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TBD from US Patent US11530198: "Compositions and methods for treating infections"
Assay data:50 Active, 50 Activity ≤ 1 µM, 50 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Biological Assay from Article 10.3109/14756360903179443: "Synthesis and biological evaluation of biguanide and dihydrotriazine derivatives as potential inhibitors of dihydrofolate reductase of opportunistic microorganisms."
Assay data:13 Active, 11 Activity ≤ 1 µM, 21 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed 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
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
Determination of IC50 from Article 10.1021/jm061027h: "Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis."
Assay data:9 Active, 5 Activity ≤ 1 µM, 15 Tested
Dihydrofolate Reductase (DHFR) Assay from Article 10.1021/jm070165j: "Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates."
Assay data:25 Active, 21 Activity ≤ 1 µM, 26 Tested
Determination of IC50 from Article 10.1021/jm0581718: "Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain."
Assay data:23 Active, 12 Activity ≤ 1 nM, 23 Activity ≤ 1 µM, 23 Tested
Inhibition of Toxoplasma gondii DHFR-TS expressed in Escherichia coli BL21 competent cells using DHF as substrate preincubated for 15 mins followed by substrate and NADPH addition and measured after 60 mins by resazurin dye based diaphorase-coupled assay
Assay data:28 Active, 28 Activity ≤ 1 µM, 31 Tested
Inhibition of Toxoplasma gondii TS-DHFR expressed in Escherichia coli BL21 preincubated for 15 mins followed by addition of DHF as substrate and NADPH measured after 60 mins by resazurin/diaphorase coupled assay
Assay data:14 Active, 10 Activity ≤ 1 µM, 24 Tested
Inhibition of Toxoplasma gondii DHFR by spectrophotometric assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of Toxoplasma gondii TS-DHFR using methylenetetrahydrofolate/dUMP as sustrate preincubated for 10 mins followed by substrate addition
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of Toxoplasma gondii TS-DHFR using methylenetetrahydrofolate/dUMP as sustrate at 100 uM preincubated for 10 mins followed by substrate addition
Assay data:8 Tested
Inhibition of Toxoplasma gondii TS-DHFR using methylenetetrahydrofolate/dUMP as sustrate
Inhibition of Toxoplasma gondii TS-DHFR by Michaelis-Menten plot analysis in presence of bovine serum albumin
Mixed type inhibition of Toxoplasma gondii TS-DHFR using dUMP as substrate at 25 uM by Michaelis-Menten plot analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Noncompetitive inhibition of Toxoplasma gondii TS-DHFR using methylenetetrahydrofolate as substrate at 25 uM by Michaelis-Menten plot analysis
Inhibition of wild type Toxoplasma gondii TS-DHFR expressed in Escherichia coli BL21 using dUMP and methylene-THF as substrate by kaleidagraph analysis
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Inhibition of Toxoplasma gondii thymidylate synthase
Assay data:2 Active, 2 Activity ≤ 1 µM, 8 Tested
Inhibition of Toxoplasma gondii DHFR
Assay data:3 Active, 2 Activity ≤ 1 µM, 8 Tested
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