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Inhibition of PCSK9 translation in human THP-1 cells by AlphaLISA assay
Assay data:10 Active, 3 Activity ≤ 1 µM, 10 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Modulation of CD33 pre-mRNA splicing in human K562 cells assessed as induction of exon 2 skipping measured after 18 to 24 hrs by Nano-Luciferase reporter assay
Assay data:8 Active, 1 Activity ≤ 1 µM, 10 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Cell Free Assay from US Patent US9227956: "Substituted amide compounds"
Assay data:26 Active, 6 Activity ≤ 1 µM, 33 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
AlphaLISA Assay from US Patent US9227956: "Substituted amide compounds"
Assay data:12 Active, 2 Activity ≤ 1 µM, 41 Tested
Binding affinity to 80S ribosome in human HuH7 cells expressing human C-terminal V5/6-His-tagged PCSK9 assessed as inhibition of PCSK9 secretion after 16 to 24 hrs by AlphaLISA method
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Toxicity in Crl:CD(SD) rat at 15 mg/kg/day, po daily via gavage for 14 days
Total plasma concentration in Crl:CD(SD) rat at 15 mg/kg/day, po daily via gavage for 14 days measured on day 14 post last dose up to 24 hrs
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Total Cmax in Crl:CD(SD) rat at 15 mg/kg/day, po daily via gavage for 14 days measured on day 14 post last dose up to 24 hrs
Displacement of [3H]PF-06446846 from human 80S ribosome
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Cytotoxicity against human CD34-positive hematopoietic progenitor cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Assay data:4 Active, 1 Activity ≤ 1 µM, 13 Tested
Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA
Assay data:14 Active, 4 Activity ≤ 1 µM, 14 Tested
Inhibition of human ERG by patch clamp method
Assay data:2 Active, 4 Tested
Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
Assay data:11 Active, 7 Activity ≤ 1 µM, 11 Tested
IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells).
Assay data:16 Active, 20 Activity ≤ 1 µM, 57 Tested
Inhibition of PCSK9 expression in human HeLa cells after overnight incubation by ELISA
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
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