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Nuclear factor erythroid 2-related factor 2/antioxidant responsive element (Nrf2/ARE) small molecule agonists, luciferase reporter gene qHTS assay in human keratinocytes: Summary
Assay data:1038 Active, 9667 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Same Project
Nuclear factor erythroid 2-related factor 2/antioxidant responsive element (Nrf2/ARE) small molecule agonists: luciferase reporter gene qHTS assay in human keratinocytes
Assay data:1099 Active, 1 Activity ≤ 1 nM, 143 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Same Project
Agonist activity at RXRalpha-LBD (unknown origin) assessed as transactivation by measuring increase in fluorescein-labelled coactivator PGC-1alpha peptide recruitment by Lanthascreen TR-FRET
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of CBTF-BODIPY from RXR-alpha LBD (unknown origin) at 0.03125 to 32 uM incubated for 1 hr by fluorescence polarization assay
Assay data:2 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human GAL4-fused RXRalpha LBD (T225 to T462 residues) expressed in HEK293 cells incubated for 24 hrs by Dual-Glo luciferase assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Binding affinity to human RXRalpha LBD (T225 to T462 residues) by fluorescence quenching assay
Agonist activity at human RXR-beta expressed in U2OS cells by PathHunter assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at human RXR-alpha expressed in U2OS cells by PathHunter assay
Agonist activity at human RAR-beta expressed in CHO-K1 cells by PathHunter assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
Agonist activity at human RAR-alpha expressed in CHO-K1 cells by PathHunter assay
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
Displacement of 6-(Ethyl-{5-isobutoxy-4-isopropyl-2-[(10-oxo-2,3,5,6-tetrahydro-1H,4H,10H-11-oxa-3a-aza-benzo[de]anthracene-9-carbonyl)-amino]-phenyl}-amino)-nicotinic acid from human RXRalpha-LBD by by fluorescence binding assay
Assay data:5 Active, 1 Activity ≤ 1 µM, 5 Tested
Agonist activity at GST-tagged human RXR assessed as induction of biotinylated coactivator SRC-1 peptide recruitment measured after 2 hrs by streptavidin-conjugated AlphaScreen assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Agonist activity at human RXR-alpha
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Cytochrome P450 Family 3 Subfamily A Member 4 (CYP3A4) small molecule antagonists: luciferase reporter qHTS assay
Assay data:1792 Active, 248 Activity ≤ 1 µM, 9667 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Cytochrome P450 Family 2 Subfamily C Member 19 (CYP2C19) small molecule antagonists: luciferase reporter qHTS assay
Assay data:3508 Active, 4 Activity ≤ 1 nM, 319 Activity ≤ 1 µM, 9667 Tested
Displacement of CU-6PMN from human RXRalpha LBD incubated for 2 hrs by fluorescence based assay
Assay data:5 Active, 3 Activity ≤ 1 µM, 6 Tested
Displacement of DC271 from CRABP2 (unknown origin) at 200 to 1600 nM by fluorescence assay
Assay data:2 Active, 5 Tested
Cmax in chronic hand eczema patient at 30 mg, po administered once daily for 24 weeks
Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
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