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Receptor Activity Assay from US Patent US10633388: "Pyrazolopyrimidone derivatives and methods of use thereof"
Assay data:14 Active, 11 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 14 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of SARS-CoV-2-induced cytopathy was measured 4 days after infection of EGFP-labeled Green monkey Vero cells by fluorescence imaging.
Assay data:19 Active, 7 Activity ≤ 1 µM, 134 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µM
Cytotoxicity against African green monkey Vero cells incubated for 48 hrs by SRB colorimetric assay
Assay data:1 Tested
SummaryPubMed Citation
Tmax in Cynomolgus monkey at 10 mg/kg, po upto 24 hrs by LC/MS/MS analysis
Half life in Cynomolgus monkey at 10 mg/kg, po
Cmax in Cynomolgus monkey at 10 mg/kg, po measured after 3 hrs by LC/MS/MS analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Oral bioavailability in cynomolgus monkey at 10 mg/kg
Inhibition of Cynomolgus monkey FBPase
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Cytotoxicity against African green monkey Vero cells
Drug metabolism in monkey intestinal microsomes assessed as rate of metabolism
Volume of distribution at steady state in Cynomolgus monkey at 1 mg/kg,iv and measured after 72 hrs by LC/MS/MS analysis
Half life in Cynomolgus monkey at 1 mg/kg,iv and measured after 72 hrs by LC/MS/MS analysis
Unbound clearance in Cynomolgus monkey at 1 mg/kg,iv and measured after 72 hrs by LC/MS/MS analysis
Clearance in Cynomolgus monkey at 1 mg/kg,iv and measured after 72 hrs by LC/MS/MS analysis
Unbound AUC (0 to infinity) in Cynomolgus monkey at 1 mg/kg,iv and measured after 72 hrs by LC/MS/MS analysis
AUC (0 to infinity) in Cynomolgus monkey at 1 mg/kg,iv and measured after 72 hrs by LC/MS/MS analysis
Cytotoxicity against African green monkey Vero cells assessed as cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against African green monkey COS7 cells assessed as inhibition of cell growth
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Cytotoxicity against African green monkey Vero E6 cells measured after 72 hrs by MTT assay
Assay data:4 Tested
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Assay data:2 Tested
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