Any feedback?
Please rate this page
(enzyme.php)
(0/150)

BRENDA support

BRENDA Home
show all | hide all No of entries

Information on EC 2.4.2.4 - thymidine phosphorylase and Organism(s) Escherichia coli and UniProt Accession P07650

for references in articles please use BRENDA:EC2.4.2.4
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
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.
Specify your search results
Select one or more organisms in this record: ?
This record set is specific for:
Escherichia coli
UNIPROT: P07650
Show additional data
Do not include text mining results
Include (text mining) results
Include results (AMENDA + additional results, but less precise)
Word Map
The taxonomic range for the selected organisms is: Escherichia coli
The enzyme appears in selected viruses and cellular organisms
Synonyms
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
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
animal growth regulators, blood platelet-derived endothelial cell growth factors
-
-
-
-
blood platelet-derived endothelial cell growth factor
-
-
-
-
deoxythymidine phosphorylase
-
-
-
-
dthdpase
gliostatin
-
-
-
-
gliostatins
-
-
-
-
PD-ECGF
PD-ECGF/TP platelet-derived endothelial cell growth factor
-
-
-
-
phosphorylase, thymidine
-
-
-
-
platelet-derived endothelial cell growth factor
-
-
platelet-derived endotherial cell growth factor
-
-
pyrimidine deoxynucleoside phosphorylase
-
-
-
-
pyrimidine phosphorylase
-
-
-
-
pyrimidine/purine nucleoside phosphorylase
-
TDRPASE
-
-
-
-
thymidine-orthophosphate deoxyribosyltransferase
-
-
-
-
thymidine:orthophosphate deoxy-D-ribosyltransferase
-
-
-
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
thymidine + phosphate = thymine + 2-deoxy-alpha-D-ribose 1-phosphate
show the reaction diagram
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pentosyl group transfer
-
-
-
-
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.
CAS REGISTRY NUMBER
COMMENTARY hide
9030-23-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
1-(2',6'-dideoxy-alpha-L-lyxohexafuranosyl)thymine + phosphate
thymine + 2,6-dideoxy-L-lyxohexafuranose 1-phosphate
show the reaction diagram
-
-
-
?
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine + phosphate
thymine + 2,6-dideoxy-D-ribohexafuranose 1-phosphate
show the reaction diagram
-
-
-
?
2'-deoxythymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
3'-amino-3'-deoxythymidine + phosphate
?
show the reaction diagram
at pH 8.0
-
-
?
3'-deoxy-2',3'-didehydrothymidine + phosphate
thymine + 2,3-dideoxy-2,3-didehydro-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
4-thiothymidine + phosphate
4-thiothymine + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
5'-amino-5'-deoxythymidine + phosphate
thymine + 2,5-dideoxy-5-amino-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
5'-deoxythymidine + phosphate
thymine + 2,5-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
1-(2',6'-dideoxy-alpha-L-lyxo-hexafuranosyl)thymine + phosphate
?
show the reaction diagram
-
-
-
?
1-(2',6'-dideoxy-beta-D-ribo-hexafuranosyl)thymine + phosphate
?
show the reaction diagram
-
-
-
?
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine + phosphate
?
show the reaction diagram
-
-
-
?
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione + phosphate
?
show the reaction diagram
-
56% conversion after one h
-
-
?
1-[(2R,4S,5R)-5-(aminomethyl)-4-hydroxytetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
show the reaction diagram
-
11% conversion after one h
-
-
?
1-[(2R,4S,5R)-5-(hydroxymethyl)-4-sulfanyltetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
show the reaction diagram
-
0.76% conversion after one h
-
-
?
1-[(2R,4S,5S)-4-hydroxy-5-(sulfanylmethyl)tetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
show the reaction diagram
-
39% conversion after one h
-
-
?
1-[(2R,4S,5S)-5-(chloromethyl)-4-hydroxytetrahydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione + phosphate
?
show the reaction diagram
-
24% conversion after one h
-
-
?
2'-deoxyuridine + phosphate
?
show the reaction diagram
-
-
-
?
2'-deoxyuridine + phosphate
uracil + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
-
?
3'-amino-3'-deoxythymidine + phosphate
?
show the reaction diagram
-
-
-
?
3'-deoxy-2',3'-didehydrothymidine + phosphate
?
show the reaction diagram
-
-
-
?
3'-deoxythymidine + phosphate
thymine + 2,3-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
3.2% conversion after one h
-
-
?
3'-thiothymidine + phosphate
thymine + 3-thio-2,3-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
0.76% conversion after 1 h
-
-
?
4'-thiothymidine + phosphate
?
show the reaction diagram
-
3.8% conversion after one h
-
-
?
4-thiothymidine + phosphate
4-thiothymine + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
-
?
4-thiothymidine + phosphate
?
show the reaction diagram
-
-
-
?
5'-amino-5'-deoxythymidine + phosphate
?
show the reaction diagram
-
-
-
?
5'-amino-5'-deoxythymidine + phosphate
thymine + 5-amino-2,5-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
11% conversion after 1 h
-
-
?
5'-chloro-5'-deoxythymidine + phosphate
?
show the reaction diagram
-
-
-
?
5'-chloro-5'-deoxythymidine + phosphate
thymine + 5-chloro-2,5-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
24% conversion after 1 h
-
-
?
5'-deoxythymidine + phosphate
?
show the reaction diagram
-
-
-
?
5'-deoxythymidine + phosphate
thymine + 2,5-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
68% conversion after one h
-
-
?
5'-deoxyuridine + phosphate
uracil + 5-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
-
?
5'-thiothymidine + phosphate
thymine + 5-thio-2,5-dideoxy-D-ribose 1-phosphate
show the reaction diagram
-
39% conversion after 1 h
-
-
?
5-nitro-2'-deoxyuridine + phosphate
5-nitrouracil + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
-
?
6-azathymidine + phosphate
uracil + deoxyribose-1-phosphate
show the reaction diagram
-
5.4% conversion after one h
-
-
?
deoxythymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
-
-
-
-
?
thymidine + arsenate
?
show the reaction diagram
-
-
-
-
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
show the reaction diagram
thymidine + phosphate
thymine + 2-deoxy-D-ribose 1-phosphate
show the reaction diagram
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
show the reaction diagram
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
show the reaction diagram
uracil + 2-deoxy-alpha-D-ribose 1-phosphate
2'-deoxyuridine + phosphate
show the reaction diagram
-
-
-
r
uracil + phosphate
uracil + ribose 1-phosphate
show the reaction diagram
-
88% conversion after one h
-
-
?
uridine + phosphate
uracil + D-ribose 1-phosphate
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
show the reaction diagram
-
-
-
?
thymidine + phosphate
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
show the reaction diagram
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
thymidine + phosphate
show the reaction diagram
thymine + 2-deoxy-D-ribose 1-phosphate
thymidine + phosphate
show the reaction diagram
uracil + 2-deoxy-alpha-D-ribose 1-phosphate
2'-deoxyuridine + phosphate
show the reaction diagram
-
-
-
r
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-(2'-deoxy-beta-D-threo-pentafuranosyl)thymine
-
3'-amino-3'-deoxythymidine
-
3'-Deoxythymidine
-
5'-azido-5'-deoxythymidine
-
5'-bromo-5'-deoxythymidine
-
5'-chloro-5'-deoxythymidine
-
5'-iodo-5'-deoxythymidine
-
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-fluorouracil
38% inhibition at 0.04 mM
ftorafur
ftorafur is also called tegafur
methyluridine
-
(2,4,5-trioxo-3-phenethyl-imidazolidin-1-yl)ethanoic acid
-
-
(2E)-3-phenylprop-2-enoic acid
-
(2R,3R,4S,5R)-9-(3,4-dihydroxy-5-trityloxymethyl-tetrahydrofuran-2-yl)-1,9-dihydropurin-6-one
KIN59
(6aS)-1,2,9,10-tetramethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline
uncompetitive inhibition
(E)-2-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,4-diol
-
-
(E)-2-(2-(2-chlorobenzylidene)hydrazinyl)quinoxaline
-
-
(E)-2-(2-(2-fluorobenzylidene)hydrazinyl)quinoxaline
-
-
(E)-2-(2-(3-chlorobenzylidene)hydrazinyl)quinoxaline
-
-
(E)-2-(2-(3-fluorobenzylidene)hydrazinyl)quinoxaline
-
-
(E)-2-(2-(4-fluorobenzylidene)hydrazinyl)quinoxaline
-
-
(E)-3-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2-diol
-
-
(E)-3-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
-
-
(E)-4-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2-diol
-
-
(E)-4-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,3-diol
-
-
(E)-4-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
-
-
(E)-4-methoxy-2-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
-
-
(E)-5-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2,4-triol
-
-
(E)-5-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-2,4,6-triol
-
-
(E)-N'-(2,3-dimethoxybenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(2,4-dichlorobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(2-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(2-nitrobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(3,5-dichloro-2-hydroxybenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(3-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(3-hydroxy-5-methoxybenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(4-chlorobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(4-cyanobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(4-nitrobenzylidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(5-bromo-2-methoxybenzlidene)isoquinoline-3-carbohydrazide
-
(E)-N'-(anthracen-9-ylmethylen)isoquinoline-3-carbohydrazide
-
(R)-1-[3-fluoro-2-(phosphonomethoxy)-propyl]thymine
-
93% inhibition at 0.01 mM
(R)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]thymine
-
98% inhibition at 0.01 mM
(Z)-N'-(1-(4-nitrophenyl)ethylidene)isoquinoline-3-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-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-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
-
-
1-(2''-deoxy-beta-D-threo-pentafuranosyl)thymine
-
1-(2'-deoxy-beta-D-threo-pentafuranosyl)thymine
-
1-(2-hydroxyethoxymethyl)thymine
-
-
1-benzyl-imidazolidine-2,4,5-trione
-
-
1-[2-(phosphonomethoxy)ethyl]thymine
-
complete inhibition at 0.01 mM
2'-fluoro-3'-azido-2',3'-dideoxyuridine
N3FddU
2,2'-O-anhydrouridine
-
-
2,3,5-trihydroxy-6',7-dimethoxyflavone
-
2-(2',5'-dihydroxyphenyl)quinazolin-4(3H)-one
-
-
2-(2-methyl-1H-indol-3-yl)-N'-(2,4,6-trihydroxybenzylidene)acetohydrazide
-
2-(2-methyl-1H-indol-3-yl)-N'-(2-methylbenzylidene)acetohydrazide
-
2-(2-methyl-1H-indol-3-yl)-N'-(2-nitrobenzylidene)acetohydrazide
-
2-(2-methyl-1H-indol-3-yl)-N'-(3-methylbenzylidene)acetohydrazide
-
2-(2-methyl-1H-indol-3-yl)-N'-(3-nitrobenzylidene)acetohydrazide
-
2-(2-methyl-1H-indol-3-yl)-N'-(4-methylbenzylidene)acetohydrazide
-
2-(2-methyl-1H-indol-3-yl)-N'-(4-nitrobenzylidene)acetohydrazide
-
2-(3',4'-dihydroxyphenyl)quinazolin-4(3H)-one
-
-
2-(3'-ethoxy-4'-hydroxyphenyl)quinazolin-4(3H)-one
-
-
2-(3'-hydroxy-4'-methoxyphenyl)quinazolin-4(3H)-one
-
-
2-(3'-hydroxyphenyl)quinazolin-4(3H)-one
-
-
2-(4'-hydroxyphenyl)quinazolin-4(3H)-one
-
-
2-mercapto-7H-pyrrolo[2,3-d]pyrimidin-4(3H)-one
-
25% inhibition at 0.045 mM
2-[(5-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
-
2-[(5-(3-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]propanoic acid
-
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-(4-chlorophenyl)-4H-1,2,4-triazol-3-yl)thio]propanoic acid
-
2-[(5-(4-methylphenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
-
2-[(5-(4-nitrophenyl)-4H-1,2,4-triazol-3-yl)thio]acetic acid
-
2H-1-benzopyran-2-one
uncompetitive inhibition
3'-amino-3'-deoxythymidine
-
3'-azidothymidine
AZT
3'-Deoxythymidine
-
3,3',4',5-tetrahydroxy-6-methoxyflavone
mixed-type inhibition
3-(2,4,5-trioxo-3-phenethyl-imidazolidin-1-yl)-propionamide
-
-
3-(anilinomethyl)-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-([(1-benzyl-2-hydroxyethyl)imino]methyl)-4Hchromen-4-one
-
-
3-([(2, 4-dichlorophenyl)imino]methyl)-4H-chromen-4-one
-
-
3-([(2-([-(4-oxo-4H-chromen-3-yl)methylidene]amino)ethyl)imino] methyl)-4H-chromen-4-one
-
-
3-([(2-benzoyl-4-chlorophenyl)imino]methyl)-4Hchromen-4-one
-
-
3-([(2-methyl-6-nitrophenyl)imino]methyl)-4Hchromen-4-one
-
-
3-([(3-hydroxy-2-pyridinyl)imino]methyl)-4H-chromen-4-one
-
-
3-([(3-methoxy-4-methylphenyl)imino]methyl)-4Hchromen-4-one
-
-
3-([(3-methylphenyl)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-chloroanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(2-methoxyanilino)methyl]-5-phenyl-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-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(3-methoxyanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
-
3-[(3-methoxyanilino)methyl]-5-phenyl-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-(3-chlorobenzyl)-2,4,5-trioxo-imidazolidin-1-yl]-propionamide
-
-
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
4,5-diphenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
-
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-(trifluoromethyl)phenyl)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-(2,5-difluorobenzyl)-N-(m-tolyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(o-tolyl)piperazine-1-carbothioamide
-
4-(2,5-difluorobenzyl)-N-(p-tolyl)piperazine-1-carbothioamide
-
4-methoxy-7H-furo[3,2-g][1]benzopyran-7-one
-
5'-bromo-5'-deoxythymidine
-
5'-iodo-5'-deoxythymidine
-
5'-O-(2'',4''-dichlorobenzoyl)-thymidine-3'-O-2'',4''-dichlorobenzoate
-
5'-O-(2''-methoxybenzoyl)-thymidine
-
5'-O-(3''-bromobenzoyl)-thymidine
competitive inhibition
5'-O-(4''-bromobenzoyl)-thymidine-3'-O-4''-bromobenzoate
noncompetitive inhibition
5'-O-(4''-methoxybenzoyl)-thymidine
competitive inhibition
5'-O-(4''-methylbenzoyl)-thymidine
competitive inhibition
5'-O-trityl-inosine
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-(3-chlorophenyl)-4H-1,2,4-triazole-3-thiol
-
5-(3-pyridyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-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-chlorophenyl)-4H-1,2,4-triazole-3-thiol
-
5-(4-pyridyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
binding mode, modeling
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-[(2'-nitroimidazol-1'-yl)methyl]uracil
-
IC50: 0.0244 mM
5-bromo-6-[(4'-nitroimidazol-1'-yl)methyl]uracil
-
IC50: 0.0066 mM
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'-nitroimidazol-1'-yl)methyl]uracil
-
IC50: 0.0217 mM
5-chloro-6-[(4'-nitroimidazol-1'-yl)methyl]uracil
-
IC50: 0.007 mM
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracil hydrochloride
-
-
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl]uracilhydrochloride
-
-
5-fluoro-1-(tetrahydrofur-2-yl)uracil
-
-
5-fluoro-6-(1H-imidazol-1-ylmethyl)pyrimidine-2,4(1H,3H)-dione
-
-
5-fluoro-6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
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-[(4H-1,2,4-triazol-4-ylamino)methyl]pyrimidine-2,4(1H,3H)-dione
-
-
6-(1H-imidazol-1-ylmethyl)pyrimidine-2,4(1H,3H)-dione
-
-
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-(4H-1,2,4-triazol-4-ylmethyl)pyrimidine-2,4(1H,3H)-dione
-
-
6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
6-amino-5-bromouracil
6-aminothymine
-
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-[(2'-aminoimidazol-1'-yl)methyl]-5-bromouracil
-
IC50: 0.0000187 mM
6-[(2'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
-
IC50: below 0.0000206 mM
6-[(2'-aminoimidazol-1'-yl)methyl]uracil
-
IC50: 0.00056 mM
6-[(2'-nitroimidazol-1'-yl)methyl]uracil
-
IC50: 0.0024 mM
6-[(4'-aminoimidazol-1'-yl)methyl]-5-bromouracil
-
IC50: 0.00065 mM
6-[(4'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
-
IC50: 0.00073 mM
6-[(4'-aminoimidazol-1'-yl)methyl]uracil
-
IC50: 0.1014 mM
6-[(4'-nitroimidazol-1'-yl)methyl]uracil
-
IC50: 0.0138 mM
7-deazaxanthine
7-hydroxy-6-methoxy-2H-1-benzopyran-2-one
non-competitive inhibition
8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b']dipyran-2-one
uncompetitive inhibition
cycloheximide
-
-
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
-
flavone
uncompetitive inhibition
KIN56
-
IC50: 0.232 mM
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-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(2,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(2-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(2-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(3-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(4-(dimethylamino)benzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(4-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-(4-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
N'-[-(4-oxo-4H-chromen-3-yl)methylidene]propanohydrazide
-
-
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-(adamantan-1-yl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
-
NSC 122612
-
0.12 mM, 27% inhibition
NSC 19791
-
0.89 mM, 14% inhibition
NSC 23145
-
0.105 mM, 23% inhibition
NSC 298251
-
0.1 mM, 30% inhibition
NSC 3056
-
0.089 mM, 24% inhibition
NSC 309091
-
0.13 mM, 21% inhibition
NSC 357688
-
0.09 mM, 28% inhibition
NSC 43275
-
0.106 mM, 16% inhibition
NSC 6487
-
0.089 mM, 6% inhibition
NSC 65043
-
0.093 mM, 84% inhibition, linear competitive
NSC 659977
-
0.134 mM, 60% inhibition
NSC 81031
-
0.93 mM, 15% inhibition
ribose 1-phosphate
-
competitive
SO42-
-
inhibition reversed by phosphate
thymine
the substrate is a non-competitive inhibitor of the enzyme
xanthine
-
13% inhibition at 0.158 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-2,3,4,7-tetrahydro-1H-pyrrolo[2,3-d]pyrimidin-1-yl)octyl]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-methyl-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)ethoxy]methyl]phosphonic acid
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.35
1-(2',6'-dideoxy-alpha-L-lyxohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.3 - 0.33
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
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
0.19 - 0.3
thymidine
0.35
1-(2',6'-dideoxy-alpha-L-lyxo-hexafuranosyl)thymine
25°C, pH 6.5
0.33
1-(2',6'-dideoxy-beta-D-ribo-hexafuranosyl)thymine
25°C, pH 6.5
0.3
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
25°C, pH 6.5
0.32
2'-deoxyuridine
-
0.4
3'-amino-3'-deoxythymidine
25°C, pH 6.5
0.35
3'-deoxy-2',3'-didehydrothymidine
25°C, pH 6.5
10
3'-Deoxythymidine
-
in 50 mM phosphate buffer, pH 6.8
0.25 - 0.28
4-thiothymidine
0.4
5'-amino-5'-deoxythymidine
25°C, pH 6.5
0.3
5'-chloro-5'-deoxythymidine
25°C, pH 6.5
0.4 - 32
5'-Deoxythymidine
0.23
5-nitro-2'-deoxyuridine
0.89
phosphate
-
-
0.24 - 2.5
thymidine
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.45
1-(2',6'-dideoxy-alpha-L-lyxohexafuranosyl)thymine
in 50 mM potassium phosphate buffer (pH 6.5), at 25°C
0.1 - 0.6
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
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
130 - 198
thymidine
0.45
1-(2',6'-dideoxy-alpha-L-lyxo-hexafuranosyl)thymine
25°C, pH 6.5
0.1
1-(2',6'-dideoxy-beta-D-ribo-hexafuranosyl)thymine
25°C, pH 6.5
0.6
1-(2',6'-dideoxy-beta-D-ribohexafuranosyl)thymine
25°C, pH 6.5
35
2'-deoxyuridine
-
1.1
3'-amino-3'-deoxythymidine
25°C, pH 6.5
0.4
3'-deoxy-2',3'-didehydrothymidine
25°C, pH 6.5
63
4-thiothymidine
0.58
5'-amino-5'-deoxythymidine
25°C, pH 6.5
1.7
5'-chloro-5'-deoxythymidine
-
260
5'-Deoxythymidine
-
20
5-nitro-2'-deoxyuridine
198 - 1770
thymidine
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
680
thymidine
at pH 7.4 and 37°C
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.45
1-(2'-deoxy-beta-D-threo-pentafuranosyl)thymine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
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
0.0042
5-fluorouracil
at pH 7.4 and 37°C
0.45
ftorafur
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.12
methyluridine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.06
uridine
in 50 mM potassium phosphate buffer, pH 6.5, 25°C
0.3497
(2E)-3-phenylprop-2-enoic acid
pH 7.0, 30°C
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
25°C, pH 6.5
1.5
1-(2-hydroxyethoxymethyl)thymine
-
pH 7.5, 25°C, activity with 4-thiothymidine
0.4 - 0.5
2,2'-O-anhydrouridine
0.1131
2,3,5-trihydroxy-6',7-dimethoxyflavone
pH 7.0, 30°C
0.4203
2H-1-benzopyran-2-one
pH 7.0, 30°C
0.6
3'-amino-3'-deoxythymidine
25°C, pH 6.5
0.85
3'-Deoxythymidine
25°C, pH 6.5
0.0768
3,3',4',5-tetrahydroxy-6-methoxyflavone
pH 7.0, 30°C
0.044
4,4'-[(2R,3S)-2,3-dimethylbutane-1,4-diyl]di(benzene-1,2-diol)
pH 7.0, 30°C
0.3442
4-methoxy-7H-furo[3,2-g][1]benzopyran-7-one
pH 7.0, 30°C
0.4
5'-bromo-5'-deoxythymidine
25°C, pH 6.5
0.4
5'-iodo-5'-deoxythymidine
25°C, pH 6.5
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
0.039 - 0.146
5'-O-trityl-inosine
0.4 - 0.45
5-fluoro-1-(tetrahydrofur-2-yl)uracil
0.000051
5-fluoro-6-(1H-imidazol-1-ylmethyl)pyrimidine-2,4(1H,3H)-dione
-
-
0.001
5-fluoro-6-([[2-hydroxy-1-(hydroxymethyl)ethyl]amino]methyl)pyrimidine-2,4(1H,3H)-dione
-
-
0.000011
5-fluoro-6-[(2-aminoimidazol-1-yl)methyl]uracil
-
-
0.00037
5-fluoro-6-[(4H-1,2,4-triazol-4-ylamino)methyl]pyrimidine-2,4(1H,3H)-dione
-
-
0.0047
6-(1H-imidazol-1-ylmethyl)pyrimidine-2,4(1H,3H)-dione
-
-
0.054
6-(4H-1,2,4-triazol-4-ylmethyl)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
0.1934
7-hydroxy-6-methoxy-2H-1-benzopyran-2-one
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
0.1951
flavone
pH 7.0, 30°C
0.45
ftorafur
25°C, pH 6.5
12.5
NSC 65043
-
-
additional information
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.085
(2,4,5-trioxo-3-phenethyl-imidazolidin-1-yl)ethanoic acid
Escherichia coli
-
pH 7.4, 25°C
0.0032
(E)-2-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,4-diol
Escherichia coli
-
pH 7.4, 25°C
0.0376
(E)-2-(2-(2-chlorobenzylidene)hydrazinyl)quinoxaline
Escherichia coli
-
pH 7.4, 25°C
0.0336
(E)-2-(2-(2-fluorobenzylidene)hydrazinyl)quinoxaline
Escherichia coli
-
pH 7.4, 25°C
0.0734 - 0.0935
(E)-2-(2-(3-chlorobenzylidene)hydrazinyl)quinoxaline
0.0661
(E)-2-(2-(3-fluorobenzylidene)hydrazinyl)quinoxaline
Escherichia coli
-
pH 7.4, 25°C
0.0581
(E)-2-(2-(4-fluorobenzylidene)hydrazinyl)quinoxaline
Escherichia coli
-
pH 7.4, 25°C
0.0355
(E)-3-((2-(quinoxalin-2-yl)hydrazono)methyl)benzene-1,2-diol
Escherichia coli
-
pH 7.4, 25°C
0.0632
(E)-3-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
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
0.0334
(E)-4-((2-(quinoxalin-2-yl)hydrazono)methyl)phenol
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
0.0276
(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
0.115
1-benzyl-imidazolidine-2,4,5-trione
Escherichia coli
-
pH 7.4, 25°C
0.0595
2-(2',5'-dihydroxyphenyl)quinazolin-4(3H)-one
Escherichia coli
-
at pH 7.0 and 30°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
0.0429
2-(3',4'-dihydroxyphenyl)quinazolin-4(3H)-one
Escherichia coli
-
at pH 7.0 and 30°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
0.295
2-(3'-hydroxyphenyl)quinazolin-4(3H)-one
Escherichia coli
-
at pH 7.0 and 30°C
0.234
2-(4'-hydroxyphenyl)quinazolin-4(3H)-one
Escherichia coli
-
at pH 7.0 and 30°C
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
0.04
3-(2,4,5-trioxo-3-phenethyl-imidazolidin-1-yl)-propionamide
Escherichia coli
-
pH 7.4, 25°C
0.1041
3-(anilinomethyl)-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.473
3-([(1-benzyl-2-hydroxyethyl)imino]methyl)-4Hchromen-4-one
Escherichia coli
-
pH 7.6
0.04
3-([(2, 4-dichlorophenyl)imino]methyl)-4H-chromen-4-one
Escherichia coli
-
pH 7.6
0.15
3-([(2-([-(4-oxo-4H-chromen-3-yl)methylidene]amino)ethyl)imino] methyl)-4H-chromen-4-one
Escherichia coli
-
pH 7.6
0.076
3-([(2-benzoyl-4-chlorophenyl)imino]methyl)-4Hchromen-4-one
Escherichia coli
-
pH 7.6
0.48
3-([(2-methyl-6-nitrophenyl)imino]methyl)-4Hchromen-4-one
Escherichia coli
-
pH 7.6
0.34
3-([(3-hydroxy-2-pyridinyl)imino]methyl)-4H-chromen-4-one
Escherichia coli
-
pH 7.6
0.02
3-([(3-methoxy-4-methylphenyl)imino]methyl)-4Hchromen-4-one
Escherichia coli
-
pH 7.6
0.067
3-([(3-methylphenyl)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
0.08724
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
0.1338
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
0.04061
3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
Escherichia coli
-
at pH 7.4 and 25°C
0.0844
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
0.066
3-[3-(3-chlorobenzyl)-2,4,5-trioxo-imidazolidin-1-yl]-propionamide
Escherichia coli
-
pH 7.4, 25°C
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
0.146
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
0.044
5'-O-trityl-inosine
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
0.062
5-(3-chlorophenyl)-4H-1,2,4-triazole-3-thiol
Escherichia coli
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
0.08873
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
0.1876
5-(4-chlorophenyl)-4H-1,2,4-triazole-3-thiol
Escherichia coli
pH 7.4, 25°C
0.0823
5-(4-pyridyl)-4-phenyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
Escherichia coli
pH 7.4, 25°C
0.0244
5-bromo-6-[(2'-nitroimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.0244 mM
0.0066
5-bromo-6-[(4'-nitroimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.0066 mM
0.0217
5-chloro-6-[(2'-nitroimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.0217 mM
0.007
5-chloro-6-[(4'-nitroimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.007 mM
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
0.0016
6-amino-5-bromouracil
Escherichia coli
-
in 0.1 M potassium phosphate buffer (pH 7.4), at 25°C
0.0000187
6-[(2'-aminoimidazol-1'-yl)methyl]-5-bromouracil
Escherichia coli
-
IC50: 0.0000187 mM
0.0000206
6-[(2'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
Escherichia coli
-
IC50: below 0.0000206 mM
0.00056
6-[(2'-aminoimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.00056 mM
0.0024
6-[(2'-nitroimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.0024 mM
0.00065
6-[(4'-aminoimidazol-1'-yl)methyl]-5-bromouracil
Escherichia coli
-
IC50: 0.00065 mM
0.00073
6-[(4'-aminoimidazol-1'-yl)methyl]-5-chlorouracil
Escherichia coli
-
IC50: 0.00073 mM
0.1014
6-[(4'-aminoimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.1014 mM
0.0138
6-[(4'-nitroimidazol-1'-yl)methyl]uracil
Escherichia coli
-
IC50: 0.0138 mM
0.0065 - 0.041
7-deazaxanthine
0.0002
cycloheximide
Escherichia coli
-
at pH 7.0 and 30°C
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
0.232
KIN56
Escherichia coli
-
IC50: 0.232 mM
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
0.0056
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
0.0066
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
0.0039
N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
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
0.0048
N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
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
0.0199
N'-(4-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
Escherichia coli
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
0.146
N'-[-(4-oxo-4H-chromen-3-yl)methylidene]propanohydrazide
Escherichia coli
-
pH 7.6
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
0.0422
N-(adamantan-1-yl)-4-(2,5-difluorobenzyl)piperazine-1-carbothioamide
Escherichia coli
pH 7.4, 25°C
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
0.0114
[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
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5
-
assay at
7.1
-
assay at
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
the amino acid sequence of thymidine phosphorylase (TP) is extremely conserved. For instance, human TP shares 39% sequence identity with Escherichia coli TP
metabolism
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
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
43000
-
x * 43000, SDS-PAGE
46000
-
2 * 46000
90000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 43000, SDS-PAGE
dimer
homodimer
additional information
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
hanging drop vapor diffusion method
-
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
53
-
77% loss of activity after 10 min, phosphate or 2'-deoxyribose-1-phosphate stabilize
55
-
99% loss of activity after 10 min, phosphate or 2'-deoxyribose-1-phosphate stabilize
additional information
-
phosphate or pentose 1-phosphate ester substrates stabilize against heat inactivation
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
crystals are stable to X-rays at room temperature for at least 5 days
-
phosphate or pentose 1-phosphate ester substrates stabilize against heat inactivation
-
stability depends on protein concentration
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20°C, 10 mM Tris-HCl, pH 7.3, stable for several months
-
4°C, gradual loss of activity
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
native enzyme
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
co-expressed with uridine phosphorylase in Escherichia coli BL21(DE3) cells
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
synthesis
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Barbas, C.F.; Wong, C.H.
Overexpression and substrate specificity studies of phosphodeoxyribomutase and thymidine phosphorylase
Bioorg. Chem.
19
261-269
1991
Escherichia coli
-
Manually annotated by BRENDA team
Schwartz, M.
Thymidine phosphorylase from Escherichia coli
Methods Enzymol.
51
442-445
1978
Escherichia coli
Manually annotated by BRENDA team
Zimmerman, M.
Deoxyribosyl transfer. II. Nucleoside:pyrimidine deoxyribosyltransferase activity of three partially purified thymidine phosphorylases
J. Biol. Chem.
239
2622-2627
1964
Escherichia coli, Escherichia coli B / ATCC 11303, Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Cook, W.J.; Koszalka, G.W.; Hall, W.W.; Burns, C.L.; Ealick, S.E.
Crystallization and preliminary x-ray investigation of thymidine phosphorylase from Escherichia coli
J. Biol. Chem.
262
3788-3789
1987
Escherichia coli
Manually annotated by BRENDA team
Walter, M.R.; Cook, W.J.; Cole, L.B.; Short, S.A.; Koszalka, G.W.; Krenitsky, T.A.; Ealick, S.E.
Three-dimensional structure of thymidine phosphorylase from Escherichia coli at 2.8 A resolution
J. Biol. Chem.
265
14016-14022
1990
Escherichia coli
Manually annotated by BRENDA team
Krenitsky, T.A.; Tuttle, J.V.
Correlation of substrate-stabilization patterns with proposed mechanisms for three nucleoside phosphorylases
Biochim. Biophys. Acta
703
247-249
1982
Escherichia coli
Manually annotated by BRENDA team
Voytek, P.
Purification of thymidine phosphorylase from Escherichia coli and its photoinactivation in the presence of thymine, thymidine, and some halogenated analogs
J. Biol. Chem.
250
3660-3665
1975
Escherichia coli
Manually annotated by BRENDA team
Finnis, C.; Dodsworth, N.; Pollitt, C.E.; Carr, G.; Sleep, D.
Thymidine phosphorylase activity of platelet-derived endothelial cell growth factor is responsible for endothelial cell mitogenicity
Eur. J. Biochem.
212
201-210
1993
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Rick, S.W.; Abashkin, Y.G.; Hilderbrandt, R.L.; Burt, S.K.
Computational studies of the domain movement and the catalytic mechanism of thymidine phosphorylase
Proteins
37
242-252
1999
Escherichia coli
Manually annotated by BRENDA team
Focher, F.; Spadari, S.
Thymidine phosphorylase: a two-face janus in anticancer chemotherapy
Curr. Cancer Drug Targets
1
141-153
2001
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Mendieta, J.; Martin-Santamaria, S.; Priego, E.M.; Balzarini, J.; Camarasa, M.J.; Perez-Perez, M.J.; Gago, F.
Role of histidine-85 in the catalytic mechanism of thymidine phosphorylase as assessed by targeted molecular dynamics simulations and quantum mechanical calculations
Biochemistry
43
405-414
2004
Escherichia coli (P07650)
Manually annotated by BRENDA team
McNally, V.A.; Gbaj, A.; Douglas, K.T.; Stratford, I.J.; Jaffar, M.; Freeman, S.; Bryce, R.A.
Identification of a novel class of inhibitor of human and Escherichia coli thymidine phosphorylase by in silico screening
Bioorg. Med. Chem. Lett.
13
3705-3709
2003
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Liekens, S.; Hernandez, A.I.; Ribatti, D.; De Clercq, E.; Camarasa, M.J.; Perez-Perez, M.J.; Balzarini, J.
The nucleoside derivative 5'-O-trityl-inosine (KIN59)suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action
J. Biol. Chem.
279
29598-29605
2004
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Reigan, P.; Edwards, P.N.; Gbaj, A.; Cole, C.; Barry, S.T.; Page, K.M.; Ashton, S.E.; Luke, R.W.; Douglas, K.T.; Stratford, I.J.; Jaffar, M.; Bryce, R.A.; Freeman, S.
Aminoimidazolylmethyluracil analogues as potent inhibitors of thymidine phosphorylase and their bioreductive nitroimidazolyl prodrugs
J. Med. Chem.
48
392-402
2005
Escherichia coli, Homo sapiens (P19971), Homo sapiens
Manually annotated by BRENDA team
Panova, N.G.; Shcheveleva, E.V.; Alexeev, C.S.; Mukhortov, V.G.; Zuev, A.N.; Mikhailov, S.N.; Esipov, R.S.; Chuvikovsky, D.V.; Miroshnikov, A.I.
Use of 4-thiouridine and 4-thiothymidine in studies on pyrimidine nucleoside phosphorylases
Mol. Biol.
38
770-776
2004
Escherichia coli
-
Manually annotated by BRENDA team
Panova, N.G.; Alexeev, C.S.; Kuzmichov, A.S.; Shcheveleva, E.V.; Gavryushov, S.A.; Polyakov, K.M.; Kritzyn, A.M.; Mikhailov, S.N.; Esipov, R.S.; Miroshnikov, A.I.
Substrate specificity of Escherichia coli thymidine phosphorylase
Biochemistry
72
21-28
2007
Escherichia coli, Escherichia coli (P07650)
Manually annotated by BRENDA team
Gbaj, A.; Edwards, P.N.; Reigan, P.; Freeman, S.; Jaffar, M.; Douglas, K.T.
Thymidine phosphorylase from Escherichia coli: tight-binding inhibitors as enzyme active-site titrants
J. Enzyme Inhib. Med. Chem.
21
69-73
2006
Escherichia coli
Manually annotated by BRENDA team
Kalman, T.I.; Lai, L.
6-Substituted 5-fluorouracil derivatives as transition state analogue inhibitors of thymidine phosphorylase
Nucleosides Nucleotides Nucleic Acids
24
367-373
2005
Escherichia coli
Manually annotated by BRENDA team
Liekens, S.; Balzarini, J.; Hernandez, A.I.; De Clercq, E.; Priego, E.M.; Camarasa, M.J.; Perez-Perez, M.J.
Thymidine phosphorylase is noncompetitively inhibited by 5-O-trityl-inosine (KIN59) and related compounds
Nucleosides Nucleotides Nucleic Acids
25
975-980
2006
Escherichia coli, Homo sapiens (P19971), Homo sapiens
Manually annotated by BRENDA team
Hatano, A.; Harano, A.; Takigawa, Y.; Naramoto, Y.; Toda, K.; Nakagomi, Y.; Yamada, H.
Kinetic parameters and recognition of thymidine analogues with varying functional groups by thymidine phosphorylase
Bioorg. Med. Chem.
16
3866-3870
2008
Escherichia coli
Manually annotated by BRENDA team
Pomeisl, K.; Holy, A.; Votruba, I.; Pohl, R.
Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase
Bioorg. Med. Chem. Lett.
18
1364-1367
2008
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Reigan, P.; Gbaj, A.; Stratford, I.J.; Bryce, R.A.; Freeman, S.
Xanthine oxidase-activated prodrugs of thymidine phosphorylase inhibitors
Eur. J. Med. Chem.
43
1248-1260
2008
Escherichia coli, Homo sapiens (P19971), Homo sapiens
Manually annotated by BRENDA team
Pomeisl, K.; Votruba, I.; Holy, A.; Pohl, R.
Syntheses of pyrimidine acyclic nucleoside phosphonates as potent inhibitors of thymidine phosphorylase (PD-ECGF) from SD-lymphoma
Nucleosides Nucleotides Nucleic Acids
26
1025-1028
2007
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Jain, H.V.; Rasheed, R.; Kalman, T.I.
The role of phosphate in the action of thymidine phosphorylase inhibitors: implications for the catalytic mechanism
Bioorg. Med. Chem. Lett.
20
1648-1651
2010
Escherichia coli, Homo sapiens (P19971)
Manually annotated by BRENDA team
Khan, K.M.; Ambreen, N.; Hussain, S.; Perveen, S.; Choudhary, M.I.
Schiff bases of 3-formylchromone as thymidine phosphorylase inhibitors
Bioorg. Med. Chem.
17
2983-2988
2009
Escherichia coli
Manually annotated by BRENDA team
Bronckaers, A.; Gago, F.; Balzarini, J.; Liekens, S.
The dual role of thymidine phosphorylase in cancer development and chemotherapy
Med. Res. Rev.
29
903-953
2009
Geobacillus stearothermophilus, Escherichia coli, Homo sapiens, Mus musculus, Rattus norvegicus, Salmonella enterica subsp. enterica serovar Typhimurium
Manually annotated by BRENDA team
Panova, N.; Alexeev, C.; Polyakov, K.; Gavryushov, S.; Kritzyn, A.; Mikhailov, S.
Substrate specificity of thymidine phosphorylase of E. coli: role of hydroxyl groups
Nucleosides Nucleotides Nucleic Acids
27
1211-1214
2008
Escherichia coli
Manually annotated by BRENDA team
Marak, D.; Otmar, M.; Votruba, I.; Dracinsky, M.; Krecmerova, M.
8-Aza-7,9-dideazaxanthine acyclic nucleoside phosphonate inhibitors of thymidine phosphorylase
Bioorg. Med. Chem. Lett.
21
652-654
2011
Escherichia coli, Homo sapiens
Manually annotated by BRENDA team
Serra, I.; Serra, C.D.; Rocchietti, S.; Ubiali, D.; Terreni, M.
Stabilization of thymidine phosphorylase from Escherichia coli by immobilization and post immobilization techniques
Enzyme Microb. Technol.
49
52-58
2011
Escherichia coli
Manually annotated by BRENDA team
Rajabi, M.; Mansell, D.; Freeman, S.; Bryce, R.A.
Structure-activity relationship of 2,4,5-trioxoimidazolidines as inhibitors of thymidine phosphorylase
Eur. J. Med. Chem.
46
1165-1171
2011
Escherichia coli
Manually annotated by BRENDA team
Ding, Q.; Ou, L.; Wei, D.; Wei, X.
Optimum induction of recombinant thymidine phosphorylase and its application
Nucleosides Nucleotides Nucleic Acids
30
360-368
2011
Escherichia coli
Manually annotated by BRENDA team
Javaid, S.; Saad, S.M.; Perveen, S.; Khan, K.M.; Choudhary, M.I.
2-Arylquinazolin-4(3H)-ones: A novel class of thymidine phosphorylase inhibitors
Bioorg. Chem.
63
142-151
2015
Escherichia coli
Manually annotated by BRENDA team
Shahzad, S.A.; Yar, M.; Bajda, M.; Jadoon, B.; Khan, Z.A.; Naqvi, S.A.; Shaikh, A.J.; Hayat, K.; Mahmmod, A.; Mahmood, N.; Filipek, S.
Synthesis and biological evaluation of novel oxadiazole derivatives: a new class of thymidine phosphorylase inhibitors as potential anti-tumor agents
Bioorg. Med. Chem.
22
1008-1015
2014
Escherichia coli
Manually annotated by BRENDA team
Petaccia, M.; Gentili, P.; Besker, N.; DAbramo, M.; Giansanti, L.; Leonelli, F.; La Bella, A.; Gradella Villalva, D.; Mancini, G.
Kinetics and mechanistic study of competitive inhibition of thymidine phosphorylase by 5-fluoruracil derivatives
Colloids Surf. B Biointerfaces
140
121-127
2016
Escherichia coli (P07650), Escherichia coli
Manually annotated by BRENDA team
Xiong, S.; Wang, Y.; Wang, X.; Wang, J.; Li, J.; Zhang, G.; Zhang, R.; Xie, L.; Wang, H.
Enzymatic synthesis of 2-deoxyuridine by whole cell catalyst co-expressing uridine phosphorylase and thymidine phosphorylase through auto-induction system
J. Biosci. Bioeng.
118
723-727
2014
Escherichia coli
Manually annotated by BRENDA team
Serra, I.; Bavaro, T.; Cecchini, D.; Daly, S.; Albertini, A.; Terreni, M.; Ubiali, D.
A comparison between immobilized pyrimidine nucleoside phosphorylase from Bacillus subtilis and thymidine phosphorylase from Escherichia coli in the synthesis of 5-substituted pyrimidine 2'-deoxyribonucleosides
J. Mol. Catal. B
95
16-22
2013
Escherichia coli
-
Manually annotated by BRENDA team
Taha, M.; Ismail, N.H.; Imran, S.; Rahim, F.; Wadood, A.; Al Muqarrabun, L.M.; Khan, K.M.; Ghufran, M.; Ali, M.
In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase
Bioorg. Chem.
68
80-89
2016
Escherichia coli
Manually annotated by BRENDA team
Javaid, S.; Ishtiaq, M.; Shaikh, M.; Hameed, A.; Choudhary, M.I.
Thymidine esters as substrate analogue inhibitors of angiogenic enzyme thymidine phosphorylase in vitro
Bioorg. Chem.
70
44-56
2017
Escherichia coli (P0C037)
Manually annotated by BRENDA team
Uddin, I.; Taha, M.; Rahim, F.; Wadood, A.
Synthesis and molecular docking study of piperazine derivatives as potent inhibitor of thymidine phosphorylase
Bioorg. Chem.
78
324-331
2018
Escherichia coli (P0C037)
Manually annotated by BRENDA team
Iftikhar, F.; Yaqoob, F.; Tabassum, N.; Jan, M.S.; Sadiq, A.; Tahir, S.; Batool, T.; Niaz, B.; Ansari, F.L.; Choudhary, M.I.; Rashid, U.
Design, synthesis, in-vitro thymidine phosphorylase inhibition, in-vivo antiangiogenic and in-silico studies of C-6 substituted dihydropyrimidines
Bioorg. Chem.
80
99-111
2018
Escherichia coli (P0C037)
Manually annotated by BRENDA team
Shahzad, S.A.; Yar, M.; Khan, Z.A.; Shahzadi, L.; Naqvi, S.A.R.; Mahmood, A.; Ullah, S.; Shaikh, A.J.; Sherazi, T.A.; Bale, A.T.; Kukulowicz, J.; Bajda, M.
Identification of 1,2,4-triazoles as new thymidine phosphorylase inhibitors future anti-tumor drugs
Bioorg. Chem.
85
209-220
2019
Escherichia coli (P0C037)
Manually annotated by BRENDA team
Zaman, K.; Rahim, F.; Taha, M.; Wadood, A.; Adnan Ali Shah, S.; Gollapalli, M.; Ullah, F.; Ahmed, A.
Synthesis, thymidine phosphorylase, angiogenic inhibition and molecular docking study of isoquinoline derivatives
Bioorg. Chem.
89
102999
2019
Escherichia coli (P0C037), Escherichia coli
Manually annotated by BRENDA team
Taha, M.; Aldhamin, E.A.J.; Almandil, N.B.; Anouar, E.H.; Uddin, N.; Alomari, M.; Rahim, F.; Adalat, B.; Ibrahim, M.; Nawaz, F.; Iqbal, N.; Alghanem, B.; Altolayyan, A.; Khan, K.M.
Synthesis of indole based acetohydrazide analogs Their in vitro and in silico thymidine phosphorylase studies
Bioorg. Chem.
98
103745
2020
Escherichia coli (P0C037)
Manually annotated by BRENDA team
Bera, H.; Chigurupati, S.
Recent discovery of non-nucleobase thymidine phosphorylase inhibitors targeting cancer
Eur. J. Med. Chem.
124
992-1003
2016
Escherichia coli (P0C037), Homo sapiens (P19971)
Manually annotated by BRENDA team
Javaid, S.; Shaikh, M.; Fatima, N.; Choudhary, M.I.
Natural compounds as angiogenic enzyme thymidine phosphorylase inhibitors in vitro biochemical inhibition, mechanistic, and in silico modeling studies
PLoS ONE
14
e0225056
2019
Escherichia coli (P0C037)
Manually annotated by BRENDA team