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Literature summary extracted from

  • Gangjee, A.; Qiu, Y.; Li, W.; Kisliuk, R.L.
    Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates (2008), J. Med. Chem., 51, 5789-5797.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.1.1.45 medicine inhibition of TS and DHFR enzymes has found clinical utility as antitumor, antimicrobial and antiprotozoal agents Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
2.1.1.45 molecular modeling of complex with inhibitor N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid. The 6-methyl moiety of of the inhibitor makes important hydrophobic contacts with Trp109 and also serves to lock the 5-position side chain into favorable, low-energy conformations for thymidlyate synthase binding Escherichia coli
2.1.1.45 molecular modeling of complex with inhibitor N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid. The 6-methyl moiety of of the inhibitor makes important hydrophobic contacts with Trp109 and also serves to lock the 5-position side chain into favorable, low-energy conformations for thymidlyate synthase binding Toxoplasma gondii
2.1.1.45 molecular modeling of complex with inhibitor N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid. The 6-methyl moiety of of the inhibitor makes important hydrophobic contacts with Trp109 and also serves to lock the 5-position side chain into favorable, low-energy conformations for thymidlyate synthase binding Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.3 2-amino-4-oxo-6-methyl-5-phenylsulfanylthieno[2,3-d]pyrimidine
-
 Escherichia coli
1.5.1.3 2-amino-4-oxo-6-methyl-5-phenylsulfanylthieno[2,3-d]pyrimidine
-
 Homo sapiens
1.5.1.3 2-amino-4-oxo-6-methyl-5-phenylsulfanylthieno[2,3-d]pyrimidine
-
 Toxoplasma gondii
1.5.1.3 2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-5-[(4-chlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-5-[(4-chlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-5-[(4-chlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-5-[(4-fluorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-5-[(4-fluorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-5-[(4-fluorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
 Escherichia coli
1.5.1.3 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
 Homo sapiens
1.5.1.3 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
-
 Toxoplasma gondii
1.5.1.3 methotrexate
-
 Escherichia coli
1.5.1.3 methotrexate
-
 Homo sapiens
1.5.1.3 methotrexate
-
 Toxoplasma gondii
1.5.1.3 additional information inhibitor synthesis and molecular modelling Escherichia coli
1.5.1.3 additional information inhibitor synthesis and molecular modelling Homo sapiens
1.5.1.3 additional information inhibitor synthesis and molecular modelling Toxoplasma gondii
1.5.1.3 N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl)-L-glutamic acid binding mode, overview Escherichia coli
1.5.1.3 N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl)-L-glutamic acid binding mode, overview Homo sapiens
1.5.1.3 N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl)-L-glutamic acid binding mode, overview Toxoplasma gondii
1.5.1.3 nolatrexed
-
 Escherichia coli
1.5.1.3 nolatrexed
-
 Homo sapiens
1.5.1.3 nolatrexed
-
 Toxoplasma gondii
1.5.1.3 pemetrexed
-
 Escherichia coli
1.5.1.3 pemetrexed
-
 Homo sapiens
1.5.1.3 pemetrexed
-
 Toxoplasma gondii
1.5.1.3 raltitrexed
-
 Escherichia coli
1.5.1.3 raltitrexed
-
 Homo sapiens
1.5.1.3 raltitrexed
-
 Toxoplasma gondii
1.5.1.3 trimethoprim
-
 Escherichia coli
1.5.1.3 trimethoprim
-
 Homo sapiens
1.5.1.3 trimethoprim
-
 Toxoplasma gondii
2.1.1.45 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 Escherichia coli
2.1.1.45 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 Homo sapiens
2.1.1.45 10-propargyl-5,8-dideazafolate i.e. PDDF. Dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme Toxoplasma gondii
2.1.1.45 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 human and Toxoplasma gondii enzyme Escherichia coli
2.1.1.45 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 Homo sapiens
2.1.1.45 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 human and Escherichia coli enzyme Toxoplasma gondii
2.1.1.45 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 human and Toxoplasma gondii enzyme Escherichia coli
2.1.1.45 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 Homo sapiens
2.1.1.45 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 human and Escherichia coli enzyme Toxoplasma gondii
2.1.1.45 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 human and Toxoplasma gondii enzyme Escherichia coli
2.1.1.45 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 Homo sapiens
2.1.1.45 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 human and Escherichia coli enzyme Toxoplasma gondii
2.1.1.45 N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydrothieno(2,3-d)pyrimidin-5-yl)sulfanyl)benzoyl)-L-glutamic acid
-
 Homo sapiens
2.1.1.45 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
2.1.1.45 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 Escherichia coli
2.1.1.45 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 Homo sapiens
2.1.1.45 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 Toxoplasma gondii
2.1.1.45 pemetrexed dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Toxoplasma gondii enzyme Escherichia coli
2.1.1.45 pemetrexed dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on Escherichia coli and Toxoplasma gondii enzyme Homo sapiens
2.1.1.45 pemetrexed dual inhibitor of thymidylate synthase and dihydrofolate reductase. Comparison with inhibitory effect on human and Escherichia coli enzyme Toxoplasma gondii

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Escherichia coli
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 ?
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Toxoplasma gondii
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 ?
1.5.1.3 7,8-dihydrofolate + NADPH + H+ Homo sapiens
-
 5,6,7,8-tetrahydrofolate + NADP+
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP Homo sapiens inhibition of thymidylate synthase or of DHFR leads to thymineless death of eukaryotic organisms 7,8-dihydrofolate + dTMP
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.3 Escherichia coli
-
-
-
1.5.1.3 Homo sapiens P00374
-
-
1.5.1.3 Toxoplasma gondii
-
-
-
2.1.1.45 Escherichia coli
-
-
-
2.1.1.45 Homo sapiens P04818
-
-
2.1.1.45 Toxoplasma gondii
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Escherichia coli 5,6,7,8-tetrahydrofolate + NADP+
-
 ?
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Toxoplasma gondii 5,6,7,8-tetrahydrofolate + NADP+
-
 ?
1.5.1.3 7,8-dihydrofolate + NADPH + H+
-
 Homo sapiens 5,6,7,8-tetrahydrofolate + NADP+
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP
-
 Homo sapiens 7,8-dihydrofolate + dTMP
-
 ?
2.1.1.45 5,10-methylenetetrahydrofolate + dUMP inhibition of thymidylate synthase or of DHFR leads to thymineless death of eukaryotic organisms Homo sapiens 7,8-dihydrofolate + dTMP
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.5.1.3 DHFR
-
 Escherichia coli
1.5.1.3 DHFR
-
 Toxoplasma gondii
1.5.1.3 DHFR
-
 Homo sapiens
2.1.1.45 TS-DHFR
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.5.1.3 NADPH
-
 Escherichia coli
1.5.1.3 NADPH
-
 Toxoplasma gondii
1.5.1.3 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.3 0.000008
-
-
 Toxoplasma gondii N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl)-L-glutamic acid
1.5.1.3 0.0000088
-
-
 Escherichia coli methotrexate
1.5.1.3 0.00001
-
-
 Escherichia coli trimethoprim
1.5.1.3 0.00002
-
-
 Homo sapiens methotrexate
1.5.1.3 0.00002
-
-
 Homo sapiens N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl)-L-glutamic acid
1.5.1.3 0.000031
-
-
 Toxoplasma gondii 2-amino-5-[(4-chlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000033
-
-
 Toxoplasma gondii methotrexate
1.5.1.3 0.000034
-
-
 Toxoplasma gondii 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000038
-
-
 Toxoplasma gondii 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000044
-
-
 Toxoplasma gondii 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000048
-
-
 Toxoplasma gondii 2-amino-5-[(4-fluorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000056
-
-
 Toxoplasma gondii 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000056
-
-
 Toxoplasma gondii 2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.000064
-
-
 Toxoplasma gondii 2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.00012
-
-
 Toxoplasma gondii 2-amino-4-oxo-6-methyl-5-phenylsulfanylthieno[2,3-d]pyrimidine
1.5.1.3 0.0002
-
-
 Escherichia coli N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl)-L-glutamic acid
1.5.1.3 0.00043
-
-
 Toxoplasma gondii permetrexed
1.5.1.3 0.00056
-
-
 Homo sapiens 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0012
-
-
 Escherichia coli 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0015
-
-
 Homo sapiens 2-amino-5-[(4-chlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0025
-
-
 Homo sapiens 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0026
-
-
 Homo sapiens 2-amino-5-[(4-fluorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0028
-
-
 Escherichia coli 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0028
-
-
 Homo sapiens 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0028
-
-
 Escherichia coli 2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0029
-
-
 Homo sapiens 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0035
-
-
 Homo sapiens 2-amino-4-oxo-6-methyl-5-phenylsulfanylthieno[2,3-d]pyrimidine
1.5.1.3 0.0056
-
-
 Homo sapiens 2-amino-5-[(3,5-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.0066
-
-
 Homo sapiens permetrexed
1.5.1.3 0.0068
-
-
 Toxoplasma gondii trimethoprim
1.5.1.3 0.022
-
-
 Homo sapiens 2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.028
-
-
 Escherichia coli 2-amino-5-[(4-chlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.028
-
-
 Escherichia coli 2-amino-5-[(2,5-dimethoxyphenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.032
-
-
 Escherichia coli 2-amino-5-[(4-fluorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.035
-
-
 Escherichia coli 2-amino-4-oxo-6-methyl-5-phenylsulfanylthieno[2,3-d]pyrimidine
1.5.1.3 0.035
-
-
 Escherichia coli 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.058
-
-
 Escherichia coli 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
1.5.1.3 0.23
-
-
 Escherichia coli permetrexed
1.5.1.3 0.34
-
-
 Homo sapiens trimethoprim
2.1.1.45 0.000019
-
-
 Escherichia coli 10-propargyl-5,8-dideazafolate
2.1.1.45 0.000036
-
-
 Toxoplasma gondii N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
2.1.1.45 0.00004
-
-
 Escherichia coli N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
2.1.1.45 0.00004
-
-
 Homo sapiens N-[4-[(2-amino-6-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-5-yl)sulfanyl]benzoyl]-L-glutamic acid
2.1.1.45 0.00004
-
 potent inhibitor of human TS and of human DHFR, it is a novel dual TS-DHFR inhibitor, 330-fold more potent than pemetrexed Homo sapiens N-(4-((2-amino-6-methyl-4-oxo-3,4-dihydrothieno(2,3-d)pyrimidin-5-yl)sulfanyl)benzoyl)-L-glutamic acid
2.1.1.45 0.000054
-
 potent inhibitor of human TS and moderate inhibitor of human DHFR Homo sapiens N-(4-((2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo(2,3-d)pyrimidin-5-yl)thio)benzoyl)-L-glutamic acid
2.1.1.45 0.000085
-
-
 Homo sapiens 10-propargyl-5,8-dideazafolate
2.1.1.45 0.00011
-
-
 Homo sapiens 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.00011
-
-
 Homo sapiens 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.00012
-
-
 Homo sapiens 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.00043
-
-
 Toxoplasma gondii 10-propargyl-5,8-dideazafolate
2.1.1.45 0.0012
-
-
 Toxoplasma gondii 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.0012
-
-
 Toxoplasma gondii 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.0012
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 Escherichia coli 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.0012
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 Toxoplasma gondii 2-amino-6-methyl-5-[(4-nitrophenyl)sulfanyl]thieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.0023
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 Escherichia coli 2-amino-5-[(3,4-dichlorophenyl)sulfanyl]-6-methylthieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.0024
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 Escherichia coli 2-amino-6-methyl-5-(2-naphthylsulfanyl)thieno[2,3-d]pyrimidin-4(3H)-one
2.1.1.45 0.0028
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 Toxoplasma gondii pemetrexed
2.1.1.45 0.0095
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 Homo sapiens pemetrexed
2.1.1.45 0.076
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 Escherichia coli pemetrexed