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Half-life in human
Assay data:5 Tested
SummaryPubMed Citation
Bioavailability in dog at 1 mg/kg, iv measured after 30 mins by LC-MS/MS analysis
Assay data:2 Tested
Bioavailability in rat at 0.5 mg/kg, iv measured after 30 mins by LC-MS/MS analysis
Solubility of the compound at pH 7 incubated for 12 hrs by UPLC analysis
Activation of PXR (unknown origin) in human DPX2 cells assessed as maximal efficacy at 15 uM relative to control
SummaryPubMed CitationRelated BioAssays by Target
Unbound fraction in human plasma
Selectivity index, ratio of EC50 for antiviral activity against HIV-1 G140S/Q148R mutant to EC50 for antiviral activity against wild-type HIV-1
Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of viral replication
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of HIV-1 integrase DTG-resistant H51Y/R263K double mutant
Assay data:1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of HIV-1 integrase DTG-resistant R263K mutant
Inhibition of HIV-1 integrase DTG-resistant G118R mutant
Inhibition of HIV-1 integrase RAL-resistant G140S/Q148H double mutant
SummaryCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of HIV-1 integrase G140S/Q148K double mutant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
OCT2 Inhibition Assay from US Patent US11548901: "Substituted 1,4-methanopyrido[1′,2′:4,5]pyrazino[1,2-a]pyrimidines for treating viral infections"
Assay data:19 Active, 11 Activity ≤ 1 µM, 23 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Various Assay from Article 10.1021/acs.jmedchem.1c00409: "Perspectives on SARS-CoV-2 Main Protease Inhibitors."
Assay data:473 Active, 1 Activity ≤ 1 nM, 248 Activity ≤ 1 µM, 795 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition Assay from US Patent US10689399: "Substituted 3,4,5,6,8,10,14,14a-octahydro-2h-2,6-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazocines and methods for treating viral infections"
Inhibition Assay from US Patent US9663528: "Substituted 1,2,3,4,6,8,12,12a-octahydro-1,4-methanodipyrido[1,2-a:1',2'-d]pyrazines and methods for treating viral infections"
Assay data:18 Active, 10 Activity ≤ 1 µM, 22 Tested
Antiviral activity against HIV1 3B
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of HIV integrase strand transfer activity
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 4 Tested
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