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Fluorescence Polarization Assay from US Patent US11028041: "Second generation GRP94-selective inhibitors"
Assay data:16 Active, 12 Activity ≤ 1 µM, 18 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
PDE Enzyme Inhibitor Assays from Article 10.1021/jm060113e: "A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability."
Assay data:26 Active, 2 Activity ≤ 1 nM, 26 Activity ≤ 1 µM, 26 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Unbound fraction in Beagle dog at 1.5 mg/kg, po or 0.5 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Assay data:1 Tested
SummaryPubMed Citation
Unbound fraction in Beagle dog at 1.5 mg/kg, po or 0.4 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Half-life in Beagle dog at 1.5 mg/kg, po or 0.5 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Unbound volume of distribution at steady state in Beagle dog at 1.5 mg/kg, po or 0.5 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Volume of distribution at steady state in Beagle dog at 1.5 mg/kg, po or 0.5 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Unbound clearance in Beagle dog blood at 1.5 mg/kg, po or 0.5 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Clearance in Beagle dog blood at 1.5 mg/kg, po or 0.5 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Oral bioavailability in Beagle dog at 1.5 mg/kg measured upto 24 hrs by LC-MS/MS analysis
Assay data:2 Tested
Half-life in Beagle dog at 1.5 mg/kg, po or 0.4 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Unbound volume of distribution at steady state in Beagle dog at 1.5 mg/kg, po or 0.4 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Volume of distribution at steady state in Beagle dog at 1.5 mg/kg, po or 0.4 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Unbound clearance in Beagle dog blood at 1.5 mg/kg, po or 0.4 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Clearance in Beagle dog blood at 1.5 mg/kg, po or 0.4 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Intrinsic clearance in dog hepatocytes incubated upto 45 mins by LC-MS/MS analysis
Assay data:8 Tested
Half life in Beagle dog at 1 mg/kg, iv measured upto 24 hrs by LC-MS/MS analysis
Oral bioavailability in Beagle dog at 1 mg/kg measured upto 24 hrs by LC-MS/MS analysis
Plasma protein binding in dog relative to control
Apparent permeability across apical to basolateral side in dog MDCK cells
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