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Synergistic agonist activity at human HIF-2alpha expressed in human Hep3B cells assessed as induction of EPO transcription at 5 uM pretreated with FG4592 followed by compound addition and measured after 12 hrs by qRT-PCR analysis
Assay data:16 Active, 16 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in VEGFA transcription level at 0.2 uM incubated for 24 hrs by RT-PCR analysis relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in VEGFA transcription level at 2 uM incubated for 24 hrs by RT-PCR analysis relative to control
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in NDRG1 transcription level at 0.2 uM incubated for 24 hrs by RT-PCR analysis relative to control
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in NDRG1 transcription level at 2 uM incubated for 24 hrs by RT-PCR analysis relative to control
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in PGK1 transcription level at 20 uM incubated for 24 hrs by RT-PCR analysis relative to control
Assay data:10 Tested
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in GLUT1 transcription level at 20 uM incubated for 24 hrs by RT-PCR analysis relative to control
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in VEGFA transcription level at 20 uM incubated for 24 hrs by RT-PCR analysis relative to control
Agonist activity at human HIF-2alpha expressed in human 786-0 cells assessed as increase in NDRG1 transcription level at 20 uM incubated for 24 hrs by RT-PCR analysis relative to control
Agonist activity at human HIF-2alpha expressed in human 786-0 cells expressing HRE luciferase reporter gene assessed as increase of HIF stabilization at 20 uM incubated for 24 hrs by Steady-lumi luciferase assay
Assay data:27 Tested
Binding affinity to HIF-2alpha/ARNT (unknown origin) assessed as change in melting temperature at 10 uM by protein thermal shift assay
Assay data:34 Tested
Induction of HIF-2alpha stabilization in human Hep3B cells assessed as HIF-1alpha level at 16 to 1000 nM incubated for 24 hrs by immunoblot analysis
Induction of HIF-2alpha stabilization in human Hep3B cells assessed as HIF-1alpha level at 1 to 100 uM incubated for 24 hrs by immunoblot analysis
Assay data:3 Tested
Binding affinity to human ARNT (85 to 465 residues) expressed in Escherichia coli Rosetta 2 (DE3) assessed as increase in melting temperature at 200 uM measured after 30 mins by differential scanning fluorimetry analysis
Binding affinity to human ARNT (85 to 465 residues) expressed in Escherichia coli Rosetta 2 (DE3) assessed as increase in melting temperature at 10 uM measured after 10 mins by differential scanning fluorimetry analysis
Scintillation Proximity Assay (SPA) from US Patent US10597366: "Aryl ethers and uses thereof"
Assay data:303 Active, 218 Activity ≤ 1 µM, 325 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Agonist activity at HIF-2 in human 786-O cells assessed as fold increase in EPO level at 10 uM after 24 hrs by qPCR analysis
Agonist activity at HIF-2 in human 786-O cells assessed as increase in cyclin D1 level after 24 hrs by qPCR analysis
Agonist activity at HIF-2 in human 786-O cells assessed as increase in GULT1 level after 24 hrs by qPCR analysis
Agonist activity at HIF-2 in human 786-O cells assessed as increase in VEGF level after 24 hrs by qPCR analysis
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