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ICMT Biochemical Assay from US Patent US11834430: "Compounds useful as inhibitors of isoprenylcysteine carboxyl methyltransferase"
Assay data:118 Active, 18 Activity ≤ 1 nM, 114 Activity ≤ 1 µM, 119 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of human isoprenylcysteine carboxyl methyltransferase expressed in Saccharomyces cerevisiae membranes using AFC as substrate in presence of 14C-SAM incubated for 30 min by scintillation counting method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of ICMT in human AD293 cells transfected GFP-fused K-Ras4B assessed as induction of K-Ras mislocalization at 5 uM by laser scanning confocal microscopic analysis
Inhibition of ICMT in human AD293 cells transfected GFP-fused K-Ras4B-CVIL assessed as induction of K-Ras mislocalization at 5 uM by laser scanning confocal microscopic analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of ICMT in human AD293 cells transfected GFP-fused K-Ras4B assessed as induction of K-Ras4B mislocalization at 5 uM by laser scanning confocal microscopic analysis
Assay data:2 Active, 2 Tested
Inhibition of ICMT in human AD293 cells transfected GFP-fused K-Ras4A assessed as induction of K-Ras4A mislocalization at 5 uM by laser scanning confocal microscopic analysis
Inhibition of ICMT in human AD293 cells transfected GFP-fused N-Ras assessed as induction of N-Ras mislocalization at 5 uM by laser scanning confocal microscopic analysis
Inhibition of ICMT in human AD293 cells transfected GFP-fused H-Ras assessed as induction of H-Ras mislocalization at 5 uM by laser scanning confocal microscopic analysis
Inhibition of ICMT in human PC3 cells assessed as decrease in AKT phosphorylation at 10 uM measured after 24 hrs by Western blot analysis
Inhibition of ICMT in human PC3 cells assessed as decrease in ERK1/2 phosphorylation at 10 uM measured after 24 hrs by Western blot analysis
Inhibition of ICMT in human PC3 cells assessed as decrease in MEK1/2 phosphorylation at 10 uM measured after 24 hrs by Western blot analysis
Inhibition of ICMT in human PC3 cells assessed as decrease in Ras-GTP complex formation at 10 uM preincubated for 48 hrs followed by compound washout and subsequent compound addition measured after 72 hrs by Pull down assay
Inhibition of ICMT in human PC3 cells assessed as induction of mislocalization of endogenous Ras preincubated for 48 hrs followed by compound washout and subsequent compound addition measured after 72 hrs by Hoechst 33258 staining-based confocal microscopic analysis
Inhibition of ICMT in human PC3 cells assessed as induction of mislocalization of endogenous Ras at 5 uM preincubated for 48 hrs followed by compound washout and subsequent compound addition measured after 72 hrs by Hoechst 33258 staining-based confocal microscopic analysis
Inhibition of recombinant human ICMT expressed in Sf9 insect cell membranes using biotin-farnesyl-L-cysteine as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by scintillation counting analysis
Assay data:2 Active, 3 Tested
Inhibition of recombinant human ICMT expressed in Sf9 insect cell membranes at 50 uM using biotin-farnesyl-L-cysteine as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by scintillation counting analysis relative to control
Assay data:34 Tested
Inhibition of recombinant human ICMT expressed in baculovirus infected Sf9 insect cells using SAM as substrate preincubated for 30 mins followed by substrate addition and measured after 90 mins by MTase-Glo assay
Assay data:10 Active, 9 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of human isoprenylcysteine carboxyl methyltransferase expressed in yeast His10myc3N-Icmt membranes using AFC substrate and [14C]-SAM and incubated for 30 mins by liquid scintillation counting based methyltransferase vapor diffusion assay
Assay data:4 Active, 1 Activity ≤ 1 µM, 13 Tested
Competitive inhibition of human isoprenylcysteine carboxyl methyltransferase expressed in yeast His10myc3N-Icmt membranes using increasing AFC substrate levels and fixed [14C]-SAM level by Lineweaver-Burk plot analysis
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