TSN

Summary

TSN (translin, HGNC:12379) is a protein-coding gene on chromosome 2q14.3, encoding Translin (Q15631). DNA-binding protein that specifically recognizes consensus sequences at the breakpoint junctions in chromosomal translocations, mostly involving immunoglobulin (Ig)/T-cell receptor gene segments.

This gene encodes a DNA-binding protein which specifically recognizes conserved target sequences at the breakpoint junction of chromosomal translocations. Translin polypeptides form a multimeric structure that is responsible for its DNA-binding activity. Recombination-associated motifs and translin-binding sites are present at recombination hotspots and may serve as indicators of breakpoints in genes which are fused by translocations. These binding activities may play a crucial role in chromosomal translocation in lymphoid neoplasms. This protein encoded by this gene, when complexed with translin-associated protein X, also forms a Mg ion-dependent endoribonuclease that promotes RNA-induced silencing complex (RISC) activation. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 7247 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 18 total
• Druggable target: yes
• MANE Select transcript: NM_004622

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:12379
Approved symbol	TSN
Name	translin
Location	2q14.3
Locus type	gene with protein product
Status	Approved
Aliases	TRSLN, BCLF-1, REHF-1
Ensembl gene	ENSG00000211460
Ensembl biotype	protein_coding
OMIM	600575
Entrez	7247

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 8 protein_coding, 4 nonsense_mediated_decay, 2 retained_intron, 2 protein_coding_CDS_not_defined

ENST00000389682, ENST00000409193, ENST00000455432, ENST00000467324, ENST00000478165, ENST00000481818, ENST00000483698, ENST00000490104, ENST00000490717, ENST00000495112, ENST00000498545, ENST00000536142, ENST00000898259, ENST00000898260, ENST00000898261, ENST00000920039

RefSeq mRNA: 2 — MANE Select: NM_004622 NM_001261401, NM_004622

CCDS: CCDS33284, CCDS58723

Canonical transcript exons

ENST00000389682 — 6 exons

Exon	Start	End
ENSE00001506648	121765134	121767853
ENSE00001506653	121755651	121755845
ENSE00003597672	121763005	121763084
ENSE00003625381	121757240	121757333
ENSE00003682442	121758710	121758806
ENSE00003690825	121761409	121761524

Expression profiles

Bgee: expression breadth ubiquitous, 295 present calls, max score 97.29.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 37.5187 / max 531.8351, expressed in 1823 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
22348	37.2803	1823
22347	0.2270	99
22350	0.0114	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	97.29	gold quality
secondary oocyte	CL:0000655	96.53	gold quality
skin of hip	UBERON:0001554	96.34	gold quality
cranial nerve II	UBERON:0000941	96.09	gold quality
upper leg skin	UBERON:0004262	95.89	gold quality
ganglionic eminence	UBERON:0004023	95.57	gold quality
embryo	UBERON:0000922	95.28	gold quality
oocyte	CL:0000023	95.01	gold quality
diaphragm	UBERON:0001103	95.00	gold quality
germinal epithelium of ovary	UBERON:0001304	94.91	gold quality
islet of Langerhans	UBERON:0000006	94.90	gold quality
superficial temporal artery	UBERON:0001614	94.71	gold quality
hair follicle	UBERON:0002073	94.61	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	94.57	gold quality
ventricular zone	UBERON:0003053	94.42	gold quality
cortical plate	UBERON:0005343	94.19	gold quality
penis	UBERON:0000989	94.07	gold quality
endometrium	UBERON:0001295	94.00	gold quality
adult organism	UBERON:0007023	93.89	gold quality
cauda epididymis	UBERON:0004360	93.80	gold quality
medial globus pallidus	UBERON:0002477	93.79	gold quality
tibia	UBERON:0000979	93.77	gold quality
calcaneal tendon	UBERON:0003701	93.77	gold quality
palpebral conjunctiva	UBERON:0001812	93.65	gold quality
caput epididymis	UBERON:0004358	93.64	gold quality
globus pallidus	UBERON:0001875	93.57	gold quality
corpus epididymis	UBERON:0004359	93.56	gold quality
middle temporal gyrus	UBERON:0002771	93.51	gold quality
mucosa of sigmoid colon	UBERON:0004993	93.51	gold quality
bone marrow	UBERON:0002371	93.48	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-CURD-114	yes	8.08
E-ANND-3	yes	6.98

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

83 targeting TSN, 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-3613-3P	100.00	76.36	7965
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-3658	99.96	73.87	4379
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-144-3P	99.94	73.98	2698
HSA-MIR-4760-3P	99.93	70.50	2385
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-3529-3P	99.90	73.55	3045
HSA-MIR-137-3P	99.87	74.74	2401
HSA-MIR-221-5P	99.86	65.45	1052
HSA-MIR-8073	99.86	65.21	1118
HSA-MIR-548AR-3P	99.85	71.26	3889
HSA-MIR-4799-5P	99.82	70.60	2663
HSA-MIR-4420	99.82	70.08	1624
HSA-MIR-548AZ-3P	99.82	70.56	3549
HSA-MIR-548BC	99.82	70.61	3524
HSA-MIR-548E-3P	99.82	70.59	3514

Literature-anchored findings (GeneRIF, showing 22)

• Sedimentation equilibrium studies using fluorescein-labeled single-stranded DNA support a model in which translin forms an annular structure of eight subunits, an oblate ellipsoid that binds single-stranded DNA at chromosomal breakpoints. (PMID:11705401)
• study of reactivity of two -SH groups and stidu of proximity of Cys-225 residues (PMID:11876655)
• At high enough concentrations, translin binds duplex DNA by selectively loading from the free ends, which apparently results in clamping of strands at the duplex ends. (PMID:12484770)
• The core protein of HCV can interact with translin protein. This can partly explain the molecular mechanism for hepatocellular carcinoma and lymphoma caused by HCV (PMID:12532453)
• TB-RBP post-transcriptionally stabilizes TRAX and both proteins are needed for normal cell proliferation (PMID:14711818)
• structure of human translin at 2.2 A resolution is reported in space group C222; translin forms a tetramer; this suggests that the multimerization of translin is flexible; the flexibility may be related to the binding to DNA/RNA (PMID:15039555)
• Results suggest that translin might be involved in the control of recombination at d(GT)n.d(AC)n microsatellites and in telomere maintenance. (PMID:15544804)
• Translin “chaperones” Trax and forms heteromeric complex that is DNA binding competent (PMID:15919079)
• Results describe a circular dichroism analysis of complexes formed between human translin and the microsatellite and telomeric oligodeoxynucleotides d(GT)(12) and d(TTAGGG)(5). (PMID:16218753)
• Human translin exhibits a stable octameric state and binds ssDNA/RNA/dsDNA targets, all of which get attenuated when GTP is added (PMID:16411762)
• Findings implicate abnormal dendritic trafficking of BDNF mRNA in the pathophysiology of neuropsychiatric disorders linked to the translin G196A mutation. (PMID:19805324)
• C3PO endonuclease is an asymmetric octamer barrel consisting of six translin and two TRAX subunits which activates RISC by degrading the Ago2-nicked passenger strand of siRNA. (PMID:21552258)
• Translin B3 motif, corresponding to TRAX B3 residues, contributes towards its DNA binding activity. (PMID:22427937)
• The data demonstrates that the configuration of translin and translin-RNA complexes in solution is a dimer of tetramers, which undergoes conformational transitions. (PMID:23980029)
• The selectivity of PLCbeta toward certain genes lies in the rate at which the RNA is hydrolyzed by C3PO. (PMID:24338081)
• this study argues against a mechanism by which translin octamers may “dissociate and reassemble” upon RNA binding and report a novel “open”-barrel structure of human translin revealing a feasible DNA/RNA entryway into the cavity. (PMID:25433126)
• These findings indicate that miRNA depletion in dicer deficiency is due to the combined loss of miRNA-generating activity and catabolic function of TN/TX. (PMID:25457613)
• Translin and Trax control telomere-associated transcript levels in human cells in a telomere-specific fashion. (PMID:27183912)
• results indicate that UPF1 can dissociate miRNAs from their mRNA targets, making the miRNAs susceptible to Tudor-staphylococcal/micrococcal-like nuclease (TSN)-mediated miRNA decay. (PMID:28827400)
• Role of amino acid residues important for nucleic acid binding in human Translin (PMID:31442605)
• Functional characterization of testis-brain RNA-binding protein, TB-RBP/Translin, in translational regulation. (PMID:33268667)
• Biochemical characterization of clinically relevant mutations of human Translin. (PMID:36098897)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	tsn	ENSDARG00000041830
mus_musculus	Tsn	ENSMUSG00000026374
rattus_norvegicus	Tsn	ENSRNOG00000002319
drosophila_melanogaster	trsn	FBGN0033528

Paralogs (1): TSNAX (ENSG00000116918)

Protein

Protein identifiers

Translin — Q15631 (reviewed: Q15631)

Alternative names: Component 3 of promoter of RISC

All UniProt accessions (5): A0A0J9YVW2, A0A0J9YX41, E9PGT1, Q15631, H7C1D4

UniProt curated annotations — full annotation on UniProt →

Function. DNA-binding protein that specifically recognizes consensus sequences at the breakpoint junctions in chromosomal translocations, mostly involving immunoglobulin (Ig)/T-cell receptor gene segments. Seems to recognize single-stranded DNA ends generated by staggered breaks occurring at recombination hot spots. Exhibits both single-stranded and double-stranded endoribonuclease activity. May act as an activator of RNA-induced silencing complex (RISC) by facilitating endonucleolytic cleavage of the siRNA passenger strand.

Subunit / interactions. Ring-shaped heterooctamer of six TSN and two TSNAX subunits, DNA/RNA binding occurs inside the ring.

Subcellular location. Cytoplasm. Nucleus.

Similarity. Belongs to the translin family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q15631-1	1	yes
Q15631-2	2

RefSeq proteins (2): NP_001248330, NP_004613* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002848	Translin_fam	Family
IPR016068	Translin_N	Homologous_superfamily
IPR016069	Translin_C	Homologous_superfamily
IPR033956	Translin	Family
IPR036081	Translin_sf	Homologous_superfamily

Pfam: PF01997

UniProt features (23 total): helix 12, modified residue 3, region of interest 2, strand 2, splice variant 2, chain 1, turn 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
1J1J	X-RAY DIFFRACTION	2.2
3QB5	X-RAY DIFFRACTION	2.95
3PJA	X-RAY DIFFRACTION	3
4WYV	X-RAY DIFFRACTION	3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q15631-F1	92.91	0.85

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 (3): 187, 190, 199

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-426486	Small interfering RNA (siRNA) biogenesis

MSigDB gene sets: 165 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_DN, GOMF_ENDONUCLEASE_ACTIVITY, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GOMF_NUCLEASE_ACTIVITY, GCGCTTT_MIR518B_MIR518C_MIR518D, PATIL_LIVER_CANCER, SHEDDEN_LUNG_CANCER_GOOD_SURVIVAL_A5, WEI_MYCN_TARGETS_WITH_E_BOX, GOBP_POST_TRANSCRIPTIONAL_REGULATION_OF_GENE_EXPRESSION, FISCHER_G2_M_CELL_CYCLE, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN, GARY_CD5_TARGETS_DN, PARK_HSC_AND_MULTIPOTENT_PROGENITORS, CAIRO_HEPATOBLASTOMA_UP, TIEN_INTESTINE_PROBIOTICS_24HR_UP

GO Biological Process (3): siRNA processing (GO:0030422), regulatory ncRNA-mediated post-transcriptional gene silencing (GO:0035194), RNA metabolic process (GO:0016070)

GO Molecular Function (12): DNA binding (GO:0003677), single-stranded DNA binding (GO:0003697), RNA binding (GO:0003723), mRNA binding (GO:0003729), endonuclease activity (GO:0004519), hydrolase activity (GO:0016787), identical protein binding (GO:0042802), sequence-specific DNA binding (GO:0043565), nucleic acid binding (GO:0003676), nuclease activity (GO:0004518), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (7): male germ cell nucleus (GO:0001673), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), endoplasmic reticulum (GO:0005783), cytosol (GO:0005829), endoribonuclease complex (GO:1902555)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Gene Silencing by RNA	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
nucleic acid binding	2
DNA binding	2
binding	2
intracellular membrane-bounded organelle	2
cytoplasm	2
regulatory ncRNA processing	1
post-transcriptional gene silencing	1
regulatory ncRNA-mediated gene silencing	1
nucleic acid metabolic process	1
RNA binding	1
nuclease activity	1
catalytic activity	1
protein binding	1
catalytic activity, acting on a nucleic acid	1
cation binding	1
germ cell nucleus	1
nuclear lumen	1
intracellular anatomical structure	1
endomembrane system	1
endonuclease complex	1

Protein interactions and networks

STRING

1696 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TSN	TSNAX	Q99598	992
TSN	ZBTB18	Q99592	834
TSN	AKAP4	Q5JQC9	801
TSN	DICER1	Q9UPY3	765
TSN	AGO2	Q9UKV8	738
TSN	SPANXA1	Q9NS26	711
TSN	PDIA3	P30101	700
TSN	CALR	P27797	572
TSN	KIF17	Q9P2E2	542
TSN	FMR1	Q06787	540
TSN	C1D	Q13901	506
TSN	B2M	P01884	467
TSN	RBM44	Q6ZP01	462
TSN	SND1	Q7KZF4	453
TSN	PRM2	P04554	432

IntAct

92 interactions, top by confidence:

A	B	Type	Score
TSN	TSNAX	psi-mi:“MI:0915”(physical association)	0.920
TSN	TSNAX	psi-mi:“MI:0407”(direct interaction)	0.920
TSNAX	TSN	psi-mi:“MI:0914”(association)	0.920
TSN	TSN	psi-mi:“MI:0915”(physical association)	0.670
TSN	NTAQ1	psi-mi:“MI:0915”(physical association)	0.560
MORF4L2	TSN	psi-mi:“MI:0915”(physical association)	0.560
TSN	DVL3	psi-mi:“MI:0915”(physical association)	0.560
TSN	LNX1	psi-mi:“MI:0915”(physical association)	0.560
TSN	PICK1	psi-mi:“MI:0915”(physical association)	0.560
TSN	GORASP2	psi-mi:“MI:0915”(physical association)	0.560
UBE2K	TSN	psi-mi:“MI:0915”(physical association)	0.560
SDCBP	TSN	psi-mi:“MI:0915”(physical association)	0.560
TSN	UBE2I	psi-mi:“MI:0915”(physical association)	0.560
STRAP	CDK2AP1	psi-mi:“MI:0914”(association)	0.530
TSN	GIT2	psi-mi:“MI:0915”(physical association)	0.510
GIT2	TSN	psi-mi:“MI:0915”(physical association)	0.510
TSN	E2	psi-mi:“MI:0915”(physical association)	0.370
TSN	FXR1	psi-mi:“MI:0915”(physical association)	0.370
TSN	SIN3A	psi-mi:“MI:0915”(physical association)	0.370
TSNAX		psi-mi:“MI:0914”(association)	0.350
AGO2	TSN	psi-mi:“MI:0914”(association)	0.350
PRNP	WDR91	psi-mi:“MI:0914”(association)	0.350

BioGRID (140): TSN (Affinity Capture-MS), TSN (Affinity Capture-MS), TSN (Co-fractionation), TSN (Co-fractionation), TSN (Co-fractionation), TSNAX (Co-fractionation), TSN (Affinity Capture-MS), TSN (Affinity Capture-MS), TSN (Affinity Capture-MS), TSN (Affinity Capture-MS), TSN (Proximity Label-MS), TSN (Affinity Capture-MS), TSN (Affinity Capture-MS), TSN (Affinity Capture-MS), TSN (Affinity Capture-RNA)

ESM2 similar proteins: A0MT11, A1Z3X3, A2AGL3, A4FUD6, B0LPN4, E9PZQ0, F1LMY4, P16960, P21817, P48553, P59016, P97891, Q08DM8, Q15413, Q15631, Q2HJ18, Q2KJA6, Q4R6R4, Q58EN8, Q5E9L7, Q5R7P2, Q5RCC1, Q5ZJZ6, Q5ZKK2, Q62348, Q63616, Q6GNI4, Q6NRC7, Q6P1I3, Q6R327, Q7Z3V4, Q7ZUV0, Q80YV4, Q8BHL5, Q8C8N2, Q8IWV8, Q8K114, Q8K2G4, Q8VIJ8, Q91W86

Diamond homologs: P79769, P97891, Q08DM8, Q15631, Q5R7P2, Q62348, Q9P7V3

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	13
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

729 predictions. Top by Δscore:

Variant	Effect	Δscore
2:121757315:GGTGC:G	donor_gain	1.0000
2:121757329:GGACA:G	donor_gain	1.0000
2:121757330:GACA:G	donor_gain	1.0000
2:121757330:GACAG:G	donor_gain	1.0000
2:121757334:G:GG	donor_gain	1.0000
2:121758701:T:TA	acceptor_gain	1.0000
2:121758703:T:TA	acceptor_gain	1.0000
2:121758706:CTAGT:C	acceptor_loss	1.0000
2:121758708:A:AG	acceptor_gain	1.0000
2:121758708:AGT:A	acceptor_loss	1.0000
2:121758709:G:GA	acceptor_gain	1.0000
2:121758803:ACAG:A	donor_loss	1.0000
2:121758804:CAG:C	donor_loss	1.0000
2:121758805:AGGT:A	donor_loss	1.0000
2:121758806:GG:G	donor_loss	1.0000
2:121758807:G:T	donor_loss	1.0000
2:121758807:GTTT:G	donor_gain	1.0000
2:121761406:CAGA:C	acceptor_loss	1.0000
2:121761407:A:AG	acceptor_gain	1.0000
2:121761408:G:GG	acceptor_gain	1.0000
2:121761408:G:T	acceptor_loss	1.0000
2:121761520:TGGCA:T	donor_gain	1.0000
2:121761521:GGCA:G	donor_gain	1.0000
2:121761521:GGCAG:G	donor_gain	1.0000
2:121761522:GCA:G	donor_gain	1.0000
2:121761522:GCAG:G	donor_gain	1.0000
2:121761523:CA:C	donor_gain	1.0000
2:121761525:G:GG	donor_gain	1.0000
2:121762993:T:G	acceptor_gain	1.0000
2:121763003:A:AC	acceptor_loss	1.0000

AlphaMissense

1473 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
2:121757309:C:G	H46D	1.000
2:121761410:T:C	F87L	1.000
2:121761412:T:A	F87L	1.000
2:121761412:T:G	F87L	1.000
2:121761422:T:A	W91R	1.000
2:121761422:T:C	W91R	1.000
2:121763053:T:C	L141P	1.000
2:121763058:G:A	G143R	1.000
2:121763058:G:C	G143R	1.000
2:121763059:G:A	G143E	1.000
2:121763083:T:C	L151P	1.000
2:121765138:G:C	R153T	1.000
2:121765138:G:T	R153M	1.000
2:121765139:G:C	R153S	1.000
2:121765139:G:T	R153S	1.000
2:121765141:T:C	L154P	1.000
2:121765147:T:A	V156D	1.000
2:121765156:T:A	V159E	1.000
2:121765210:T:C	L177P	1.000
2:121765221:T:C	F181L	1.000
2:121765222:T:C	F181S	1.000
2:121765223:T:A	F181L	1.000
2:121765223:T:G	F181L	1.000
2:121765225:G:C	R182P	1.000
2:121765231:T:A	L184H	1.000
2:121765231:T:C	L184P	1.000
2:121765237:T:C	L186P	1.000
2:121765239:A:G	K187E	1.000
2:121765240:A:T	K187I	1.000
2:121765241:A:C	K187N	1.000

dbSNP variants (sampled 300 via entrez): RS1000298419 (2:121756016 C>T), RS1000351325 (2:121762709 C>G,T), RS1000777299 (2:121767366 C>G,T), RS1001243966 (2:121761828 T>A,C), RS1001248236 (2:121760826 A>G), RS1001614987 (2:121757170 A>G), RS1001827052 (2:121755466 C>A,T), RS1001901616 (2:121755678 G>A,C,T), RS1002285122 (2:121766881 G>C), RS1002504422 (2:121754299 A>G,T), RS1002634182 (2:121760491 C>T), RS1003187751 (2:121765112 T>C), RS1003239255 (2:121753987 A>G,T), RS1003252886 (2:121758867 T>C), RS1003287437 (2:121758839 TTAAG>T)

Disease associations

OMIM: gene MIM:600575 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5725062 (SINGLE PROTEIN)

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 4 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	Kd	1.007	nM	CHEMBL5653589
9.00	ED50	1.007	nM	CHEMBL5653589

PubChem BioAssay actives

1 with measured affinity, of 10 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-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149664: Binding affinity to human TSN incubated for 45 mins by Kinobead based pull down assay	kd	0.0010	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression	2
sodium arsenite	increases expression, affects cotreatment, increases abundance	2
Resveratrol	affects cotreatment, increases expression, decreases expression	2
bisphenol F	increases expression	1
dicrotophos	decreases expression	1
2,4,6-tribromophenol	decreases expression	1
triphenyl phosphate	affects expression	1
sodium arsenate	decreases expression	1
decabromobiphenyl ether	decreases expression	1
tetrabromobisphenol A	decreases expression	1
manganese chloride	affects cotreatment, increases abundance, increases expression	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	affects cotreatment, increases expression	1
CGP 52608	affects binding, increases reaction	1
abrine	decreases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	increases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
bisphenol AF	increases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	affects expression, increases abundance	1
Arsenic	affects cotreatment, increases abundance, increases expression	1
Benzo(a)pyrene	increases expression	1
Coumestrol	affects cotreatment, increases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Ivermectin	decreases expression	1
Manganese	affects cotreatment, increases abundance, increases expression	1
Ozone	increases abundance, affects expression	1
Plant Extracts	affects cotreatment, increases expression	1
Ribonucleotides	affects binding	1
Tobacco Smoke Pollution	increases expression	1

ChEMBL screening assays

7 unique, capped per target: 7 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5652706	Binding	Binding affinity to human TSN 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.