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Arrayscan Assay from US Patent US9701664: "Fused 1,4-dihydrodioxin derivatives as inhibitors of heat shock transcription factor 1"
Assay data:44 Active, 29 Activity ≤ 1 µM, 44 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Titre Blue Assay from US Patent US9701664: "Fused 1,4-dihydrodioxin derivatives as inhibitors of heat shock transcription factor 1"
Assay data:117 Active, 1 Activity ≤ 1 nM, 112 Activity ≤ 1 µM, 117 Tested
Cell-Based ELISA (Cellisa) Assay from US Patent US9701664: "Fused 1,4-dihydrodioxin derivatives as inhibitors of heat shock transcription factor 1"
Assay data:202 Active, 188 Activity ≤ 1 µM, 202 Tested
Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression system
Assay data:8 Active, 3 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 11 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression system
Assay data:6 Active, 5 Activity ≤ 1 µM, 11 Tested
Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-4-oxobutyl)(methyl)carbamoyl)phenyl)-3-imino-3H-xanthene-4,5-disulfonic acid from pirin (unknown origin) by fluorescence polarization assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 11 Tested
Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA
Assay data:9 Active, 8 Activity ≤ 1 µM, 24 Tested
Inhibition of full length human recombinant GST-tagged BRAF (S429 to E741 residues) expressed in baculovirus expression system using Ser/Thr 03 mixture as substrate by Z'-Lyte assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of human recombinant BRAF (S429 to E741 residues) expressed in mammalian expression system at 1 uM by KINOMEScan assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of human recombinant PDGFRB (V582 to Y1009 residues) expressed in bacterial expression system at 1 uM by KINOMEScan assay relative to control
Inhibition of human recombinant PDGFRA (V575 to D1002 residues) expressed in mammalian expression system at 1 uM by KINOMEScan assay relative to control
Inhibition of human recombinant KIT (I571 to D952 residues) expressed in bacterial expression system at 1 uM by KINOMEScan assay relative to control
Kinetic aqueous solubility of the compound in pH 7.4 PBS at 100 uM after 120 mins by RP-HPLC method
Assay data:3 Active, 1 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Lipophilicity, log D of the compound at pH 7.4 by RP-HPLC method
Assay data:7 Tested
SummaryPubMed Citation
Intrinsic clearance in CD1 mouse liver microsomes at 1 uM by LC-MS/MS analysis
Binding affinity to recombinant human pirin by surface plasma resonance method
Assay data:8 Active, 9 Activity ≤ 1 µM, 16 Tested
Antiproliferative activity against human SKOV3 cells after 96 hrs by CellTiter Blue assay
Assay data:14 Active, 22 Activity ≤ 1 µM, 22 Tested
Growth inhibition of human U2OS cells after 96 hrs by CellTiter Blue assay
Inhibition of KIT (unknown origin) using Tyr 06 as substrate after 1 hr by Z'-Lyte assay
Inhibition of human recombinant His tagged PDGFRB cytoplasmic domain (556 to 1108 residues) expressed in baculovirus expression system using Tyr 04 as substrate after 1 hr by Z'-Lyte assay
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