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Induction of TLR4 protein degradation in human THP-1 cells at 1.25 to 20 uM incubated for 24 hrs by Western blot analysis
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to mouse TLR4 in RAW264.7 cells assessed as thermal stabilization at 1 uM and measured after 12 hrs by CETSA analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at LPD-RK stimulated human TRL4 overexpressed in HEK293 cells assessed as inhibition of NF kappa B/Ap-1 activation preincubated with compound for 30 mins followed by LPD-RK stimulation measured after 22 hrs by SEAP reporter assay
Inhibition of TLR4 in HEK293 cells assessed as reduction in LPS-stimulated NF-kappaB activation at 20 uM incubated for 16 to 24 hrs by SEAP reporter gene assay relative to control
Inhibition of TLR4 in human Kupffer cells assessed as reduction in HMGB-1 stimulated TNF-alpha secretion at 10 nM preincubated for 1 hr followed by HMGB-1 addition and measured after 24 hrs by ELISA relative to control
Inhibition of TLR4 in HEK293 cells assessed as reduction in LPS-stimulated NF-kappaB activation at 10 uM incubated for 16 to 24 hrs by SEAP reporter gene assay relative to control
Assay data:2 Tested
Antagonist activity at human TLR4 expressed in HEK-blue hTLR4/MD2-CE14 cells cotransfected with pISRE-TA plasmid assessed as reduction in ISRE activation incubated for overnight by dual-Glo luciferase assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human TLR4 expressed in HEK-blue hTLR4/MD2-CE14 cells cotransfected with pNiFty plasmid assessed as reduction in NF-kappaB activation incubated for overnight by dual-Glo luciferase assay
Inhibition of human TLR4 expressed in HEK293-Blue hTLR4 cells assessed as SEAP expression
Assay data:3 Tested
Binding affinity to TLR4 in human THP-1 monocytes after 48 hrs by ELISA
Inhibition of LPS-stimulated TLR4 activation in HEK-Blue-hTLR4 cells assessed as reduction in SEAP release preincubated for 15 mins followed by LPS stimulation and measured after 16 hrs by microplate reader assay
Assay data:5 Active, 5 Tested
Antagonist activity at human TLR4 in HEK-Blue hTLR4 cells assessed as inhibition of LPS-induced receptor activation at 0.1 to 100 uM preincubated with LPS followed by compound addition and measured 24 hrs by Quanti-Blue based SEAP reporter gene assay
Assay data:4 Tested
Antagonist activity at human TLR4 in HEK-Blue hTLR4 cells assessed as inhibition of LPS-induced receptor activation preincubated with LPS followed by compound addition and measured 24 hrs by Quanti-Blue based SEAP reporter gene assay
Assay data:26 Active, 3 Activity ≤ 1 µM, 26 Tested
Binding affinity to MD2 (unknown origin) assessed as dissociation constant by spectrofluorimetric analysis
Assay data:2 Active, 2 Tested
Antagonist activity at human TLR4 expressed in human whole blood assessed as inhibition of LPS stimulated TNF level preincubated for 30 mins followed by stimulation and measured after 20 hrs by multiplate reader assay
Antagonist activity at human TLR4 expressed in human PBMC cells assessed as inhibition of LPS stimulated TNF level preincubated for 30 mins followed by stimulation and measured after 20 hrs by multiplate reader assay
Agonist activity at TLR4 in HEK-Blue hTLR4 cells at 0.1 to 100 uM incubated for 24 hrs by Quanti-Blue based SEAP assay
Agonist activity at human TLR4 expressed in HEK-Blue hTLR4 cells assessed as activation of NFkappaB incubated for 6 to 16 hrs by SEAP reporter gene based assay
Binding affinity to NTA sensor chip immobilized recombinant human TLR4/MD2 assessed as association rate constant by surface plasmon resonance analysis
Binding affinity to NTA sensor chip immobilized recombinant human TLR4/MD2 assessed as dissociation rate kinetics by surface plasmon resonance analysis
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