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Partial agonist activity at GAL4-tagged human CAR LBD expressed in HEK293T cells at 3 uM incubated for 12 to 14 hrs by dual-Glo luciferase assay
Assay data:4 Active, 4 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human GAL4 DBD-fused CAR LBD (48 to 324 residues) transfected in HEK293T cells assessed as fold activation at 10 uM incubated for 14 to 16 hrs by Renilla/Firefly dual-luciferase reporter assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
CAR Indigo Bioscience nuclear receptor screen
SummaryRelated BioAssays by Target
CAR In-house nuclear receptor screen
Agonist activity against human CAR in human HEK293T cells co-expressing pFR/pRL-Luc assessed as receptor activation at 10 uM incubated for 14 to 16 hrs by hybrid reporter gene assay relative to bexarotene
Assay data:3 Tested
Agonist activity at human CAR
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Transactivation of CAR (unknown origin) assessed as upregulation of CYP2B6
Assay data:1 Active, 1 Tested
Transactivation of CAR (unknown origin) assessed as upregulation of CYP2B6 at 3 to 8 microg/ml
Transactivation of CAR (unknown origin) assessed as upregulation of CYP2B6 at 0.1 to 1 microg/ml
Agonist activity at Polyhistidine-tagged human CAR LBD expressed in Escherichia coli by FRET-based assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at recombinant human constitutive androstane receptor assessed as induction of CYP2 at 3.16 uM relative to control
Agonist activity at human CAR in human primary hepatocytes assessed as slight increase in CYP2B6 level at 0.5 to 5 uM incubated for 72 hrs by Western blot analysis
Agonist activity at human CAR in human primary hepatocytes assessed as increase in CYP2B6 gene expression at 0.5 to 5 uM incubated for 24 hrs by RT-PCR analysis
Agonist activity at human CAR in human primary hepatocytes assessed as increase in CYP2B6 gene expression at 1 mM incubated for 24 hrs by RT-PCR analysis
Agonist activity at human CAR in human primary hepatocytes assessed as increase in CYP2B6 level incubated for 72 hrs by Western blot analysis
Agonist activity at human CAR in human primary hepatocytes assessed as increase in CYP2B6 gene expression incubated for 24 hrs by RT-PCR analysis
Assay data:2 Tested
Ratio of Emax to EC50 for agonist activity at human CAR transfected in human HepG2 cells cotransfected with CYP2B6 by luciferase reporter gene assay
Assay data:26 Tested
Agonist activity at human CAR transfected in human HepG2 cells cotransfected with CYP2B6 incubated for 23 hrs by luciferase reporter gene assay relative to control
Assay data:29 Tested
Agonist activity at human CAR transfected in human HepG2 cells cotransfected with CYP2B6 incubated for 23 hrs by luciferase reported gene assay
Assay data:25 Active, 16 Activity ≤ 1 µM, 29 Tested
Antagonist activity at recombinant human pFA-CMV fused CAR LBD transfected in HEK293T cells assessed as reduction in CITCO-induced CAR activation at 1 uM incubated for 12 to 14 hrs by dual glo luciferase reporter gene assay
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