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Agonist activity at RXRbeta-LBD (unknown origin) assessed as transactivation by measuring increase in fluorescein-labelled coactivator D22 peptide recruitment by Lanthascreen TR-FRET assay
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human RXR-beta expressed in U2OS cells by PathHunter assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human RXR-beta expressed in U2OS cells assessed as maximum relative efficacy at 100 uM by PathHunter assay relative to 9-cis-retinoic acid
Assay data:1 Tested
Agonist activity at human RXRbeta (294 to 533 residues) in Cos7 cells transfected with LBD-Gal4 and pGL435 Gal4 UAS Luc reporter plasmid at 10 uM by reporter gene assay
FLIPR Assay from US Patent US11166958: "4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament"
Assay data:16 Active, 14 Activity ≤ 1 µM, 20 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Agonist activity against human RXRbeta 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 RXRbeta transfected in human HEK293T cells co-expressing pFR/pRL-Luc incubated for 14 to 16 hrs by hybrid reporter gene assay relative to bexarotene
Assay data:41 Tested
Agonist activity at human RXRbeta transfected in human HEK293T cells co-expressing pFR/pRL-Luc at 30 uM incubated for 14 to 16 hrs by hybrid reporter gene assay
Assay data:5 Tested
Agonist activity at human RXRbeta transfected in human HEK293T cells co-expressing pFR/pRL-Luc incubated for 14 to 16 hrs by hybrid reporter gene assay
Assay data:32 Active, 16 Activity ≤ 1 µM, 43 Tested
Competitive antagonist activity at human RXRB/RXRB expressed in African green monkey COS7 cells assessed as reduction in bexarotene-induced receptor activation at 1 uM by RXRE-dependent luciferase reporter gene assay
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at recombinant human pFA-CMV fused RXRbeta LBD expressed in HEK293T cells transfected with pFR-luciferase plasmid and pRL-SV40 plasmid at 10 uM incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay
Assay data:3 Active, 3 Tested
Inhibition of GAL4-fused human RXR transcriptional activity expressed in CHOK1 cells after 2 days by luciferase reporter gene assay
Agonist activity at RXRbeta (unknown origin) at < 20 uM
Agonist activity at RXR in human HepG2 cells assessed as induction of CYP3A4 expression at 100 nM incubated for 24 hrs by quantitative real-time PCR method relative to untreated control
Assay data:11 Tested
Antagonist activity against human RXR binding domain and activation domain expressed in human HCT116 cells assessed as reduction in bexarotene-induced rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay
Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity at 1000 nM incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay relative to bexarotene
Assay data:9 Tested
Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity at 100 nM incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay relative to bexarotene
Assay data:4 Active, 12 Tested
Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity at 25 nM incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay relative to bexarotene
Assay data:10 Tested
Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay
Assay data:11 Active, 11 Activity ≤ 1 µM, 13 Tested
Agonist activity RXRbeta (unknown origin)
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