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NR1I3

gene
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Also known as MB67CAR1CAR

Summary

NR1I3 (nuclear receptor subfamily 1 group I member 3, HGNC:7969) is a protein-coding gene on chromosome 1q23.3, encoding Nuclear receptor subfamily 1 group I member 3 (Q14994). Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes.

This gene encodes a member of the nuclear receptor superfamily, and is a key regulator of xenobiotic and endobiotic metabolism. The protein binds to DNA as a monomer or a heterodimer with the retinoid X receptor and regulates the transcription of target genes involved in drug metabolism and bilirubin clearance, such as cytochrome P450 family members. Unlike most nuclear receptors, this transcriptional regulator is constitutively active in the absence of ligand but is regulated by both agonists and inverse agonists. Ligand binding results in translocation of this protein to the nucleus, where it activates or represses target gene transcription. These ligands include bilirubin, a variety of foreign compounds, steroid hormones, and prescription drugs. In addition to drug metabolism, the CAR protein is also reported to regulate genes involved in glucose metabolism, lipid metabolism, cell proliferation, and circadian clock regulation. Multiple transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 9970 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): intellectual disability (Limited, GenCC)
  • Clinical variants (ClinVar): 119 total
  • Druggable target: yes — 26 molecules with ChEMBL bioactivity
  • Transcription factor: yes — 68 downstream targets (CollecTRI)
  • MANE Select transcript: NM_005122

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:7969
Approved symbolNR1I3
Namenuclear receptor subfamily 1 group I member 3
Location1q23.3
Locus typegene with protein product
StatusApproved
AliasesMB67, CAR1, CAR
Ensembl geneENSG00000143257
Ensembl biotypeprotein_coding
OMIM603881
Entrez9970

Gene structure

Transcript identifiers

Ensembl transcripts: 40 — 29 protein_coding, 5 nonsense_mediated_decay, 4 protein_coding_CDS_not_defined, 2 retained_intron

ENST00000367979, ENST00000367980, ENST00000367981, ENST00000367982, ENST00000367983, ENST00000367984, ENST00000367985, ENST00000412844, ENST00000428574, ENST00000437437, ENST00000442691, ENST00000464422, ENST00000479324, ENST00000488651, ENST00000491193, ENST00000502848, ENST00000502985, ENST00000503547, ENST00000504010, ENST00000505005, ENST00000505944, ENST00000506018, ENST00000506209, ENST00000507215, ENST00000508387, ENST00000508740, ENST00000510951, ENST00000511676, ENST00000511748, ENST00000511944, ENST00000512340, ENST00000512372, ENST00000515452, ENST00000515621, ENST00000904616, ENST00000904617, ENST00000904618, ENST00000904619, ENST00000904620, ENST00000904621

RefSeq mRNA: 15 — MANE Select: NM_005122 NM_001077469, NM_001077470, NM_001077471, NM_001077472, NM_001077473, NM_001077474, NM_001077475, NM_001077476, NM_001077477, NM_001077478, NM_001077479, NM_001077480, NM_001077481, NM_001077482, NM_005122

CCDS: CCDS1228, CCDS41427, CCDS41428, CCDS41429, CCDS41430, CCDS44260, CCDS44261, CCDS44262, CCDS53405, CCDS53406, CCDS53407, CCDS53408, CCDS53409, CCDS53410, CCDS53411

Canonical transcript exons

ENST00000367983 — 9 exons

ExonStartEnd
ENSE00001689568161229669161229926
ENSE00002033498161238041161238203
ENSE00002373394161233169161233338
ENSE00002535530161236459161236598
ENSE00003547133161231329161231474
ENSE00003593328161231117161231233
ENSE00003628138161232807161232946
ENSE00003655223161235847161235977
ENSE00003672215161230813161230918

Expression profiles

Bgee: expression breadth ubiquitous, 171 present calls, max score 98.43.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2385 / max 130.7451, expressed in 35 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter IDTPM avgSamples expressed
156200.144925
156190.078713
156170.01495

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
right lobe of liverUBERON:000111498.43gold quality
liverUBERON:000210793.00gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047380.80gold quality
cortical plateUBERON:000534374.32gold quality
buccal mucosa cellCL:000233673.18silver quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099173.06gold quality
nucleus accumbensUBERON:000188272.99gold quality
adult mammalian kidneyUBERON:000008272.31gold quality
hindlimb stylopod muscleUBERON:000425271.48gold quality
caudate nucleusUBERON:000187370.44gold quality
gastrocnemiusUBERON:000138870.41gold quality
muscle of legUBERON:000138370.36gold quality
putamenUBERON:000187469.23gold quality
prefrontal cortexUBERON:000045168.97gold quality
ganglionic eminenceUBERON:000402367.05gold quality
bone marrow cellCL:000209266.79silver quality
heart left ventricleUBERON:000208466.77gold quality
right frontal lobeUBERON:000281066.01gold quality
stromal cell of endometriumCL:000225565.91gold quality
cardiac ventricleUBERON:000208265.89gold quality
right hemisphere of cerebellumUBERON:001489065.24gold quality
cerebellar cortexUBERON:000212965.07gold quality
cerebellar hemisphereUBERON:000224565.03gold quality
cingulate cortexUBERON:000302764.98gold quality
muscle organUBERON:000163064.91gold quality
monocyteCL:000057664.85gold quality
duodenumUBERON:000211464.78gold quality
mononuclear cellCL:000084264.71gold quality
apex of heartUBERON:000209864.67gold quality
anterior cingulate cortexUBERON:000983564.67gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3no2.87

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

68 targets.

TargetRegulation
ABCB1Activation
ABCC2Activation
ABCC3Activation
ABCC4Activation
ABCC6Activation
ACOX1Unknown
ADAM2
AKR1B15
APOA1
APOC3
APP
BDNFUnknown
BPIFA4P
CA1
CA12
CDKN1AActivation
CTSEUnknown
CYP1A1
CYP1A2
CYP21A1P
CYP24A1Unknown
CYP2B6Activation
CYP2C18Unknown
CYP2C19
CYP2C8
CYP2C9Unknown
CYP3A4Unknown
CYP3A5Activation
CYP7A1
DLST

JASPAR motifs

MotifNameFamily
MA1534.1NR1I3Thyroid hormone receptor-related factors (NR1)
MA1534.2NR1I3Thyroid hormone receptor-related factors (NR1)

JASPAR matrix evidence (PMIDs): PMID:12896978

Upstream regulators (CollecTRI, top): AHR, ELK1, GLI3, HNF4A, MSC, NCOA2, NCOA3, NR0B2, NR1I2, NR1I3, NR3C1, PPARA, RARA, SRF

Literature-anchored findings (GeneRIF, showing 40)

  • CAR antagonizes ER-mediated transcriptional activity by squelching limiting amounts of p160 coactivators, such as SRC-1 and GRIP-1. (PMID:12114525)
  • Transcriptional regulation of the human CYP3A4 gene by the constitutive androstane receptor. (PMID:12130689)
  • Regulation of human CYP2C9 by the constitutive androstane receptor: discovery of a new distal binding site. (PMID:12181452)
  • identified as a key regulator of acetaminophen metabolism and hepatotoxicity (PMID:12376703)
  • Substantial interindividual differences exist in hepatic constitutive androstane receptor expression; a 240-fold interindividual variability in hepatic mRNA levels has been detected. (PMID:12485946)
  • A distal glucocorticoid response element located within the CAR promoter is described, and evidence is presented that this element is capable of of conferring transcriptional activation via the glucocorticoid pathway. (PMID:12511605)
  • activation requires subnuclear targeting by peroxisome proliferator-activated receptor gamma coactivator-1 alpha (PMID:12551939)
  • control of steroid, heme, and carcinogen metabolism by this protein in transgenic mice (PMID:12644700)
  • Induces bilirubin clearance when expressed in transgenic mice (PMID:12644704)
  • Alternatively spliced isoforms of the constitutive androstane receptor. (PMID:12799447)
  • CAR-RXR heterodimers and CAR monomers can contribute to the gene activating function of phenobarbital response enhancer modules in CAR target genes (PMID:12896978)
  • stabilization of helix 12 by a contact between its C terminus and the lysine of helix 4 has the same impact in human and mouse constitutive androstane receptor (CAR) (PMID:15151997)
  • pregnane X receptor (PXR) and constitutively activated receptor (CAR) mediate induction of CYP3A5 in human liver and intestine (PMID:15252010)
  • The antiemetic meclizine is both an agonist ligand for mouse CAR and an inverse agonist for human CAR. (PMID:15272053)
  • negative regulation of CAR, a glucocorticoid-responsive gene, via proinflammatory cytokine interleukin 1beta (IL-1beta) (PMID:15382119)
  • The two cis-acting elements, the distal PBREM and the proximal OARE, within the chromatin structure are both regulated by CAR in response to okadaic acid and TCPOBOP to maximally induce the CYP2B6 promoter. (PMID:15563456)
  • studies identified several amino acids within helices 3 (Asn(165)), 5 (Val(199)), 11 (Tyr(326), Ile(330), and Gln(331)), and 12 (Leu(343) and Ile(346)) that contribute to the high basal activity of human CAR (PMID:15572376)
  • NR1I3 has a role in regulating both liver homeostasis and tumorigenesis in response to xenobiotic stresses (PMID:15831521)
  • there is cross talk between distal CAR/PXR sites and HNF4alpha binding sites in the CYP2C9 promoter and that the HNF4alpha sites are required for maximal induction of the CYP2C9 promoter. (PMID:15919766)
  • role in transcriptional regulation of CYP2C8 (PMID:15933212)
  • hCAR mediates the methotrexate induction of hSULT2A1. (PMID:17276571)
  • observations suggest that HNF4alpha1 positively regulates hCAR expression in normal developing and adult livers, whereas HNF4alpha7 represses hCAR gene expression in hepatocellular carcinoma (PMID:17464991)
  • interindividual variation in the expression level of CAR probably determines variation in expression and activity of a broad scope of xenobiotic metabolism genes (PMID:17576804)
  • Role of aryl hydrocarbon receptor in drug metabolism demonstrates in vivo up-regulation of androstane receptor through chemical exposure. (PMID:17596880)
  • Inter-individual/inter-ethnic variations of docetaxel and doxorubicin pharmacokinetics or pharmacodynamics exist, but genotypic variability of CAR cannot account for this variability. (PMID:17876342)
  • the human cathepsin E gene is regulated by the constitutive androstane receptor (PMID:17888866)
  • PPARalpha ligands not only serve as PPARalpha agonists but possibly act as CAR antagonists. (PMID:17962186)
  • genetic polymorphisms in CAR may have an indirect effect on drug disposition–REVIEW (PMID:18154449)
  • R16A at the membrane may mediate the PB signal to initiate CAR nuclear translocation, through a mechanism including its dimerization and inhibition of PP1beta activity. (PMID:18202305)
  • CAR requires early growth response 1 to activate the human cytochrome P450 2B6 gene (PMID:18303024)
  • In this review, constitutive active/androstane receptor (CAR) is a nuclear receptor that plays a critical role in modulating hepatic energy metabolism. (PMID:18305370)
  • CAR may influence the expression of genes involved in not only the metabolism of endogenous and exogenous substances but also in the cell proliferation. (PMID:18331826)
  • ATF5 is abundant in the liver, activates CYP2B6, and cooperates with CAR in sustaining the hepatic-specific expression of this P450 in human hepatocytes and hepatoma cells. (PMID:18332083)
  • SF3a3 functions as a co-repressor of Constitutive Androstane Receptor transcriptional activity, in addition to its canonical function. (PMID:18713018)
  • Bioactive terpenoids and flavonoids from Ginkgo biloba extract induce the expression of hepatic drug-metabolizing enzymes through pregnane X receptor, constitutive androstane receptor, and aryl hydrocarbon receptor-mediated pathways. (PMID:19034627)
  • CAR expression may be mediated by phosphorylated Elk-1 via the SAPK signaling pathway (PMID:19302787)
  • ER8 motif is highly conserved in the CYP1A1 proximal promoter sequences of various species, suggesting a fundamental role of CAR in the xenobiotic-induced expression of CYP1A1 and CYP1A2 independent of aryl hydrocarbon receptor (PMID:19682433)
  • A genetic variation at the CAR gene locus is associated with BMD, suggesting an involvement of the CAR gene in bone metabolism (PMID:19702932)
  • Results characterize the conserved threonine 38 of human constitutive active/androstane receptor (CAR) as the primary residue that regulates nuclear translocation and activation of CAR. (PMID:19858220)
  • Data observed that OSM positively augmented the CAR and UGT1A1 expressions and CAR-mediated signaling in vivo and in vitro, through cross talk between the nuclear CAR receptor and the plasma membrane OSM receptor, via the MAPK cascade. (PMID:20197307)

Cross-species orthologs

188 orthologs

OrganismSymbolGene ID
danio_rerionr1h5ENSDARG00000031046
danio_reriorarabENSDARG00000034893
danio_rerioraraaENSDARG00000056783
danio_reriororcENSDARG00000087195
mus_musculusNr1i3ENSMUSG00000005677
rattus_norvegicusNr1i3ENSRNOG00000003260
drosophila_melanogasterHr96FBGN0015240
caenorhabditis_elegansWBGENE00001062
caenorhabditis_elegansWBGENE00003608
caenorhabditis_elegansWBGENE00003611
caenorhabditis_elegansWBGENE00003614
caenorhabditis_elegansWBGENE00003615
caenorhabditis_elegansWBGENE00003617
caenorhabditis_elegansWBGENE00003618
caenorhabditis_elegansWBGENE00003620
caenorhabditis_elegansWBGENE00003624
caenorhabditis_elegansWBGENE00003632
caenorhabditis_elegansWBGENE00003634
caenorhabditis_elegansWBGENE00003638
caenorhabditis_elegansWBGENE00003640
caenorhabditis_elegansWBGENE00003641
caenorhabditis_elegansWBGENE00003642
caenorhabditis_elegansWBGENE00003643
caenorhabditis_elegansWBGENE00003644
caenorhabditis_elegansWBGENE00003645
caenorhabditis_elegansWBGENE00003646
caenorhabditis_elegansWBGENE00003648
caenorhabditis_elegansWBGENE00003649
caenorhabditis_elegansWBGENE00003651
caenorhabditis_elegansWBGENE00003653
caenorhabditis_elegansWBGENE00003655
caenorhabditis_elegansWBGENE00003658
caenorhabditis_elegansWBGENE00003660
caenorhabditis_elegansWBGENE00003662
caenorhabditis_elegansnhr-73WBGENE00003663
caenorhabditis_elegansnhr-77WBGENE00003667
caenorhabditis_elegansWBGENE00003669
caenorhabditis_elegansnhr-81WBGENE00003671
caenorhabditis_elegansnhr-82WBGENE00003672
caenorhabditis_elegansWBGENE00003676
caenorhabditis_elegansWBGENE00003677
caenorhabditis_elegansWBGENE00003680
caenorhabditis_elegansWBGENE00003682
caenorhabditis_elegansWBGENE00003684
caenorhabditis_elegansWBGENE00003685
caenorhabditis_elegansWBGENE00003686
caenorhabditis_elegansWBGENE00003688
caenorhabditis_elegansWBGENE00003689
caenorhabditis_elegansWBGENE00003692
caenorhabditis_elegansWBGENE00003693
caenorhabditis_elegansWBGENE00003694
caenorhabditis_elegansWBGENE00003696
caenorhabditis_elegansWBGENE00003698
caenorhabditis_elegansWBGENE00003699
caenorhabditis_elegansWBGENE00003700
caenorhabditis_elegansWBGENE00003702
caenorhabditis_elegansWBGENE00003704
caenorhabditis_elegansWBGENE00003705
caenorhabditis_elegansWBGENE00003707
caenorhabditis_elegansWBGENE00003708
caenorhabditis_elegansWBGENE00003712
caenorhabditis_elegansWBGENE00003713
caenorhabditis_elegansWBGENE00003714
caenorhabditis_elegansWBGENE00003715
caenorhabditis_elegansWBGENE00003716
caenorhabditis_elegansWBGENE00003717
caenorhabditis_elegansWBGENE00003718
caenorhabditis_elegansWBGENE00003720
caenorhabditis_elegansWBGENE00003721
caenorhabditis_elegansWBGENE00003722
caenorhabditis_elegansWBGENE00003723
caenorhabditis_elegansWBGENE00003724
caenorhabditis_elegansWBGENE00003725
caenorhabditis_elegansWBGENE00003728
caenorhabditis_elegansWBGENE00004786
caenorhabditis_elegansWBGENE00006471
caenorhabditis_elegansunc-55WBGENE00006790
caenorhabditis_elegansWBGENE00007367
caenorhabditis_elegansWBGENE00008056
caenorhabditis_elegansnhr-165WBGENE00008158
caenorhabditis_elegansWBGENE00008208
caenorhabditis_elegansnhr-169WBGENE00008289
caenorhabditis_elegansWBGENE00008309
caenorhabditis_elegansnhr-174WBGENE00008474
caenorhabditis_elegansWBGENE00008619
caenorhabditis_elegansWBGENE00008630
caenorhabditis_elegansWBGENE00008778
caenorhabditis_elegansWBGENE00008830
caenorhabditis_elegansWBGENE00008884
caenorhabditis_elegansWBGENE00008901
caenorhabditis_elegansnhr-265WBGENE00009608
caenorhabditis_elegansWBGENE00010017
caenorhabditis_elegansWBGENE00010180
caenorhabditis_elegansWBGENE00010186
caenorhabditis_elegansWBGENE00010215
caenorhabditis_elegansWBGENE00010410
caenorhabditis_elegansWBGENE00010600
caenorhabditis_elegansWBGENE00010601
caenorhabditis_elegansWBGENE00010602
caenorhabditis_elegansWBGENE00010603
caenorhabditis_elegansWBGENE00010604
caenorhabditis_elegansWBGENE00011002
caenorhabditis_elegansWBGENE00011150
caenorhabditis_elegansWBGENE00011396
caenorhabditis_elegansWBGENE00011520
caenorhabditis_elegansWBGENE00011565
caenorhabditis_elegansWBGENE00011566
caenorhabditis_elegansWBGENE00011568
caenorhabditis_elegansnhr-217WBGENE00011651
caenorhabditis_elegansWBGENE00011750
caenorhabditis_elegansWBGENE00012050
caenorhabditis_elegansWBGENE00012056
caenorhabditis_elegansWBGENE00012446
caenorhabditis_elegansWBGENE00012449
caenorhabditis_elegansWBGENE00012596
caenorhabditis_elegansWBGENE00012703
caenorhabditis_elegansWBGENE00013067
caenorhabditis_elegansWBGENE00013483
caenorhabditis_elegansnhr-276WBGENE00013512
caenorhabditis_elegansWBGENE00013584
caenorhabditis_elegansWBGENE00013940
caenorhabditis_elegansWBGENE00014068
caenorhabditis_elegansnhr-245WBGENE00014189
caenorhabditis_elegansWBGENE00014193
caenorhabditis_elegansWBGENE00015497
caenorhabditis_elegansWBGENE00015758
caenorhabditis_elegansWBGENE00015897
caenorhabditis_elegansWBGENE00015900
caenorhabditis_elegansWBGENE00015901
caenorhabditis_elegansWBGENE00015902
caenorhabditis_elegansWBGENE00016091
caenorhabditis_elegansWBGENE00016233
caenorhabditis_elegansWBGENE00016364
caenorhabditis_elegansWBGENE00016365
caenorhabditis_elegansWBGENE00016366
caenorhabditis_elegansWBGENE00016367
caenorhabditis_elegansWBGENE00016368
caenorhabditis_elegansWBGENE00016517
caenorhabditis_elegansWBGENE00016772
caenorhabditis_elegansWBGENE00016926
caenorhabditis_elegansWBGENE00016927
caenorhabditis_elegansWBGENE00017503
caenorhabditis_elegansWBGENE00017512
caenorhabditis_elegansWBGENE00017961
caenorhabditis_elegansWBGENE00018189
caenorhabditis_elegansWBGENE00018265
caenorhabditis_elegansWBGENE00018266
caenorhabditis_elegansWBGENE00018404
caenorhabditis_elegansWBGENE00018412
caenorhabditis_elegansWBGENE00018415
caenorhabditis_elegansWBGENE00018539
caenorhabditis_elegansWBGENE00018541
caenorhabditis_elegansWBGENE00018542
caenorhabditis_elegansWBGENE00018544
caenorhabditis_elegansWBGENE00018545
caenorhabditis_elegansWBGENE00018622
caenorhabditis_elegansWBGENE00019115
caenorhabditis_elegansWBGENE00019116
caenorhabditis_elegansWBGENE00019741
caenorhabditis_elegansWBGENE00019742
caenorhabditis_elegansWBGENE00019743
caenorhabditis_elegansWBGENE00020015
caenorhabditis_elegansWBGENE00020062
caenorhabditis_elegansWBGENE00020152
caenorhabditis_elegansWBGENE00020153
caenorhabditis_elegansWBGENE00020385
caenorhabditis_elegansWBGENE00020460
caenorhabditis_elegansWBGENE00020555
caenorhabditis_elegansWBGENE00020750
caenorhabditis_elegansWBGENE00020849
caenorhabditis_elegansWBGENE00020850
caenorhabditis_elegansWBGENE00020851
caenorhabditis_elegansWBGENE00020852
caenorhabditis_elegansWBGENE00021163
caenorhabditis_elegansWBGENE00021522
caenorhabditis_elegansWBGENE00021610
caenorhabditis_elegansWBGENE00021611
caenorhabditis_elegansWBGENE00021617
caenorhabditis_elegansWBGENE00022097
caenorhabditis_elegansWBGENE00022637
caenorhabditis_elegansWBGENE00022639
caenorhabditis_elegansWBGENE00022640
caenorhabditis_elegansWBGENE00022726
caenorhabditis_elegansWBGENE00022756
caenorhabditis_elegansWBGENE00022805
caenorhabditis_elegansWBGENE00044353
caenorhabditis_elegansWBGENE00044699
caenorhabditis_elegansWBGENE00045515

Paralogs (18): NR1H4 (ENSG00000012504), NR1H3 (ENSG00000025434), RORA (ENSG00000069667), RARB (ENSG00000077092), VDR (ENSG00000111424), PPARD (ENSG00000112033), THRA (ENSG00000126351), NR1D1 (ENSG00000126368), NR1H2 (ENSG00000131408), RARA (ENSG00000131759), PPARG (ENSG00000132170), RORC (ENSG00000143365), NR1I2 (ENSG00000144852), THRB (ENSG00000151090), RARG (ENSG00000172819), NR1D2 (ENSG00000174738), PPARA (ENSG00000186951), RORB (ENSG00000198963)

Protein

Protein identifiers

Nuclear receptor subfamily 1 group I member 3 — Q14994 (reviewed: Q14994)

Alternative names: Constitutive activator of retinoid response, Constitutive androstane receptor, Orphan nuclear receptor MB67

All UniProt accessions (9): Q14994, B7Z8R7, C0H5Y2, D6REZ7, E9PCF2, Q6GZ69, Q6GZ70, Q6GZ72, Q6GZ81

UniProt curated annotations — full annotation on UniProt →

Function. Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes. Transactivates both the phenobarbital responsive element module of the human CYP2B6 gene and the CYP3A4 xenobiotic response element.

Subunit / interactions. Interacts with ECT2. Heterodimer of NR1I3 and RXR. Interacts with PSMC4. Directly interacts with DNAJC7. The DNAJC7-NR1I3 complex may also include HSP90. Interacts with CRY1. Interacts with CRY2 in a ligand-dependent manner.

Subcellular location. Nucleus. Cytoplasm. Cytoskeleton.

Tissue specificity. Predominantly expressed in liver.

Post-translational modifications. Phosphorylated at Thr-38 by PKC, dephosphorylation of Thr-38 is required for nuclear translocation and activation.

Domain organisation. Composed by a short N-terminal domain followed by the DNA binding, hinge, and ligand binding/dimerization domains.

Induction. By dexamethasone.

Similarity. Belongs to the nuclear hormone receptor family. NR1 subfamily.

Isoforms (15)

UniProt IDNamesCanonical?
Q14994-11yes
Q14994-22
Q14994-33
Q14994-44
Q14994-55
Q14994-66
Q14994-77
Q14994-88
Q14994-99
Q14994-1010
Q14994-1111
Q14994-1212
Q14994-1313
Q14994-1514
Q14994-1615

RefSeq proteins (15): NP_001070937, NP_001070938, NP_001070939, NP_001070940, NP_001070941, NP_001070942, NP_001070943, NP_001070944, NP_001070945, NP_001070946, NP_001070947, NP_001070948, NP_001070949, NP_001070950, NP_005113* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000536Nucl_hrmn_rcpt_lig-bdDomain
IPR001628Znf_hrmn_rcptDomain
IPR001723Nuclear_hrmn_rcptFamily
IPR001728ThyrH_rcptFamily
IPR013088Znf_NHR/GATAHomologous_superfamily
IPR035500NHR-like_dom_sfHomologous_superfamily
IPR050234Nuclear_hormone_rcpt_NR1Family

Pfam: PF00104, PF00105

UniProt features (34 total): helix 14, splice variant 7, strand 4, sequence variant 2, zinc finger region 2, chain 1, domain 1, DNA-binding region 1, turn 1, modified residue 1

Structure

Experimental structures (PDB)

2 structures.

PDBMethodResolution (Å)
1XVPX-RAY DIFFRACTION2.6
1XV9X-RAY DIFFRACTION2.7

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q14994-F190.900.73

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): 38

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

IDPathway
R-HSA-383280Nuclear Receptor transcription pathway

MSigDB gene sets: 86 (showing top): GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_OSTEOBLAST_DIFFERENTIATION, PID_REG_GR_PATHWAY, TERAMOTO_OPN_TARGETS_CLUSTER_7, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM4, CAIRO_HEPATOBLASTOMA_DN, TGANTCA_AP1_C, GOBP_OSSIFICATION, SANSOM_APC_TARGETS_DN, MODULE_113, GOBP_INTRACELLULAR_RECEPTOR_SIGNALING_PATHWAY, RIZ_ERYTHROID_DIFFERENTIATION_APOBEC2, BIOCARTA_NUCLEARRS_PATHWAY, TGGAAA_NFAT_Q4_01, CHIANG_LIVER_CANCER_SUBCLASS_PROLIFERATION_DN

GO Biological Process (8): negative regulation of transcription by RNA polymerase II (GO:0000122), osteoblast differentiation (GO:0001649), signal transduction (GO:0007165), cell differentiation (GO:0030154), intracellular receptor signaling pathway (GO:0030522), positive regulation of transcription by RNA polymerase II (GO:0045944), regulation of DNA-templated transcription (GO:0006355), negative regulation of DNA-templated transcription (GO:0045892)

GO Molecular Function (12): RNA polymerase II transcription regulatory region sequence-specific DNA binding (GO:0000977), RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), DNA-binding transcription activator activity, RNA polymerase II-specific (GO:0001228), DNA-binding transcription factor activity (GO:0003700), nuclear receptor activity (GO:0004879), zinc ion binding (GO:0008270), sequence-specific double-stranded DNA binding (GO:1990837), DNA binding (GO:0003677), protein binding (GO:0005515), sequence-specific DNA binding (GO:0043565), metal ion binding (GO:0046872)

GO Cellular Component (6): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), cytoskeleton (GO:0005856)

Reactome top-level categories

Rollup of top-1 pathways:

CategoryPathways
Generic Transcription Pathway1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure4
regulation of transcription by RNA polymerase II3
RNA polymerase II transcription regulatory region sequence-specific DNA binding3
transcription by RNA polymerase II2
DNA-templated transcription2
regulation of DNA-templated transcription2
transcription cis-regulatory region binding2
DNA-binding transcription factor activity, RNA polymerase II-specific2
negative regulation of DNA-templated transcription1
ossification1
cell differentiation1
cell communication1
cellular process1
signaling1
regulation of cellular process1
cellular response to stimulus1
cellular developmental process1
intracellular signal transduction1
positive regulation of DNA-templated transcription1
regulation of gene expression1
regulation of RNA biosynthetic process1
negative regulation of RNA biosynthetic process1
cis-regulatory region sequence-specific DNA binding1
chromatin1
DNA-binding transcription factor activity1
DNA-binding transcription activator activity1
positive regulation of transcription by RNA polymerase II1
transcription regulator activity1
intracellular receptor signaling pathway1
signaling receptor activity1
ligand-modulated transcription factor activity1
transition metal ion binding1
double-stranded DNA binding1
sequence-specific DNA binding1
nucleic acid binding1
binding1
DNA binding1
cation binding1
chromosome1
intracellular membrane-bounded organelle1

Protein interactions and networks

STRING

1363 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
NR1I3CYP3A4P05184903
NR1I3NR0B2Q15466888
NR1I3CYP2B6P20813840
NR1I3XPR1Q9UBH6807
NR1I3RXRAP19793806
NR1I3CYP7A1P22680797
NR1I3CYP1A1P04798777
NR1I3CYP3A7P24462770
NR1I3PPIGQ13427720
NR1I3CYP1A2P05177694
NR1I3CYP2C9P11712691
NR1I3UGT1A1P22309684
NR1I3UGT1A6P19224683
NR1I3UGT1A4P22310681
NR1I3NCOA1Q15788674

IntAct

24 interactions, top by confidence:

ABTypeScore
NR1I3FOSpsi-mi:“MI:0915”(physical association)0.560
RXRApsi-mi:“MI:0914”(association)0.500
NR1I3psi-mi:“MI:0915”(physical association)0.500
NR1I3psi-mi:“MI:0914”(association)0.500
NR1I3HSP90AB1psi-mi:“MI:0915”(physical association)0.400
CDC37NR1I3psi-mi:“MI:0915”(physical association)0.400
CHD9NR1I3psi-mi:“MI:0915”(physical association)0.400
NR1I3SNRPD3psi-mi:“MI:0915”(physical association)0.370
SNX13NR1I3psi-mi:“MI:0915”(physical association)0.370
NR1I3EP300psi-mi:“MI:0915”(physical association)0.370
RXRApsi-mi:“MI:0914”(association)0.350
ESR1ESYT2psi-mi:“MI:0914”(association)0.350
NR1I3MED14psi-mi:“MI:0914”(association)0.350
NR1I3HSPA8psi-mi:“MI:0914”(association)0.350
NR1I3psi-mi:“MI:0914”(association)0.350
glnANR1I3psi-mi:“MI:0915”(physical association)0.000

BioGRID (73): RXRA (Reconstituted Complex), NCOA3 (Reconstituted Complex), NCOA2 (Affinity Capture-MS), MED13 (Affinity Capture-MS), MED12 (Affinity Capture-MS), MED1 (Affinity Capture-MS), UBB (Affinity Capture-MS), MED23 (Affinity Capture-MS), MED24 (Affinity Capture-MS), MED14 (Affinity Capture-MS), PPM1B (Affinity Capture-MS), MED4 (Affinity Capture-MS), NCOA1 (Affinity Capture-MS), MED17 (Affinity Capture-MS), MED15 (Affinity Capture-MS)

ESM2 similar proteins: A2T7D9, A3RGC1, O35627, O42295, O42450, O54915, O57606, O75469, P04625, P11473, P15204, P18113, P18115, P18117, P18119, P37242, P48281, P55055, P62044, P62045, P68305, P68306, Q02777, Q02965, Q13133, Q14994, Q1L673, Q28037, Q28570, Q28571, Q5E9B6, Q60644, Q62685, Q62755, Q8MIM3, Q8SQ01, Q90382, Q91241, Q91279, Q91424

Diamond homologs: A2T7D9, A2T928, A3RGC1, G5EFF5, O00482, O13124, O18531, O35627, O42101, O42295, O42392, O42450, O54915, O57606, O75469, O97716, P03373, P04625, P10276, P10827, P10828, P11416, P11473, P13053, P13631, P15204, P18113, P18115, P18117, P18119, P18514, P18911, P22448, P33242, P33244, P37242, P41235, P48281, P49700, P49701

SIGNOR signaling

5 interactions.

AEffectBMechanism
NR1I3up-regulatesRXRAbinding
NR0B2down-regulatesNR1I3binding
NR1I3“up-regulates quantity by expression”CYP2B6“transcriptional regulation”
NR1I3“up-regulates quantity by expression”UGT1A1“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance46
Likely benign13
Benign6

Top pathogenic / likely-pathogenic (0)

SpliceAI

1532 predictions. Top by Δscore:

VariantEffectΔscore
1:161231475:C:CCacceptor_gain1.0000
1:161233339:C:CCacceptor_gain1.0000
1:161235846:CTGT:Cdonor_gain1.0000
1:161235853:T:Adonor_gain1.0000
1:161229951:C:CTacceptor_gain0.9900
1:161229952:A:Tacceptor_gain0.9900
1:161230811:A:ACdonor_gain0.9900
1:161230812:C:CCdonor_gain0.9900
1:161231229:CCCCA:Cacceptor_gain0.9900
1:161231230:CCCAC:Cacceptor_gain0.9900
1:161231470:GGGAA:Gacceptor_gain0.9900
1:161231471:GGAA:Gacceptor_gain0.9900
1:161231472:GAA:Gacceptor_gain0.9900
1:161231473:AA:Aacceptor_gain0.9900
1:161231474:AC:Aacceptor_loss0.9900
1:161231475:CTGT:Cacceptor_loss0.9900
1:161231476:T:Cacceptor_loss0.9900
1:161231477:G:Cacceptor_gain0.9900
1:161232800:CACT:Cdonor_loss0.9900
1:161232801:ACTC:Adonor_loss0.9900
1:161232802:CTCA:Cdonor_loss0.9900
1:161232803:TCA:Tdonor_loss0.9900
1:161232804:CA:Cdonor_loss0.9900
1:161232805:A:ACdonor_gain0.9900
1:161232805:ACCGG:Adonor_loss0.9900
1:161232806:C:Adonor_loss0.9900
1:161232806:C:CCdonor_gain0.9900
1:161232945:GG:Gacceptor_gain0.9900
1:161232947:C:CCacceptor_gain0.9900
1:161233336:TCA:Tacceptor_gain0.9900

AlphaMissense

2282 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
1:161235858:A:GM76T0.995
1:161236497:A:CF23L0.995
1:161236497:A:TF23L0.995
1:161236499:A:GF23L0.995
1:161236470:C:AK32N0.993
1:161236470:C:GK32N0.993
1:161236464:G:CF34L0.992
1:161236464:G:TF34L0.992
1:161236466:A:GF34L0.992
1:161236474:C:GC31S0.986
1:161236475:A:TC31S0.986
1:161236461:G:CF35L0.985
1:161236461:G:TF35L0.985
1:161236463:A:GF35L0.985
1:161235977:C:AR36S0.984
1:161235977:C:GR36S0.984
1:161236459:C:GR36T0.984
1:161236525:C:GC14S0.984
1:161236526:A:TC14S0.984
1:161235885:C:AR67M0.983
1:161235885:C:GR67T0.983
1:161232809:G:CF182L0.982
1:161232809:G:TF182L0.982
1:161232811:A:GF182L0.982
1:161235884:C:AR67S0.982
1:161235884:C:GR67S0.982
1:161235898:A:GC63R0.981
1:161231393:G:CF210L0.980
1:161231393:G:TF210L0.980
1:161231395:A:GF210L0.980

dbSNP variants (sampled 300 via entrez): RS1000251589 (1:161232290 A>C), RS1000363224 (1:161238888 A>G), RS1000692194 (1:161237396 G>A,T), RS1000743440 (1:161230686 A>G), RS1001166754 (1:161237691 T>A), RS1002712528 (1:161232053 C>A), RS1002821577 (1:161239207 G>C), RS1002862982 (1:161236962 TTTTG>T), RS1003378311 (1:161237670 A>G), RS1003602303 (1:161235442 A>AT), RS1004047752 (1:161231972 C>A,T), RS1004274202 (1:161238253 G>T), RS1004390814 (1:161230489 A>G), RS1004444571 (1:161230224 C>T), RS1005256160 (1:161239511 A>G)

Disease associations

OMIM: gene MIM:603881 | disease phenotypes: MIM:610253

GenCC curated gene-disease

DiseaseClassificationInheritance
intellectual disabilityLimitedAutosomal dominant

Mondo (2): Kleefstra syndrome 1 (MONDO:0027407), intellectual disability (MONDO:0001071)

Orphanet (1): Kleefstra syndrome (Orphanet:261494)

HPO phenotypes

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

GWAS associations

0 associations (top):

MeSH disease descriptors (2)

DescriptorNameTree numbers
D008607Intellectual DisabilityC10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
C563043Kleefstra Syndrome (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL5503 (SINGLE PROTEIN), CHEMBL6195507 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

26 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,340,406 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL104CLOTRIMAZOLE456,325
CHEMBL1064SIMVASTATIN4123,163
CHEMBL1082AMOXICILLIN4113,048
CHEMBL111RIMONABANT415,726
CHEMBL112ACETAMINOPHEN4157,242
CHEMBL121ROSIGLITAZONE458,849
CHEMBL1272REPAGLINIDE433,453
CHEMBL1324TOLCAPONE413,819
CHEMBL139DICLOFENAC4125,009
CHEMBL1481GLIMEPIRIDE433,335
CHEMBL157101KETOCONAZOLE475,361
CHEMBL160CYCLOSPORINE4168,247
CHEMBL1946170REGORAFENIB412,678
CHEMBL2103772RACECADOTRIL41,787
CHEMBL404108LUMIRACOXIB421,145
CHEMBL408TROGLITAZONE438,856
CHEMBL521IBUPROFEN4228,490
CHEMBL56337EPALRESTAT4110
CHEMBL603ZAFIRLUKAST423,220
CHEMBL691ETHINYL ESTRADIOL440,543
CHEMBL6966VERAPAMIL4
CHEMBL715OLANZAPINE4
CHEMBL957BOSENTAN4
CHEMBL1625260TIRACIZINE2
CHEMBL383634GLIQUIDONE2
CHEMBL296468BMS-3870321

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

PharmGKB clinical annotations

8 annotations.

VariantTypeLevelDrugsPhenotypes
rs10538494Toxicity3docetaxelAnemia;Nasopharyngeal Neoplasms
rs2307424Metabolism/PK3efavirenzHIV infectious disease
rs2501873Toxicity3docetaxelAnemia;Nasopharyngeal Neoplasms
rs2501873Dosage4warfarin
rs2502815Toxicity3docetaxelAnemia;Nasopharyngeal Neoplasms
rs3003596Metabolism/PK3efavirenzHIV infectious disease
rs75114882Toxicity3docetaxelNasopharyngeal Neoplasms;Neutropenia
rs9725457Toxicity3docetaxelAnemia;Nasopharyngeal Neoplasms

PharmGKB variants

12 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs2307424NR1I332.621efavirenz
rs2501873NR1I332.002warfarin;docetaxel
rs2502815NR1I332.501docetaxel
rs3003596NR1I331.001efavirenz
rs4073054NR1I3, TOMM40L0.000
rs11584174NR1I30.000
rs55802895NR1I30.000
rs75114882NR1I331.501docetaxel
rs10538494NR1I332.501docetaxel
rs9725457NR1I332.501docetaxel
rs2307418NR1I3, TOMM40L0.000
rs3003593NR1I30.000

GtoPdb / IUPHAR curated pharmacology

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

Target class: nhr — 1I. Vitamin D receptor-like receptors

Most potent curated ligand interactions (8 total), top 8:

LigandActionAffinityParameter
TCPOBOPAgonist7.7pEC50
CITCOAgonist7.3pEC50
meclizineAntagonist7.16pIC50
DL5055Activation6.46pEC50
androstanolInverse agonist6.4pIC50
androstenolInverse agonist6.4pIC50
5β-pregnane-3,20-dioneAgonist6.17pEC50
clotrimazoleAntagonist6.16pIC50

Binding affinities (BindingDB)

1 measured of 1 human assays (1 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValue
CHEMBL3764725IC501410 nM

ChEMBL bioactivities

259 potent at pChembl≥5 of 288 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.00EC501nMCHEMBL5426747
9.00EC501nMCHEMBL5434244
9.00EC501nMCHEMBL5419791
9.00EC501nMCHEMBL5429867
9.00EC501nMCHEMBL5400735
8.70EC502nMCHEMBL5396305
8.70EC502nMCHEMBL5439022
8.60IC502.5nMCHEMBL458603
8.59IC502.6nMCHEMBL458603
8.52EC503nMCHEMBL5408637
8.44EC503.6nMCHEMBL458603
8.40EC504nMCHEMBL5425742
8.30EC505nMCHEMBL458603
8.30EC505nMCHEMBL5401908
8.22EC506nMCHEMBL5435896
8.15EC507nMCHEMBL5397287
8.15EC507nMCHEMBL5411992
8.15EC507nMCHEMBL5437829
8.10EC508nMCHEMBL5423627
8.05EC509nMCHEMBL5437100
8.05EC509nMCHEMBL5398624
8.00EC5010nMCHEMBL5421493
8.00EC5010nMCHEMBL5396096
7.96EC5011nMCHEMBL5432712
7.96EC5011nMCHEMBL5399445
7.93IC5011.7nMCHEMBL3763793
7.92EC5012nMCHEMBL458603
7.89EC5013nMCHEMBL5433607
7.89EC5013nMCHEMBL458603
7.89IC5012.8nMCHEMBL3763793
7.86IC5013.9nMCHEMBL3763399
7.85EC5014nMCHEMBL5434877
7.82EC5015nMCHEMBL5438918
7.80EC5016nMCHEMBL5409045
7.77EC5017nMCHEMBL5399505
7.75EC5018nMCHEMBL5440050
7.72EC5019nMCHEMBL5435703
7.71IC5019.5nMCHEMBL3763536
7.70IC5020.1nMCHEMBL3763664
7.70EC5020nMCHEMBL458603
7.68IC5020.9nMCHEMBL3764750
7.67IC5021.2nMCHEMBL3765064
7.66IC5022.1nMCHEMBL3763725
7.64EC5023nMCHEMBL5409712
7.62IC5024.1nMCHEMBL3764168
7.60EC5025nMCHEMBL5398624
7.60IC5025nMPK-11195
7.50IC5031.9nMCHEMBL3764583
7.49IC5032.6nMCLOTRIMAZOLE
7.46EC5035nMCHEMBL5417795

PubChem BioAssay actives

197 with measured affinity, of 1279 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
3-(1-benzyltriazol-4-yl)-2-(4-chlorophenyl)imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0010uM
3-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]-2-(4-methoxyphenyl)imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0010uM
[2-chloro-5-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]phenyl]methanol2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0010uM
3-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]-2-(4-fluorophenyl)imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0010uM
1-[2-chloro-5-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]phenyl]ethanone2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0010uM
3-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]-2-[4-(trifluoromethyl)phenyl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0010uM
2-(3,4-dichlorophenyl)-3-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0020uM
2-(4-chlorophenyl)-3-[1-[(4-chlorophenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0020uM
6-(4-chlorophenyl)-5-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]imidazo[2,1-b][1,3]thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0030uM
3-[1-[(4-chloro-3-nitrophenyl)methyl]triazol-4-yl]-2-(4-chlorophenyl)imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0040uM
2-(4-chlorophenyl)-3-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0050uM
(E)-1-[6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]-N-[(3,4-dichlorophenyl)methoxy]methanimine1686019: Agonist activity at human CARec500.0050uM
2-chloro-5-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]aniline2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0060uM
6-(4-chlorophenyl)-5-[1-[(4-chlorophenyl)methyl]triazol-4-yl]imidazo[2,1-b][1,3]thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0070uM
(NE)-N-[[2-chloro-5-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]phenyl]methylidene]hydroxylamine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0070uM
5-(1-benzyltriazol-4-yl)-6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0070uM
2-chloro-5-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]benzaldehyde2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0080uM
2-(4-chlorophenyl)-3-[1-[(4-methylsulfonylphenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0090uM
3-[1-[[4-chloro-3-(methoxymethyl)phenyl]methyl]triazol-4-yl]-2-(4-chlorophenyl)imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0090uM
6-(4-chlorophenyl)-5-[1-(pyridin-2-ylmethyl)triazol-4-yl]imidazo[2,1-b][1,3]thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0100uM
5-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]-3-[(3,4-dichlorophenyl)methyl]-1,2-oxazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0100uM
1-[2-chloro-5-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]phenyl]propan-1-one2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0110uM
2-(4-chlorophenyl)-3-[1-[(4-methylsulfanylphenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0110uM
cyclohexyl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0117uM
6-(4-chlorophenyl)-5-[2-[(3,4-dichlorophenyl)methyl]-1,3-thiazol-4-yl]imidazo[2,1-b][1,3]thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0130uM
cyclopentyl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0139uM
5-[6-(4-chlorophenyl)imidazo[2,1-b][1,3]thiazol-5-yl]-3-[(3,4-dichlorophenyl)methyl]-1,2,4-oxadiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0140uM
2-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]-5-[(3,4-dichlorophenyl)methyl]-1,3,4-thiadiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0150uM
6-(3,4-dichlorophenyl)-5-[1-[(3,4-dichlorophenyl)methyl]triazol-4-yl]imidazo[2,1-b][1,3]thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0160uM
2-(4-chlorophenyl)-3-[1-[(3,4-dichlorophenyl)methyl]pyrrol-2-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0170uM
4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]-2-[(3,4-dichlorophenyl)methyl]-1,3-thiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0180uM
2-(4-chlorophenyl)-3-[1-[(3,4-dimethoxyphenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0190uM
propan-2-yl N-[11-(2-cyclopentyloxyacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0195uM
cyclobutyl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0201uM
propan-2-yl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0209uM
propan-2-yl N-[11-[2-(2,2-dimethylpropoxy)acetyl]-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0212uM
cyclopropyl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0221uM
2-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]-5-[(3,4-dichlorophenyl)methyl]-1,3,4-oxadiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0230uM
propan-2-yl N-[11-(2-cyclohexyloxyacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0241uM
N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide2136258: Antagonist activity at human CAR LBD (151 to 349 residues) expressed in HepG2 cells co-expressed with pGL5-luc luciferase assessed as reduction in CAR activation measured after 1 to 4 hrs by LanthaScreen TR-FRET assayic500.0250uM
tert-butyl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0319uM
5-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]-3-[(3,4-dichlorophenyl)methyl]-1,2,4-oxadiazole2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0350uM
propan-2-yl N-[11-(2-butan-2-yloxyacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0353uM
ethyl N-[11-(2-pyrrol-1-ylacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0370uM
propan-2-yl N-[11-(2-cyclobutyloxyacetyl)-5,6-dihydrobenzo[b][1]benzazepin-2-yl]carbamate1276954: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluorescein-PGC1 alpha coactivator recruitment after 1 hr by TR-FRET assayic500.0376uM
2-(4-chlorophenyl)-3-[1-(1-phenylethyl)triazol-4-yl]imidazo[1,2-a]pyridine2028247: Agonist activity at human CAR LBD in human HepG2 cells incubated for 24 hrs by firefly luciferase reporter assayec500.0400uM
2-(4-chlorophenyl)-3-[1-[2-(3,4-dichlorophenyl)ethyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0400uM
2-(4-chlorophenyl)-3-[1-[(4-methoxyphenyl)methyl]triazol-4-yl]imidazo[1,2-a]pyridine2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0400uM
2-(3-methylphenyl)-1H-quinazoline-4-thione2136257: Partial agonist activity at human CAR LBD (151 to 349 residues) expressed in HepG2 cells coexpressed with pGL5-luc luciferase measured after 1 to 4 hrs by LanthaScreen TR-FRET assayec500.0550uM
4-[[4-[2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl]triazol-1-yl]methyl]benzonitrile2028243: Agonist activity at human recombinant GST-tagged CAR LBD incubated for 1 to 4 hrs in presence of fluorescein-labeled PGC1alpha by lanthascreen TR-FRET assayec500.0600uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oximedecreases expression, affects reaction, increases cleavage, increases response to substance, affects binding (+8 more)43
Phenobarbitalaffects localization, increases activity, affects reaction, affects cotreatment, increases reaction (+5 more)18
Clotrimazoleincreases activity, increases localization, increases reaction, affects binding, decreases reaction (+2 more)13
1,4-bis(2-(3,5-dichloropyridyloxy))benzenedecreases reaction, increases expression, increases activity, decreases expression, increases reaction (+4 more)9
PK 11195decreases activity, decreases reaction, affects cotreatment, increases reaction, affects binding (+3 more)8
artemisininaffects expression, affects binding, increases activity, increases expression6
Diethylhexyl Phthalateincreases expression, decreases reaction, increases activity, affects binding, decreases activity6
bisphenol Adecreases reaction, decreases activity, affects binding, increases activity5
4-nonylphenolincreases activity, affects binding, decreases activity, increases expression, increases reaction (+2 more)5
Androstenolsincreases expression, affects activity, affects binding, decreases activity, increases activity (+3 more)5
Methoxychlorincreases expression, increases reaction, affects binding, increases activity, decreases reaction5
Cyclosporineaffects expression, affects cotreatment, decreases expression, increases expression5
androstan-3-olaffects binding, decreases activity, decreases reaction, increases activity4
o,p’-DDTincreases reaction, increases activity, decreases reaction, increases expression, affects binding4
Phenytoinaffects reaction, increases expression, affects binding, increases reaction, increases activity (+1 more)4
Triclosanaffects cotreatment, decreases expression, affects binding, decreases activity, increases activity4
Permethrinincreases expression, decreases activity, decreases reaction, increases reaction, affects binding (+2 more)4
diethyl phthalateaffects binding, increases activity3
butylbenzyl phthalateaffects binding, increases activity3
pyreneaffects cotreatment, decreases reaction, increases expression, increases activity3
propiconazoleaffects cotreatment, decreases expression, affects binding, increases activity3
panaxytrioldecreases reaction, increases expression, affects binding, increases reaction, increases activity3
tebuconazoleaffects binding, decreases activity, affects cotreatment, decreases expression3
bisphenol Baffects binding, decreases reaction, decreases activity, increases activity3
bisphenol Zaffects binding, increases activity, decreases reaction, decreases activity3
bisphenol AFaffects binding, decreases reaction, decreases activity, increases activity3
Resveratroldecreases expression, decreases activity, affects binding, decreases response to substance, increases activity (+1 more)3
Troglitazoneaffects cotreatment, affects expression, decreases expression, increases activity, increases expression3
Alitretinoinaffects binding, affects cotreatment, increases reaction, increases activity3
Acetaminophenincreases reaction, increases response to substance, decreases expression, affects cotreatment3

ChEMBL screening assays

163 unique, capped per target: 131 binding, 26 admet, 6 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1211340FunctionalAgonist activity at CAR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assaySynthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. — Bioorg Med Chem Lett
CHEMBL1743246ADMETConstitutive androstane receptor inverse agonistCasarett and Doull’s Toxicology The Basic Science of Poisons, 7th edition
CHEMBL1961842BindingEffect on CAR(NR1I3) dependent reporter activity in HEK293 cells at 20 uMRegulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. — Nature

Cellosaurus cell lines

11 cell lines: 8 cancer cell line, 3 embryonic stem cell

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

CellosaurusNameCategorySex
CVCL_A4U2SEES3-1V human NR1I3, clone1Embryonic stem cellMale
CVCL_A4U3SEES3-1V human NR1I3, clone2Embryonic stem cellMale
CVCL_A4U4SEES3-1V human NR1I3, clone3Embryonic stem cellMale
CVCL_B6AAHepaRG CAR KOCancer cell lineFemale
CVCL_B6ATHepaRG PXR/CAR KOCancer cell lineFemale
CVCL_C0V4HepG2 CAR-CYP2B6 clone 6Cancer cell lineMale
CVCL_C0V5HepG2 CAR-CYP2B6 clone 7Cancer cell lineMale
CVCL_C0V6HepG2 CAR-CYP2B6 clone 10Cancer cell lineMale
CVCL_XI49HepaRG-CARCancer cell lineFemale
CVCL_XI50HepG2-CARCancer cell lineMale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT05657860PHASE4COMPLETEDGuanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479PHASE4RECRUITINGMetformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829PHASE4WITHDRAWNValbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198PHASE4NOT_YET_RECRUITINGDeutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT02270736PHASE3COMPLETEDClinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability
NCT02304302PHASE2COMPLETEDDown Syndrome Memantine Follow-up Study
NCT03862950PHASE2COMPLETEDA Trial of Metformin in Individuals With Fragile X Syndrome (Met)
NCT04529226PHASE2UNKNOWNStudy to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis
NCT04821856PHASE2COMPLETEDEvaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability
NCT05273320PHASE1COMPLETEDClinical Trial of Nabilone for Aggression in Adults With Intellectual and Developmental Disabilities
NCT05301361PHASE1ENROLLING_BY_INVITATIONSensitivity of the NIH Toolbox to Stimulant Treatment in Intellectual Disabilities
NCT06016764PHASE1COMPLETEDUse of MRI and cTBS for Catatonia in Autism
NCT06586827PHASE1COMPLETEDImpact of Competency-Based Training and Technical Assistance Employment Outcomes of Individuals With ID/DD
NCT07531940PHASE1NOT_YET_RECRUITINGEscalating Doses of Memantine in Down Syndrome (MEDS-123)
NCT03479476PHASE2/PHASE3COMPLETEDA Trial of Metformin in Individuals With Fragile X Syndrome
NCT02616796PHASE1/PHASE2COMPLETEDEffects of Social Gaze Training on Brain and Behavior in Fragile X Syndrome
NCT06860672EARLY_PHASE1RECRUITINGClinical Trial of the Dual Vector Base Editor for the Treatment of the CHD3-R1025W Mutation
NCT00597948Not specifiedCOMPLETEDHealthy Lifestyles for People With Intellectual Disabilities
NCT01087320Not specifiedRECRUITINGGenome Medical Sequencing for Gene Discovery
NCT01652963Not specifiedUNKNOWNPicture-based Computerised Assessment and Training of Cognitive Behaviour Therapy Skills
NCT01695395Not specifiedCOMPLETEDMental Health Care Provision for Adults With Intellectual Disability and a Mental Disorder
NCT01867554Not specifiedCOMPLETEDResearch and Characterization of New Genes Involved in Intellectual Disability
NCT01915381Not specifiedCOMPLETEDImproving Adherence Healthy Lifestyle With a Smartphone Application Based on Adults With Intellectual Disabilities
NCT01988623Not specifiedCOMPLETEDPivotal Response Treatment for Individuals With Intellectual Disabilities
NCT02099773Not specifiedCOMPLETEDSupport Staff-client Interactions With Augmentative and Alternative Communication
NCT02136849Not specifiedCOMPLETEDInter-regional Project of the Great Western Exploration Approach for Exome Molecular Causes Severe Intellectual Disability Isolated or Syndromic
NCT02225041Not specifiedCOMPLETEDSedation Strategy and Cognitive Outcome After Critical Illness in Early Childhood
NCT02414438Not specifiedCOMPLETEDEstablishing the Clinical Utility of First StepDx PLUS and NextStepDx PLUS Study
NCT02451761Not specifiedCOMPLETEDApparently Balanced Chromosomal Translocation/ Next-generation Sequencing/ Intellectual Disability
NCT02461420Not specifiedACTIVE_NOT_RECRUITINGMapping the Genotype, Phenotype, and Natural History of Phelan-McDermid Syndrome
NCT02461459Not specifiedACTIVE_NOT_RECRUITINGAutism Spectrum Disorder (ASD) and Intellectual Disability (ID) Determinants in Tuberous Sclerosis Complex (TSC)
NCT02486081Not specifiedCOMPLETEDDevelopment and Application-Smart Football for Movement Evaluation and Training in the Special Education Population
NCT02504502Not specifiedCOMPLETEDEnhancing Genomic Laboratory Reports to Enhance Communication and Empower Patients
NCT02513277Not specifiedCOMPLETEDDiabetes Screening & Prevention for People With Learning (Intellectual) Disabilities:STOP Diabetes Study
NCT02561754Not specifiedCOMPLETEDWeight Management for Adolescents With IDD
NCT02591446Not specifiedCOMPLETEDTranscranial Magnetic Stimulation Studies in Autism Spectrum Disorders
NCT02714868Not specifiedCOMPLETEDEvaluation of Project TEAM (Teens Making Environmental and Activity Modifications)
NCT02721394Not specifiedUNKNOWNFCT With Young Children With ID in the UK: A Feasibility Project V.1
NCT02746614Not specifiedCOMPLETEDPsychomotor Therapy Effects in Adaptive Behavior and Motor Proficiency in Intellectual Disability
NCT02836405Not specifiedCOMPLETEDTMS for the Investigation of Brain Plasticity in Autism Spectrum Disorders

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

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This page pulls from 80 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot