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2.1.1.45: thymidylate synthase

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

Word Map on EC 2.1.1.45

Reaction

5,10-methylenetetrahydrofolate
+
dUMP
=
dihydrofolate
 +
dTMP

Synonyms

BgDHFR-TS, bifunctional TS-DHFR, DFR-TS, DHFR-TS, DHFR–TS, dihydrofolate reductase-thymidylate synthase, dTMP synthase, HTS, human TS, LBRM_06_0830, methylenetetrahydrofolate:dUMP C-methyltransferase, More, Thy1, ThyA, thymidylate synthase, thymidylate synthase A, thymidylate synthase-dihydrofolate reductase, thymidylate synthetase, ThyX, TMP synthetase, TMPS, TS, TS-DHFR, TSase, TYMS, Y110A7A.4

ECTree

     2 Transferases
         2.1 Transferring one-carbon groups
             2.1.1 Methyltransferases
                2.1.1.45 thymidylate synthase

KI Value

KI Value on EC 2.1.1.45 - thymidylate synthase

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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000018
(2R)-2-(5-[[(1-hydroxy-3-methyl-5,10a-dihydrobenzo[f]quinazolin-9-yl)methyl]amino]-1-oxo-1,3-dihydro-2H-isoindol-2-yl)butanedioic acid
22°C
0.0027
1,3-propanediphosphonic acid
pH 7.2, 22°C
0.016
1-(2'-deoxyribosyl)-8-azapurin-2-one 5'-monophosphate
-
-
0.12
1-(beta-D-2'-deoxyribofuranosyl)-1,6-dihydro-8-azapurin-2(3H,6H)-one 5'-monophosphate
-
-
0.022 - 0.0321
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
0.0049 - 0.0085
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
0.0008 - 0.0014
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
0.0013 - 0.00191
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
0.0034 - 0.00746
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
0.0017 - 0.0093
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
0.0075
10-formyldihydropteroylglutamate
-
-
0.0007
10-formyldihydropteroylheptaglutamate
-
-
0.0016
10-formyldihydropteroylpentaglutamate
-
-
0.0001
10-Formyltetrahydrofolylheptaglutamate
-
-
0.0024
10-Formyltetrahydrofolylmonoglutamate
-
-
0.02
10-formyltetrahydropteroylmonoglutamate
-
-
0.00477
2',5-difluoro-ara-UMP
-
0.4328
2'-deoxy-2',2'-difluorouridine 5'-dihydrogen
-
0.0103
2'-fluoro-ara-UMP
-
0.03
2,4-diamino pteridine
-
-
0.0013
2,4-diamino quinazoline
-
-
0.003
2,4-diamino quinazoline antifolate
-
-
0.002
2-(4-hydroxy[1,1'-biphenyl]-3-yl)-4-methyl-1H-isoindole-1,3(2H)-dione
pH not specified in the publication, temperature not specified in the publication
0.013
2-[2-(3-methoxyphenoxy)propyl]-4-methyl-1H-isoindole-1,3(2H)-dione
pH not specified in the publication, temperature not specified in the publication
0.025
4'-[(4-methyl-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl][1,1'-biphenyl]-2-carbonitrile
pH not specified in the publication, temperature not specified in the publication
0.024
4,5,6,7-tetrachloro-2-[3-(phenylsulfanyl)propyl]-1H-isoindole-1,3(2H)-dione
pH not specified in the publication, temperature not specified in the publication
0.01
5-bromo-2'-deoxyuridine 5'-monophosphate
-
-
0.0054 - 0.0066
5-bromoacetamido-5'-deoxythymidine
0.000002 - 0.0001
5-fluoro-2'-deoxyuridine 5'-monophosphate
0.0011 - 0.0054
5-fluoro-2'-deoxyuridine-5'-monophosphate
0.000001 - 0.002
5-fluoro-2'-deoxyuridylic acid
0.00001 - 0.000013
5-Formyl-2'-deoxyuridylic acid
0.00001 - 0.00004
5-Mercapto-2'-deoxyuridylic acid
0.000029
5-Nitro-2'-deoxyuridine 5'-monophosphate
-
-
0.000039
5-trifluoromethyl-2'-deoxyuridine 5'-monophosphate
-
-
0.00001
5-trifluoromethyl-2'-deoxyuridylic acid
-
-
5 - 5.2
aminofolate
0.015 - 0.0347
aminopterin
0.0015
bromo-2'-deoxyuridine
-
L1210 parental enzyme
0.0003
chloro-2'-deoxyuridine
-
L1210 parental enzyme
0.000004
Cibacron blue
-
-
0.00000006 - 0.0000028
D1694
0.000001 - 0.0000015
D1694 pentaglutamate
0.0075
deaza-aminopterin
-
-
0.0014 - 0.00303
dihydrofolate
0.0084
dithiophosphate
-
-
0.024 - 0.24
dTMP
12
glyceraldehyde 3-phosphate
-
-
0.0037
hydroxymethyl-2'-deoxyuridine
-
L1210 parental enzyme
0.00768
iodo-2'-deoxyuridine
-
L1210 parental enzyme
0.0029
methasquin
-
-
0.023 - 0.073
methopterin
0.000000095 - 0.413
methotrexate
0.000348
nolatrexed
pH 7.4, 25°C, recombinant enzyme
0.00029
pemetrexed
pH 7.4, 25°C, recombinant enzyme
0.0001 - 0.00022
Procion blue
0.0000059 - 0.0000113
propylene diphosphonate
0.0132
pteroyldiglutamate
-
-
0.0034
Pteroylheptaglutamate
-
-
0.002
pteroylhexaglutamate
-
-
0.0076
pteroylmonoglutamate
-
-
0.001
pteroylpentaglutamate
-
-
0.0006
pteroyltetraglutamate
-
-
0.0034
Pteroyltriglutamate
-
-
0.6 - 0.9
pyridoxal 5'-phosphate
-
-
0.00000635
pyrimethamine
pH 7.4, 25°C, recombinant enzyme
0.0044
quinaspar
-
-
0.0000931
raltitrexed
pH 7.4, 25°C, recombinant enzyme
0.0013
SK 28,757
-
-
0.0015
SK 28,758
-
-
0.0029
SK 28,815
-
-
-
0.00012
tetrahydromethotrexate
-
-
0.0017
thiophosphate
-
-
0.001 - 0.333
thymidine phosphate
0.0000176 - 0.852
trimethoprim
0.000000597
trimetrexate
pH 7.4, 25°C, recombinant enzyme
0.000038
ZD9331
pH 7.2, 22°C
additional information
additional information
-