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Metabolic stability assessed as bovine recombinant adenosine deaminase-mediated 3'-deoxyinosine metabolite formation by measuring shift in maximum absorption at 62.5 uM measured upto 2 hrs by UV absorption spectra based analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Metabolic stability assessed as bovine recombinant adenosine deaminase-mediated 3'-deoxyinosine metabolite formation by measuring shift in maximum absorption at 62.5 uM measured after 2 mins by UV absorption spectra based analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to recombinant mouse ADA assessed as inhibition constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to human erythrocytic ADA assessed as inhibition constant by spectrophotometric analysis
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to ADA (unknown origin) assessed as inhibition constant
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Luciferase Reporter Assay from US Patent US11472811: "Pyrazolotriazolopyrimidine derivatives as A2A receptor antagonist"
Assay data:185 Active, 11 Activity ≤ 1 nM, 185 Activity ≤ 1 µM, 185 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
ADA Enzyme Inhibition Assay from Article 10.1021/jm801427r: "Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors."
Assay data:7 Active, 3 Activity ≤ 1 µM, 14 Tested
ADA Inhibition Assay from Article 10.1021/jm0499559: "Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors."
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
ADA Inhibition Assay from Article 10.1021/jm0306374: "Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors."
Assay data:22 Active, 19 Activity ≤ 1 µM, 22 Tested
ADA Inhibition Assay from Article 10.1016/S0960-894X(03)00026-X: "Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors."
Assay data:3 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 7 Tested
ADA Inhibition Assay from Article 10.1021/ja038606l: "A highly potent non-nucleoside adenosine deaminase inhibitor: efficient drug discovery by intentional lead hybridization."
Assay data:4 Active, 2 Activity ≤ 1 µM, 4 Tested
ADA Inhibition Assay from Article 10.1021/jm700931t: "Inhibition of adenosine deaminase by analogues of adenosine and inosine, incorporating a common heterocyclic base, 4(7)-amino-6(5)H-imidazo[4,5-d]pyridazin-7(4)one."
Assay data:5 Tested
Substrate activity at calf Intestinal mucosa adenosine deaminase assessed as Vmax by Lineweaver-Burk plot analysis
Assay data:6 Tested
Substrate activity at calf Intestinal mucosa adenosine deaminase assessed as km by Lineweaver-Burk plot analysis
Prodrug conversion in rat brain assessed as rate of adenosine deaminase-mediated didanosine formation by HPLC analysis
Assay data:2 Tested
Prodrug conversion in rat blood assessed as rate of adenosine deaminase-mediated didanosine formation by HPLC analysis
Prodrug conversion in rat blood assessed as Vmax for adenosine deaminase-mediated didanosine formation by HPLC analysis
Assay data:4 Tested
Prodrug conversion in rat blood assessed as Km for adenosine deaminase-mediated didanosine formation by HPLC analysis
Inhibition of human erythrocytes ADA assessed as equilibrium dissociation constant by measuring reduction in formation of inosine using adenosine as substrate
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 3 Tested
Inhibition of human erythrocytes ADA assessed as reduction in formation of inosine using adenosine as substrate
Assay data:2 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
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