RXRB

gene
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Also known as NR2B2H-2RIIBPRCoR-1RXRbetaRXR-beta

Summary

RXRB (retinoid X receptor beta, HGNC:10478) is a protein-coding gene on chromosome 6p21.32, encoding Retinoic acid receptor RXR-beta (P28702). Receptor for retinoic acid.

This gene encodes a member of the retinoid X receptor (RXR) family of nuclear receptors which are involved in mediating the effects of retinoic acid (RA). The encoded protein forms homodimers with the retinoic acid, thyroid hormone, and vitamin D receptors, increasing both DNA binding and transcriptional function on their respective response elements. This gene lies within the major histocompatibility complex (MHC) class II region on chromosome 6. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene.

Source: NCBI Gene 6257 — RefSeq curated summary.

At a glance

  • GWAS associations: 1
  • Clinical variants (ClinVar): 69 total
  • Druggable target: yes — 6 molecules with ChEMBL bioactivity
  • Transcription factor: yes — 19 downstream targets (CollecTRI)
  • MANE Select transcript: NM_021976

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:10478
Approved symbolRXRB
Nameretinoid X receptor beta
Location6p21.32
Locus typegene with protein product
StatusApproved
AliasesNR2B2, H-2RIIBP, RCoR-1, RXRbeta, RXR-beta
Ensembl geneENSG00000204231
Ensembl biotypeprotein_coding
OMIM180246
Entrez6257

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 10 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay

ENST00000374680, ENST00000374685, ENST00000481441, ENST00000483281, ENST00000483821, ENST00000865272, ENST00000865273, ENST00000865274, ENST00000865275, ENST00000865276, ENST00000865277, ENST00000865278, ENST00000912952

RefSeq mRNA: 3 — MANE Select: NM_021976 NM_001270401, NM_001291989, NM_021976

CCDS: CCDS4768, CCDS59007

Canonical transcript exons

ENST00000374680 — 10 exons

ExonStartEnd
ENSE000017269563319916933199416
ENSE000018545413320024233200665
ENSE000019461503319358833194829
ENSE000034583313319557033195702
ENSE000034903953319494533195050
ENSE000035136133319536333195454
ENSE000035689553319776233197941
ENSE000035807253319643433196606
ENSE000036298153319830833198464
ENSE000036440743319590733196036

Expression profiles

Bgee: expression breadth ubiquitous, 134 present calls, max score 96.26.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 28.4122 / max 143.4359, expressed in 1813 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
7310519.63791798
731048.54371751
731030.1937109
731020.036917

Top tissues by expression

134 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
right lobe of thyroid glandUBERON:000111996.26gold quality
granulocyteCL:000009496.06gold quality
mucosa of stomachUBERON:000119996.05gold quality
left lobe of thyroid glandUBERON:000112096.03gold quality
right coronary arteryUBERON:000162595.92gold quality
right uterine tubeUBERON:000130295.75gold quality
body of uterusUBERON:000985395.72gold quality
thyroid glandUBERON:000204695.71gold quality
right ovaryUBERON:000211895.59gold quality
pituitary glandUBERON:000000795.58gold quality
endocervixUBERON:000045895.57gold quality
right hemisphere of cerebellumUBERON:001489095.50gold quality
apex of heartUBERON:000209895.35gold quality
tibial nerveUBERON:000132395.34gold quality
muscle layer of sigmoid colonUBERON:003580595.30gold quality
spleenUBERON:000210695.28gold quality
esophagogastric junction muscularis propriaUBERON:003584195.25gold quality
adenohypophysisUBERON:000219695.20gold quality
left ovaryUBERON:000211995.18gold quality
lower esophagus muscularis layerUBERON:003583395.13gold quality
lower esophagusUBERON:001347395.12gold quality
left uterine tubeUBERON:000130395.07gold quality
cerebellumUBERON:000203795.00gold quality
cerebellar cortexUBERON:000212995.00gold quality
cerebellar hemisphereUBERON:000224595.00gold quality
tibial arteryUBERON:000761094.96gold quality
popliteal arteryUBERON:000225094.94gold quality
fundus of stomachUBERON:000116094.93gold quality
small intestine Peyer’s patchUBERON:000345494.88gold quality
ascending aortaUBERON:000149694.86gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

ExperimentMarker?Max mean expression
E-ANND-3no2.35

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

19 targets.

TargetRegulation
ABCG1
ALDH1A1Activation
CD74
CRYAB
CTNNB1
GH1
GPRC5A
ICAM1Unknown
IFNGActivation
LRP1
PCP2
PKD1Activation
PTHRepression
RARBActivation
RBP1Repression
RBP2Unknown
SUPT7L
TRH
TSHB

JASPAR motifs

MotifNameFamily
MA0855.1RXRBRXR-related receptors (NR2)
MA1555.1RXRBRXR-related receptors (NR2)

JASPAR matrix evidence (PMIDs): PMID:15019979, PMID:14559106

Upstream regulators (CollecTRI, top): THRA

miRNA regulators (miRDB)

57 targeting RXRB, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-4747-5P100.0067.902681
HSA-MIR-5196-5P100.0067.982761
HSA-MIR-3689D100.0066.141181
HSA-MIR-6851-5P100.0065.631294
HSA-MIR-513A-5P100.0069.772465
HSA-MIR-607799.9968.042299
HSA-MIR-101-3P99.9475.032230
HSA-MIR-3682-5P99.9367.971163
HSA-MIR-4731-5P99.8967.232537
HSA-MIR-990299.8969.152250
HSA-MIR-449299.8768.253611
HSA-MIR-76599.8468.242442
HSA-MIR-6739-5P99.8067.872806
HSA-MIR-11181-3P99.7566.382205
HSA-MIR-6733-5P99.7467.942759
HSA-MIR-1212499.6869.172700
HSA-MIR-6887-3P99.6667.831778
HSA-MIR-29899.6367.561916
HSA-MIR-613299.6065.831554
HSA-MIR-6836-5P99.6065.621538
HSA-MIR-315399.5567.592337
HSA-MIR-4753-5P99.5468.511356
HSA-MIR-6828-5P99.3169.211433
HSA-MIR-4685-5P99.2565.991563
HSA-MIR-6837-5P99.2565.471632
HSA-MIR-125399.1267.081688
HSA-MIR-7854-3P99.0866.261117
HSA-MIR-62298.9966.481050
HSA-MIR-6770-5P98.9766.761853
HSA-MIR-3922-5P98.7766.531059

Literature-anchored findings (GeneRIF, showing 13)

  • The role of retinoid X receptor messenger RNA expression in curatively resected non-small cell lung cancer (PMID:11839661)
  • polymorphism is unrelated to schizophrenia or alcoholism. (PMID:11840500)
  • Family studies revealed significant linkage disequilibrium between the RXRB alleles and a number of HLA-DPB1 alleles. (PMID:12175732)
  • Diminished RXRbeta expression might be related to prostate cancer progression. Because responsiveness to retinoic acid treatments depends on expression of different receptors, it is important to study their expression before therapy. (PMID:12514092)
  • partial dissociation of TR/retinoid X receptor heterodimer complex from the TRE is involved in the suppression of transcription induced by polychlorinated biphenyls (PMID:14985366)
  • The retinoid X receptor, beta is expressed widely and can be found in almost every tissue. (PMID:15608692)
  • In the RXRB polymorphism, no genotype TT is observed in patients with psoriasis guttata with a positive personal history of repeated tonsillitis (p(corr) = 0.001). (PMID:17341859)
  • In healthy elderly men reduction of RXRbeta expression in peripheral blood mononuclear cells might be a common feature of physiological senescence. (PMID:17916375)
  • PPARgamma/retinoid X receptor complex released from activated platelets in microparticles was internalized by a monocytic cell line. (PMID:18217139)
  • A fatty acid-binding protein 7/RXRbeta pathway enhances survival and proliferation in triple-negative breast cancer. (PMID:22322885)
  • RXR interaction is necessary for NPM-RAR-mediated myeloid maturation arrest. (PMID:24183235)
  • Data show that pregnane X receptor/retinoid X receptor PXR/RXR-[alpha], RXR-[beta], or RXR-[gamma] expression was noted in 9 (16.4%), 9 (16.4%), and 10 (18.2%) pancreatic adenocarcinoma cases, respectively. (PMID:26355550)
  • Genetic variant of RXR involved in the vitamin D metabolic pathway was linked to HCV infection outcomes among a high-risk Chinese population. (PMID:33246082)

Cross-species orthologs

31 orthologs

OrganismSymbolGene ID
danio_reriorxrbbENSDARG00000002006
danio_reriorxrbaENSDARG00000078954
mus_musculusRxrbENSMUSG00000039656
rattus_norvegicusRxrbENSRNOG00000000464
drosophila_melanogasteruspFBGN0003964
drosophila_melanogasterHr78FBGN0015239
drosophila_melanogasterHr83FBGN0037436
caenorhabditis_elegansWBGENE00003626
caenorhabditis_elegansWBGENE00003650
caenorhabditis_elegansnhr-69WBGENE00003659
caenorhabditis_elegansWBGENE00003683
caenorhabditis_elegansWBGENE00003706
caenorhabditis_elegansWBGENE00003719
caenorhabditis_elegansWBGENE00003726
caenorhabditis_elegansWBGENE00007547
caenorhabditis_elegansWBGENE00008221
caenorhabditis_elegansWBGENE00011097
caenorhabditis_elegansWBGENE00011098
caenorhabditis_elegansWBGENE00011099
caenorhabditis_elegansWBGENE00011100
caenorhabditis_elegansWBGENE00015395
caenorhabditis_elegansWBGENE00015396
caenorhabditis_elegansWBGENE00015397
caenorhabditis_elegansWBGENE00015705
caenorhabditis_elegansWBGENE00016975
caenorhabditis_elegansWBGENE00017198
caenorhabditis_elegansWBGENE00017787
caenorhabditis_elegansWBGENE00020748
caenorhabditis_elegansWBGENE00021848
caenorhabditis_elegansWBGENE00022423
caenorhabditis_elegansWBGENE00044354

Paralogs (11): HNF4A (ENSG00000101076), NR2E1 (ENSG00000112333), NR2C1 (ENSG00000120798), RXRG (ENSG00000143171), NR2F6 (ENSG00000160113), HNF4G (ENSG00000164749), NR2F1 (ENSG00000175745), NR2C2 (ENSG00000177463), NR2F2 (ENSG00000185551), RXRA (ENSG00000186350), NR2E3 (ENSG00000278570)

Protein

Protein identifiers

Retinoic acid receptor RXR-betaP28702 (reviewed: P28702)

Alternative names: Nuclear receptor subfamily 2 group B member 2, Retinoid X receptor beta

All UniProt accessions (5): A0A0S2Z4M5, A0A0S2Z570, E9PK75, P28702, Q5STP9

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE).

Subunit / interactions. Homodimer (in vitro). Heterodimer with other retinoic acid receptor family members. Binds DNA preferentially as a RAR/RXR heterodimer. Interacts with NR1H3. Interacts with AKAP13.

Subcellular location. Nucleus. Cytoplasm.

Tissue specificity. Expressed in aortic endothelial cells (at protein level). Expressed in monocytes. Expressed in a variety of tumor cell lines.

Domain organisation. Composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal ligand-binding domain.

Induction. Down-regulated by aging.

Similarity. Belongs to the nuclear hormone receptor family. NR2 subfamily.

Isoforms (2)

UniProt IDNamesCanonical?
P28702-11yes
P28702-32

RefSeq proteins (3): NP_001257330, NP_001278918, NP_068811* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000003Retinoid-X_rcpt/HNF4Family
IPR000536Nucl_hrmn_rcpt_lig-bdDomain
IPR001628Znf_hrmn_rcptDomain
IPR001723Nuclear_hrmn_rcptFamily
IPR013088Znf_NHR/GATAHomologous_superfamily
IPR035500NHR-like_dom_sfHomologous_superfamily
IPR050274Nuclear_hormone_rcpt_NR2Family

Pfam: PF00104, PF00105

UniProt features (37 total): helix 12, compositionally biased region 8, region of interest 6, strand 2, zinc finger region 2, chain 1, domain 1, modified residue 1, DNA-binding region 1, splice variant 1, sequence conflict 1, turn 1

Structure

Experimental structures (PDB)

7 structures.

PDBMethodResolution (Å)
7A78X-RAY DIFFRACTION1.72
5KYAX-RAY DIFFRACTION2.6
5HJPX-RAY DIFFRACTION2.6
5I4VX-RAY DIFFRACTION2.61
1H9UX-RAY DIFFRACTION2.7
5KYJX-RAY DIFFRACTION2.8
1UHLX-RAY DIFFRACTION2.9

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P28702-F172.810.49

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 25

Function

Pathways and Gene Ontology

Reactome pathways

18 pathways

IDPathway
R-HSA-1989781PPARA activates gene expression
R-HSA-383280Nuclear Receptor transcription pathway
R-HSA-5362517Signaling by Retinoic Acid
R-HSA-9029558NR1H2 & NR1H3 regulate gene expression linked to lipogenesis
R-HSA-9029569NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux
R-HSA-9031525NR1H2 & NR1H3 regulate gene expression to limit cholesterol uptake
R-HSA-9031528NR1H2 & NR1H3 regulate gene expression linked to triglyceride lipolysis in adipose
R-HSA-9623433NR1H2 & NR1H3 regulate gene expression to control bile acid homeostasis
R-HSA-9632974NR1H2 & NR1H3 regulate gene expression linked to gluconeogenesis
R-HSA-1430728Metabolism
R-HSA-162582Signal Transduction
R-HSA-212436Generic Transcription Pathway
R-HSA-400206Regulation of lipid metabolism by PPARalpha
R-HSA-556833Metabolism of lipids
R-HSA-73857RNA Polymerase II Transcription
R-HSA-74160Gene expression (Transcription)
R-HSA-9006931Signaling by Nuclear Receptors
R-HSA-9024446NR1H2 and NR1H3-mediated signaling

MSigDB gene sets: 258 (showing top): GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_MUSCLE_TISSUE_DEVELOPMENT, KEGG_ADIPOCYTOKINE_SIGNALING_PATHWAY, MACLACHLAN_BRCA1_TARGETS_DN, GOBP_CELLULAR_RESPONSE_TO_LIPID, MORF_SNRP70, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOBP_GROWTH, GOBP_STRIATED_MUSCLE_CELL_DIFFERENTIATION, GOBP_VENTRICULAR_CARDIAC_MUSCLE_CELL_DIFFERENTIATION, GOBP_MUSCLE_CELL_PROLIFERATION, BROWNE_HCMV_INFECTION_12HR_UP, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, USF_C

GO Biological Process (16): in utero embryonic development (GO:0001701), maternal placenta development (GO:0001893), nervous system development (GO:0007399), hormone-mediated signaling pathway (GO:0009755), cell differentiation (GO:0030154), positive regulation of bone mineralization (GO:0030501), mRNA transcription by RNA polymerase II (GO:0042789), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944), retinoic acid receptor signaling pathway (GO:0048384), ventricular cardiac muscle cell differentiation (GO:0055012), cardiac muscle cell proliferation (GO:0060038), positive regulation of vitamin D receptor signaling pathway (GO:0070564), cellular response to retinoic acid (GO:0071300), regulation of DNA-templated transcription (GO:0006355), nuclear receptor-mediated steroid hormone signaling pathway (GO:0030518)

GO Molecular Function (15): RNA polymerase II transcription regulatory region sequence-specific DNA binding (GO:0000977), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), DNA-binding transcription activator activity, RNA polymerase II-specific (GO:0001228), nuclear steroid receptor activity (GO:0003707), nuclear receptor activity (GO:0004879), zinc ion binding (GO:0008270), chromatin DNA binding (GO:0031490), retinoic acid-responsive element binding (GO:0044323), sequence-specific double-stranded DNA binding (GO:1990837), transcription cis-regulatory region binding (GO:0000976), DNA binding (GO:0003677), DNA-binding transcription factor activity (GO:0003700), protein binding (GO:0005515), sequence-specific DNA binding (GO:0043565), metal ion binding (GO:0046872)

GO Cellular Component (7): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytosol (GO:0005829), RNA polymerase II transcription regulator complex (GO:0090575), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-9 pathways:

CategoryPathways
NR1H2 and NR1H3-mediated signaling6
Signaling by Nuclear Receptors2
Regulation of lipid metabolism by PPARalpha1
Generic Transcription Pathway1
RNA Polymerase II Transcription1
Metabolism of lipids1
Metabolism1
Gene expression (Transcription)1
Signal Transduction1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure4
transcription by RNA polymerase II2
DNA-templated transcription2
regulation of DNA-templated transcription2
regulation of transcription by RNA polymerase II2
nuclear receptor-mediated signaling pathway2
transcription cis-regulatory region binding2
RNA polymerase II transcription regulatory region sequence-specific DNA binding2
DNA-binding transcription factor activity, RNA polymerase II-specific2
DNA binding2
nuclear lumen2
chordate embryonic development1
placenta development1
developmental process involved in reproduction1
anatomical structure development1
maternal process involved in female pregnancy1
system development1
signal transduction1
cellular response to hormone stimulus1
cellular developmental process1
bone mineralization1
regulation of bone mineralization1
positive regulation of ossification1
positive regulation of biomineral tissue development1
mRNA transcription1
positive regulation of RNA biosynthetic process1
positive regulation of DNA-templated transcription1
hormone-mediated signaling pathway1
cardiac muscle cell differentiation1
striated muscle cell proliferation1
cardiac muscle tissue growth1
vitamin D receptor signaling pathway1
regulation of vitamin D receptor signaling pathway1
positive regulation of intracellular signal transduction1
response to retinoic acid1
cellular response to lipid1
cellular response to oxygen-containing compound1
regulation of gene expression1
regulation of RNA biosynthetic process1
steroid hormone receptor signaling pathway1

Protein interactions and networks

STRING

1094 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
RXRBCOL11A2P13942804
RXRBSLC39A7Q92504797
RXRBHSD17B8Q92506795
RXRBRGL2O15211770
RXRBRARS1P54136761
RXRBRARAP10276757
RXRBRARBP10826755
RXRBKIFC1Q9BW19745
RXRBRPS18P25232735
RXRBCNOT7Q9UIV1671
RXRBRING1Q06587665
RXRBPFDN6O15212665
RXRBPPARDQ03181595
RXRBNCOR1O75376584
RXRBPPARAQ07869545

IntAct

122 interactions, top by confidence:

ABTypeScore
RXRBRARApsi-mi:“MI:0915”(physical association)0.950
RARARXRBpsi-mi:“MI:0915”(physical association)0.950
RARBRXRBpsi-mi:“MI:0915”(physical association)0.810
RXRBRARBpsi-mi:“MI:0915”(physical association)0.810
RARANCOR1psi-mi:“MI:0914”(association)0.800
RXRBNR1H4psi-mi:“MI:0915”(physical association)0.790
NR1H4RXRBpsi-mi:“MI:0915”(physical association)0.790
RARGRXRBpsi-mi:“MI:0915”(physical association)0.740
RXRBNR1H3psi-mi:“MI:0915”(physical association)0.720

BioGRID (97): RXRB (Two-hybrid), NR1H3 (Two-hybrid), RXRB (Affinity Capture-Western), RXRB (Affinity Capture-Western), RXRB (Affinity Capture-Western), RXRB (Affinity Capture-MS), RXRB (Two-hybrid), SPOP (Two-hybrid), NCOA1 (Two-hybrid), ADRBK1 (Affinity Capture-MS), CCNK (Affinity Capture-MS), CDC42BPB (Affinity Capture-MS), C2CD5 (Affinity Capture-MS), POLR3F (Affinity Capture-MS), AFF4 (Affinity Capture-MS)

ESM2 similar proteins: A0A0G2JUG7, A1YER5, A1YFY1, A2T6X5, B2DD29, C0HBT3, O08629, O15156, O15169, O35730, O60307, O95343, P0C0T2, P28702, P28704, P29353, P50241, P98083, Q06587, Q0IHB0, Q13263, Q2V2M9, Q2YDU3, Q3U1V8, Q3U2S4, Q4KMP7, Q5DU25, Q5JU85, Q5PRF9, Q5R7W7, Q5RBI7, Q5RJI5, Q5TJF3, Q5TJF7, Q62233, Q62318, Q66J69, Q68DC2, Q6MGB6, Q6ZRS2

Diamond homologs: A2T928, A2T929, A4IIG7, O35507, O42295, O42450, O57606, O77245, O97716, P03373, P04625, P10276, P10826, P10827, P10828, P11416, P12813, P13631, P15204, P17671, P18113, P18115, P18117, P18119, P18514, P18515, P18516, P18911, P19793, P22448, P22605, P22736, P22829, P28699, P28700, P28701, P28702, P28704, P28705, P37242

SIGNOR signaling

24 interactions.

AEffectBMechanism
RXRBup-regulatesPPARAbinding
RXRBup-regulatesPPARDbinding
RXRBup-regulatesPPARGbinding
RXRBup-regulatesNR1H2binding
RARBup-regulatesRXRBbinding
RARGup-regulatesRXRBbinding
RXRBup-regulatesRARAbinding
RXRBup-regulatesRARBbinding
RXRB“up-regulates quantity by expression”RARB“transcriptional regulation”
RXRBup-regulatesRARGbinding
“all-trans-retinoic acid”“up-regulates activity”RXRB“chemical activation”
bexarotene“up-regulates activity”RXRB“chemical activation”
“9-cis-retinoic acid”“up-regulates activity”RXRB“chemical activation”
RXRB“up-regulates activity”THRbinding
RXRBup-regulatesRARbinding
RXRBup-regulatesTHRbinding
RXRBup-regulatesNR4A2binding
RXRBup-regulatesNR2F1binding
RXRBup-regulatesNR2F2binding
RXRBup-regulatesTHRAbinding
RXRBup-regulatesTHRBbinding
RXRBup-regulatesNRIP1binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 50 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
SUMOylation of intracellular receptors975.6×2e-13
Nuclear Receptor transcription pathway1260.1×1e-16
PPARA activates gene expression614.2×2e-04
Activation of anterior HOX genes in hindbrain development during early embryogenesis511.4×2e-03

GO biological processes:

GO termPartnersFoldFDR
intracellular receptor signaling pathway5103.3×3e-07
retinoic acid receptor signaling pathway794.5×3e-10
mRNA transcription by RNA polymerase II641.3×1e-06

Disease & clinical

Clinical variants and AI predictions

ClinVar

69 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance48
Likely benign10
Benign4

Top pathogenic / likely-pathogenic (0)

SpliceAI

1289 predictions. Top by Δscore:

VariantEffectΔscore
6:33194827:AACC:Aacceptor_loss1.0000
6:33194829:CCT:Cacceptor_loss1.0000
6:33194940:CTCAC:Cdonor_loss1.0000
6:33194941:TCA:Tdonor_loss1.0000
6:33194942:CACCG:Cdonor_loss1.0000
6:33194943:A:Tdonor_loss1.0000
6:33194944:C:CGdonor_loss1.0000
6:33194944:CCGT:Cdonor_gain1.0000
6:33194947:T:TAdonor_gain1.0000
6:33194948:C:Adonor_gain1.0000
6:33194964:A:ACdonor_gain1.0000
6:33194965:C:CCdonor_gain1.0000
6:33194965:CTT:Cdonor_gain1.0000
6:33194967:T:TAdonor_gain1.0000
6:33195049:ATCTG:Aacceptor_loss1.0000
6:33195050:TCTGG:Tacceptor_loss1.0000
6:33195051:C:CCacceptor_gain1.0000
6:33195051:CTGGG:Cacceptor_loss1.0000
6:33195056:A:ACacceptor_gain1.0000
6:33195060:C:CTacceptor_gain1.0000
6:33195061:A:Tacceptor_gain1.0000
6:33195568:A:ACdonor_gain1.0000
6:33195569:C:CCdonor_gain1.0000
6:33195588:A:ACdonor_gain1.0000
6:33195589:C:CCdonor_gain1.0000
6:33196032:TTTGG:Tacceptor_gain1.0000
6:33196470:AACGC:Adonor_gain1.0000
6:33196474:C:CAdonor_gain1.0000
6:33197756:CCTTA:Cdonor_loss1.0000
6:33197757:CTTA:Cdonor_loss1.0000

AlphaMissense

3418 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
6:33194707:A:GL526P1.000
6:33194707:A:TL526H1.000
6:33194719:A:CL522R1.000
6:33194719:A:GL522P1.000
6:33194719:A:TL522H1.000
6:33194721:G:CF521L1.000
6:33194721:G:TF521L1.000
6:33194722:A:CF521C1.000
6:33194722:A:GF521S1.000
6:33194723:A:GF521L1.000
6:33194728:T:AD519V1.000
6:33194731:A:TI518N1.000
6:33194743:C:AG514V1.000
6:33194743:C:TG514D1.000
6:33194746:A:TI513N1.000
6:33194749:A:GL512P1.000
6:33194749:A:TL512H1.000
6:33194754:G:CF510L1.000
6:33194754:G:TF510L1.000
6:33194755:A:GF510S1.000
6:33194756:A:GF510L1.000
6:33194757:G:CF509L1.000
6:33194757:G:TF509L1.000
6:33194759:A:GF509L1.000
6:33194760:A:CF508L1.000
6:33194760:A:TF508L1.000
6:33194761:A:CF508C1.000
6:33194761:A:GF508S1.000
6:33194762:A:GF508L1.000
6:33194762:A:TF508I1.000

dbSNP variants (sampled 300 via entrez): RS1000491541 (6:33194538 G>C,T), RS1000612226 (6:33194223 A>G), RS1001539000 (6:33195886 A>G), RS1001951266 (6:33201835 C>G), RS1002841616 (6:33200610 T>C), RS1002954205 (6:33200336 C>T), RS1003135587 (6:33194110 C>T), RS1003618541 (6:33193816 A>T), RS1004364381 (6:33197627 C>G,T), RS1004436689 (6:33197399 G>C,T), RS1004639676 (6:33195088 G>A), RS1005322811 (6:33201152 G>A,T), RS1005603478 (6:33201445 C>G), RS1005687293 (6:33193889 G>GGA), RS1006477418 (6:33200563 C>A,T)

Disease associations

OMIM: gene MIM:180246 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

1 associations (top):

StudyTraitp-value
GCST002160_5Wegener’s granulomatosis2.000000e-50

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL1870 (SINGLE PROTEIN), CHEMBL2363070 (PROTEIN FAMILY), CHEMBL2363071 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 326,531 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1023BEXAROTENE440,951
CHEMBL1071OXAPROZIN451,044
CHEMBL38TRETINOIN4194,008
CHEMBL705ALITRETINOIN439,246
CHEMBL295416PIRINIXIC ACID2830
CHEMBL75133IRX-42042452

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: nhr — 2B. Retinoid X receptors

Most potent curated ligand interactions (7 total), top 7:

LigandActionAffinityParameter
LG100268Agonist8.5pIC50
AGN194204Agonist8.44pIC50
alitretinoinAgonist8.2pIC50
LG100754Antagonist8.0pIC50
bexaroteneAgonist7.7pIC50
[3H]9-cis-retinoic acidFull agonist7.7pKd
compound 28 [Heitel et al., 2019]Agonist6.51pEC50

ChEMBL bioactivities

382 potent at pChembl≥5 of 442 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.89EC500.13nMCHEMBL2325917
9.85EC500.14nMCHEMBL2321917
9.30Ki0.5nMTRETINOIN
9.15EC500.7nMCHEMBL5404648
9.10EC500.8nMIRX-4204
8.85EC501.4nMCHEMBL5404648
8.70Ki2nMCHEMBL111589
8.70EC502nMCHEMBL69091
8.62Ki2.4nMCHEMBL337393
8.60Kd2.5nMCHEMBL69091
8.59EC502.6nMALITRETINOIN
8.59EC502.6nMCHEMBL5404648
8.52EC503nMCHEMBL328481
8.44Kd3.6nMIRX-4204
8.42Ki3.8nMALITRETINOIN
8.41Ki3.9nMCHEMBL133915
8.41Ki3.9nMCHEMBL130374
8.40Ki4nMCHEMBL92284
8.40Ki4nMCHEMBL42314
8.40Ki4nMCHEMBL41422
8.35EC504.5nMTRETINOIN
8.30Ki5nMCHEMBL162334
8.28Ki5.2nMCHEMBL130231
8.23Ki5.9nMBEXAROTENE
8.22Ki6nMCHEMBL348797
8.22EC506nMALITRETINOIN
8.15Ki7nMCHEMBL93518
8.13Ki7.4nMCHEMBL130232
8.13Ki7.4nMALITRETINOIN
8.12Ki7.5nMCHEMBL288436
8.10Ki8nMCHEMBL423465
8.10EC507.9nMCHEMBL4547228
8.10EC508nMCHEMBL111589
8.09Ki8.2nMCHEMBL424269
8.07Ki8.5nMCHEMBL133896
8.05EC509nMCHEMBL109847
8.05Ki9nMALITRETINOIN
8.05Ki9nMCHEMBL109581
8.00EC5010nMCHEMBL423465
8.00Ki9.9nMCHEMBL131122
8.00Ki10nMCHEMBL41260
8.00Ki10nMCHEMBL41146
7.99Ki10.2nMCHEMBL89241
7.96Ki11nMCHEMBL41890
7.96Kd11nMALITRETINOIN
7.94Ki11.5nMCHEMBL111217
7.92EC5012nMCHEMBL166201
7.92Ki12nMCHEMBL208316
7.92Ki12nMCHEMBL109847
7.92Ki12nMCHEMBL2372524

PubChem BioAssay actives

334 with measured affinity, of 1003 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
4-[methyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]benzoic acid726704: Agonist activity at RXR (unknown origin) in presence of RAR agonist Am80ec500.0001uM
4-[(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)-propylamino]benzoic acid726704: Agonist activity at RXR (unknown origin) in presence of RAR agonist Am80ec500.0001uM
tretinoin41913: Binding affinity for retinoic acid receptor RAR betaki0.0005uM
trans-(1R,2R)-2-[5-[3,5-bis(trifluoromethyl)phenyl]-4-phenyl-1,3-oxazol-2-yl]cyclopropane-1-carboxylic acid2024929: Agonist activity at full length human RXR beta expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assayec500.0007uM
(2E,4E)-3-methyl-5-[(1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid167592: Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR betaec500.0008uM
(2E,4E,6Z)-7-(3-methoxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-3-methylocta-2,4,6-trienoic acid199784: Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR betaki0.0020uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(3,5-difluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0024uM
(2E,4E)-3-methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid167593: Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-betakd0.0025uM
alitretinoin199801: Effective concentrations against Retinoic acid receptor RXR-betaec500.0026uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-3-propan-2-yl-5-thiophen-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0039uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(4-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0039uM
(Z)-3-[7-[2-(2,2-difluoroethoxy)-3,5-di(propan-2-yl)phenyl]-1-benzofuran-2-yl]-2-fluorobut-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0040uM
(2E,4E,6Z)-7-[3,5-ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0040uM
4-[(E)-N-hydroxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assayki0.0050uM
(2E,4E,6E)-7-[2-(2,2-difluoroethoxy)-3,5-bis(2-methylbutan-2-yl)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0052uM
Bexarotene199232: Selective activity towards retinoid X receptor-betaki0.0059uM
4-[(E)-C-(3-bromo-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-N-hydroxycarbonimidoyl]benzoic acid199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assayki0.0060uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(3-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0074uM
6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0075uM
4-[ethyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]benzoic acid1630288: 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 assayec500.0079uM
4-[(E)-N-methoxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assayki0.0080uM
(2E,4E,6Z)-7-[2-butoxy-5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0082uM
(2E,4E,6Z)-7-[2-ethoxy-5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0085uM
(2E,4E,6Z)-7-(3-ethoxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-3-methylocta-2,4,6-trienoic acid199782: Transcriptional activation of Retinoid X receptor RXR betaec500.0090uM
(2E,4E,6Z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-6,7-dihydronaphthalen-2-yl)octa-2,4,6-trienoic acid199784: Inhibition of [3H]-Targretin binding to Retinoid X receptor RXR betaki0.0090uM
(2E,4E,6Z)-3-methyl-7-[3-(1,1,2,2,2-pentafluoroethyl)-5-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0099uM
(E)-3-[4-[3,5-ditert-butyl-2-(3-fluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0100uM
(E)-3-[4-[3,5-ditert-butyl-2-(2,2,2-trifluoroethoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0100uM
(2E,4E,6E)-7-(3,5-ditert-butylphenyl)-3-methylocta-2,4,6-trienoic acid199807: Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR betaki0.0102uM
(E)-3-[4-[2-ethoxy-3,5-di(propan-2-yl)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0110uM
(2E,4E,6E)-7-[3,5-ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0115uM
(E)-3-[4-[3,5-ditert-butyl-2-(3,3-difluoropropoxy)phenyl]-1-benzothiophen-2-yl]but-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0120uM
4-[(E)-N-ethoxy-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid199802: Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-betaec500.0120uM
(2E,4E)-6-[(6-tert-butyl-1,1-dimethyl-2,3-dihydroinden-4-yl)-propylamino]-3-methylhexa-2,4-dienoic acid263923: Binding affinity to RXRbetaki0.0120uM
(E)-3-[4-(3,5-ditert-butyl-2-heptoxyphenyl)-1-benzothiophen-2-yl]but-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0120uM
[[(2S)-1-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]phosphonic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0120uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-3-phenyl-5-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0123uM
6-[ethyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]pyridine-3-carboxylic acid1630288: 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 assayec500.0138uM
6-[ethyl-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)amino]pyridine-3-carboxylic acid1630288: 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 assayec500.0138uM
4-[(E)-N-(cyanomethoxy)-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)carbonimidoyl]benzoic acid199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assayki0.0140uM
4-[(E)-C-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)-N-prop-2-enoxycarbonimidoyl]benzoic acid199806: Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assayki0.0150uM
(E)-3-[4-[3,5-di(propan-2-yl)-2-propoxyphenyl]-1-benzothiophen-2-yl]but-2-enoic acid199814: Displacement of [3H]9-cis-RA from Retinoic X receptor betaki0.0150uM
(2E,4E)-3-methyl-5-[2-[(E)-2-(2,6,6-trimethylcyclohexen-1-yl)ethenyl]furan-3-yl]penta-2,4-dienoic acid199805: Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR betakd0.0150uM
(2E,4E,6E)-7-[3,5-ditert-butyl-2-(2,2,2-trifluoroethoxy)phenyl]-6-fluoro-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0155uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(2-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0160uM
trans-(1S,2S)-2-[5-[3,5-bis(trifluoromethyl)phenyl]-4-phenyl-1,3-oxazol-2-yl]cyclopropane-1-carboxylic acid2024929: Agonist activity at full length human RXR beta expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assayec500.0160uM
(E)-3-[5-[3,5-bis(trifluoromethyl)phenyl]-4-phenyl-1,3-oxazol-2-yl]-2-methylprop-2-enoic acid2024929: Agonist activity at full length human RXR beta expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assayec500.0170uM
(2E,4E,6Z)-3-methyl-7-[5-(1,1,2,2,2-pentafluoroethyl)-3-propan-2-yl-2-propoxyphenyl]octa-2,4,6-trienoic acid199652: Displacement of [3H]9-cis-RA from RXR beta receptor in CV-1 cellski0.0172uM
3-[4-chloro-6-(4,4-dimethyl-2,3-dihydroquinolin-1-yl)pyrimidin-2-yl]oxypropanoic acid2099261: Partial agonist activity at recombinant human RXR beta LBD (298 to 533 residues) expressed in Escherichia coli Rosetta incubated for 16 hrs by Gal4-hybrid reporter gene based Dual-glo luciferase assayec500.0180uM
2-[ethyl-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)amino]pyrimidine-5-carboxylic acid1630288: 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 assayec500.0182uM

CTD chemical–gene interactions

78 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Alitretinoindecreases reaction, increases activity, affects activity, affects cotreatment, increases reaction (+2 more)7
Tretinoinincreases expression, increases activity, affects binding, affects cotreatment6
bisphenol Aincreases expression, affects binding, decreases reaction, increases activity, affects cotreatment5
Decitabineincreases expression, decreases expression, decreases reaction2
Valproic Acidaffects expression, decreases expression2
2-hydroxyphytanic acidaffects binding1
testosterone enanthateaffects expression1
2,4-dichlorophenolincreases activity1
triphenyl phosphateaffects expression1
diethyl phthalateaffects binding1
triphenyltin hydroxideaffects activity, affects binding1
diisononyl phthalateaffects binding1
mono-(2-ethylhexyl)phthalateaffects binding1
butyraldehydedecreases expression1
dinonylphthalateaffects binding1
2,4,6-trichlorophenolaffects binding, decreases reaction, increases activity1
dimethyl phthalateaffects binding1
manganese chloridedecreases expression, increases abundance1
di-n-hexyl phthalateaffects binding1
butylbenzyl phthalateaffects binding1
4-hydroxy-2-nonenaldecreases expression1
didecyl phthalateaffects binding1
nickel sulfateincreases expression1
phthalic acidaffects binding1
di-n-pentyl phthalateaffects binding1
2-tert-butylphenolincreases activity1
tetrachlorodianaffects binding, decreases reaction, increases activity1
diisodecyl phthalateaffects binding1
3,4-dichlorophenolincreases activity1
pentanaldecreases expression1

ChEMBL screening assays

211 unique, capped per target: 183 binding, 28 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1021934BindingActivity at Gal4-tagged human RXRbeta receptor expressed in human HeLa cells assessed as relative transcriptional activity by luciferase reporter assay relative to CD3254Modulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers. — J Med Chem
CHEMBL1021935FunctionalAntagonist activity at Gal4-tagged human RXRbeta receptor expressed in human HeLa cells assessed as inhibition of CD3254-induced transcription at >=10 uM by luciferase reporter assayModulating retinoid X receptor with a series of (E)-3-[4-hydroxy-3-(3-alkoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl]acrylic acids and their 4-alkoxy isomers. — J Med Chem

Cellosaurus cell lines

9 cell lines: 5 cancer cell line, 3 embryonic stem cell, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_A5Z7SEES3-1V human RXRB, clone1Embryonic stem cellMale
CVCL_A5Z8SEES3-1V human RXRB, clone2Embryonic stem cellMale
CVCL_A5Z9SEES3-1V human RXRB, clone3Embryonic stem cellMale
CVCL_D1QFAbcam K-562 RXRB KOCancer cell lineFemale
CVCL_D2M1Abcam Raji RXRB KOCancer cell lineMale
CVCL_LF54GeneBLAzer RXRbeta-UAS-bla HEK 293TTransformed cell lineFemale
CVCL_TJ89HAP1 RXRB (-) 1Cancer cell lineMale
CVCL_TJ90HAP1 RXRB (-) 2Cancer cell lineMale
CVCL_WQ49Abcam Jurkat RXRB KOCancer cell lineMale

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.