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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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
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
Primary qHTS for inhibitors of nuclear receptor binding SET domain protein 2 (NSD2) in an RCH-ACV wild type WT cells (2C)
Assay data:2970 Active, 9 Activity ≤ 1 nM, 1016 Activity ≤ 1 µM, 10037 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Primary qHTS for inhibitors of nuclear receptor binding SET domain protein 2 (NSD2) in an isogenic RCH-ACV NSD2 p.E1099K mutant (9B)
Assay data:2826 Active, 4 Activity ≤ 1 nM, 946 Activity ≤ 1 µM, 10037 Tested
Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry
Assay data:368 Active, 78 Activity ≤ 1 µM, 5114 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Depositor
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antiproliferative activity against human WM266.4 cells after 96 hrs by CellTiter Blue assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Drug uptake in NCr nude mouse tumor xenografted with human SKOV3 cells at 20 mg/kg, po qd measured after 33 days
Fraction unbound in NCr-Fox1 nude mouse plasma at 20 mg/kg, po after 24 hrs by LC-MS/MS based equilibrium dialysis method
Unbound fraction in BALB/c mouse plasma at 5 mg/kg, po after 24 hrs by LC-MS/MS method
Antiproliferative activity against human SKOV3 cells assessed as free compound concentration required for 50% growth inhibition after 96 hrs by CellTiter Blue assay
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 bisamide probe binding to pirin in human SKOV3 cells by SILAC-based quantitative mass spectrometry pull down assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSPA1A mRNA level preincubated for 1 hr followed by 17-AAG addition measured after 6 hrs by Western blot method
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
qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation
Assay data:347 Active, 1 Activity ≤ 1 nM, 215 Activity ≤ 1 µM, 650 Tested
qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary
Assay data:378 Active, 203 Activity ≤ 1 µM, 2480 Tested
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