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Inhibition of Escherichia coli DHFR assessed as inhibition constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of Escherichia coli DfrA1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of Escherichia coli DHFR
Assay data:3 Active, 3 Activity ≤ 1 µM, 5 Tested
Inhibition of Escherichia coli DHFR in presence of NADPH
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Enzymatic Assay from Article 10.1016/j.chembiol.2006.05.008: "MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells."
Assay data:6 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
Inhibition Assay from Article 10.1016/j.chembiol.2004.08.014: "Multicopy suppressors for novel antibacterial compounds reveal targets and drug efflux susceptibility."
Assay data:7 Active, 6 Activity ≤ 1 µM, 7 Tested
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/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:2 Active, 1 Activity ≤ 1 µM, 10 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
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
Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2003.07.023: "Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria."
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Determination of IC50 Values from Article 10.1021/jm060570v: "A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region."
Assay data:8 Active, 3 Activity ≤ 1 µM, 19 Tested
Determination of the Inhibition Constant KI from Article 10.1021/jm060570v: "A 2.13 A structure of E. coli dihydrofolate reductase bound to a novel competitive inhibitor reveals a new binding surface involving the M20 loop region."
Inhibition of recombinant Escherichia coli DHFR
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of recombinant Escherichia coli DHFR expressed in Escherichia coli BL21(DE3) cells assessed as reduction in NADPH oxidation using dihydrofolate as substrate preincubated for 5 mins followed by substrate addition
Assay data:9 Active, 3 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
Competitive inhibition of Escherichia coli DHFR by Dixon plot analysis
Assay data:5 Active, 5 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Ratio of IC50 to Ki for Escherichia coli DHFR
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Uncompetitive inhibition of Escherichia coli DHFR by Lineweaver-Burk plot analysis in presence of NADPH
Assay data:3 Active, 1 Activity ≤ 1 µM, 5 Tested
Competitive inhibition of Escherichia coli DHFR by Lineweaver-Burk plot analysis in presence of H2F
Assay data:5 Active, 4 Activity ≤ 1 µM, 5 Tested
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