XPO4

Summary

XPO4 (exportin 4, HGNC:17796) is a protein-coding gene on chromosome 13q12.11, encoding Exportin-4 (Q9C0E2). Mediates the nuclear export of proteins (cargos), such as EIF5A, SMAD3 and isoform M2 of PKM (PKM2).

XPO4 belongs to a large family of karyopherins (see MIM 602738) that mediate the transport of proteins and other cargo between the nuclear and cytoplasmic compartments (Lipowsky et al., 2000 [PubMed 10944119]).

Source: NCBI Gene 64328 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 108 total
• Druggable target: yes
• MANE Select transcript: NM_022459

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17796
Approved symbol	XPO4
Name	exportin 4
Location	13q12.11
Locus type	gene with protein product
Status	Approved
Aliases	FLJ13046, KIAA1721
Ensembl gene	ENSG00000132953
Ensembl biotype	protein_coding
OMIM	611449
Entrez	64328

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 6 protein_coding, 1 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000255305, ENST00000465018, ENST00000490513, ENST00000909776, ENST00000909777, ENST00000936072, ENST00000936073, ENST00000953408

RefSeq mRNA: 2 — MANE Select: NM_022459 NM_001372061, NM_022459

CCDS: CCDS41872

Canonical transcript exons

ENST00000255305 — 23 exons

Exon	Start	End
ENSE00001417012	20855627	20855765
ENSE00001424505	20843770	20843886
ENSE00001591634	20808436	20808581
ENSE00001611432	20822132	20822289
ENSE00001660313	20786965	20787057
ENSE00001671424	20788486	20788616
ENSE00001685369	20796076	20796256
ENSE00001689661	20787481	20787598
ENSE00001695714	20827067	20827179
ENSE00001723749	20800156	20800325
ENSE00001750493	20796764	20797057
ENSE00001763697	20799165	20799339
ENSE00001779427	20821704	20821878
ENSE00001781734	20809791	20809967
ENSE00001787822	20807457	20807634
ENSE00001797468	20809083	20809225
ENSE00001798261	20800831	20800990
ENSE00001832020	20902670	20902746
ENSE00001943005	20777329	20783919
ENSE00002029291	20842895	20843048
ENSE00002685281	20790462	20790580
ENSE00003461946	20868596	20868701
ENSE00003632528	20862717	20862858

Expression profiles

Bgee: expression breadth ubiquitous, 226 present calls, max score 96.97.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 17.6269 / max 214.7140, expressed in 1793 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
136371	12.8657	1759
136372	2.6124	1290
136373	1.0393	677
136374	1.0306	677
136361	0.0496	14
136362	0.0293	15

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	96.97	gold quality
biceps brachii	UBERON:0001507	95.18	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	94.79	gold quality
secondary oocyte	CL:0000655	89.79	gold quality
hindlimb stylopod muscle	UBERON:0004252	89.61	gold quality
oocyte	CL:0000023	89.27	gold quality
deltoid	UBERON:0001476	87.03	gold quality
muscle of leg	UBERON:0001383	86.11	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	86.10	gold quality
tendon	UBERON:0000043	85.46	gold quality
gastrocnemius	UBERON:0001388	85.31	gold quality
skeletal muscle tissue	UBERON:0001134	85.20	gold quality
calcaneal tendon	UBERON:0003701	85.06	gold quality
muscle organ	UBERON:0001630	84.94	gold quality
skeletal muscle organ	UBERON:0014892	84.93	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	84.02	gold quality
tibialis anterior	UBERON:0001385	83.85	silver quality
gluteal muscle	UBERON:0002000	82.83	gold quality
adrenal tissue	UBERON:0018303	82.21	gold quality
muscle tissue	UBERON:0002385	82.13	gold quality
diaphragm	UBERON:0001103	80.74	gold quality
ventricular zone	UBERON:0003053	80.54	gold quality
endothelial cell	CL:0000115	79.70	silver quality
islet of Langerhans	UBERON:0000006	78.94	gold quality
sural nerve	UBERON:0015488	78.89	gold quality
heart left ventricle	UBERON:0002084	78.76	gold quality
cardiac ventricle	UBERON:0002082	78.53	gold quality
ganglionic eminence	UBERON:0004023	78.51	gold quality
tendon of biceps brachii	UBERON:0008188	78.36	gold quality
monocyte	CL:0000576	78.15	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	5.57

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SOX9

miRNA regulators (miRDB)

331 targeting XPO4, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4692	100.00	67.32	2066
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4514	99.99	67.10	1870
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-520G-5P	99.99	66.76	658
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-3692-3P	99.98	70.27	2139
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-433-3P	99.98	69.37	1203
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-3688-3P	99.97	72.02	2834

Literature-anchored findings (GeneRIF, showing 9)

• A short peptide representing the minimal interaction domain in Smad3 effectively competes with Smad3 association to exportin 4 and blocks nuclear export of Smad3 in vivo. (PMID:16449645)
• Data suggest that XPO4 could be involved in the progression of human hepatocellular carcinoma. (PMID:21332550)
• These results demonstrate that Exp4 acts as a Sox9 co-regulator that directly regulates binding of Sox9 to its target genes. (PMID:21991335)
• Methylation status of XPO4 in peripheral blood mononuclear cells (PBMCs) tended to be a noninvasive biomarker to predict hepatocellular carcinoma (HCC) and the progression of hepatitis B virus (HBV)infection. (PMID:24597692)
• Knockdown of exportins 4, 5, and 7 altered thyroid hormone receptor shuttling dynamics, and when exportins 5 and 7 were overexpressed, TR distribution shifted toward the cytosol. (PMID:25911113)
• XPO4 copy number variation duplication was associated with histological severity of non-alcoholic fatty liver disease. (PMID:26293807)
• Molecular structure of the exportin Xpo4 in complex with RanGTP and the hypusine-containing translation factor eIF5A has been reported. (PMID:27306458)
• Copy number variation and expression of exportin-4 associates with severity of fibrosis in metabolic associated fatty liver disease. (PMID:34388518)
• Exportin 4 DNA promoter methylation in liver fibrosis. (PMID:38722973)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	xpo4	ENSDARG00000010281
mus_musculus	Xpo4	ENSMUSG00000021952
rattus_norvegicus	Xpo4	ENSRNOG00000010137
caenorhabditis_elegans		WBGENE00022087

Paralogs (2): XPO7 (ENSG00000130227), RANBP17 (ENSG00000204764)

Protein

Protein identifiers

Exportin-4 — Q9C0E2 (reviewed: Q9C0E2)

All UniProt accessions (1): Q9C0E2

UniProt curated annotations — full annotation on UniProt →

Function. Mediates the nuclear export of proteins (cargos), such as EIF5A, SMAD3 and isoform M2 of PKM (PKM2). In the nucleus binds cooperatively to its cargo and to the GTPase Ran in its active GTP-bound form. Docking of this trimeric complex to the nuclear pore complex (NPC) is mediated through binding to nucleoporins. Upon transit of a nuclear export complex into the cytoplasm, disassembling of the complex and hydrolysis of Ran-GTP to Ran-GDP (induced by RANBP1 and RANGAP1, respectively) cause release of the cargo from the export receptor. XPO4 then return to the nuclear compartment and mediate another round of transport. The directionality of nuclear export is thought to be conferred by an asymmetric distribution of the GTP- and GDP-bound forms of Ran between the cytoplasm and nucleus. Catalyzes the nuclear export of hypusinated EIF5A; a small cytoplasmic protein that enters nucleus and accumulates within nucleolus if not exported back by XPO4. Specifically mediates nuclear export of isoform M2 of PKM (PKM2) following PKM2 deacetylation by SIRT6. Also mediates the nuclear import of SOX transcription factors SRY and SOX2.

Subunit / interactions. Interacts with Ran and cargo proteins in a GTP-dependent manner.

Subcellular location. Cytoplasm. Nucleus.

Similarity. Belongs to the exportin family.

RefSeq proteins (2): NP_001358990, NP_071904* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR011989	ARM-like	Homologous_superfamily
IPR014877	XPO1_C_dom	Domain
IPR016024	ARM-type_fold	Homologous_superfamily
IPR044189	XPO4/7-like	Family

Pfam: PF08767

UniProt features (6 total): modified residue 2, sequence variant 2, chain 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9C0E2-F1	88.96	0.67

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 (2): 464, 521

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 196 (showing top): AAGCAAT_MIR137, HNF3ALPHA_Q6, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, MODULE_255, GOBP_POSITIVE_REGULATION_OF_INTRACELLULAR_PROTEIN_TRANSPORT, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, MODULE_317, GOBP_REGULATION_OF_PROTEIN_EXPORT_FROM_NUCLEUS, GOMF_GTPASE_BINDING, MONNIER_POSTRADIATION_TUMOR_ESCAPE_UP, GOBP_POSITIVE_REGULATION_OF_INTRACELLULAR_TRANSPORT, GOBP_NUCLEAR_TRANSPORT, GTGCCTT_MIR506

GO Biological Process (5): protein export from nucleus (GO:0006611), positive regulation of protein export from nucleus (GO:0046827), glycolytic process (GO:0006096), protein transport (GO:0015031), nuclear transport (GO:0051169)

GO Molecular Function (3): nuclear export signal receptor activity (GO:0005049), small GTPase binding (GO:0031267), protein binding (GO:0005515)

GO Cellular Component (5): nucleus (GO:0005634), nuclear pore (GO:0005643), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
nuclear export	2
intracellular protein transport	1
protein export from nucleus	1
positive regulation of nucleocytoplasmic transport	1
regulation of protein export from nucleus	1
positive regulation of intracellular protein transport	1
phosphoglycerate kinase activity	1
phosphoglycerate mutase activity	1
phosphopyruvate hydratase activity	1
pyruvate kinase activity	1
pyruvate metabolic process	1
generation of precursor metabolites and energy	1
aerobic respiration	1
carbohydrate catabolic process	1
pyridine nucleotide catabolic process	1
glyceraldehyde-3-phosphate dehydrogenase [NAD(P)+] (phosphorylating) activity	1
ADP catabolic process	1
ATP metabolic process	1
nicotinamide nucleotide metabolic process	1
transport	1
intracellular protein localization	1
establishment of protein localization	1
intracellular transport	1
nucleocytoplasmic carrier activity	1
GTPase binding	1
binding	1
intracellular membrane-bounded organelle	1
nuclear envelope	1
nuclear protein-containing complex	1
nuclear lumen	1
intracellular anatomical structure	1
cytoplasm	1

Protein interactions and networks

STRING

1046 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
XPO4	XPOT	O43592	973
XPO4	CSE1L	P55060	906
XPO4	XPO1	O14980	894
XPO4	XPO6	Q96QU8	820
XPO4	IPO13	O94829	775
XPO4	RANGAP1	P46060	765
XPO4	TYMS	P04818	723
XPO4	EIF5A	P10159	708
XPO4	EIF5AL1	Q6IS14	685
XPO4	XPO5	Q9HAV4	685
XPO4	THOC2	Q8NI27	650
XPO4	RANBP3	Q9H6Z4	644
XPO4	EIF5A2	Q9GZV4	634
XPO4	SMAD3	P84022	621
XPO4	IPO11	Q9UI26	617

IntAct

161 interactions, top by confidence:

A	B	Type	Score
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
SCN2B	EXOC5	psi-mi:“MI:0914”(association)	0.640
TNFSF13B	IPO8	psi-mi:“MI:0914”(association)	0.640
ILVBL	COG7	psi-mi:“MI:0914”(association)	0.640
B3GAT3	GOLIM4	psi-mi:“MI:0914”(association)	0.640
GYPA	TCAF2	psi-mi:“MI:0914”(association)	0.640
EPHA1	EXOC5	psi-mi:“MI:0914”(association)	0.530
COMTD1	IFRD1	psi-mi:“MI:0914”(association)	0.530
PTGER3	PIK3R2	psi-mi:“MI:0914”(association)	0.530
VASN	AP3B1	psi-mi:“MI:0914”(association)	0.530
FZD10	NRP1	psi-mi:“MI:0914”(association)	0.530
VSIG2	TTI1	psi-mi:“MI:0914”(association)	0.530
CD274	TTI1	psi-mi:“MI:0914”(association)	0.530
CD70	METTL15	psi-mi:“MI:0914”(association)	0.530
CA14	EXOC5	psi-mi:“MI:0914”(association)	0.530
ILVBL	EIF2B5	psi-mi:“MI:0914”(association)	0.530
ILVBL	SLC33A1	psi-mi:“MI:0914”(association)	0.530
CD40	EXOC5	psi-mi:“MI:0914”(association)	0.530
NPTN	TNPO2	psi-mi:“MI:0914”(association)	0.530
C3orf18	SPAG9	psi-mi:“MI:0914”(association)	0.530
LPAR1	TMEM223	psi-mi:“MI:0914”(association)	0.530

BioGRID (156): XPO4 (Two-hybrid), XPO4 (Affinity Capture-RNA), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS), XPO4 (Affinity Capture-MS)

ESM2 similar proteins: A5D785, A5WW24, O00410, O04375, O04376, O15397, O35638, O46563, O60518, O95373, Q08AM6, Q16401, Q499Y0, Q569Z2, Q5IFJ8, Q5R9G4, Q5R9J2, Q5ZLT0, Q5ZMR9, Q68F38, Q6GMY9, Q704U0, Q7PC79, Q7TMY7, Q802D3, Q8AY73, Q8BIV3, Q8BKC5, Q8GUL2, Q8K2V6, Q8N3U4, Q8VI75, Q8WVM7, Q91YE6, Q924C1, Q96P70, Q99NF8, Q9C0E2, Q9D3E6, Q9DGN0

Diamond homologs: Q499Y0, Q5ZMR9, Q802D3, Q9C0E2, Q9ESJ0

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 163 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:

Pathway	Partners	Fold	FDR
G alpha (q) signalling events	10	5.5×	3e-03

GO biological processes:

GO term	Partners	Fold	FDR
T cell costimulation	6	16.2×	5e-04
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	8	12.6×	1e-04
phospholipase C-activating G protein-coupled receptor signaling pathway	11	10.4×	9e-06
positive regulation of cytosolic calcium ion concentration	9	7.6×	6e-04
G protein-coupled receptor signaling pathway	17	4.4×	1e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	91
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

4740 predictions. Top by Δscore:

Variant	Effect	Δscore
13:20783741:C:CT	donor_gain	1.0000
13:20783753:G:A	donor_gain	1.0000
13:20783765:TCTAA:T	donor_gain	1.0000
13:20783770:A:C	donor_gain	1.0000
13:20783796:T:TA	donor_gain	1.0000
13:20787605:A:C	acceptor_gain	1.0000
13:20787644:T:C	acceptor_gain	1.0000
13:20790581:C:CC	acceptor_gain	1.0000
13:20796252:TTGGA:T	acceptor_gain	1.0000
13:20796253:TGGA:T	acceptor_gain	1.0000
13:20796254:GGA:G	acceptor_gain	1.0000
13:20796255:GA:G	acceptor_gain	1.0000
13:20796257:C:CC	acceptor_gain	1.0000
13:20796257:C:CG	acceptor_loss	1.0000
13:20796759:CTTA:C	donor_loss	1.0000
13:20796760:TTAC:T	donor_loss	1.0000
13:20796761:TA:T	donor_loss	1.0000
13:20796762:A:AC	donor_gain	1.0000
13:20796762:ACCTC:A	donor_loss	1.0000
13:20796763:C:CC	donor_gain	1.0000
13:20796763:CCT:C	donor_gain	1.0000
13:20796763:CCTCT:C	donor_gain	1.0000
13:20797056:AC:A	acceptor_gain	1.0000
13:20797057:CC:C	acceptor_gain	1.0000
13:20797058:C:CC	acceptor_gain	1.0000
13:20799159:TGTTA:T	donor_loss	1.0000
13:20799160:GTTAC:G	donor_loss	1.0000
13:20799161:TTA:T	donor_loss	1.0000
13:20799162:TACCT:T	donor_loss	1.0000
13:20799163:A:T	donor_loss	1.0000

AlphaMissense

7577 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
13:20788495:C:T	G1013E	1.000
13:20788496:C:G	G1013R	1.000
13:20788496:C:T	G1013R	1.000
13:20790505:C:T	G958E	1.000
13:20790506:C:G	G958R	1.000
13:20790506:C:T	G958R	1.000
13:20796111:A:G	L921P	1.000
13:20796120:A:G	L918P	1.000
13:20796123:A:G	L917P	1.000
13:20809913:A:G	W410R	1.000
13:20809913:A:T	W410R	1.000
13:20827114:A:G	W265R	1.000
13:20827114:A:T	W265R	1.000
13:20842916:A:G	W236R	1.000
13:20842916:A:T	W236R	1.000
13:20855711:T:A	K124N	1.000
13:20855711:T:G	K124N	1.000
13:20855712:T:A	K124I	1.000
13:20855751:A:T	V111D	1.000
13:20862826:C:G	A70P	1.000
13:20862830:A:C	F68L	1.000
13:20862830:A:T	F68L	1.000
13:20862832:A:G	F68L	1.000
13:20862837:A:T	V66D	1.000
13:20868611:A:G	C54R	1.000
13:20868670:C:G	R34P	1.000
13:20868671:G:T	R34S	1.000
13:20787571:G:C	C1025W	0.999
13:20788504:A:G	L1010P	0.999
13:20788516:A:G	L1006P	0.999

dbSNP variants (sampled 300 via entrez): RS1000008065 (13:20893882 TG>T), RS1000014578 (13:20903130 G>C), RS1000050154 (13:20867506 A>G), RS1000093314 (13:20857582 C>T), RS1000153341 (13:20868483 G>T), RS1000157866 (13:20873933 C>G), RS1000165020 (13:20858031 C>T), RS1000195030 (13:20804104 C>G), RS1000204662 (13:20890743 G>A), RS1000213315 (13:20784998 C>G), RS1000242756 (13:20803842 G>A), RS1000250505 (13:20873350 G>A), RS1000297042 (13:20847947 A>T), RS1000301591 (13:20836776 C>A,T), RS1000304065 (13:20902127 C>T)

Disease associations

OMIM: gene MIM:611449 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST006269_794	General cognitive ability	3.000000e-09
GCST007045_38	PR interval	9.000000e-16
GCST010152_3	Neuroblastoma or malignant cutaneous melanoma	2.000000e-06
GCST010321_145	PR interval	1.000000e-51
GCST90000025_1037	Appendicular lean mass	3.000000e-11

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0004337	intelligence
EFO:0004462	PR interval
EFO:0004980	appendicular lean mass

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6067406 (SINGLE PROTEIN)

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.24	Kd	5.695	nM	CHEMBL3752910
8.23	ED50	5.944	nM	CHEMBL3752910

PubChem BioAssay actives

1 with measured affinity, of 2 total; 1 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149964: Binding affinity to human XPO4 incubated for 45 mins by Kinobead based pull down assay	kd	0.0057	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Tetrachlorodibenzodioxin	affects expression, decreases expression	3
Estradiol	increases expression	2
Valproic Acid	decreases expression	2
Cadmium Chloride	increases abundance, increases expression	2
aristolochic acid I	decreases expression	1
2,4,6-tribromophenol	increases expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
bisphenol A	decreases expression	1
decabromobiphenyl ether	increases expression	1
trichostatin A	affects expression	1
arsenite	affects binding, decreases reaction	1
sodium arsenite	decreases expression	1
butyraldehyde	decreases expression	1
tetrabromobisphenol A	increases expression	1
coumarin	increases phosphorylation	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1
di-n-butylphosphoric acid	affects expression	1
pentabrominated diphenyl ether 100	increases expression	1
jinfukang	decreases expression	1
Resveratrol	increases expression, affects cotreatment	1
Sunitinib	decreases expression	1
Acrolein	affects cotreatment, increases oxidation, increases abundance	1
Air Pollutants	affects cotreatment, increases abundance, increases oxidation	1
Arsenic	affects methylation	1
Atrazine	decreases expression	1
Benzo(a)pyrene	decreases expression	1
Cadmium	increases abundance, increases expression	1
Cisplatin	decreases expression	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5653006	Binding	Binding affinity to human XPO4 incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Clinical trials (associated diseases)

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