
pH not specified in the publication, 30°C
0.0188
5'-O-(4''-methoxybenzoyl)-thymidine
Escherichia coli
pH not specified in the publication, 30°C
0.0185
5'-O-(4''-methylbenzoyl)-thymidine
Escherichia coli
pH not specified in the publication, 30°C
0.03495
5,5'-butane-1,4-diylbis(4-(4-nitrophenyl)-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
Escherichia coli
at pH 7.4 and 25°C
0.12469
5,5'-butane-1,4-diylbis(4-heptyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
Escherichia coli
at pH 7.4 and 25°C
0.02874
5,5'-butane-1,4-diylbis(4-hexyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
Escherichia coli
at pH 7.4 and 25°C
0.11328
5,5'-butane-1,4-diylbis(4-methyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
Escherichia coli
at pH 7.4 and 25°C
0.06829
5,5'-butane-1,4-diylbis(4-octyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
Escherichia coli
at pH 7.4 and 25°C
0.07935
5,5'-butane-1,4-diylbis(4-phenyl-3-[(3-methylbut-2-en-1-yl)sulfanyl])-4H-1,2,4-triazole
Escherichia coli
at pH 7.4 and 25°C
0.02183
5-(2-bromophenyl)-3-[(2-chloroanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.0176
5-(2-bromophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.0872
5-(2-chlorophenyl)-3-(((4-chlorophenyl)amino)(phenyl)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0464
5-(2-chlorophenyl)-3-((thiazol-2-ylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.1123
5-(3-pyridyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
Escherichia coli
pH 7.4, 25°C
0.0384
5-(4-chlorophenyl)-3-(((2-nitrophenyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0693
5-(4-chlorophenyl)-3-(((3,3-diphenylpropyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0237
5-(4-chlorophenyl)-3-(((4-hydroxyphenyl)amino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0297
5-(4-chlorophenyl)-3-((2-methyl-1H-imidazol-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0582
5-(4-chlorophenyl)-3-((4-(2-methoxyphenyl)piperazin-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0832
5-(4-chlorophenyl)-3-((4-cyclohexylpiperazin-1-yl)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0506
5-(4-chlorophenyl)-3-((cyclohexylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.0228
5-(4-chlorophenyl)-3-((dicyclohexylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.1171
5-(4-chlorophenyl)-3-((naphthalen-1-ylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.1505
5-(4-chlorophenyl)-3-((thiazol-2-ylamino)methyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH 7.4, 25°C
0.08873
5-(4-chlorophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.05821
5-(4-chlorophenyl)-3-[(2-methylanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.03824
5-(4-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH and temperature not specified in the publication
0.0823
5-(4-pyridyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
Escherichia coli
pH 7.4, 25°C
0.1112
5-(benzylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.09505
5-(methylsulfanyl)-2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0056
5-bromo-6-[[(1,3-dihydroxypropan-2-yl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.024
5-bromo-6-[[(2-hydroxyethyl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.00036
5-chloro-6-[([4-oxo-8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-2-yl]sulfanyl)methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.000035
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride
Homo sapiens
pH and temperature not specified in the publication
0.001
5-chloro-6-[[(1,3-dihydroxypropan-2-yl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.039
5-chloro-6-[[(2-hydroxyethyl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.034
5-iodo-6-[[(piperidin-1-yl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.05
5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH and temperature not specified in the publication
0.03095
5-sulfanylidene-2-(thiophen-2-yl)-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.05813
5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.0032
5-[(E)-[2-(quinoxalin-2-yl)hydrazinylidene]methyl]benzene-1,2,4-triol
Homo sapiens
pH and temperature not specified in the publication
0.00012
6-(((1,3-dihydroxypropan-2-yl)amino)methyl)-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.017
6-amino-5-bromopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.0084
6-[(dimethylamino)methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.028
6-[(dipentylamino)methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.1
6-[(dipropylamino)methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
above, pH and temperature not specified in the publication
0.036
6-[[(2,3-dihydroxypropyl)(methyl)amino]methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.012
6-[[(2-hydroxyethyl)amino]methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.087
6-[[bis(2-ethoxyethyl)amino]methyl]-5-iodopyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.0066
7-(4-tert-butylphenyl)-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0015 - 0.0097
7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
0.1
7-(methylsulfanyl)-2-phenyl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5(4H)-one
Homo sapiens
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.0462
7-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.08749
7-[4-(4-tert-butylbenzene-1-sulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Escherichia coli
at pH 7.4 and 25°C
0.16189
7-[4-(benzenesulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
Escherichia coli
at pH 7.4 and 25°C
0.0263
8-phenyl-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00004
8-[4-(pentafluoro-lambda6-sulfanyl)phenyl]-2-sulfanylidene-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.342
ethyl (3-benzyl-2,4,5-trioxoimidazolidin-1-yl)acetate
Homo sapiens
pH and temperature not specified in the publication
0.02564
ethyl 4-(4-chlorophenyl)-2-oxo-6-([(pyridin-4-yl)formohydrazido]methyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.00914
ethyl 4-(4-chlorophenyl)-2-oxo-6-([[(5-phenyl-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl)methyl]amino]methyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.03226
ethyl 4-(4-chlorophenyl)-2-oxo-6-[[(E)-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)amino]methyl]-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.05334
ethyl 4-(4-chlorophenyl)-6-((3-methyl-5-oxo-2H-pyrazol-1(5H)-yl)methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.08735
ethyl 4-(4-chlorophenyl)-6-([(E)-[(4-chlorophenyl)methylidene]amino]methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.118
ethyl 4-(4-chlorophenyl)-6-([(E)-[(4-methoxyphenyl)methylidene]amino]methyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.1505
ethyl 4-(4-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.00657
ethyl 4-(4-chlorophenyl)-6-[([[5-(4-chlorophenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.0118
ethyl 4-(4-chlorophenyl)-6-[([[5-(4-methoxyphenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.00109
ethyl 4-(4-chlorophenyl)-6-[([[5-(4-methylphenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.1291
ethyl 6-((1H-imidazol-1-yl)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.04065
ethyl 6-((2-aminobenzoyloxy)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetra-hydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.0385 - 0.1236
ethyl 6-((benzylamino)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
0.09525
ethyl 6-(benzoyloxymethyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.06464
ethyl 6-([(E)-[(4-bromophenyl)methylidene]amino]methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.279
ethyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.0145
ethyl 6-[([[5-(4-bromophenyl)-2-sulfanylidene-1,3,4-oxadiazol-3(2H)-yl]methyl]amino)methyl]-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.357
ethyl [2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]acetate
Homo sapiens
pH and temperature not specified in the publication
0.303
ethyl [3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetate
Homo sapiens
pH and temperature not specified in the publication
0.03971
methyl 1-cyclopropyl-6-fluoro-4-oxo-7-[4-(phenylacetyl)piperazin-1-yl]-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.07391
methyl 1-cyclopropyl-6-fluoro-7-[4-(4-methylbenzene-1-sulfonyl)piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.15322
methyl 1-cyclopropyl-6-fluoro-7-[4-(4-nitrobenzene-1-sulfonyl)piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.09681
methyl 1-cyclopropyl-6-fluoro-7-[4-(morpholine-4-carbonyl)piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.05199
methyl 1-cyclopropyl-6-fluoro-7-[4-[2-(4-methylanilino)-2-oxoethyl]piperazin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.4147
methyl 4-(2,3-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3971
methyl 4-(2-fluoro-4-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.4241
methyl 4-(3,4-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3943
methyl 4-(3-bromo-4,5-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.4046
methyl 4-(3-chloro-4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.4005
methyl 4-(4-acetoxy-3-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.4439
methyl 4-(4-chlorophenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3967
methyl 4-(4-hydroxy-3,5-dimethoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.4489
methyl 4-(4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3874
methyl 4-(4-methoxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3736
methyl 4-(furan-2-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.389
methyl 4-butyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3454
methyl 4-isobutyl-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3226
methyl 6-methyl-2-oxo-4-(4-(trifluoromethyl)phenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3506
methyl 6-methyl-2-oxo-4-(thiophen-3-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3143
methyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.3035
methyl 6-methyl-4-(4-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.386
methyl 6-methyl-4-(5-methylfuran-2-yl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.4857
methyl 6-methyl-4-(5-methylthiophen-2-yl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
Escherichia coli
at pH 7.0 and 30°C
0.11057
methyl 7-(4-acetylpiperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.05618
methyl 7-[4-(4-chlorobenzene-1-sulfonyl)piperazin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate
Escherichia coli
at pH 7.4 and 25°C
0.0116
methyl-4-((2-(2-(2-methyl-1H-indol-3-yl)acetyl)hydrazono)methyl)benzoate
Escherichia coli
pH 7.4, 25°C
0.0012
N'-(2,3-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0033
N'-(2,4-dichlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0056
N'-(2,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0092
N'-(2,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0185
N'-(2-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0073
N'-(2-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0066
N'-(2-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0361
N'-(2-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0014
N'-(3,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0024
N'-(3,5-dichloro-2-hydroxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0039
N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0011
N'-(3-aminobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0184
N'-(3-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0274
N'-(3-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0048
N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0046
N'-(3-hydroxy-4-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0185
N'-(3-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0311
N'-(4-(dimethylamino)benzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0188
N'-(4-(dimethylamino)benzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0199
N'-(4-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0164
N'-(4-chlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0221
N'-(4-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0053
N'-(4-hydroxy-3,5-dimethoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.006
N'-(4-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0082
N'-(4-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
pH 7.4, 25°C
0.0367
N'-(5-bromo-2-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0394
N'-(anthracen-9-ylmethylene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 25°C
0.0256
N-((5-(4-chlorophenyl)-2-thioxo-1,3,4-oxadiazole-3(2H)-yl)methyl)3(trifluoromethyl) benzamide
Homo sapiens
pH 7.4, 25°C
0.0191
N-(2-bromophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0011
N-(2-chlorophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0016
N-(3,4-dichlorophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0146
N-(3-bromophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.0246
N-(4-bromophenyl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.00382
N-(4-oxo-2-sulfanylidene-8-[[4-(trifluoromethyl)phenyl]methyl]-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea
Homo sapiens
pH and temperature not specified in the publication
0.02992
N-(8-benzyl-4-oxo-2-sulfanylidene-1,2,3,4-tetrahydropyrazolo[1,5-a][1,3,5]triazin-7-yl)thiourea
Homo sapiens
pH and temperature not specified in the publication
0.0422
N-(adamantan-1-yl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
0.1706
N-[(E)-(2,3-dihydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.2295
N-[(E)-(3,4-dihydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.0068
N-[(E)-(3,5-dibromo-2-hydroxylphenyl)methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1603
N-[(E)-(3-chlorophenyl)methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.158
N-[(E)-(4-bromophenyl)methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.159
N-[(E)-(4-chlorophenyl)methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1834
N-[(E)-1-(2,5-dihydroxylphenyl)ethylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.173
N-[(E)-1-(2,5-dihydroxylphenyl)propylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1769
N-[(E)-1-(2,6-dihydroxylphenyl)ethylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.2041
N-[(E)-[3,4-bis(methoxy)phenyl]methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.1903
N-[(E)-[3-ethoxy-2-hydroxylphenyl]methylidene]-4-hydroxylbenzohydrazide
Escherichia coli
at pH 7.0 and 30°C
0.06545
symplocomoside
Homo sapiens
pH and temperature not specified in the publication
0.085
[2,4,5-trioxo-3-(2-phenylethyl)imidazolidin-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.236
[3-[(2-methylphenyl)methyl]-2,4,5-trioxoimidazolidin-1-yl]acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.0017 - 0.027
[8-(2,4-dioxo-2,3,4,6-tetrahydro-1H-pyrrolo[3,4-d]pyrimidin-1-yl)octyl]phosphonic acid
0.0073 - 0.0151
[8-(2,4-dioxo-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]phosphonic acid
0.000045
[[(2R,4S)-2-(hydroxymethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.00025
[[(2R,4S)-2-(hydroxymethyl)-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]methyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.000015
[[(2S,4S)-2-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonothioyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.000011
[[(2S,4S)-2-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.00022
[[(3R,4R)-3-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.000045
[[(3R,4R)-3-hydroxy-4-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]methyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.00019
[[(3S)-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonothioyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.00035
[[(3S)-3-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)pyrrolidin-1-yl]carbonyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.0003
[[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-(prop-2-en-1-yloxy)ethoxy]methyl]phosphonic acid
Rattus norvegicus
-
about, pH 6.7
0.00075
[[2-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-1-phenoxyethoxy]methyl]phosphonic acid
Rattus norvegicus
-
pH 6.7
0.013
2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.04332
2-benzyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.03956
2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.03956
2-phenyl-5-sulfanylidene-5,6-dihydro[1,2,4]triazolo[1,5-a][1,3,5]triazin-7(4H)-one
Homo sapiens
pH and temperature not specified in the publication
0.04061
3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.04061
3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Homo sapiens
pH and temperature not specified in the publication
0.044
5'-O-trityl-inosine
Escherichia coli
-
i.e. KIN59, IC50: 0.044 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
0.044
5'-O-trityl-inosine
Escherichia coli
-
IC50: 0.044 mM, reversible, noncompetitive inhibition with respect to thymidine and phosphate
0.067
5'-O-trityl-inosine
Homo sapiens
-
i.e. KIN59, IC50: 0.067 mM, noncompetitively inhibits, when thymidine or phosphate is the variable substrate. Suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
0.04
5-bromo-6-[[(2,3-dihydroxypropyl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH and temperature not specified in the publication
0.1
5-bromo-6-[[(2,3-dihydroxypropyl)amino]methyl]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
above, pH and temperature not specified in the publication
0.00002
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
Escherichia coli
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.000023
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
Homo sapiens
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.0016
6-amino-5-bromouracil
Escherichia coli
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.0068
6-amino-5-bromouracil
Homo sapiens
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.017
6-amino-5-bromouracil
Homo sapiens
pH and temperature not specified in the publication
0.0000187
6-[(2'-aminoimidazol-1'-yl)methyl]-5-bromouracil
Escherichia coli
-
IC50: 0.0000187 mM
0.000019
6-[(2'-aminoimidazol-1'-yl)methyl]-5-bromouracil
Homo sapiens
IC50: 0.000019 mM
0.0000206
6-[(2'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
Escherichia coli
-
IC50: below 0.0000206 mM
0.000049
6-[(2'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
Homo sapiens
IC50: below 0.000049 mM
0.00073
6-[(4'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
Escherichia coli
-
IC50: 0.00073 mM
0.0015
7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0097
7-(4-tert-butylphenyl)-2-[[(5-chloro-2-methylidene-6-oxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl]sulfanyl]-2,3-dihydropyrazolo[1,5-a][1,3,5]triazin-4(1H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0065
7-deazaxanthine
Escherichia coli
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.0168
7-deazaxanthine
Escherichia coli
pH and temperature not specified in the publication
0.045
7-deazaxanthine
Homo sapiens
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.0385
ethyl 6-((benzylamino)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.1236
ethyl 6-((benzylamino)methyl)-4-(4-chlorophenyl)-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate
Escherichia coli
pH 7.0, 30°C
0.0017
[8-(2,4-dioxo-2,3,4,6-tetrahydro-1H-pyrrolo[3,4-d]pyrimidin-1-yl)octyl]phosphonic acid
Homo sapiens
-
enzyme purified from placenta, pH not specified in the publication, temperature not specified in the publication
0.0068
[8-(2,4-dioxo-2,3,4,6-tetrahydro-1H-pyrrolo[3,4-d]pyrimidin-1-yl)octyl]phosphonic acid
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.027
[8-(2,4-dioxo-2,3,4,6-tetrahydro-1H-pyrrolo[3,4-d]pyrimidin-1-yl)octyl]phosphonic acid
Homo sapiens
-
recombinant enzyme, pH not specified in the publication, temperature not specified in the publication
0.0073
[8-(2,4-dioxo-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]phosphonic acid
Homo sapiens
-
recombinant enzyme, pH not specified in the publication, temperature not specified in the publication
0.0114
[8-(2,4-dioxo-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]phosphonic acid
Escherichia coli
-
pH not specified in the publication, temperature not specified in the publication
0.0151
[8-(2,4-dioxo-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]phosphonic acid
Homo sapiens
-
enzyme purified from placenta, pH not specified in the publication, temperature not specified in the publication
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.01
-
mitochondrial neurogastrointestinal encephalomyopathy syndrome patient, leukocytes
0.2 - 0.32
-
leukocytes of heterozygous individuals in enzyme mutation and mitochondrial neurogastrointestinal encephalomyopathy syndrome
1.5
purified native enzyme, pH 8.0, 37°C, substrate 5-fluorouridine or 5'-deoxy-5-fluorouridine
1100
8.1
purified native enzyme, pH 8.0, 37°C, substrate 5-fluoro-2'-deoxyuridine
additional information
additional information
-
no activities in other tissues than liver from TP-/-UP-/- mice
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
10
-
assay at, pH 10 is used because 2-deoxy-D-ribose 1-phosphate is heat labile at pH 7.4
6.5
7.4
7.5
7.5 - 8
-
rapid decrease of activity above and below this range
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.5 - 8
-
rapid decrease of activity above and below this range
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
25
37
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pI VALUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
676235, 676248, 685542, 685594, 686525, 689265, 702614, 702642, 705495, 705995, 721807, 722138, 722187, 723306, 735751, 735769
-
-
brenda
-
UniProt
brenda
-
638439, 638442, 638445, 638449, 638451, 638456, 638459, 638460, 638461, 638462, 638463, 638464, 638466, 638467, 638468, 638469, 658387, 658657, 658872, 659360
-
-
brenda
-
-
-
brenda
-
686594, 686997, 686998, 686999, 687024, 687155, 687928, 688212, 688264, 688302, 688582, 689162, 689163, 689244, 689262, 689263, 689265, 689271, 689292, 690021, 690098, 690197
-
-
brenda
-
703240, 703930, 704898, 704933, 704973, 705495, 706011, 721729, 721807, 723107, 723800, 735645, 735920
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
thymidine phosphorylase mRNA levels are low and statistically not different in whole basal cell carcinoma cells and normal skin and are strongly downregulated in laser capture microdissected-basal cell carcinoma cells as compared with laser capture microdissected-normal epidermis
brenda
higher PyNpase levels in tumor tissue than in normal tissue or tissue adjacent to the tumor, PyNpase levels independent of age, gender, history of recurrence, multiplicity, tumor size, tumor shape, pathological stage (Ta, T1-4), PyNpase levels differ between histological stages being highest in G3, and between papillary versus non-papillary growth pattern, higher PyPnase levels in high-risk group (G3 or Tis or T2) than in low-risk group (primary, single, G1 and Ta)
brenda
-
presurgery serum from 47 patients with ovarian cancer, and control serum from women with normal ovaries, treated surgically due to nononcological reasons. Significant higher enzyme activity in malignant serum specimen from ovarian cancer patients when compared to the control
brenda
-
thymidine phosphorylase shows a characteristic pattern of distribution dependent on the phase of the menstrual cycle: enzyme expression moves from stroma to epithelium as the cycle progresses34 and is inversely correlated with estradiol concentrations
brenda
patients with PD-ECGF/TP-positive tumors have a poorer prognosis than those with negative tumors
brenda
-
cholangiocarcinoma-derived cell line, which has a naturally high level of endogenous thymidine phosphorylase
brenda
-
the cytoplasmic level of heterogeneous nuclear ribonucleoprotein K is significantly correlated with the elevated expression of thymidine phosphorylase, and high levels of both proteins are predictive of a poor prognosis in nasopharyngeal carcinoma
brenda
-
the enzyme is strongly induced in the serum-deprived nasopharyngeal carcinoma cells, the serum deprivation-triggered upregulation of the enzyme is due to mRNA stabilization, not protein stabilization or transcriptional activation requiring the mRNA CU-rich element sequence and heterogeneous nuclear ribonucleoprotein K, overview
brenda
-
the enzyme is strongly induced in the serum-deprived nasopharyngeal carcinoma cells, the serum deprivation-triggered upregulation of the enzyme is due to mRNA stabilization, not protein stabilization or transcriptional activation requiring the mRNA CU-rich element sequence and heterogeneous nuclear ribonucleoprotein K, overview
brenda
-
tissue from 47 patiens with ovarian cancer after surgery. Significant higher enzyme activity in malignant tissue from ovarian cancer patients when compared to the control
brenda
-
tissue from 47 patiens with ovarian cancer after surgery. Significant higher enzyme activity in malignant tissue from ovarian cancer patients when compared to the control
brenda
-
shows significantly greater activity in cancer tissues than in normal tissues
brenda
additional information
higher PyNpase levels in normal tissue adjacent to tumor, AN, than in normal tissue, N
brenda
the enzyme is highly upregulated in a variety of solid tumours
brenda
patients with PD-ECGF/TP-positive tumors have a poorer prognosis than those with negative tumors
brenda
-
enzyme activity is higher in cancer tiddue than in adjacent normal tissue
brenda
-
enzyme activity is higher in cancer tiddue than in adjacent normal tissue
brenda
-
no differences in thymidine phosphorylase activity between man and women or with increasing age
brenda
-
thymidine phosphorylase activity in normal liver tissue adjacent to hepatocellular carcinoma is related to tumor occurrence and may predict postoperative tumor recurrence. Patients who have a high thymidine phosphorylase level in normal liver tissue have significantly earlier recurrence compared with patients who have a low thymidine phosphorylase level. Patients who have a low thymidine phosphorylase level in adjacent liver tissue have a 0.387fold higher risk of postoperative recurrence compared with patients who have a high TP level
brenda
the liver is the major site of pyrimidine metabolism and contains high levels of thymidine phosphorylase (TP)
brenda
the mean thymidine phosphorylase concentration in non-small cell lung cancer tissue is statistically higher than that of normal lung tissue
brenda
the mean thymidine phosphorylase concentration in non-small cell lung cancer tissue is statistically higher than that of normal lung tissue
brenda
-
similar distribution of thymidine phosphorylase and thymidine kinase, EC 2.7.1.21, immunohistochemical analysis, overview
brenda
-
the enzyme is strongly induced in the serum-deprived nasopharyngeal carcinoma cells, the serum deprivation-triggered upregulation of the enzyme is due to mRNA stabilization, not protein stabilization or transcriptional activation requiring the mRNA CU-rich element sequence and heterogeneous nuclear ribonucleoprotein K, overview
brenda
-
high expression level, two alternative enzyme forms, a 27 kDa splice variant and another form containing five additional amino acids on the N-terminus, the second form is processed at Thr6 instead of Ala11
brenda
-
surrounding cancer nests or along the invasive margin of cancer
brenda
additional information
-
the enzyme is produced by macrophages and exists in neutrophils and cancer cells
brenda
additional information
-
not detected in most of non-tumoral glandular epithelial cells
brenda
additional information
-
enzyme expression analysis in cell and tissues, overview
brenda
additional information
-
enzyme expression analysis in cancer patients, overview
brenda
additional information
-
the enzyme is upregulated in a wide variety of solid tumors including breast and colorectal cancers, association of the enzyme with tumor grade is evident in bladder, cervical, and renal cell cancer, but not in the other investigated cancers, in most cases, the enzyme appeared to be associated with poor prognosis, overview
brenda
additional information
thymidine phosphorylase (TP) expression is extremely low in healthy human tissues
brenda
additional information
molecular weight and homodimer structure of human hepatic enzyme is similar to those of the enzymes from human amniochorion, blood platelet, placenta, psoriatic lesions, and the recombinant enzyme from a colorectal tumor. Detection by human placenta TP antisera binding to various preparations of hepatic TP
brenda
additional information
-
molecular weight and homodimer structure of human hepatic enzyme is similar to those of the enzymes from human amniochorion, blood platelet, placenta, psoriatic lesions, and the recombinant enzyme from a colorectal tumor. Detection by human placenta TP antisera binding to various preparations of hepatic TP
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
additional information
-
the mechanism behind the secretion of thymidine phosphorylase is possibly a posttranslational process whereby serine residues of the enzyme are covalently linked to phosphate groups of nucleotides, leading to the formation of a nucleotidylated protein that can be secreted
-
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
evolution
the amino acid sequence of thymidine phosphorylase (TP) is extremely conserved. For instance, human TP shares 39% sequence identity with Escherichia coli TP
evolution
the amino acid sequence of thymidine phosphorylase (TP) is extremely conserved. For instance, human TP shares 39% sequence identity with Escherichia coli TP
evolution
the enzyme is identical to the platelet-derived endothelial cell growth factor (PD-ECGF). Amino acid sequence homology between hepatic thymidine phosphorylase and PD-ECGF
malfunction
-
deficiency of the cytosolic enzyme thymidine phosphorylase causes a multisystem disorder called mitochondrial neurogastrointestinal encephalomyopathy syndrome with symptoms gastrointestinal dysfunction, muscle involvement and neurological deterioration, overview
malfunction
-
thymidine phosphorylase promotes angiogenesis. The mechanism of endometrial angiogenesis involves the enzyme and stimulation by ovarian steroids of production of angiogenic regulators by endometrial epithelium and stroma which then act on the endothelium
malfunction
-
a loss-of-function mutation is involved in mitochondrial neurogastrointestinal encephalomyopathy, an autosomal recessive human disorder associated with multiple deletions of skeletal muscle mitochondrial DNA, overview. Corrleation of tumor development and progression with intratumoral thymidine phsophorylase levels, overview
malfunction
-
knocking down enzyme expression enhances the cytotoxicity and cell growth inhibition of tamoxifen
malfunction
-
collagen-, collagen-related peptide-, adenosine diphosphate-and/or thrombin-induced platelet aggregation are significantly attenuated in enzyme deficient platelets. Tymp deficiency also significantly decreases agonist-induced P-select in expression
malfunction
EGF receptor inhibition may lead to TP overexpression, which decreases the efficacy of infusional 5-fluorouracil (5FU) regimens, while enhancing that of bolus schedules. Tissue hypoxia secondary to low hemoglobin levels may induce TP overexpression, and subsequently, a relative resistance to infusional 5FU
malfunction
overexpression of human thymidine phosphorylase (hTP) has been associated with cancer aggressiveness and poor prognosis by triggering proangiogenic and antiapoptotic signaling
malfunction
mutation of the TP gene is associated with mitochondrial neurogastrointestinal encephalomyopathy (MNGIE), an autosomal recessive human disease exhibiting multiple deletions of skeletal muscle mitochondrial DNA (peripheral neuropathy, myopathy, leukoencephalopathy, lactic acidosis, gastrointestinal dysmotility, progressive external ophthalmoplegia, and thin body habitus)
malfunction
overexpression of thymidine phosphorylase (TP) causes diseases like psoriasis, chronic inflammatory disease, tumor angiogenesis and rheumatoid arthritis etc. The inhibition of this enzyme is vital to secure life from serious threats
malfunction
upregulation of the enzyme increases the expression of vascular endothelial growth factor, basic fibroblast growth factor, interleukin-8 and tumour necrosis factor alpha. In contrast, enzyme knockdown inhibits tumor growth, suppresses microvessel formation and decreases the expression of angiogenesis-related proteins
metabolism
thymidine phosphorylase is a catabolic enzyme in thymidine metabolism
metabolism
-
the enzyme is involved in the thymidine salvage pathway and competes with thymidine kinase, overview. Thymidine plays a central role in both proliferation and angiogensis, overview
metabolism
-
the enzyme participates in the thymidine salvage pathway maintaining the thymidine pool in the cell
metabolism
the intracellular catabolism of thymidine mediated via TP produces 2DDR-1P as a metabolic biproduct, which is subsequently converted to 2DDR by the nonenzymatic dephosphorylation. This 2DDR is then secreted from the cells to exhibit the angiogenic effects. Both TP and 2DDR directly stimulate the endothelial cell migration through the activation of focal adhesion kinase (FAK) and the formation of focal adhesions. TP and 2DDR roles in tumour development, overview
metabolism
the intracellular catabolism of thymidine mediated via TP produces 2DDR-1P as a metabolic biproduct, which is subsequently converted to 2DDR by the nonenzymatic dephosphorylation. This 2DDR is then secreted from the cells to exhibit the angiogenic effects. Both TP and 2DDR directly stimulate the endothelial cell migration through the activation of focal adhesion kinase (FAK) and the formation of focal adhesions
metabolism
thymidine phosphorylase (TP) is the key enzyme of the pyrimidine salvage pathway, which speedup the conversion of thymidine and 2'-deoxyuridine to their respective bases and 2-deoxy-D-ribose 1-phosphate
physiological function
the enzyme is the sole endothelial mitogenic and angiogenic factor, it plays a role in the stimulation of chemotaxis and thymidine incorporation into endothelial cells in vitro and angiogenesis in vivo
physiological function
-
thymidine phosphorylase is a key regulator of the angiogenic potential of colony-forming units and endothelial progenitor cell cultures, overview. The enzyme is a survival factor, it protects against apoptosis, stimulates endothelial cell migration and enhances wound healing in vitro and angiogenesis in vivo, overview
physiological function
-
2-deoxy-D-ribose, a downstream mediator of thymidine phosphorylase, regulates tumor angiogenesis and progression, mechanism, overview
physiological function
-
heterogeneous nuclear ribonucleoprotein K and thymidine phosphorylase prevent hypoxia-induced apoptosis in nasopharyngeal carcinoma cells, overview
physiological function
-
the enzyme plays an important role in the female reproductive cycle, and is also involved in a wide variety of chronic inflammatory diseases. Dual role of thymidine phosphorylase in cancer development and chemotherapy, acts as thymidine salvage enzyme and as platelet-derived endothelial cell growth factor inducing endothelial cell migration in vitro and angiogenesis in vivo, overview. The enzyme promotes tumor growth and metastasis by preventing apoptosis and inducing angiogenesis. The enzyme is also indispensable for the activation of the extensively used 5-fluorouracil prodrug capecitabine. Role of thymidine phosphorylase in angiogenesis, mediators are matrix metalloproteinases, interleukin-8, P-selectin, and vascular epithelial growth factor, detailed overview
physiological function
-
the enzyme promotes the survival and neurite outgrowth of cortical neurons
physiological function
-
thymidine phosphorylase inhibits vascular smooth muscle cell proliferation via upregulation of STAT3. Overexpression of thymidine phosphorylase increases STAT3 phosphorylation and expression in vascular smooth muscle cells via Lyn. STAT3 protein but not STAT3 phosphorylation is necessary for thymidine phosphorylase inhibited vascular smooth muscle cell proliferation
physiological function
-
transient decrease of mRNA and protein expression by 87.1% and 72.5%, respectively, using siRNAleads to significant decrease in migration of KKU-M139 cells, and suppresses migration and tube formation of human umbilical vein endothelial cells. siRNA also reduces the ability of thymidine phosphorylase to resist hypoxia-induced apoptosis, while suppression of thymidine phosphorylase reduces the sensitivity of KKU-M139 cells to 5-fluorouracil
physiological function
thymidine phosphorlyase is a key enzyme in the pyrimidine salvage pathway and involved in thymidine homeostasis in cells
physiological function
thymidine phosphorylase is not essential for Mycoplasma pneumoniae survival
physiological function
-
the enzyme participates in platelet signaling and promotes thrombosis by platelet activation
physiological function
thymidine phosphorylase (TP), an enzyme involved in pyrimidine salvage pathway, is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. The enzyme function in cancer development. TP activity is also shown to augment the levels of hypoxia-inducible factor (HIF)-1alpha during in vitro hypoxia in RT112 cells. Eventually, TP acts in concert with HIF-1a to induce VEGF secretion. Additionally, TP and VEGF are coexpressed in various human cancers and display a cooperative role in neovascularization. TP dramatically reduces the apoptotic index in various cancer cells. TP inactivates and eventually reduces the bioavailability of 5-trifluorothymidine (TFT), a clinically used anticancer drug
physiological function
thymidine phosphorylase (TP), an enzyme involved in pyrimidine salvage pathway, is identical to platelet-derived endothelial cell growth factor (PD-ECGF) and gliostatin. TP activity is also shown to augment the levels of hypoxia-inducible factor (HIF)-1alpha during in vitro hypoxia in RT112 cells. Eventually, TP acts in concert with HIF-1a to induce VEGF secretion. Additionally, TP and VEGF are coexpressed in various human cancers and display a cooperative role in neovascularization. TP dramatically reduces the apoptotic index in various cancer cells
physiological function
thymidine phosphorylase (TP) is a nucleoside-metabolizing enzyme that plays a key role in 5-fluorouracil (5FU) pharmacokinetics, as well as in the inflammatory response, neoangiogenesis and apoptosis. TP expression is regulated by hypoxia, inflammatory cytokines and antitumoral agents
physiological function
thymidine phosphorylase (TP) catalyzes the reversible phosphorolysis of thymidine, deoxyuridine, and their analogues to their respective nucleobases and 2-deoxy-alpha-D-ribose-1-phosphate. TP is a key enzyme in the pyrimidine salvage pathways. Activity of the enzyme is crucial in angiogenesis, cancer chemotherapy, radiotherapy, and tumor imaging
physiological function
thymidine phosphorylase is an important enzyme of the pyrimidine salvage pathways. It catalyzes the reversible phosphorolysis of thymidine, deoxyuridine, but not deoxycytidine, and their analogues, to their respective nucleobases and 2-deoxy-alpha-D-ribose-1-phosphate. The biological significance of TP has several aspects. It has a role in maintaining the integrity of the blood vessels, and its activity is an essential step in the regulation of intra- or extracellular thymidine concentration and homeostasis in mammalian cells. The enzyme is identical to the platelet-derived endothelial cell growth factor (PD-ECGF) which is involved in the process of angiogenesis, neoplastic tissue growth, and metastases. Thymidine phosphorylase is involved regulation of intra- or extracellular thymidine concentration and angiogenesis
physiological function
the enzyme promotes angiogenesis and tumor growth in intrahepatic cholangiocarcinoma
physiological function
the enzyme mediates SARS-CoV-2 spike protein-induced thrombosis
physiological function
-
thymidine phosphorylase is not essential for Mycoplasma pneumoniae survival
-
additional information
elevated enzyme levels are associated with tumor angiogenesis, metastasis and poor prognosis
additional information
-
elevated enzyme levels are associated with tumor angiogenesis, metastasis and poor prognosis
additional information
-
the cytoplasmic level of heterogeneous nuclear ribonucleoprotein K is significantly correlated with the elevated expression of thymidine phosphorylase, and high levels of both proteins are predictive of a poor prognosis in nasopharyngeal carcinoma
additional information
the important residues of enzyme TP responsible for activity are Ser117, Ser217, His116, Lys221, Arg202, Tyr199, Thr118, Arg146, Leu148, Thr151, Gly152, and Ile214, computational structure-function analysis
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
100000
110000
45000
47000
50000
55000
58000
-
2 * 58000, SDS-PAGE, enzyme is capable of being converted to a less active form larger in MW and possibly trimeric or tetrameric in structure
90000
47000
-
2 * 47000, SDS-disc gel electrophoresis
47000
x * 47000, calculated from amino acid sequence
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
dimer
homodimer
additional information
?
x * 47000, calculated from amino acid sequence
dimer
-
three-dimensional structure, 2 identical subunits, each subunit is composed of a small alpha-helical domain and a large alpha/beta domain
dimer
-
2 * 58000, SDS-PAGE, enzyme is capable of being converted to a less active form larger in MW and possibly trimeric or tetrameric in structure
dimer
-
2 * 47000, SDS-disc gel electrophoresis
homodimer
2 * 52000, SDS-PAGE, 2 * 49885, sedimentation equilibrium analysis, 2 * 49785-49882, mass spectrometry (2 methods)
additional information
-
three-dimensional enzyme structure by molecular dynamic simulation
additional information
-
each subunit contains a large mixed alpha-helical and beta-sheet domain, separated from a smaller alpha-helical domain by a large cleft. The active site consists of the thymine-binding site in the alpha-domain and the phosphate-binding site across the cleft in the a/b domain
additional information
modeling of monomer-dimer-tetramer transition, for the transition model of the subunits aggregation, the non-linear regression fitting yielded the equilibrium association constants (Ka) in absorbance units. Amino acid sequence determination, overview
additional information
-
modeling of monomer-dimer-tetramer transition, for the transition model of the subunits aggregation, the non-linear regression fitting yielded the equilibrium association constants (Ka) in absorbance units. Amino acid sequence determination, overview
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
proteolytic modification
-
two alternative enzyme forms, a 27 kDa splice variant and another form containing five additional amino acids on the N-terminus, the second form is processed at Thr6 instead of Ala11
additional information
-
the mechanism behind the secretion of thymidine phosphorylase is possibly a posttranslational process whereby serine residues of the enzyme are covalently linked to phosphate groups of nucleotides, leading to the formation of a nucleotidylated protein that can be secreted
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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
analysis of crystal structure of recombinant Escherichia coli TP in complex with 2'-fluoro-3'-azido-2',3'-dideoxyuridine (N3FddU) and 3'-azidothymidine (AZT) at 1.50 A and 1.52 A resolutions, respectively. Analysis of the free enzyme crystal structure at 2.8 A resolution
analysis of crystal structure of recombinant human TP in complex with 5-iodouracil (5IUR) at 3.0 A and 2.5 A resolutions, respectively
purified recombinant thymidine phosphorylase, free and in complex with 5-iodouracil, X-ray diffraction structure determination and analysis at 3.0 A and 2.5 A resolutions, respectively
structure of HTP bound to the small molecule inhibitor 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracil hydrochloride, glutathione S-transferase fused to thymidine phosphorylase residues 12482 (based on Swissprot accession number P19971) via a thrombin-cleavable linker, crystallizationd at 15°C using the hanging-drop vapor method
X-ray diffraction structure determination and analysis of the free enzyme at 3.5 A resolution, and of the in complex with the small and potent inhibitor 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil at 2.1 A resolution
-
sitting drop vapor diffusion method, using 0.2 M potassium thiocyanate, 0.1 M bis-Tris propane, 20% (w/v) PEG 3350 pH 7.5 (unliganded enzyme), or 0.1 M Bicine, 1.6 M (NH4)2SO4 pH 9.0 (in complex with thymidine), or 0.1 M citric acid, 10% (w/v) PEG 6000 pH 5.0 (in complex with uridine)
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
D203A
I214A
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme
K115A
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme
K115E
L148R
R202S
Y199F
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme
Y199L
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type enzyme
additional information
D203A
site-directed mutagenesis, the mutant enzyme shows 50fold reduced catalytic efficiency compared to the wild-type enzyme, the mutant also shows pronounced resistance to the inhibitory effect of 5'-O-tritylinosine, and it keeps full sensitivity to the competitive inhibitors 6-aminothymine and 6-amino-5-bromouracil
D203A
-
site-directed mutagenesis, the mutant shows 60% reduced phosphorolytic activity compared to the wild-type enzyme. The mutant is inhibited by 6-aminothymine 6-amino-5-bromouracil, like the wild-type enzyme, but not by 5'-O-tritylinosine, in contrast to the wild-type enzyme
K115E
-
loss of enzymic activity. Expression of mutant in rat vascular smooth muscle cell does not have significant effect on cell proliferation
L148R
-
loss of enzymic activity. Expression of mutant in rat vascular smooth muscle cell does not have significant effect on cell proliferation
R202S
-
loss of enzymic activity. Expression of mutant in rat vascular smooth muscle cell does not have significant effect on cell proliferation
additional information
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gene silencing results in a significant increase in basal and oxidative stress-induced apoptosis, the effect is abrogated by supplementation with 2-deoxy-D-ribose-1-phosphate
additional information
-
downregulation of the enzyme by siRNA. Double knockout mutant cells, TP-/-UP-/-, lacking thymidine phosphorylase and uridine phosphorylase activities, show 100fold higher thymidine levels than the wild-type
additional information
transfection of TP into KB cells renders them highly resistant to apoptosis caused by hypoxia
additional information
-
generation of double knockout mutant mice, TP-/-UP-/-, lacking thymidine phosphorylase and uridine phosphorylase activities, the mutant plasma thymidine levels are 5fold higher than in wild-type, but no alterations in mtDNA or pathological changes in the muscles occur in the knockout mice. Only in the brain, mitochondrial DNA depletion, respiratory chain defects and histological alterations, brain-specific phenotype, overview
additional information
-
generation of thymidine phosphorylase, TP, and uridine phosphorylase, UP, EC 2.4.2.3, double knockout mice, TP-/-UP-/- by insertion mutagenesis, which show severe TP deficiency, increased thymidine and deoxyuridine levels in tissues and elevated mitochondrial deoxythymidine triphosphate. As consequences of the nucleotide pool imbalances, brains of mutant mice developed partial depletion of mtDNA, deficiencies of respiratory chain complexes and encephalopathy, accounting for the pathogenesis of mitochondrial neurogastrointestinal encephalopathy, overview. Mitochondria respiratory chain deficiency in the brain of TP-/-UP-/- mice, overview
additional information
-
generation of thymidine phosphorylase, TP, and uridine phosphorylase, UP, EC 2.4.2.3, double knockout mice, TP-/-UP-/- by insertion mutagenesis, which show severe TP deficiency, increased thymidine and deoxyuridine levels in tissues and elevated mitochondrial deoxythymidine triphosphate. As consequences of the nucleotide pool imbalances, brains of mutant mice developed partial depletion of mtDNA, deficiencies of respiratory chain complexes and encephalopathy, accounting for the pathogenesis of mitochondrial neurogastrointestinal encephalopathy, overview. Mitochondria respiratory chain deficiency in the brain of TP-/-UP-/- mice, overview
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
53
-
77% loss of activity after 10 min, phosphate or 2'-deoxyribose-1-phosphate stabilize
55
additional information
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phosphate or pentose 1-phosphate ester substrates stabilize against heat inactivation
55
-
99% loss of activity after 10 min, phosphate or 2'-deoxyribose-1-phosphate stabilize
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
2-mercaptoethanol and sucrose stabilize during preincubation procedure with ammonium sulfate
-
phosphate or pentose 1-phosphate ester substrates stabilize against heat inactivation
-
quite labile during purification
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20°C, phosphate buffer containing 2% mannitol, stable for over 1 year, human enzyme
-
4°C, 10 mM potassium phosphate, pH 7.5, 10 mM 2-mercaptoethanol, 20% sucrose, stable for 3 months
-
4°C, storage results in a decrease of the 120 kDA component, an increase of the high molecular weight component, and a loss of activity
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
homogeneity
native enzyme
native enzyme 5130fold from liver cytosol to apparent homogeneity by anion exchange and hydrophobic interaction chromatography, and dialysis, followed by hydroxyapatite chromatography
Ni Sepharose 6 column chromatography and Superdex 200 gel filtration
partial
Q-Sepharose column chromatography and phenyl Sepharose column chromatography
recombinant enzyme from Escherichia coli strain BL21(DE3) by calmodulin affinity chromatography, cleavage of the calmodulin binding protein tag by enterokinase, removal by chromatography on soybean trypsin inhibitor-sepharose
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recombinant wild-type and mutan enzymes from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and gel filtration
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
co-expressed with uridine phosphorylase in Escherichia coli BL21(DE3) cells
-
expressed in Escherichia coli BL21(DE3) cells
expression of the calmodulin binding protein-tagged enzyme in Escherichia coli strain BL21(DE3) cells transformed with the pCal-n-EK/TP and pGroESL vectors
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expression of wild-type and mutan enzymes in Escherichia coli strain BL21(DE3)
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
chorionic gonadotropin36 and a combination of progesterone and transforming growth factor b1 upregulate the enzyme expression. The enzyme is also upregulated in several diseases, detailed overview
-
EGF receptor inhibition may lead to TP overexpression, and tissue hypoxia secondary to low hemoglobin levels may induce TP overexpression
the enzyme expression is is inversely correlated with estradiol concentrations in the endometrium
-
the enzyme is increased in COVID-19 patients in an acuity-dependent manner
the enzyme is strongly induced in the serum-deprived nasopharyngeal carcinoma cell lines TW-01, TW-02, and TW-04, the serum deprivation-triggered upregulation of the enzyme is due to mRNA stabilization, not protein stabilization or transcriptional activation requiring the mRNA CU-rich element sequence and heterogeneous nuclear ribonucleoprotein K, mechanism and kinetics, overview
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treatment with 0.005-0.04 mM tamoxifen decreases mRNA and protein levels through AKT inactivation
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
-
methods to measure thymidine and deoxyuridine concentrations and thymidine phosphorylase activity in biological samples. Thymidine phosphorylase activity can be measured by an endpoint determination of the thymine formed after 1 h incubation of the buffy coat homogenate in the presence of a large excess of its substrate thymidine, either spectrophotometrically or by HPLC-UV. The protocols allow the detection of thymidine phosphorylase dysfunction in patients with mitochondrial neurogastrointestinal encephalomyopathy, MNGIE
medicine
synthesis
medicine
-
tumor-associated macrophages that express thymidine phosphorylase may be a good target for chermotherapy of thymidine phosphorylase positive solid tumors
medicine
-
thymidine phosphorylase activity might be useful in diagnostic characterization of ovarian cancer
medicine
structural insight into the binding mode of the inhibitor to this important drug target forms the basis for designing novel inhibitors for use in anticancer therapy
medicine
thymidine phosphorylase expression seems to be an important prognostic indicator in gastric cancer patients only when the enzyme is located in tumor cells
medicine
-
thymidine phosphorylase activity in normal liver tissue adjacent to hepatocellular carcinoma is related to tumor occurrence and may predict postoperative tumor recurrence. Patients who have a high thymidine phosphorylase level in normal liver tissue have significantly earlier recurrence compared with patients who have a low thymidine phosphorylase level. Patients who have a low thymidine phosphorylase level in adjacent liver tissue have a 0.387fold higher risk of postoperative recurrence compared with patients who have a high TP level
medicine
thymidine phosphorylase expression is associated with response to capecitabine plus irinotecan in patients with metastatic colorectal cancer
medicine
there is no tumour-selective depletion of thymidine and there does not appear to be any potential benefit of combining antibody-targeted thymidine phosphorylase with the thymidylate synthase inhibitor raltitrexed
medicine
expression of PD-ECGF/TP may play an important role in the progression of solid tumors, and inhibitors of thymidine phosphorylase and analogs of the degradation products of thymidine may suppress the growth of tumors by promoting apoptosis
medicine
mitochondrial neurogastrointestinal encephalomyopathy is an autosomal recessive disorder characterized by ptosis and progressive external ophthalmoplegia, peripheral neuropathy, severe gastrointestinal dysmotility, cachexia and leukoencephalopathy, morphologically abnormal mitochondria and defects of respiratory chain enzymes. Patients harbor depletion, multiple deletions, and point mutations of mitochondrial DNA. This disorder is caused by loss-offunction mutations in the gene encoding thymidine phosphorylase. In patients with mitochondrial neurogastrointestinal encephalomyopathy, thymidine phosphorylase activity is very low or absent resulting in dramatically elevated levels of plasma thymidine and deoxyuridine. It is hypothesized that the increased levels of thymidine and deoxyuridine cause mitochondrial nucleotide pool imbalances that, in turn, generate mtDNA alterations
medicine
-
because pancreatic cancer is sensitive to 5-fluorouracil, thymidine phosphorylase-activated oral drug capecitabine in tumoral and endothelial cells and tumor infiltrating thymidine phosphorylase-positive macrophages could increase the concentration of 5-fluorouracil at tumor site, thus resulting in an enhanced antitumor activity
medicine
-
thymidine phosphorylase is a predictor of response to capecitabine-based chemotherapy in gastric cancer patients
medicine
-
the ThdPase expression in tumors may be a predictive marker for the effectiveness in response to chemotherapy with irinotecan and 5'-deoxy-5-fluoridine
medicine
-
thymidine phosphorylase expression correlates well with tumor grade, metastasis and shorter patient survival in colorectal, pancreatic, renal, ovarian, cervical, bladder and non-small cell lung cancer, loss of function mutants of thymidine phosphorylase case the disease mitochondrial neurogastrointestinal encephalomyopathy
medicine
-
thymidine phosphorylase is an independent prognostic and therapeutic marker for nasopharyngeal carcinoma
medicine
-
thymidine phosphorylase serum levels reflect the prognosis of patients with colorectal cancer, particularly the risk of liver metastasis
medicine
-
thymidine phosphorylase expression at the invasive front of tumor may be an important prognostic factor for T3 rectal cancer
medicine
-
dThdPase plays an important role in tumor angiogenesis in ductal adenocarcinoma of the pancreas
medicine
-
thymidine phosphorylase enzymatic activity may be associated with lymph node metastasis
medicine
-
the thymidine phosphorylase/dihydropyrimidine dehydrogenase ratio may be useful as prognostic factor in patients with pancreatic cancer
medicine
-
thymidine phosphorylase plays a role in oropharyngeal tumourigenesis and 5-fluorouracil activation in the adjuvant setting of oropharyngeal squamous cell carcinoma patients
medicine
-
thymidine phosphorylase expression in cancer-infiltrating inflammatory cells can affect lymph node metastasis and patients' survival in gastric cancer
medicine
-
thymidine phosphorylase is a predictive factor of therapeutic efficacy of capecitabine chemotherapy for breast cancer
medicine
-
thymidine phosphorylase may be involved in up-regulating P-selectin expression in breast cancer cells, tumor cell thymidine phosphorylase correlates with tumor cell P-selectin but not with endothelial cell P-selectin in vascular endothelial cells
medicine
-
thymidine phosphorylase delivers information about endometrial cancer progression
medicine
-
in gastric cancer, thymidine phosphorylase expression of the cancer cells, not stromal cells may play an important role in tumor growth by microvessel formation
medicine
-
gliostatin and vascular endothelial growth factor have synergistic effects on angiogenesis in rheumatoid synovitis
medicine
-
there is no significant association between the occurrence of palmar-plantar erythrodysesthesia after capecitabine treatment and higher tumor thymidine phosphorylase levels
medicine
-
expression of thymidine phosphorylase mRNA is a useful predictive parameter for the survival of postoperative gastric cancer patients after 5-fluorouracilbased adjuvant chemotherapy
medicine
-
a high level of thymidine phosphorylase gene expression is significantly associated with favorable diagnosis of patients treated with 5-fluorouracil-based chemotherapy
medicine
-
immunhistochemical evaluation of thymidine phosphorylase expression is a promising predictor of therapeutic benefit from docetaxel-modulated capecitabine for metastatic breast cancer
medicine
-
low tumour expression level of thymidine phosphorylase is linked with improved outcome for colorectal cancer patients treated with 5-fluorouracil, low thymidine phosphorylase protein expression is predictive of good response to 5-fluorouracil chemotherapy
medicine
-
thymidine phosphorylase expression in breast cancer can represent a biomarker of sensitivity to capecitabine treatment
medicine
use of thymidine phosphorylase inhibitors might offer a promising strategy for cancer treatment
medicine
-
thymidine phosphorylase is a promising target for the treatment of vascular obstructive diseases, effect on cancer cells, detailed overview
medicine
-
methods to measure thymidine and deoxyuridine concentrations and thymidine phosphorylase activity in biological samples. Thymidine phosphorylase activity can be measured by an endpoint determination of the thymine formed after 1 h incubation of the buffy coat homogenate in the presence of a large excess of its substrate thymidine, either spectrophotometrically or by HPLC-UV. The protocols allow the detection of thymidine phosphorylase dysfunction in patients with mitochondrial neurogastrointestinal encephalomyopathy, MNGIE
medicine
thymidine phosphorylase is identified as a prime target for developing anticancer therapies
medicine
thymidine phosphorylase is involved regulation of intra- or extracellular thymidine concentration, angiogenesis, cancer chemotherapy, radiotherapy, as well as tumor imaging
medicine
plasma enzyme level is correlated with the COVID-19 associated thrombotic event, inflammation, and organ damage. Plasma enzyme is also positively correlated with COVID-19 patients who have respiratory symptoms. Targeting the enzyme with tipiracil is an effective medicine for COVID-19
medicine
enzyme inhibition is a therapeutic strategy for COVID-19-associated thrombosis
synthesis
-
immobilization of enzyme on solid support with the aim to have a stable and recyclable biocatalyst for nucleoside synthesis. Immobilization by ionic adsorption on amine-functionalized agarose and Sepabeads results in more than 85% activity recovery. Cross-linking with aldehyde dextran, MW20 kDa, decreases the percentage of expressed activity after immobilization by about 25%, but results in up to 6fold and 3fold higher stability than the soluble enzyme and the non-cross-linked counterpart, respectively, at pH 10 and 37°C. The preparation can be successfully used for the one-pot synthesis of 5-fluoro-2'-deoxyuridine starting from 2'-deoxyuridine or thymidine and 5-fluorouracil. In both cases, the reaction proceeds at the same rate leading to 62% conversion in 1 h
synthesis
-
construction of Escherichia coli expression vector pDEOA and use of lactose instead of IPTG to induce expression. The use of lactose at concentrations above 0.5 mmol/l has an induction effect similar to that of IPTG but results in a longer initial induction time and better cell growth. The thymidine phosphorylase induced by lactose is very stable at 50°C. Intact pDEOA cells induced by lactose can be used as a source of thymidine phosphorylase. Under standard reaction conditions, several deoxynucleosides are effectively produced from thymidine
EXTERNAL LINKS (specific for EC-Number 2.4.2.4)
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Release 2026.1 (March 2026)
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