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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
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
Phosphotyrosine (PY) ELISA from Article 10.1016/j.bmc.2009.08.044: "Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors."
Assay data:11 Active, 1 Activity ≤ 1 µM, 17 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."
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 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
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
Inhibition of MAPK (unknown origin)
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive/number tested for 8 weeks; 5/5
Assay data:1 Tested
SummaryPubMed Citation
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive/number tested for 8 weeks; 4/5
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive/number tested for 8 weeks; 2/5
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive/number tested for 3 weeks; 0/5
Assay data:3 Tested
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive for trophozoites/number tested for 8 weeks; 0/5
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive for trophozoites/number tested for 3 weeks; 0/5
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive for lesions/number tested for 8 weeks; 0/5
Evaluated for inhibitory growth of Pneumocystis carinii cysts in lungs administered at the dose of 10 mg/kg expressed as number of lungs positive for lesions/number tested for 3 weeks; 0/5
Inhibition of Pneumocystis carinii DHFR expressed in Escherichia coli Rosetta-gami B (DE3) assessed as reduction in consumption of NADPH using DHFA as substrate
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed Citation
Antipneumocystis activity against Pneumocystis carinii after 24 to 72 hrs by ATP-based luciferin-luciferase assay
Assay data:21 Active, 19 Activity ≤ 1 µM, 21 Tested
Inhibition of Pneumocystis carinii DHFR K37Q/F69N mutant by spectrophotometric assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of Pneumocystis carinii DHFR K37Q mutant by spectrophotometric assay
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