General Information of the Protein
Protein ID
PT04149
Protein Name
Retinoic acid receptor RXR-alpha
Secondarily
Protein Name
Nuclear receptor subfamily 2 group B member 1
Retinoid X receptor alpha
Gene Name
RXRA
Secondarily
Gene Name
Nr2b1
Sequence
MDTKHFLPLDFSTQVNSSSLSSPTGRGSMAAPSLHPSLGPGLGSPLGSPGQLHSPISTLSSPINGMGPPFSVISSPMGPHSMSVPTTPTLGFETGSPQLNSPMNPVSSSEDIKPPLGLNGVLKVPAHPSGNMSSFTKHICAICGDRSSGKHYGVYSCEGCKGFFKRTVRKDLTYTCRDNKDCLIDKRQRNRCQYCRYQKCLAMGMKREAVQEERQRGKDRNENEVESTSSANEDMPVEKILEAELAVEPKTETYVEANMGLNPSSPNDPVTNICQAADKQLFTLVEWAKRIPHFSELPLDDQVILLRAGWNELLIASFSHRSIAVKDGILLATGLHVHRNSAHSAGVGAIFDRVLTELVSKMRDMQMDKTELGCLRAIVLFNPDSKGLSNPAEVEALREKVYASLEAYCKHKYPEQPGRFAKLLLRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQTT
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Organism
Rattus norvegicus, Rat
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 2
>
Nuclear hormone receptor subfamily 2 group B
>
Nuclear hormone receptor subfamily 2 group B member 1
Function
Receptor for retinoic acid that acts as a transcription factor (By similarity). Forms homo- or heterodimers with retinoic acid receptors (RARs) and binds to target response elements in response to their ligands, all-trans or 9-cis retinoic acid, to regulate gene expression in various biological processes (By similarity). The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 to regulate transcription (By similarity). The high affinity ligand for retinoid X receptors (RXRs) is 9-cis retinoic acid (By similarity). In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone deacetylation, chromatin condensation and transcriptional suppression (By similarity). On ligand binding, the corepressors dissociate from the receptors and coactivators are recruited leading to transcriptional activation (By similarity). Serves as a common heterodimeric partner for a number of nuclear receptors, such as RARA, RARB and PPARA (By similarity). The RXRA/RARB heterodimer can act as a transcriptional repressor or transcriptional activator, depending on the RARE DNA element context (By similarity). The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes (PubMed:8381967). Together with RARA, positively regulates microRNA-10a expression, thereby inhibiting the GATA6/VCAM1 signaling response to pulsatile shear stress in vascular endothelial cells (By similarity). Acts as an enhancer of RARA binding to RARE DNA element (By similarity). May facilitate the nuclear import of heterodimerization partners such as VDR and NR4A1 (By similarity). Promotes myelin debris phagocytosis and remyelination by macrophages (By similarity). Plays a role in the attenuation of the innate immune system in response to viral infections, possibly by negatively regulating the transcription of antiviral genes such as type I IFN genes (By similarity). Involved in the regulation of calcium signaling by repressing ITPR2 gene expression, thereby controlling cellular senescence (By similarity).
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Uniprot ID
Q05343
Ensembl ID
ENSG00000186350
Subcellular Location
Nucleus
Cytoplasm
Mitochondrion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000044 , CV-1
Compound ID Compound Name Compound Formula
CP0044243
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)CYCLOPROPYL]PYRIDINE-3-CARBOXYLIC ACID
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C24H29NO2
 1
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
CP0058430
5-{2-[3,5-Diisopropyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-cyclopent-1-enyl}-3-methyl-penta-2,4-dienoic acid
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C25H31F3O3
 1
1
IC50 = 2.3 nM
   TI
   LI
   LO
   TS
CP0170202
5-{2-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-cyclopent-1-enyl}-3-methyl-penta-2,4-dienoic acid
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C26H35FO3
 1
1
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
CP0101584
5-[2-(3,5-Diisopropyl-2-propoxy-phenyl)-cyclopent-1-enyl]-3-methyl-penta-2,4-dienoic acid
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C26H36O3
 1
1
IC50 = 4.5 nM
   TI
   LI
   LO
   TS
CP0291714
5-{2-[2-(2,2-Difluoro-ethoxy)-3,5-diisopropyl-phenyl]-cyclopent-1-enyl}-3-methyl-penta-2,4-dienoic acid
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C25H32F2O3
 1
1
IC50 = 5.1 nM
   TI
   LI
   LO
   TS
CP0189339
5-{3-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C25H31FO3S
 1
1
IC50 = 6.8 nM
   TI
   LI
   LO
   TS
CP0006755
(2E,4E,6Z)-7-[3,5-Di-tert-butyl-2-(2,2-difluoro-ethoxy)-phenyl]-3-methyl-octa-2,4,6-trienoic acid
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C25H34F2O3
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0101753
(2E,4E)-5-{3-[3,5-Di-tert-butyl-2-(3,3-difluoro-propoxy)-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C27H34F2O3S
 1
1
IC50 = 8.7 nM
   TI
   LI
   LO
   TS
CP0036256
5-{3-[3-tert-Butyl-5-ethyl-2-(3-fluoro-propoxy)-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C25H31FO3S
 1
1
IC50 = 10.3 nM
   TI
   LI
   LO
   TS
CP0090012
5-{3-[3,5-Diisopropyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C24H27F3O3S
 1
1
IC50 = 10.4 nM
   TI
   LI
   LO
   TS
CP0101874
5-{3-[2-(2,2-Difluoro-ethoxy)-3,5-diisopropyl-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C24H28F2O3S
 1
1
IC50 = 11.4 nM
   TI
   LI
   LO
   TS
CP0170373
5-{2-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-furan-3-yl}-3-methyl-penta-2,4-dienoic acid
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C25H31FO4
 1
1
IC50 = 11.6 nM
   TI
   LI
   LO
   TS
CP0043990
5-{3-[3-tert-Butyl-2-(2,2-difluoro-ethoxy)-5-ethyl-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C24H28F2O3S
 1
1
IC50 = 15.5 nM
   TI
   LI
   LO
   TS
CP0091221
5-[3',5'-Di-tert-butyl-2'-(3-fluoro-propoxy)-biphenyl-2-yl]-3-methyl-penta-2,4-dienoic acid
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C29H37FO3
 1
1
IC50 = 46.3 nM
   TI
   LI
   LO
   TS
CP0036217
5-[2'-(3-Fluoro-propoxy)-3',5'-diisopropyl-biphenyl-2-yl]-3-methyl-penta-2,4-dienoic acid
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C27H33FO3
 1
1
IC50 = 49.6 nM
   TI
   LI
   LO
   TS
CP0036189
5-[2'-(2,2-Difluoro-ethoxy)-3',5'-diisopropyl-biphenyl-2-yl]-3-methyl-penta-2,4-dienoic acid
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C26H30F2O3
 1
1
IC50 = 79.9 nM
   TI
   LI
   LO
   TS
CP0054590
5-{3-[3,5-Diisopropyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-pyridin-4-yl}-3-methyl-penta-2,4-dienoic acid
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C25H28F3NO3
 1
1
IC50 = 271.2 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0291714
5-{2-[2-(2,2-Difluoro-ethoxy)-3,5-diisopropyl-phenyl]-cyclopent-1-enyl}-3-methyl-penta-2,4-dienoic acid
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C25H32F2O3
 1
1 Ki = 0.9 nM
CP0058430
5-{2-[3,5-Diisopropyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-cyclopent-1-enyl}-3-methyl-penta-2,4-dienoic acid
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C25H31F3O3
 1
1 Ki = 1 nM
CP0101584
5-[2-(3,5-Diisopropyl-2-propoxy-phenyl)-cyclopent-1-enyl]-3-methyl-penta-2,4-dienoic acid
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C26H36O3
 1
1 Ki = 1.9 nM
CP0101753
(2E,4E)-5-{3-[3,5-Di-tert-butyl-2-(3,3-difluoro-propoxy)-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C27H34F2O3S
 1
1 Ki = 1.9 nM
CP0170202
5-{2-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-cyclopent-1-enyl}-3-methyl-penta-2,4-dienoic acid
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C26H35FO3
 1
1 Ki = 1.9 nM
CP0101874
5-{3-[2-(2,2-Difluoro-ethoxy)-3,5-diisopropyl-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C24H28F2O3S
 1
1 Ki = 2.2 nM
CP0006755
(2E,4E,6Z)-7-[3,5-Di-tert-butyl-2-(2,2-difluoro-ethoxy)-phenyl]-3-methyl-octa-2,4,6-trienoic acid
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C25H34F2O3
 1
1 Ki = 3 nM
CP0043990
5-{3-[3-tert-Butyl-2-(2,2-difluoro-ethoxy)-5-ethyl-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C24H28F2O3S
 1
1 Ki = 3.2 nM
CP0189339
5-{3-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C25H31FO3S
 1
1 Ki = 3.4 nM
CP0170373
5-{2-[2-(3-Fluoro-propoxy)-3,5-diisopropyl-phenyl]-furan-3-yl}-3-methyl-penta-2,4-dienoic acid
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C25H31FO4
 1
1 Ki = 6.2 nM
CP0090012
5-{3-[3,5-Diisopropyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C24H27F3O3S
 1
1 Ki = 8.7 nM
CP0036256
5-{3-[3-tert-Butyl-5-ethyl-2-(3-fluoro-propoxy)-phenyl]-thiophen-2-yl}-3-methyl-penta-2,4-dienoic acid
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C25H31FO3S
 1
1 Ki = 9.9 nM
CP0036217
5-[2'-(3-Fluoro-propoxy)-3',5'-diisopropyl-biphenyl-2-yl]-3-methyl-penta-2,4-dienoic acid
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C27H33FO3
 1
1 Ki = 15.2 nM
CP0044243
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)CYCLOPROPYL]PYRIDINE-3-CARBOXYLIC ACID
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C24H29NO2
 1
1 Ki = 18 nM
CP0091221
5-[3',5'-Di-tert-butyl-2'-(3-fluoro-propoxy)-biphenyl-2-yl]-3-methyl-penta-2,4-dienoic acid
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C29H37FO3
 1
1 Ki = 20.9 nM
CP0036189
5-[2'-(2,2-Difluoro-ethoxy)-3',5'-diisopropyl-biphenyl-2-yl]-3-methyl-penta-2,4-dienoic acid
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C26H30F2O3
 1
1 Ki = 29.6 nM
CP0054590
5-{3-[3,5-Diisopropyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-pyridin-4-yl}-3-methyl-penta-2,4-dienoic acid
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C25H28F3NO3
 1
1 Ki = 48 nM