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Inhibition of human TS
Assay data:18 Active, 18 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Thymidylate synthase (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of thymidylate synthase (unknown origin) assessed as inhibition constant
Reduction in intracellular TS activity in human IGROV-1 cells assessed as residual activity measured at 5 uM by tritium release assay relative to control
Assay data:3 Tested
SummaryPubMed CitationRelated BioAssays by Target
Reduction in intracellular TS activity in human IGROV-1 cells measured at 2.5 uM by tritium release assay relative to control
Assay data:2 Tested
Reduction in intracellular TS activity in human IGROV-1 cells measured at 1.25 uM by tritium release assay relative to control
Mixed type inhibition of human TS assessed as inhibitor dissociation constant by measuring changes in slope of the double reciprocal plot using dTMP as substrate by UV-Vis spectroscopy based analysis
Non competitive type inhibition of human TS assessed as inhibition constant using varying levels of mTHF as substrate by UV-Vis spectroscopy based analysis
Inhibition Assay from US Patent US9422297: "Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof"
Assay data:13 Active, 6 Activity ≤ 1 µM, 27 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Tritium Release Assay from Article 10.1111/j.1747-0285.2010.01010.x: "Fragment-based discovery of novel thymidylate synthase leads by NMR screening and group epitope mapping."
Assay data:4 Active, 2 Activity ≤ 1 µM, 14 Tested
Inhibition Assay from Article 10.1016/j.chembiol.2003.11.012: "Inhibitor specificity via protein dynamics: insights from the design of antibacterial agents targeted against thymidylate synthase."
Assay data:7 Active, 4 Activity ≤ 1 µM, 7 Tested
Inhibition Assay from Article 10.1016/S1074-5521(01)00067-9: "Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase."
Assay data:2 Active, 7 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Thymidylate Synthase (TS) Assay from Article 10.1021/jm900490a: "Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents."
Assay data:19 Active, 19 Activity ≤ 1 µM, 19 Tested
Thymidylate Synthase (TS) Assay from Article 10.1021/jm701052u: "Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors."
Assay data:17 Active, 12 Activity ≤ 1 µM, 19 Tested
Thymidylate Synthase (TS) Assay from Article 10.1021/jm058276a: "Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1)."
Assay data:12 Active, 7 Activity ≤ 1 µM, 17 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Dihydrofolate Reductase (DHFR) Assay from Article 10.1021/jm058234m: "Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolate reductase and thymidylate synthase and a"
Assay data:6 Active, 5 Activity ≤ 1 µM, 6 Tested
Thymidylate Synthase (TS) Assay from Article 10.1021/jm051187d: "Antibacterial agent discovery using thymidylate synthase biolibrary screening."
Assay data:17 Active, 9 Activity ≤ 1 µM, 19 Tested
Thymidylate Synthase (TS) Assay from Article 10.1107/S0907444905022638: "The structure of Cryptococcus neoformans thymidylate synthase suggests strategies for using target dynamics for species-specific inhibition."
Potency index, ratio of pemetrexed IC50 to test compound IC50 for inhibition of thymidylate synthase (unknown origin) by spectrophotometric analysis
Inhibition of human thymidylate synthase expressed in Escherichia coli using 6R,S-tetrahydrofolate and dUMP as substrate by spectrophotometric analysis
Assay data:3 Active, 3 Tested
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