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Agonist activity at human RAR-alpha expressed in CHO-K1 cells by PathHunter assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human RAR-alpha expressed in CHO-K1 cells assessed as maximum relative efficacy at 100 uM by PathHunter assay relative to 9-cis-retinoic acid
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human RARalpha (177 to 462 residues) in Cos7 cells transfected with LBD-Gal4 and pGL435 Gal4 UAS Luc reporter plasmid at 10 uM by reporter gene assay
Agonist activity at human GAL4 DBD-fused RARalpha LBD (177 to 462 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
Transactivation assays from US Patent US10752616: "Bicycloheteroaryl-heteroaryl-benzoic acid compounds as retinoic acid receptor beta (RARβ) agonists"
Assay data:46 Active, 2 Activity ≤ 1 nM, 46 Activity ≤ 1 µM, 46 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Competitive Assay from Article 10.1016/S1074-5521(99)80084-2: "Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists."
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
Retinoid Competition Binding Assay from Article 10.1006/jmbi.2000.4032: "Structural basis for isotype selectivity of the human retinoic acid nuclear receptor."
Assay data:9 Active, 3 Activity ≤ 1 nM, 9 Activity ≤ 1 µM, 9 Tested
Retinoid Nuclear Receptor Activity from US Patent US10188615: "Alkoxy compounds for disease treatment"
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Agonist activity against human RARalpha 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
Antagonist activity against human RARalpha assessed as inhibition of 9-cis-RA-induced luciferase expression at 1 uM incubated for 24 hrs by luciferase reporter gene assay
Antagonist activity against human RARalpha at 1 uM incubated for 24 hrs by luciferase reporter gene assay
Activation of human RAR-alphaLBD expressed in HEK293T cells assessed as induction of receptor activation at 10 uM incubated for 12 to 14 hrs by luciferase reporter gene assay
Agonist activity at human RARalpha transfected in human HuH7 cells assessed as receptor transactivation at 1 uM by luciferase reporter gene assay
Assay data:2 Tested
Agonist activity at human RARalpha expressed in HEK293 cells assessed as increase in RARE-mediated transcription at 100 nM incubated for 24 hrs by RARE luciferase reporter gene assay relative to all-trans-retinoic acid
Inhibition of human RARalpha transfected in human HEK293 cells co-expressing CMV-beta galactosidase assessed as effect on beta-galactosidase activity at 50 uM after 48 hrs by luciferase reporter gene assay
Assay data:13 Tested
Agonist activity RARalpha (unknown origin) assessed as induction of receptor transactivation
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at RAR (unknown origin) by Alpha Screen assay
Agonist activity at RAR (unknown origin) by Alpha Screen assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
Antagonist activity at recombinant human pFA-CMV fused RARalpha LBD transfected in HEK293T cells assessed as reduction in tretinoin-induced RARalpha activation at 1 uM incubated for 12 to 14 hrs by dual glo luciferase reporter gene assay
Agonist activity at recombinant human pFA-CMV fused RARalpha LBD transfected in HEK293T cells assessed as RARalpha activation at 1 uM incubated for 12 to 14 hrs by dual glo luciferase reporter gene assay
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