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Thymidylate synthase
[no definition available]
Synonyms
TS;
TSase;
EC 2.1.1.45
Research
Bioassay Publications (37)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 20 (54.05) | 18.7374 |
| 1990's | 6 (16.22) | 18.2507 |
| 2000's | 9 (24.32) | 29.6817 |
| 2010's | 2 (5.41) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (19)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| fluorodeoxyuridylate | Lacticaseibacillus casei | Kd | 0.0050 | 2 | 2 |
Drugs with Other Measurements
2'-Deoxyuridine 5'-monophosphate substrate displacement in thymidylate synthase through 6-hydroxy-2H-naphtho[1,8-bc]furan-2-one derivatives.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Identification of the binding modes of N-phenylphthalimides inhibiting bacterial thymidylate synthase through X-ray crystallography screening.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Synthesis and biological evaluation of 8-deazahomofolic acid and its tetrahydro derivative.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogues of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).Journal of medicinal chemistry, , Volume: 29, Issue:9, 1986
Folate analogues. 25. Synthesis and biological evaluation of N10-propargylfolic acid and its reduced derivatives.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
Synthesis and antifolate properties of 5,10-methylenetetrahydro-8,10-dideazaminopterin.Journal of medicinal chemistry, , Volume: 29, Issue:9, 1986
Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin.Journal of medicinal chemistry, , Volume: 28, Issue:7, 1985
10-Propargylaminopterin and alkyl homologues of methotrexate as inhibitors of folate metabolism.Journal of medicinal chemistry, , Volume: 25, Issue:7, 1982
Folate analogues altered in the C9-N10 bridge region. 16. Synthesis and antifolate activity of 11-thiohomoaminopterin.Journal of medicinal chemistry, , Volume: 23, Issue:8, 1980
Methotrexate analogues. 12. Synthesis and biological properties of some aza homologues.Journal of medicinal chemistry, , Volume: 22, Issue:7, 1979
Methotrexate analogues. 9. Synthesis and biological properties of some 8-alkyl-7,8-dihydro analogues.Journal of medicinal chemistry, , Volume: 20, Issue:10, 1977
Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Inhibition of thymidylate synthetase by 5-alkynyl-2'-deoxyuridylates.Journal of medicinal chemistry, , Volume: 24, Issue:12, 1981
5-Cyano-2'-deoxyuridine 5'-phosphate: a potent competitive inhibitor of thymidylate synthetase.Journal of medicinal chemistry, , Volume: 22, Issue:9, 1979
Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship.Journal of medicinal chemistry, , Volume: 20, Issue:11, 1977
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase.Journal of medicinal chemistry, , Nov-08, Volume: 39, Issue:23, 1996
Fragment-based drug discovery.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Diastereoisomers of 5,10-methylene-5,6,7,8-tetrahydropteroyl-D-glutamic acid.Journal of medicinal chemistry, , Volume: 20, Issue:11, 1977
Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
5-Arylthio-substituted 2-amino-4-oxo-6-methylpyrrolo[2,3-d]pyrimidine antifolates as thymidylate synthase inhibitors and antitumor agents.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Folate analogues. 32. Synthesis and biological evaluation of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid and related compounds.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency.Journal of medicinal chemistry, , Volume: 32, Issue:4, 1989
Folate analogues. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Folate analogues. 25. Synthesis and biological evaluation of N10-propargylfolic acid and its reduced derivatives.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[omega-(2-amino-4-substituted-6,7-dihydrocyclopenta [d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
Antibacterial agent discovery using thymidylate synthase biolibrary screening.Journal of medicinal chemistry, , Oct-05, Volume: 49, Issue:20, 2006
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase.Chemistry & biology, , Volume: 10, Issue:12, 2003
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Synthesis of classical and a nonclassical 2-amino-4-oxo-6-methyl-5-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of thymidylate synthase.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Kinetics and mechanism of interaction of 10-propargyl-5,8-dideazafolate with thymidylate synthase.Journal of medicinal chemistry, , Volume: 29, Issue:4, 1986