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(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
7,8-dihydropteroylglutamate + thymidine phosphate
(6R)-N5,N10-methylene-5,6,7,8-tetrahydrofolate + 2'-deoxyuridylate
7,8-dihydrofolate + 5-methyl-2'-deoxyuridylate
(6S)-methylenetetrahydropteroylhexaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylhexaglutamate + thymidine phosphate
-
-
-
-
r
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
(6S)-tetrahydropteroyltriglutamate + 2'-deoxyuridylate
7,8-dihydropteroyltriglutamate + thymidine phosphate
-
-
-
-
r
(R)-5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
?
(R)-5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-formyltetrahydropteroylheptaglutamate + dUMP
?
-
-
-
-
r
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + 2'-deoxycytidine 5'-monophosphate
dihydrofolate + cytidine phosphate
5,10-methylenetetrahydrofolate + 2'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
5,10-methylenetetrahydrofolate + 5'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
-
some mutants are capable of forming covalent thymidylate synthase-5-fluoro-dUMP-methylenetetrahydrofolate complex
-
-
?
5,10-methylenetetrahydrofolate + 5-bromo-2'-deoxyuridine
?
-
-
-
?
5,10-methylenetetrahydrofolate + 6-fluoro-dUMP
?
-
-
-
-
?
5,10-methylenetetrahydrofolate + deoxyuridine monophosphate
7,8-dihydrofolate + deoxythymidine monophosphate
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
5,10-methylenetetrahydrofolate + uridine 5'-phosphate
dihydrofolate + TMP
5,10-methylenetetrahydrofolylheptaglutamate + 2'-deoxyuridylate
7,8-dihydrofolylheptaglutamate + thymidine phosphate
-
-
-
-
r
5,10-methylenetetrahydrofolylpentaglutamate + 2'-deoxyuridylate
7,8-dihydrofolylpentaglutamate + thymidine phosphate
-
-
-
-
r
5,10-methylenetetrahydropteroylheptaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylheptaglutamate + thymidine phosphate
5,10-methylenetetrahydropteroylpentaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylpentaglutamate + thymidine phosphate
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
methylenetetrahydropteroylglutamate + dUMP
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
r
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-dithiophosphate
7,8-dihydrofolate + ?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-thiophosphate
7,8-dihydrofolate + ?
N5,10-methylenetetrahydrofolate + 5-hydroxy-2'-deoxyuridine 5'-monophosphate
7,8-dihydrofolate + ?
-
-
-
-
?
N5,N10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
[6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
[6R]-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
-
-
-
-
r
[6R]methylenetetrahydropteroyldiglutamate + dUMP
7,8-dihydropteroyldiglutamate + thymidine phosphate
-
-
-
-
r
[6R]methylenetetrahydropteroylheptaglutamate + dUMP
7,8-dihydropteroylheptaglutamate + thymidine phosphate
-
-
-
-
r
[6R]methylenetetrahydropteroylhexaglutamate + dUMP
7,8-dihydropteroylhexaglutamate + thymidine phosphate
-
-
-
-
r
[6R]methylenetetrahydropteroylpentaglutamate + dUMP
7,8-dihydropteroylpentaglutamate + thymidine phosphate
-
-
-
-
r
[6R]methylenetetrahydropteroyltetraglutamate + dUMP
7,8-dihydropteroyltetraglutamate + thymidine phosphate
-
-
-
-
r
[6R]methylenetetrahydropteroyltriglutamate + dUMP
7,8-dihydropteroyltriglutamate + thymidine phosphate
-
-
-
-
r
additional information
?
-
(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
?
(-)-tetrahydropteroylglutamate + 2'-deoxyuridine 5'-monophosphate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
?
(6R)-N5,N10-methylene-5,6,7,8-tetrahydrofolate + 2'-deoxyuridylate
7,8-dihydrofolate + 5-methyl-2'-deoxyuridylate
-
-
-
r
(6R)-N5,N10-methylene-5,6,7,8-tetrahydrofolate + 2'-deoxyuridylate
7,8-dihydrofolate + 5-methyl-2'-deoxyuridylate
-
-
-
-
r
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
?
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
r
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
?
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
?
(6S)-tetrahydropteroylglutamate + 2-deoxyuridylate
7,8-dihydropteroylglutamate + thymidine phosphate
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
thymidylate synthase is the third enzyme in the methylene tetrahydrofolate cycle besides dihydrofolate reductase and serine hydroxymethyltransferase, in many organisms, thymidylate synthase is the only de novo source for dTMP required for DNA synthesis
-
-
?
5,10-methylene-5,6,7,8-tetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + 2'-deoxycytidine 5'-monophosphate
dihydrofolate + cytidine phosphate
-
only mutant TS N229D
-
-
?
5,10-methylenetetrahydrofolate + 2'-deoxycytidine 5'-monophosphate
dihydrofolate + cytidine phosphate
-
only mutant TS N229D
-
-
?
5,10-methylenetetrahydrofolate + 2'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
-
-
-
-
?
5,10-methylenetetrahydrofolate + 2'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
-
-
-
-
?
5,10-methylenetetrahydrofolate + 2'-fluoro-2'-deoxyuridine 5'-phosphate
7,8-dihydrofolate + ?
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
thymidylate synthase is essential for de novo synthesis of dTMP and is a key enzyme involved in DNA synthesis and transcriptional regulation of organisms
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
691522, 691589, 691614, 692016, 692158, 692480, 692655, 694120, 694481, 694482, 695129 -
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
during TS inhibition, TMP levels decrease with a subsequent increase in dUTP
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
inhibition of thymidylate synthase or of DHFR leads to thymineless death of eukaryotic organisms
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
it is a key enzyme for the synthesis of the DNA-specific nucleotide thymidylate
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
thymidylate synthase catalyses the only de novo pathway to produce thymidylate for DNA replication and repair
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
thymidylate synthase is a key enzyme in the de novo synthesis of dTMP
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
TS is a key enzyme in folate metabolism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
mTHF, TS is the sole source of de novo thymidylate which is required for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
thymidylate synthase is an essential enzyme for de novo synthesis of thymidylate (dTMP), a precursor for DNA synthesis
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
Tequatrovirus T4
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
Abies sp.
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
reverse reaction is at least 630times slower than the forward reaction
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
485357, 485363, 485365, 485369, 485371, 485372, 485374, 485382, 485383, 485388, 485397, 485402, 485406, 485409, 485413, 485416, 485417, 485421, 485425, 705044, 705333, 706772, 711474, 757061 -
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
485357, 485359, 485363, 485365, 485369, 485371, 485372, 485373, 485374, 485375, 485376, 485380, 485381, 485382, 485383, 485388, 485389, 485397, 485402, 485405, 485406, 485408, 485409, 485413, 485415, 485416, 485417, 485419, 485421, 485422, 485423, 485425, 485430, 485431 -
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
reverse reaction is at least 630times slower than the forward reaction
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
485358, 485359, 485375, 485376, 485380, 485381, 485408, 485415, 485423, 485430, 485431 -
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
485382, 485387, 485393, 485398, 485407, 485413, 485426, 485428, 485429, 702996, 703391, 703950, 705044, 711474, 718866, 719078, 719649, 720965, 720995 -
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
485359, 485364, 485375, 485376, 485381, 485382, 485384, 485387, 485389, 485393, 485395, 485398, 485400, 485403, 485404, 485407, 485408, 485413, 485415, 485419, 485422, 485423, 485426, 485428, 485429, 485430 -
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
reverse reaction is at least 630times slower than the forward reaction
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
485358, 485359, 485364, 485375, 485376, 485381, 485384, 485395, 485403, 485404, 485408, 485415, 485423, 485430 -
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
485359, 485360, 485363, 485364, 485365, 485366, 485368, 485369, 485370, 485372, 485376, 485377, 485378, 485379, 485380, 485382, 485383, 485384, 485387, 485388, 485393, 485396, 485397, 485399, 485401, 485403, 485406, 485409, 485410, 485411, 485415, 485416, 485418, 485423, 485427, 485429, 485430, 485431 -
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
485359, 485360, 485361, 485363, 485364, 485365, 485366, 485368, 485369, 485370, 485372, 485375, 485376, 485377, 485378, 485379, 485380, 485381, 485382, 485383, 485384, 485385, 485387, 485388, 485389, 485393, 485396, 485397, 485399, 485400, 485401, 485403, 485405, 485406, 485409, 485410, 485411, 485415, 485416, 485418, 485419, 485423, 485427, 485429, 485430, 485431 -
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
392255, 485359, 485360, 485363, 485365, 485368, 485369, 485382, 485383, 485384, 485386, 485387, 485390, 485391, 485393, 485398, 485402, 485403, 485413, 485415, 485426, 485427, 485430, 704570 -
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
392255, 485359, 485360, 485361, 485363, 485365, 485368, 485369, 485373, 485375, 485382, 485383, 485384, 485386, 485387, 485390, 485391, 485393, 485398, 485400, 485402, 485403, 485404, 485413, 485415, 485426, 485427, 485430 -
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
key function in DNA synthesis, repair and cell division
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
biosynthesis of thymidylic acid, only de novo source of thymidine, crucial for DNA replication in every organism
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
Tequatrovirus T4
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
Tequatrovirus T4
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
Tequintavirus T5
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
dUMP substrate binding structure analysis
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
Trypanosoma rhodesiense
-
-
-
-
?, r
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + dUMP
dihydrofolate + dTMP
-
-
-
-
?
5,10-methylenetetrahydrofolate + uridine 5'-phosphate
dihydrofolate + TMP
-
-
-
-
r
5,10-methylenetetrahydrofolate + uridine 5'-phosphate
dihydrofolate + TMP
-
-
-
-
r
5,10-methylenetetrahydropteroylheptaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylheptaglutamate + thymidine phosphate
-
-
-
-
r
5,10-methylenetetrahydropteroylheptaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylheptaglutamate + thymidine phosphate
-
-
-
-
r
5,10-methylenetetrahydropteroylpentaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylpentaglutamate + thymidine phosphate
-
-
-
-
r
5,10-methylenetetrahydropteroylpentaglutamate + 2'-deoxyuridylate
7,8-dihydropteroylpentaglutamate + thymidine phosphate
-
-
-
-
r
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
-
dehalogenation
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
dehalogenation does not require methylenetetrahydrofolate as cosubstrate
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
-
dehalogenation
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
-
dehalogenation
-
-
?
5-bromo-2'-deoxyuridine 5'-monophosphate + ?
?
-
dehalogenated by recombinant rat hepatoma enzyme
-
-
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
-
-
-
-
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
-
-
-
-
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
-
dehalogenation
-
-
?
5-iodo-2'-deoxyuridine 5'-monophosphate + ?
?
-
dehalogenated by recombinant rat hepatoma enzyme
-
-
?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-dithiophosphate
7,8-dihydrofolate + ?
-
-
-
-
?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-dithiophosphate
7,8-dihydrofolate + ?
-
-
-
-
?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-thiophosphate
7,8-dihydrofolate + ?
-
-
-
-
?
N5,10-methylenetetrahydrofolate + 2'-deoxyuridine 5'-thiophosphate
7,8-dihydrofolate + ?
-
-
-
-
?
N5,N10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
-
-
-
-
?
N5,N10-methylenetetrahydrofolate + dUMP
7,8-dihydrofolate + TMP
-
during thymidylate synthase inhibition, TMP levels decrease with a subsequent increase in dUTP
-
-
?
[6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
-
-
-
-
?
[6R,S]-5,10-methylenetetrahydropteroylglutamate + 2'-deoxyuridylate
?
-
-
-
-
r
additional information
?
-
-
thymidylate synthase form ThyX has no activity in Corynebacterium glutamicum
-
-
?
additional information
?
-
-
thymidylate synthase form ThyX has no activity in Corynebacterium glutamicum
-
-
?
additional information
?
-
-
the enzyme is specifically bound with its cognate mRNA in vitro and in vivo
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
UMP, dCMP and deoxyuridine are no substrates
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
(+) forms are inhibitors
-
-
?
additional information
?
-
-
nucleotides with large substituents on the 2' position are no substrates
-
-
?
additional information
?
-
-
enzyme catalyzes the exchange of a hydrogen atom between water and position 5 of dUMP, occurrence of reactions other than a methyl-group transfer during the interaction of the enzyme with its 2 substrates
-
-
?
additional information
?
-
chemical conversion takes place preferentially via a concerted mechanism where the hydride transfer is conjugated to thiol-elimination from the product. The substrate-enzyme covalent bond established between the C6 of the nucleotide substrate and a conserved cysteine residue is of labile character
-
-
?
additional information
?
-
-
(+) forms are inhibitors
-
-
?
additional information
?
-
-
nucleotides with large substituents on the 2' position are no substrates
-
-
?
additional information
?
-
-
enzyme catalyzes the exchange of a hydrogen atom between water and position 5 of dUMP, occurrence of reactions other than a methyl-group transfer during the interaction of the enzyme with its 2 substrates
-
-
?
additional information
?
-
-
nucleotides with large substituents on the 2' position are no substrates
-
-
?
additional information
?
-
-
enzyme catalyzes the exchange of a hydrogen atom between water and position 5 of dUMP, occurrence of reactions other than a methyl-group transfer during the interaction of the enzyme with its 2 substrates
-
-
?
additional information
?
-
-
recombinant protein is able to bind its own RNA
-
-
?
additional information
?
-
recombinant protein is able to bind its own RNA
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
inhibitors targeted at human TS designed from structures of bacterial TS may not be optimal
-
-
?
additional information
?
-
-
monofunctional enzyme
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
dCMP is no substrate, exception mutant TS N229D
-
-
?
additional information
?
-
-
dCMP is no substrate, exception mutant TS N229D
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
uridylate, cytidylate and deoxycytidylate are not substrates
-
-
?
additional information
?
-
-
bifunctional enzyme thymidilate synthase-dihydrofolate reductase, not possible to separate the 2 activities
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
-
bifunctional enzyme dihydrofolate reductase-thymidylate synthase
-
-
?
additional information
?
-
molecular mechanism of the distinct differences in substrate channeling behavior between Toxoplasma gondii TS-DHFR and Cryptosporidium hominis TS-DHFR, overview
-
-
?
additional information
?
-
-
molecular mechanism of the distinct differences in substrate channeling behavior between Toxoplasma gondii TS-DHFR and Cryptosporidium hominis TS-DHFR, overview
-
-
?
additional information
?
-
the bifunctional folate and pyrimidine-metabolising enzyme dihydrofolate reductase-thymidylate synthase dihydrofolate reductase-thymidylate synthase is expressed from a single gene as a homodimer comprising of an N-terminal DHFR domain fused via a linker peptide to a thymidylate synthase domain at the C-terminus
-
-
?
additional information
?
-
no activity with folic acid and the structurally related pterins (biopterin, dihydrobiopterin, sepiapterin and neopterin) as substrates by enzyme DHFR-TS
-
-
?
additional information
?
-
the bifunctional folate and pyrimidine-metabolising enzyme dihydrofolate reductase-thymidylate synthase dihydrofolate reductase-thymidylate synthase is expressed from a single gene as a homodimer comprising of an N-terminal DHFR domain fused via a linker peptide to a thymidylate synthase domain at the C-terminus
-
-
?
additional information
?
-
no activity with folic acid and the structurally related pterins (biopterin, dihydrobiopterin, sepiapterin and neopterin) as substrates by enzyme DHFR-TS
-
-
?
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(+)tetrahydropteroylglutamate
-
-
(2S)-2-[(4-([(2,4-diaminopteridin-6-yl)methyl](methyl)amino)phenyl)formamido]pentanedioic acid
i.e, methotrexate, A DHFR inhibitor, binds at the DHFR active site
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
(6R)-tetrahydropteroylglutamate
-
-
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo(f)quinazolin-9-yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
BW1843U89, U89, distorts the thymidylate synthase active site
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
-
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
-
(S)-2-(5-(((1,2-dihydro3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl)amino)-1-oxo-2-isoindolinyl)glutaric acid
-
BW1843U89
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
1,3-propanediphosphonic acid
allosteric inhibitor of human thymidylate synthase; stabilizes an inactive conformer of loop 181-197. Mixed inhibitor of dUMP, uncompetitive inhibitor versus methylenetetrahydrofolate below 0.00025 mM, noncompetitive above 0.001 mM, respectively. 1,3-Propanediphosphonic acid shows positive cooperativity with antifolate inhibitor ZD9331. It leads to the formation of enzyme tetramers, but not of higher oligomers
1-(2'-deoxyribosyl)8-azapurin-2-one 5'-monophosphate
-
-
1-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)-4-phenylthiosemicarbazide
-
1-(beta-D-2'-deoxyribofuranosyl)1,6-dihydro-8-azapurin-2(3H,6H)-one 5'-monophosphate
-
-
1-(beta-D-2'-Deoxyribofuranosyl)8-azapurin-2-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-bromopyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-chloropyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-fluoropyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-hydroxymethylpyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyamino-5-iodopyrimidin-2(1H)-one 5'-monophosphate
-
-
1-(beta-D-2-deoxyribofuranosyl)-4-hydroxyaminopyrimidin-2(1H)-one 5'-monophosphate
-
-
1-ethyl-3-dimethylaminopropyl carbodiimide
-
-
1-phenyl-3-(3-dimethylaminopropyl) carbodiimide
-
-
1-phenyl-3-(3-trimethylaminopropyl) carbodiimide
-
-
10-formyl-5,8-dideazafolate
-
-
10-formyl-7,8 dihydrofolate-tetra-gamma-L-glutamate
-
-
10-formyldihydropteroylglutamate
-
-
10-formyldihydropteroylheptaglutamate
-
-
10-formyldihydropteroylpentaglutamate
-
-
10-formyltetrahydrofolate
-
-
10-Formyltetrahydrofolylheptaglutamate
-
-
10-Formyltetrahydrofolylmonoglutamate
-
-
10-formyltetrahydropteroylheptaglutamate
-
-
10-formyltetrahydropteroylmonoglutamate
-
-
10-formyltetrahydropteroylpolyglutamate
-
-
10-propargyl-5,8-dideazafolate
1843U89
i.e. (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, folate-based inhibitor
2',5-difluoro-ara-UMP
slow-binding (time-dependent) inhibitor
2'-deoxy-2',2'-difluorouridine 5'-dihydrogen
classic inhibitor (no time dependence of inhibition observed)
2'-deoxy-5-fluorouridine 5'-phosphate
-
-
2'-fluoro-ara-UMP
classic inhibitor (no time dependence of inhibition observed)
2,4-diamino pteridine
-
-
2,4-diamino quinazoline antifolate
-
-
2,4-dioxo-N-(2-(1-(m-tolyl)-1H-1,2,3-triazol-4-yl)phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-sulfonamide
-
2-(2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-cyanophenyl)acetic acid
-
2-(2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-methoxyphenyl)acetic acid
-
2-(2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)phenyl) acetic acid
-
2-(2-(4-hydroxybenzylidene)hydrazinyl)-6-oxo-4-(p-tolyl)-1,6-dihydropyrimidine-5-carbonitrile
-
2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido) terephthalic acid
-
2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-chloro benzoic acid
-
2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-cyanobenzoic acid
-
2-(4-hydroxy[1,1'-biphenyl]-3-yl)-4-methyl-1H-isoindole-1,3(2H)-dione
-
2-amino-4-hydroxyquinazoline
-
-
2-amino-4-hydroxyquinazoline folic acid
2-amino-4-oxo-4,7-dihydro-pyrrolo[2,3-d]pyrimidine-methyl-phenyl-L-glutamic acid
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
2-chloro-N'-[5-methyl-4-(4-methylphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetohydrazide
-
2-hydrazinyl-1,6-dihydro-6-oxo-4-p-tolyl pyrimidine-5-carbonitrile
-
2-hydroxyethyl disulfide
-
-
2-[2-(3-methoxyphenoxy)propyl]-4-methyl-1H-isoindole-1,3(2H)-dione
-
3,3-bis(4-methoxyphenyl)-1H,3H-benzo[de]isochromen-1-one
-
induces apoptotic cell death in SK-MEL-2 and SK-MEL-28 melanoma cell lines, mediated by downregulation of Bcl-2 protein level and PARP cleavage, and independent of p53 and Bax. Pan-caspases inhibitor Z-VAD-FMK blocks the effect
3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
3-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-(carboxymethyl)benzoic acid
-
3-beta-D-ribofuranosylmaleimide
-
showdomycin
3-beta-D-ribofuranosylmaleimide 5'-phosphate
-
showdomycin 5'-phosphate
4'-[(4-methyl-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl][1,1'-biphenyl]-2-carbonitrile
-
4,5,6,7-tetrachloro-2-[3-(phenylsulfanyl)propyl]-1H-isoindole-1,3(2H)-dione
-
4-amino-N10-methylfolic acid
4-chloro-N'-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)benzohydrazide
-
5'-CGCGGTACGGACACCGCGCG-3'
-
targets the TS mRNA translation start site TSS and increases the thymidylate synthase gene transcription in HeLa cell
-
5,10-methenyltetrahydrofolylhexa-gamma-L-glutamate
-
-
5,10-methylenetetrahydrofolate
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5-bromo-2'-deoxyuridylic acid
-
-
5-bromo-N4-hydroxy-2'-deoxycytidine
-
-
5-bromoacetamido-5'-deoxythymidine
-
-
5-chloro-N4-hydroxy-2'-deoxycytidine
-
-
5-chloroacetamido-5'-deoxythymidine
-
-
5-fluoro-2'-deoxyuridine
-
comparison with inhibitory effect of FdUMP[10] and 5-fluorouraci
5-fluoro-2'-deoxyuridine 5'-(p-aminophenyl phosphate)
5-fluoro-2'-deoxyuridine 5'-monophosphate
5-fluoro-2'-deoxyuridine monophosphate
-
-
5-fluoro-2'-deoxyuridine-5'-monophosphate
-
-
5-fluoro-2'-deoxyuridylic acid
5-Fluoro-2-deoxyuridine
-
FUdR
5-fluoro-dUMP[10]
-
a 10-mer of 5-fluoro-dUMP, a suicide inhibitor of thymidylate synthase, designed to bypass resistance to 5-fluorouracil, acts as a pro-drug of 5-fluoro-dUMP
5-fluorodeoxyuridine monophosphate
-
5-fluoropyrimidine-2,4(1H,3H)-dione
-
-
5-Formyl-2'-deoxyuridylic acid
5-haloacetamido-5'-deoxythymidine
-
-
5-hydroseleno-2'-deoxyuridylic acid
-
-
5-hydroxy-methyl-2'-deoxyuridine 5'-monophosphate
-
-
5-iodo-2'-deoxyuridylic acid
-
-
5-iodoacetamido-5'-deoxythymidine
-
-
5-iodoacetamidomethyl-2'-deoxyuridine 5'-phosphate
-
-
5-Mercapto-2'-deoxyuridylic acid
5-Nitro-2'-deoxyuridine 5'-monophosphate
-
-
5-nitro-2'-deoxyuridylic acid
-
-
5-trifluoromethyl-2'-deoxyuridine 5'-monophosphate
-
-
5-trifluoromethyl-2'-deoxyuridylic acid
-
-
5F-dUMP
-
mechanism-based inhibitor
6-bromo-3,3-bis(3-chloro-4-hydroxyphenyl)-1H,3H-benzo[de]isochromen-1-one
-
induces apoptotic cell death in SK-MEL-2 and SK-MEL-28 melanoma cell lines, mediated by downregulation of Bcl-2 protein level and PARP cleavage, and independent of p53 and Bax. Pan-caspases inhibitor Z-VAD-FMK blocks the effect
6-chloro-3,3-bis(4-hydroxyphenyl)-1H,3H-benzo[de]isochromen-1-one
-
induces apoptotic cell death in SK-MEL-2 and SK-MEL-28 melanoma cell lines, mediated by downregulation of Bcl-2 protein level and PARP cleavage, and independent of p53 and Bax. Pan-caspases inhibitor Z-VAD-FMK blocks the effect
8-azapurinone deoxyribonucleoside 5'-phosphate
-
-
antifolate
inhibits activitiy of bifunctional DHFR-TS enzyme
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
BGC 9331
-
treatment results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels. BGC 9331 induces accumulation of [18F]-fluorothymidine uptake in the intestine
BGC 945
-
alpha-folate receptor targeted antifolate TS inhibitor; cyclopenta[g]quinazoline-based inhibitor. Treatment results in concentration-dependent increase in thymidine uptake in FR-positive epidermoid KB cells and in increase of membrane-associated equilibrative nucleoside transporter type 1 levels. Tumor [18F]-fluorothymidine accumulation in KB xenografts increases by more than 2fold with maximal levels at 1 to 4 hours and 4 to 24 hours after drug treatment. Quantitiative changes in tumor [18F]-fluorothymidine uptake are associated with increased tumor dUrd levels
bromo-2'-deoxyuridine
-
-
capecitabine
-
prodrug of 5-fluorouracil
chloro-2'-deoxyuridine
-
-
CQLYQRSG
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
crocetin
binding pattern of crocetin is similar to that of ralitrexed and it poses maximum MolDock score as well as the rerank score
dihydropteroylglutamate
-
-
dihydropteroylhexaglutamate
-
-
dihydropteroylpentaglutamate
-
-
dihydropteroyltriglutamate
-
-
ethyl methanesulfonate
-
-
FdUMP[10]
-
multimer of 5-fluoro-2'-deoxyuridine 5'-monophosphate, inhibits cell growth with greater potency than 5-fluorouracil and 5-fluoro-2'-deoxyuridine
fluorodeoxyuridine monophosphate
folic acid oligoglutamate
-
-
-
gefitinib
-
inhibits the expression of the transcription factor E2F-1, resulting in a down-regulation of thymidylate synthase at the mRNA and protein level; inhibits the expression of the transcription factor E2F-1, resulting in the down-regulation of thymidylate synthase at the mRNA and protein levels
glyceraldehyde 3-phosphate
-
-
hydroxymethyl-2'-deoxyuridine
-
-
Hydroxyurea
-
supresses thymidilate synthase in growing algae, but no effect on purified enzyme
LCQFYVVN
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
N',N'-diacetyl-N-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)acetohydrazide
compound induces the level of active caspase 3, and elevates the Bax/Bcl2 ratio 44fold in comparison to the control
N'-(3-chlorobenzoyl)-2-(2,4-dihydroxypyrimidine-5-sulfonamido)benzoyl hydrazide
IC50 value 0.00126 mM for A-549 cells, 0.00208 mM for OVCAR-3 cells, 0.00182 mM for SCG-7901 cells, 0.00442 mM for MDA-MB-231 cells
N'-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)-4-nitrobenzohydrazide
-
N'-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)benzohydrazide
-
N-(2-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(2-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1, 2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(2-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
compound exhibits the most potent activity against A-549 cells (IC50 1.18 microM) and prominent enzyme inhibition. It inhibits A-549 cells proliferation by arresting the cell cycle in the G1/S phase. The inhibitor can downregulate the cycle checkpoint proteins cyclin D1 and cyclin E to inhibit the cell cycle progression, and then induce intrinsic apoptosis by activating caspase-3, and reducing the ratio of bcl-2/bax
N-(3-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(3-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(3-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydrothieno(2,3-d)pyrimidin-5-yl)sulfanyl)benzoyl)-L-glutamic acid
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
N-(4-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(4-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(4-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamyl-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)-gamma-glutamyl-gamma-glutamylglutamic acid
-
-
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
-
-
N-(4-{[(2-amino-4-oxo-1,4-dihydroquinazolin-6-yl)methyl](prop-2-ynoyl)amino}benzoyl)-L-glutamic acid
-
-
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
-
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
-
-
N10-formyltetrahydrofolate
-
-
N10-propargyl-5,8-dideazafolate
PDDF, a TS folate inhibitor, binds at the TS active site. Residues that are involved in binding the folate analogue PDDF include I402, D513, L516, F520, as well as the nonconserved R603 and conserved M608 located on the C-terminal tail of the TS-domain
N4-hydroxy-2'-deoxycytidine
-
-
N4-hydroxy-5-methyl-2'-deoxycytidine
-
-
N4-hydroxy-dCMP
enzyme forms, in the presence of tetrahydrofolate, a covalently bound 5-fluoro-dUMP-thymidylate synthase complex. The tetrahydrofolate- and time-dependent, covalent binding by thymidylate synthase is accompanied by the enzyme inactivation
N5-formiminotetrahydropteroyltriglutamate
-
-
N5-formyltetrahydropteroyloligoglutamate
-
-
novobiocin
Tequatrovirus T4
-
coumarin antibiotic produced by Streptomyces nivens, at 10 mM concentration the self-splicing of primary transcripts is inhibited by about 5%, at 40 mM concentration the splicing rate is inhibited by about 50%. The splicing inhibition is strongly dependent on Mg2+
OSI-7904L
-
a liposomal thymidylate synthase inhibitor, a liposomal formulation of OSI-7904 (S)-2-(5-((1,2-dihydro-3-methyl-1-oxobenzo(f)quinazolin-9-yl)methyl)amino-1-oxo-2-isoindolynl)-glutaric acid, administered in combination with oxaliplatin every 21 days in patients with advanced colorectal carcinoma; treatment of patients with advanced colorectal carcinoma, in combination with oxaliplatin. At the highest dose level of OSI-7904L 9 mg/m2, oxaliplatin 130 mg/m2, one of nine patients experienced dose-limiting toxicity of grade 3 oral mucositis with cycle 1 and five further patients required dose reductions. The toxicity profile of stomatitis, diarrhea, nausea, fatigue, sensory neuropathy and skin rash was consistent with that expected for a thymidylate synthase inhibitor/oxaliplatin combination regimen. High interpatient variability with no detectable interaction between OSI-7904L and oxaliplatin
p-chloromercuribenzoate
-
-
propylene diphosphonate
-
mixed competitive-noncompetitive inhibitor with respect to dUMP
Pteroylheptaglutamate
-
-
pteroylpentaglutamate
-
-
pteroyltetraglutamate
-
-
pyridoxal 5'-phosphate
-
-
QFYVVNSE
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
SELSCQLY
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
trifluoromethyldeoxyuridine 5'-monophosphate
VNSELSCQ
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
YVVNSELS
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
ZD9331
antifolate inhibitor, shows positive cooperativity with 1,3-propanediphosphonic acid
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
1,1-bis-(4-hydroxyphenyl)-1H-naphtho[1,2-c]furan-3-one
-
-
10-propargyl-5,8-dideazafolate
-
-
10-propargyl-5,8-dideazafolate
-
PDDF
10-propargyl-5,8-dideazafolate
PDDF, folate-like TS inhibitor
10-propargyl-5,8-dideazafolate
-
i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
10-propargyl-5,8-dideazafolate
-
-
10-propargyl-5,8-dideazafolate
-
PDDF
10-propargyl-5,8-dideazafolate
i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
10-propargyl-5,8-dideazafolate
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10-propargyl-5,8-dideazafolate
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10-propargyl-5,8-dideazafolate
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10-propargyl-5,8-dideazafolate
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PDDF
10-propargyl-5,8-dideazafolate
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i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
10-propargyl-5,8-dideazafolate
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2-amino-4-hydroxyquinazoline folic acid
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2-amino-4-hydroxyquinazoline folic acid
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2-amino-4-hydroxyquinazoline folic acid
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2-amino-4-hydroxyquinazoline folic acid
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2-amino-4-oxo-4,7-dihydro-pyrrolo[2,3-d]pyrimidine-methyl-phenyl-L-glutamic acid
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inhibitor of Cryptosporidium hominis thymidylate synthase with 5fold selectivity over the human enzyme. Compound also has anti-cryptosporidial activity in cell culture and inhibits dihydrofolate reductase enzyme activity with IC50 values of 0.049 microM
2-amino-4-oxo-4,7-dihydro-pyrrolo[2,3-d]pyrimidine-methyl-phenyl-L-glutamic acid
potent enzyme inhibitor with anti-cryptosporidial activity in cell culture, chemical synthesis, overview. The inhibitor forms several hydrogen bonds and van der Waals interactions with the DHFR active site residues, binding close to the nicotinamide ring of NADPH. The carbonyl oxygens of the catalytic D32 hydrogen bond with N3 of the inhibitor forming a fork that holds the inhibitor in optimal position bound to the enzyme
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
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dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
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dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
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2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
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2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
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2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
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dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
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dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
2-mercaptoethanol
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
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3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
-
-
3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
-
-
3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
-
-
3,3-bis-(3-chloro-4-hydroxyphenyl)-1H,3H-[1,8-c,d]pyran-1-one
-
-
4-amino-N10-methylfolic acid
-
-
4-amino-N10-methylfolic acid
-
-
4-amino-N10-methylfolic acid
-
-
5-fluoro-2'-deoxyuridine 5'-(p-aminophenyl phosphate)
-
-
5-fluoro-2'-deoxyuridine 5'-(p-aminophenyl phosphate)
-
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
-
-
5-fluoro-2'-deoxyuridine 5'-monophosphate
FdUMP
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
very strong inhibition, pseudo-noncompetitive
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
485358, 485359, 485369, 485375, 485383, 485397, 485402, 485413, 485417, 485419, 485423, 485430
5-fluoro-2'-deoxyuridylic acid
-
-
485358, 485359, 485375, 485384, 485387, 485393, 485400, 485404, 485413, 485419, 485423, 485430
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
485359, 485366, 485369, 485375, 485377, 485378, 485379, 485383, 485384, 485385, 485387, 485393, 485397, 485400, 485411, 485419, 485423, 485430
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
392255, 485359, 485369, 485375, 485383, 485384, 485387, 485393, 485400, 485402, 485404, 485413, 485427, 485430
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-2'-deoxyuridylic acid
Tequatrovirus T4
-
-
5-fluoro-2'-deoxyuridylic acid
-
-
5-fluoro-dUMP
-
-
5-fluoro-dUMP
enzyme forms, in the presence of tetrahydrofolate, a covalently bound 5-fluoro-dUMP-thymidylate synthase complex. The tetrahydrofolate- and time-dependent, covalent binding by thymidylate synthase is accompanied by the enzyme inactivation
5-fluorodeoxyuridine
-
5-FUdR, TS-targeting chemotherapeutic agent
5-fluorodeoxyuridine
-
forms an inhibitory, ternary covalent complex with the enzyme
5-Fluoroorotate
-
-
5-fluorouracil
-
-
5-fluorouracil
-
but a major mechanism of resistance to 5-fluorouracil is overexpression of thymidylate synthase
5-fluorouracil
-
5-FU, TS-targeting chemotherapeutic agent
5-fluorouracil
-
WiDr cells: 0.005 mM inhibits growth to 22%, inhibition cannot be potentiated by leucovorin but is rescued by uridine, 0.025 mM inhibits growth to 10%, inhibition can be rescued badly by uridine to an value of 31%, SW-948 and HT-29 cells: 0.005 mM shows an antiproliferative activity that is not affected by leucovorine addition and can be rescued by uridine, 0.1 mM shows a complete inhibition that cannot be rescued by uridine
5-fluorouracil
-
transfection with p53 induces resistance to 5-fluorouracil
5-fluorouracil
-
0.001 mM inhibits growth to 13%, inhibition can be rescued by uridine, 0.005 mM inhibits growth completely, inhibition cannot be rescued by uridine
5-fluorouracil
-
comparison with inhibitory effect of FdUMP[10] and 5-fluoro-2'-deoxyuridine
5-Formyl-2'-deoxyuridylic acid
-
-
5-Formyl-2'-deoxyuridylic acid
-
-
5-Formyl-2'-deoxyuridylic acid
-
-
5-Mercapto-2'-deoxyuridylic acid
-
-
5-Mercapto-2'-deoxyuridylic acid
-
-
5-Mercapto-2'-deoxyuridylic acid
-
possesses antitumor activity against Ehrlich ascites cells
aminopterin
-
-
antrycide
-
-
atherospermidine
competitive inhibition
atherospermidine
competitive inhibition
atherospermidine
competitive inhibition
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
benzyloxycarbonylamino-N,O-didansyl-L-tyrosine
-
-
D1694
-
-
D1694 pentaglutamate
-
-
dihydrofolate
-
-
dimidium
-
-
dTMP
-
-
ethidium
-
-
fluorodeoxyuridine monophosphate
-
-
fluorodeoxyuridine monophosphate
-
-
GW1843U89
-
-
GW1843U89
-
direct folate-based inhibitor
isomoschatoline
competitive inhibition
isomoschatoline
competitive inhibition
isomoschatoline
competitive inhibition
liriodenine
competitive inhibition
liriodenine
competitive inhibition
liriodenine
competitive inhibition
LSCQLYQR
-
octapeptide to specifically target the monomer-monomer interface of the enzyme. A fast-equilibrium mechanism exists that combines trafficking in/out of the cell and degradation pathways within cells
LSCQLYQR
allosteric peptide inhibitor, binds to the dimer interface and stabilizes the inactive form of the protein
melosmine
competitive inhibition
melosmine
competitive inhibition
melosmine
competitive inhibition
methopterin
-
-
methotrexate
-
-
methotrexate
most potent inhibitor of dihydrofolate reductase activity
methotrexate
competitive inhibition
methotrexate
competitive inhibition
methotrexate
Tequatrovirus T4
-
-
methotrexate
competitive inhibition
Mg2+
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N,O-didansyl-L-tyrosine
-
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
-
-
N-ethylmaleimide
-
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
-
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
-
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
-
-
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme; dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
potent inhibitor of thymidylate synthase
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
potent inhibitor of thymidylate synthase
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
-
potent inhibitor of thymidylate synthase
nolatrexed
-
transfection with p53 induces resistance to nolatrexed
nolatrexed
upon binding, the two insert regions in thymidylate synthase, the functions of which are unclear, undergo positional shifts toward the catalytic center
pemetrexed
-
-
pemetrexed
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme
pemetrexed
-
TS-targeting chemotherapeutic agent
pemetrexed
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme
pemetrexed
-
transfection with p53 induces resistance to pemetrexed
pemetrexed
-
direct folate-based inhibitor; inhibitory to cell growth even in cell lacking thymidylate synthase activity
pemetrexed
-
dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme
Pentamidine
-
-
piritrexim
-
-
plevitrexed
-
-
prothidium
-
-
pteroylhexaglutamate
-
-
pteroylpolyglutamate
-
-
pyrimethamine
competitive inhibition
pyrimethamine
competitive inhibition
pyrimethamine
competitive inhibition
Quinazoline
-
-
Quinazoline
Tequatrovirus T4
-
-
raltitrexed
-
-
raltitrexed
-
RTX, a folate analog that is a specific inhibitor of TS; treatment can stimulate accurate recombination events in human cells. Gene conversions not associated with crossovers are specifically enhanced severalfold. Recombination events provoked by a double-strand break are not impacted by treatment with raltitrexed, nor is error-prone double-strand break repair via nonhomologous end-joining
raltitrexed
-
TS-targeting chemotherapeutic agent
raltitrexed
-
transfection with p53 induces resistance to raltitrexed
raltitrexed
upon binding, the two insert regions in thymidylate synthase, the functions of which are unclear, undergo positional shifts toward the catalytic center
raltitrexed
-
direct folate-based inhibitor
suramin
-
-
tetrahydromethotrexate
-
-
tetrahydromethotrexate
-
-
tetrahydromethotrexate
-
-
tetrahydromethotrexate
-
-
thymidine phosphate
-
-
thymidine phosphate
-
product inhibition
TomudexR
-
-
trifluoromethyldeoxyuridine 5'-monophosphate
-
-
trifluoromethyldeoxyuridine 5'-monophosphate
-
-
trifluoromethyldeoxyuridine 5'-monophosphate
Tequatrovirus T4
-
-
trimethoprim
-
-
trimethoprim
competitive inhibition
trimethoprim
competitive inhibition
trimethoprim
competitive inhibition
trimetrexate
-
-
additional information
-
5FU-LV, combination of 5-fluorouracil and leucovorin
-
additional information
inhibitory effect of antifolate drugs on enzymatic activity, and inhibitory activity of four aporphine alkaloids from Rollinia pittieri and Pseudomalmea boyacana, and some 2,4-diamino-pyrimidine antifolates, overview
-
additional information
-
inhibitory effect of antifolate drugs on enzymatic activity, and inhibitory activity of four aporphine alkaloids from Rollinia pittieri and Pseudomalmea boyacana, and some 2,4-diamino-pyrimidine antifolates, overview
-
additional information
inhibitory effect of antifolate drugs on enzymatic activity, and inhibitory activity of four aporphine alkaloids from Rollinia pittieri and Pseudomalmea boyacana, and some 2,4-diamino-pyrimidine antifolates, overview
-
additional information
-
combination of 5-FU and leucovorin, enhances the inhibition of thymidylate synthase, 0.001 mM inhibits growth to only 1%, inhibition can be rescued by uridine to an almost normal value of 83%
-
additional information
-
combination of leucovorin and 5-fluorouracil 5FU-LV, IC50 0.00016 (FM3A/0 cell)
-
additional information
analysis of enzyme susceptibility to a range of classical inhibitors normally used in the treatment of cancer, bacterial or protozoal infections, in vivo effects in presence of absence of thymidine and/or folate, overview. Modulating certain medium components can affect drug sensitivity, presumably by either competition for uptake and competition for the active site of DHFR-TS. In the case of one human thymidylate synthase inhibitor raltitrexed, the inhibitor is more potent against the intact parasite. Addition of extra glutamic acid residues not only improves retention in the cell, but also increases potency against thymidylate synthase, as it does in human cells. No inhibition by FdUMP
-
additional information
inhibitory effect of antifolate drugs on enzymatic activity, and inhibitory activity of four aporphine alkaloids from Rollinia pittieri and Pseudomalmea boyacana, and some 2,4-diamino-pyrimidine antifolates, overview
-
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0.000054 - 0.00027
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
0.00015 - 0.00019
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
0.0000046
1-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)-4-phenylthiosemicarbazide
Homo sapiens
pH 7.4, 30°C
0.000019 - 0.00043
10-propargyl-5,8-dideazafolate
0.00197
2,4-dioxo-N-(2-(1-(m-tolyl)-1H-1,2,3-triazol-4-yl)phenyl)-1, 2, 3, 4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.009
2-(2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-cyanophenyl)acetic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.011
2-(2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-methoxyphenyl)acetic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.016
2-(2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)phenyl) acetic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.000013
2-(2-(4-hydroxybenzylidene)hydrazinyl)-6-oxo-4-(p-tolyl)-1,6-dihydropyrimidine-5-carbonitrile
Homo sapiens
pH 7.4, 30°C
0.018
2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido) terephthalic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.028
2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-chloro benzoic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.011
2-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-cyanobenzoic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.00038
2-amino-4-oxo-4,7-dihydro-pyrrolo[2,3-d]pyrimidine-methyl-phenyl-L-glutamic acid
Cryptosporidium hominis
-
pH not specified in the publication, temperature not specified in the publication
0.0046 - 0.023
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.0011 - 0.0025
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.00011 - 0.0023
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
0.00023 - 0.0023
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.00069 - 0.0016
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
0.0012 - 0.0023
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.00038 - 0.0023
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.00039 - 0.0022
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.00075 - 0.0025
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
0.0011 - 0.0023
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
0.0056 - 0.028
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
0.00028 - 0.002
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
0.0013 - 0.0029
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
0.00022 - 0.0017
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
0.00012 - 0.0024
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
0.00011 - 0.0012
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
0.0000081
2-chloro-N'-[5-methyl-4-(4-methylphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetohydrazide
Homo sapiens
pH 7.4, 30°C
0.0000044
2-hydrazinyl-1,6-dihydro-6-oxo-4-p-tolyl pyrimidine-5-carbonitrile
Homo sapiens
pH 7.4, 30°C
0.01
3-(4-((2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)methyl)benzamido)-4-(carboxymethyl)benzoic acid
Cryptosporidium hominis
25°C, pH not specified in the publication
0.0000047
4-chloro-N'-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 30°C
0.000005
5-Fluoro-2-deoxyuridine
Mus musculus
-
FM3A/0 cell
0.0000028
5-fluoro-dUMP
Mus musculus
-
FM3A/0 cell
0.00031
5-fluorouracil
Mus musculus
-
FM3A/0 cell
0.000000022 - 0.000022
FdUMP[10]
0.000164
GW1843U89
Mus musculus
-
FM3A/0 cell
0.013 - 0.09
methotrexate
0.0000037
N',N'-diacetyl-N-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)acetohydrazide
Homo sapiens
pH 7.4, 30°C
0.0000042
N'-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)-4-nitrobenzohydrazide
Homo sapiens
pH 7.4, 30°C
0.0000157
N'-(5-cyano-1,6-dihydro-6-oxo-4-p-tolylpyrimidin-2-yl)benzohydrazide
Homo sapiens
pH 7.4, 30°C
0.00087
N-(2-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.0006
N-(2-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1, 2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.00013
N-(2-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.00128
N-(3-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.00056
N-(3-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.00045
N-(3-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.000046 - 0.00023
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
0.00004
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydrothieno(2,3-d)pyrimidin-5-yl)sulfanyl)benzoyl)-L-glutamic acid
Homo sapiens
potent inhibitor of human TS and of human DHFR, it is a novel dual TS-DHFR inhibitor, 330-fold more potent than pemetrexed
0.000054 - 0.00027
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
0.00165
N-(4-(1-(2-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.00158
N-(4-(1-(3-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.00074
N-(4-(1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl) phenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide
Homo sapiens
pH 7.4, 30°C
0.047
N-(4-[[(2,4-diaminopteridin-6-yl)methyl](methyl)amino]benzoyl)glutamic acid
Homo sapiens
-
-
0.0049
N-([5-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2,3-dihydrothiophen-2-yl]carbonyl)-4-methylideneglutamic acid
Homo sapiens
-
-
0.0054 - 0.23
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
0.000018 - 0.00009
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
0.000046 - 0.00023
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
0.000036 - 0.00004
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
0.0048
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]-2-fluorobenzoyl]-4-methylideneglutamic acid
Homo sapiens
-
-
0.008
N-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
-
0.00128
nolatrexed
Mus musculus
-
FM3A/0 cell
0.000036 - 0.076
pemetrexed
0.000016 - 0.0057
raltitrexed
additional information
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
0.000054
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
Homo sapiens
-
-
0.00027
(2S)-2-[([4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)sulfanyl]phenyl]carbonyl)amino]pentanedioic acid
Escherichia coli
-
-
0.00015
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
Penaeus vannamei
at 30°C
0.00019
(S)-2-(5(((1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9 yl)methyl)amino)1-oxo-2-isoindolinyl)glutaric acid
Shrimp white spot syndrome virus
at 30°C
0.000019
10-propargyl-5,8-dideazafolate
Escherichia coli
-
-
0.000085
10-propargyl-5,8-dideazafolate
Homo sapiens
-
-
0.000085
10-propargyl-5,8-dideazafolate
Homo sapiens
-
0.00017
10-propargyl-5,8-dideazafolate
Penaeus vannamei
at 30°C
0.00023
10-propargyl-5,8-dideazafolate
Shrimp white spot syndrome virus
at 30°C
0.00043
10-propargyl-5,8-dideazafolate
Toxoplasma gondii
-
-
0.0046
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.023
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
IC50 above 0.023 mM
0.023
2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
IC50 above 0.023 mM
0.0011
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.002
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0025
2-amino-5-[(2-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.00011
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
0.0012
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0023
2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00023
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.001
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0023
2-amino-5-[(3,4-dichlorophenyl)thio]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00069
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0012
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0016
2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]-pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0012
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0018
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0023
2-amino-5-[(3,5-dimethoxyphenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.00038
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0018
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0023
2-amino-5-[(3-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00039
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0022
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0022
2-amino-5-[(4-bromophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.00075
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0022
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0025
2-amino-5-[(4-chlorophenyl)sulfanyl]-6-ethylthieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0011
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0014
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0023
2-amino-6-ethyl-5-(2-naphthylthio)thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0056
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0084
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.028
2-amino-6-ethyl-5-(phenylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00028
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0017
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.002
2-amino-6-ethyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0013
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.0026
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0029
2-amino-6-ethyl-5-[(4-fluorophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00022
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
-
0.001
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0017
2-amino-6-ethyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00012
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
0.0012
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.0024
2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.00011
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Homo sapiens
-
0.0012
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Escherichia coli
-
-
0.0012
2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
Toxoplasma gondii
-
-
0.063
CQLYQRSG
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.068
CQLYQRSG
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.068
CQLYQRSG
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.3
CQLYQRSG
Homo sapiens
mutant F59A, pH not specified in the publication, temperature not specified in the publication
0.3
CQLYQRSG
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.000000022
FdUMP[10]
Mus musculus
-
FdUMP[10] strongly inhibited cell growth in both FM3A cell lines, with a much lower resistance factor than FUdR and FdUMP
0.000022
FdUMP[10]
Mus musculus
-
pH 7.4, 37°C
0.075
LCQFYVVN
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.08
LCQFYVVN
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.088
LCQFYVVN
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.12
LCQFYVVN
Homo sapiens
mutant F59A, pH not specified in the publication, temperature not specified in the publication
0.188
LCQFYVVN
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.057
LSCQLYQR
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.067
LSCQLYQR
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.068
LSCQLYQR
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.075
LSCQLYQR
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.152
LSCQLYQR
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.3
LSCQLYQR
Homo sapiens
mutant F59A, pH not specified in the publication, temperature not specified in the publication
0.3
LSCQLYQR
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.3
LSCQLYQR
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.5
LSCQLYQR
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.013
methotrexate
Enterococcus faecalis
pH not specified in the publication, temperature not specified in the publication
0.018
methotrexate
Toxoplasma gondii
-
at 30°C and pH 7.4
0.029
methotrexate
Homo sapiens
-
at 30°C and pH 7.4
0.09
methotrexate
Escherichia coli
-
at 30°C and pH 7.4
0.000046
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
Homo sapiens
-
potent dual inhibitor of human TS and human DHFR, 2-fold more potent than PDDF and 206-fold more potent than pemetrexed
0.000069
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
Escherichia coli
-
potent inhibitor of human TS
0.00023
N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo(3,2-d)pyrimidin-5-yl)methyl)benzoyl)-L-glutamic acid
Toxoplasma gondii
-
moderate inhibitor of human thymidylate synthase
0.000054
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
Homo sapiens
-
potent inhibitor of human TS and moderate inhibitor of human DHFR
0.000054
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
Homo sapiens
potent inhibitor of human TS and moderate inhibitor of human DHFR
0.00027
N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
Escherichia coli
-
moderate inhibitor of human TS
0.0054
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
Homo sapiens
-
at 30°C and pH 7.4
0.027
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
Toxoplasma gondii
-
at 30°C and pH 7.4
0.23
N-[4-[(2,4-diamino-5-methyl-furo[2,3-d]pyrimidin-6-yl)thio]-benzoyl]-L-glutamic acid
Escherichia coli
-
at 30°C and pH 7.4
0.000018
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
Escherichia coli
-
-
0.000054
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
Homo sapiens
-
-
0.00009
N-[4-[(2-amino-6-ethyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)thio]benzoyl]-L-glutamic acid
Toxoplasma gondii
-
-
0.000046
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
Homo sapiens
-
-
0.000069
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
Escherichia coli
-
-
0.00023
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl]-L-glutamic acid
Escherichia coli
-
-
0.000036
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
Toxoplasma gondii
-
-
0.00004
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
Escherichia coli
-
-
0.00004
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
Homo sapiens
-
-
0.00004
N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
Homo sapiens
-
0.000036
pemetrexed
Mus musculus
-
FM3A/0 cell
0.0028
pemetrexed
Toxoplasma gondii
-
-
0.0028
pemetrexed
Toxoplasma gondii
-
at 30°C and pH 7.4
0.0095
pemetrexed
Homo sapiens
-
-
0.0095
pemetrexed
Homo sapiens
-
0.0095
pemetrexed
Homo sapiens
-
at 30°C and pH 7.4
0.076
pemetrexed
Escherichia coli
-
-
0.076
pemetrexed
Escherichia coli
-
at 30°C and pH 7.4
0.056
QFYVVNSE
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.071
QFYVVNSE
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.081
QFYVVNSE
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.3
QFYVVNSE
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.000016
raltitrexed
Mus musculus
-
FM3A/0 cell
0.00038
raltitrexed
Homo sapiens
-
at 30°C and pH 7.4
0.0009
raltitrexed
Toxoplasma gondii
-
at 30°C and pH 7.4
0.0057
raltitrexed
Escherichia coli
-
at 30°C and pH 7.4
0.03
SELSCQLY
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.045
SELSCQLY
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.052
SELSCQLY
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.3
SELSCQLY
Homo sapiens
mutant F59A, pH not specified in the publication, temperature not specified in the publication
0.3
SELSCQLY
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.05
VNSELSCQ
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.053
VNSELSCQ
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.088
VNSELSCQ
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.3
VNSELSCQ
Homo sapiens
mutant F59A, pH not specified in the publication, temperature not specified in the publication
0.3
VNSELSCQ
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.057
YVVNSELS
Homo sapiens
mutant K47A, pH not specified in the publication, temperature not specified in the publication
0.062
YVVNSELS
Homo sapiens
wild-type, pH not specified in the publication, temperature not specified in the publication
0.075
YVVNSELS
Homo sapiens
mutant Y202A, pH not specified in the publication, temperature not specified in the publication
0.3
YVVNSELS
Homo sapiens
mutant F59A, pH not specified in the publication, temperature not specified in the publication
0.3
YVVNSELS
Homo sapiens
mutant L198A, pH not specified in the publication, temperature not specified in the publication
0.00144
ZD1694
Homo sapiens
-
wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C
0.034
ZD1694
Homo sapiens
-
mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C
additional information
N-[4-[2-(2,4-diamino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2,4-diaminopyrido[3,2-d]pyrimidin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
additional information
N-[4-[2-(2-amino-4-methylquinazolin-6-yl)ethyl]benzoyl]-4-methylideneglutamic acid
Homo sapiens
-
value above 0.05
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