SENP5

Summary

SENP5 (SUMO specific peptidase 5, HGNC:28407) is a protein-coding gene on chromosome 3q29, encoding Sentrin-specific protease 5 (Q96HI0). Protease that catalyzes two essential functions in the SUMO pathway: processing of full-length SUMO3 to its mature form and deconjugation of SUMO2 and SUMO3 from targeted proteins.

The reversible posttranslational modification of proteins by the addition of small ubiquitin-like SUMO proteins (see SUMO1; MIM 601912) is required for numerous biologic processes. SUMO-specific proteases, such as SENP5, are responsible for the initial processing of SUMO precursors to generate a C-terminal diglycine motif required for the conjugation reaction. They also have isopeptidase activity for the removal of SUMO from high molecular mass SUMO conjugates (Di Bacco et al., 2006 [PubMed 16738315]).

Source: NCBI Gene 205564 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 99 total
• Druggable target: yes
• MANE Select transcript: NM_152699

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:28407
Approved symbol	SENP5
Name	SUMO specific peptidase 5
Location	3q29
Locus type	gene with protein product
Status	Approved
Aliases	MGC27076
Ensembl gene	ENSG00000119231
Ensembl biotype	protein_coding
OMIM	612845
Entrez	205564

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 11 protein_coding, 1 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000323460, ENST00000419026, ENST00000434433, ENST00000445299, ENST00000448068, ENST00000463245, ENST00000489744, ENST00000875329, ENST00000946893, ENST00000946894, ENST00000946895, ENST00000946896, ENST00000946897

RefSeq mRNA: 2 — MANE Select: NM_152699 NM_001308045, NM_152699

CCDS: CCDS3322, CCDS77876

Canonical transcript exons

ENST00000323460 — 10 exons

Exon	Start	End
ENSE00000805061	196899924	196900062
ENSE00001245033	196929633	196929683
ENSE00001245039	196927796	196927879
ENSE00001245051	196923414	196923551
ENSE00001245102	196930813	196934714
ENSE00001245113	196885151	196886694
ENSE00003537074	196900365	196900412
ENSE00003630594	196899666	196899771
ENSE00003635057	196903533	196903610
ENSE00003843168	196867920	196868073

Expression profiles

Bgee: expression breadth ubiquitous, 273 present calls, max score 92.96.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 39.3405 / max 789.4488, expressed in 1823 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
40753	34.0410	1823
40756	3.1146	1391
40757	2.1849	886

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
tendon of biceps brachii	UBERON:0008188	92.96	gold quality
middle temporal gyrus	UBERON:0002771	92.20	gold quality
medial globus pallidus	UBERON:0002477	91.60	gold quality
tendon	UBERON:0000043	91.43	gold quality
calcaneal tendon	UBERON:0003701	91.03	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	90.91	gold quality
sural nerve	UBERON:0015488	90.64	gold quality
adrenal tissue	UBERON:0018303	89.84	gold quality
globus pallidus	UBERON:0001875	89.30	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	89.02	gold quality
stromal cell of endometrium	CL:0002255	88.78	gold quality
Brodmann (1909) area 23	UBERON:0013554	87.80	gold quality
colonic epithelium	UBERON:0000397	87.50	gold quality
corpus callosum	UBERON:0002336	86.32	gold quality
bone marrow cell	CL:0002092	86.31	gold quality
cerebellar cortex	UBERON:0002129	85.60	gold quality
cerebellar hemisphere	UBERON:0002245	85.59	gold quality
primary visual cortex	UBERON:0002436	85.59	gold quality
cerebellum	UBERON:0002037	85.47	gold quality
testis	UBERON:0000473	85.04	gold quality
tibial nerve	UBERON:0001323	85.00	gold quality
superior frontal gyrus	UBERON:0002661	84.79	gold quality
right hemisphere of cerebellum	UBERON:0014890	84.59	gold quality
tonsil	UBERON:0002372	84.57	gold quality
ganglionic eminence	UBERON:0004023	84.38	gold quality
endometrium epithelium	UBERON:0004811	84.37	gold quality
cortical plate	UBERON:0005343	84.36	gold quality
left testis	UBERON:0004533	84.20	gold quality
entorhinal cortex	UBERON:0002728	84.11	gold quality
right testis	UBERON:0004534	84.08	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-MTAB-7303	no	185.62
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

149 targeting SENP5, 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-3646	100.00	73.56	5283
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-3134	100.00	66.43	777
HSA-MIR-3120-5P	100.00	65.56	965
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-6888-3P	99.97	65.95	1170
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-495-3P	99.96	72.81	4197
HSA-LET-7D-5P	99.96	71.76	1632

Literature-anchored findings (GeneRIF, showing 10)

• Knockdown of SENP5 resulted in increased levels of SUMO-1 and SUMO-2/3, inhibition of cell proliferation, defects in nuclear morphology, and appearance of binucleate cells, revealing an essential role for SENP5 in mitosis and/or cytokinesis. (PMID:16738315)
• altered subcellular localization of SENP5 in oral squamous cell carcinoma (OSCC) cells and the correlation between SENP5 expression and the differentiation of OSCC. (PMID:18949399)
• Nucleolar protein B23/nucleophosmin regulates the vertebrate SUMO pathway through SENP3 and SENP5 proteases. (PMID:19015314)
• Low expression of SENP5 is associated with good prognosis among breast cancer patients. (PMID:24658161)
• Mild oxidative stress stabilized the SENP5 protein in the oral squamous cell carcinoma cells, and only the combination of SENP5 silencing and H2O2 application led to mitochondria fragmentation and a significant increase in cell apoptosis. (PMID:25901414)
• Results from a study on gene expression variability markers in early-stage human embryos shows that SENP5 is a putative expression variability marker for the 3-day, 8-cell embryo stage. (PMID:26288249)
• Zinc deficiency induces abnormal development of the myocardium by promoting SENP5 overexpression. (PMID:33211757)
• SUMO proteases SENP3 and SENP5 spatiotemporally regulate the kinase activity of Aurora A. (PMID:34313310)
• SENP5 promotes homologous recombination-mediated DNA damage repair in colorectal cancer cells through H2AZ deSUMOylation. (PMID:37684630)
• Peptidylprolyl isomerase A guides SENP5/GAU1 DNA-lncRNA triplex generation for driving tumorigenesis. (PMID:39433793)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
mus_musculus	Senp5	ENSMUSG00000022772
rattus_norvegicus	Senp5l1	ENSRNOG00000029315
rattus_norvegicus	Senp5	ENSRNOG00000064973
drosophila_melanogaster	Ulp1	FBGN0027603
drosophila_melanogaster	CG32110	FBGN0052110
caenorhabditis_elegans		WBGENE00006736

Paralogs (3): SENP1 (ENSG00000079387), SENP3 (ENSG00000161956), SENP2 (ENSG00000163904)

Protein

Protein identifiers

Sentrin-specific protease 5 — Q96HI0 (reviewed: Q96HI0)

Alternative names: Sentrin/SUMO-specific protease SENP5

All UniProt accessions (4): Q96HI0, C9JHT8, H7C2F8, H7C424

UniProt curated annotations — full annotation on UniProt →

Function. Protease that catalyzes two essential functions in the SUMO pathway: processing of full-length SUMO3 to its mature form and deconjugation of SUMO2 and SUMO3 from targeted proteins. Has weak proteolytic activity against full-length SUMO1 or SUMO1 conjugates. Required for cell division.

Subunit / interactions. Interacts with CCAR2.

Subcellular location. Nucleus. Nucleolus.

Similarity. Belongs to the peptidase C48 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q96HI0-1	1	yes
Q96HI0-2	2

RefSeq proteins (2): NP_001294974, NP_689912* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR003653	Peptidase_C48_C	Domain
IPR038765	Papain-like_cys_pep_sf	Homologous_superfamily
IPR045577	SENP3_5_cons_dom	Domain

Pfam: PF02902, PF19722

Enzyme classification (BRENDA):

• EC 3.4.22.B73 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)

UniProt features (13 total): active site 3, region of interest 2, sequence conflict 2, sequence variant 2, chain 1, mutagenesis site 1, compositionally biased region 1, splice variant 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
9GNX	X-RAY DIFFRACTION	1.9
9GNV	X-RAY DIFFRACTION	2.18
9GNN	X-RAY DIFFRACTION	2.36

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96HI0-F1	56.00	0.33

Functional residue map

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

Catalytic / active sites (3): 646; 663; 713

Mutagenesis-validated functional residues (1):

Position	Phenotype
713	abolishes enzymatic activity.

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-3065679	SUMO is proteolytically processed
R-HSA-2990846	SUMOylation
R-HSA-3215018	Processing and activation of SUMO
R-HSA-392499	Metabolism of proteins
R-HSA-597592	Post-translational protein modification

MSigDB gene sets: 123 (showing top): RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, ATGCAGT_MIR217, GOBP_PROTEIN_MODIFICATION_BY_SMALL_PROTEIN_REMOVAL, GOBP_PEPTIDYL_LYSINE_MODIFICATION, CAGCAGG_MIR370, GOMF_CYSTEINE_TYPE_PEPTIDASE_ACTIVITY, GOBP_PROTEIN_SUMOYLATION, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, SLEBOS_HEAD_AND_NECK_CANCER_WITH_HPV_UP, GOCC_POSTSYNAPSE, GOBP_CELL_DIVISION, GOCC_SYNAPSE, GOBP_PROTEOLYSIS, GOCC_PRESYNAPSE, GOCC_NUCLEOLUS

GO Biological Process (4): proteolysis (GO:0006508), protein sumoylation (GO:0016925), protein desumoylation (GO:0016926), cell division (GO:0051301)

GO Molecular Function (6): deSUMOylase activity (GO:0016929), SUMO-specific endopeptidase activity (GO:0070139), protein binding (GO:0005515), peptidase activity (GO:0008233), cysteine-type peptidase activity (GO:0008234), hydrolase activity (GO:0016787)

GO Cellular Component (5): nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), presynaptic cytosol (GO:0099523), postsynaptic cytosol (GO:0099524)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Processing and activation of SUMO	1
Post-translational protein modification	1
SUMOylation	1
Metabolism of proteins	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
peptidyl-lysine modification	2
nuclear lumen	2
cytosol	2
protein metabolic process	1
protein modification by small protein conjugation	1
protein modification by small protein removal	1
cellular process	1
cysteine-type peptidase activity	1
ubiquitin-like protein peptidase activity	1
ubiquitin-like protein-specific endopeptidase activity	1
binding	1
hydrolase activity	1
catalytic activity, acting on a protein	1
peptidase activity	1
catalytic activity	1
intracellular membrane-bounded organelle	1
cellular anatomical structure	1
intracellular membraneless organelle	1
presynapse	1
postsynapse	1

Protein interactions and networks

STRING

1066 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SENP5	SUMO1	P55856	900
SENP5	SUMO2	P55855	886
SENP5	GNL2	Q13823	850
SENP5	RPL37A	P12751	841
SENP5	NPM1	P06748	807
SENP5	RANGAP1	P46060	747
SENP5	UBE2I	P50550	744
SENP5	SAE1	Q9UBE0	739
SENP5	DESI1	Q6ICB0	714
SENP5	USPL1	Q5W0Q7	693
SENP5	UBA2	Q9UBT2	686
SENP5	DESI2	Q9BSY9	667
SENP5	NEDD8	Q15843	653
SENP5	PIAS4	Q8N2W9	651
SENP5	WDR53	Q7Z5U6	627

IntAct

76 interactions, top by confidence:

A	B	Type	Score
MAPK8IP1	MAPK8	psi-mi:“MI:0914”(association)	0.770
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
MIS18A	DCTN6	psi-mi:“MI:0914”(association)	0.640
MAPK8IP1	HOXC8	psi-mi:“MI:0914”(association)	0.530
DKK3	NME4	psi-mi:“MI:0914”(association)	0.530
SENP5	ESR1	psi-mi:“MI:0407”(direct interaction)	0.530
SENP5	ESR1	psi-mi:“MI:0915”(physical association)	0.530
CASQ2	PES1	psi-mi:“MI:0914”(association)	0.530
PSME1	POLR3A	psi-mi:“MI:0914”(association)	0.530
ZNRD2	MYO9A	psi-mi:“MI:0914”(association)	0.530
TUBA4A	PLD2	psi-mi:“MI:0914”(association)	0.530
ZNRD2	CCDC85C	psi-mi:“MI:0914”(association)	0.530
SENP5	H2BC9	psi-mi:“MI:0915”(physical association)	0.400
SENP5	OCIAD2	psi-mi:“MI:0915”(physical association)	0.400
	GNAT3	psi-mi:“MI:0915”(physical association)	0.400
NKX3-1	NR3C1	psi-mi:“MI:0914”(association)	0.350
ZNRD2	KRBA1	psi-mi:“MI:0914”(association)	0.350
CASQ2	TSNARE1	psi-mi:“MI:0914”(association)	0.350
CAMK2D	SETD1A	psi-mi:“MI:0914”(association)	0.350
NPM1	NVL	psi-mi:“MI:0914”(association)	0.350
LOXL3	MSI1	psi-mi:“MI:0914”(association)	0.350
ZCCHC7	ZKSCAN1	psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350
NPM1	RPS3A	psi-mi:“MI:0914”(association)	0.350
NPM3	RPS3A	psi-mi:“MI:0914”(association)	0.350
PIPSL	C1orf226	psi-mi:“MI:0914”(association)	0.350
S100B	PLEKHG3	psi-mi:“MI:0914”(association)	0.350
S100A2	PLEKHG3	psi-mi:“MI:0914”(association)	0.350
FTL	SH3PXD2B	psi-mi:“MI:0914”(association)	0.350

BioGRID (78): SUMO3 (Biochemical Activity), SUMO2 (Biochemical Activity), SUMO3 (Biochemical Activity), RABGAP1 (Biochemical Activity), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS), SENP5 (Affinity Capture-MS)

ESM2 similar proteins: A0A1D5NS60, A0JMD2, A1YFX5, A2AWL7, A2RUR9, A2T7G6, A5WWA0, A6NJL1, A6NKB5, A7KBS4, D2HQI1, F1M5M3, F1MJR8, O60284, P0CG00, P22227, P52551, P98182, Q0VCB0, Q32MG2, Q3MJ40, Q3URS2, Q4V7J0, Q4V8E9, Q5DU28, Q5DW34, Q5EAC5, Q5EXX3, Q64ET8, Q6AXV6, Q6AXY9, Q80TY4, Q80VJ6, Q86VK4, Q8BGV5, Q8BKX7, Q8C6P8, Q8IWB6, Q8IWI9, Q8NAM6

Diamond homologs: A7MBJ2, D3ZF42, O42957, O65278, P59110, Q02724, Q09353, Q5R7K7, Q5RBB1, Q6NXL6, Q6P7W0, Q8BUH8, Q8GYL3, Q8WP32, Q91ZX6, Q94F30, Q96HI0, Q9BQF6, Q9EP97, Q9EQE1, Q9GZR1, Q9H4L4, Q9HC62, Q9P0U3, Q0WKV8, Q8RWN0, O13612, Q2PS26, Q8L7S0

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 102 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.

GO biological processes:

GO term	Partners	Fold	FDR
ribosomal large subunit biogenesis	5	24.6×	1e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	78
Likely benign	2
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

1442 predictions. Top by Δscore:

Variant	Effect	Δscore
3:196868069:AGCAG:A	donor_loss	1.0000
3:196868072:AGG:A	donor_loss	1.0000
3:196899663:A:AG	acceptor_gain	1.0000
3:196899663:AAG:A	acceptor_gain	1.0000
3:196899664:A:G	acceptor_gain	1.0000
3:196899664:AG:A	acceptor_gain	1.0000
3:196899665:G:GG	acceptor_gain	1.0000
3:196899665:GG:G	acceptor_gain	1.0000
3:196899665:GGA:G	acceptor_gain	1.0000
3:196899743:G:GT	donor_gain	1.0000
3:196899755:G:GT	donor_gain	1.0000
3:196899768:A:AG	donor_gain	1.0000
3:196899792:T:G	donor_gain	1.0000
3:196899921:CAG:C	acceptor_loss	1.0000
3:196899922:A:AC	acceptor_loss	1.0000
3:196899922:A:AG	acceptor_gain	1.0000
3:196899923:G:GG	acceptor_gain	1.0000
3:196899923:GA:G	acceptor_gain	1.0000
3:196899923:GAA:G	acceptor_gain	1.0000
3:196899923:GAAA:G	acceptor_gain	1.0000
3:196899923:GAAAA:G	acceptor_gain	1.0000
3:196900063:G:C	donor_loss	1.0000
3:196900063:G:GG	donor_gain	1.0000
3:196900359:TTATA:T	acceptor_loss	1.0000
3:196900362:TAGGT:T	acceptor_loss	1.0000
3:196900364:G:A	acceptor_loss	1.0000
3:196900413:G:GG	donor_gain	1.0000
3:196903527:TTCTA:T	acceptor_loss	1.0000
3:196903528:TCTA:T	acceptor_loss	1.0000
3:196903529:CTA:C	acceptor_loss	1.0000

AlphaMissense

5059 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:196900048:T:A	W582R	1.000
3:196900048:T:C	W582R	1.000
3:196900057:G:C	D585H	1.000
3:196900058:A:C	D585A	1.000
3:196900058:A:G	D585G	1.000
3:196900058:A:T	D585V	1.000
3:196900373:T:A	N589K	1.000
3:196900373:T:G	N589K	1.000
3:196900380:G:C	G592R	1.000
3:196900381:G:A	G592D	1.000
3:196900387:T:C	L594P	1.000
3:196903547:C:A	N607K	1.000
3:196903547:C:G	N607K	1.000
3:196903548:A:C	S608R	1.000
3:196903550:C:A	S608R	1.000
3:196903550:C:G	S608R	1.000
3:196903551:T:C	F609L	1.000
3:196903553:T:A	F609L	1.000
3:196903553:T:G	F609L	1.000
3:196903567:T:C	L614P	1.000
3:196903597:G:C	R624T	1.000
3:196903598:A:C	R624S	1.000
3:196903598:A:T	R624S	1.000
3:196903599:T:A	W625R	1.000
3:196903599:T:C	W625R	1.000
3:196903600:G:C	W625S	1.000
3:196903601:G:C	W625C	1.000
3:196903601:G:T	W625C	1.000
3:196923439:T:C	L637P	1.000
3:196923442:T:C	L638S	1.000

dbSNP variants (sampled 300 via entrez): RS1000014043 (3:196907401 A>G), RS1000045566 (3:196876225 A>G), RS1000050242 (3:196921583 T>G), RS1000085752 (3:196907765 A>G), RS1000153976 (3:196886020 G>A), RS1000171524 (3:196870698 A>G), RS1000253773 (3:196918067 T>C), RS1000271766 (3:196881889 A>G), RS1000285521 (3:196879044 C>T), RS1000303829 (3:196867928 C>G), RS1000332854 (3:196873274 T>C), RS1000403927 (3:196900317 A>C,G), RS1000441145 (3:196888572 A>C), RS1000455532 (3:196930065 G>A,T), RS1000461706 (3:196873384 T>A)

Disease associations

OMIM: gene MIM:612845 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST003542_204	Night sleep phenotypes	9.000000e-06
GCST008176_5	Gestational age at birth (child effect)	7.000000e-06
GCST010725_2	Malaria	8.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0005112	gestational age

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4802012 (SINGLE PROTEIN)

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

ChEMBL bioactivities

11 potent at pChembl≥5 of 52 total, top 11 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.62	IC50	2400	nM	CHEMBL4791433
5.52	IC50	3000	nM	CHEMBL4780770
5.50	IC50	3200	nM	CHEMBL4778045
5.34	IC50	4600	nM	CHEMBL4792569
5.27	IC50	5400	nM	CHEMBL4796113
5.24	IC50	5700	nM	CHEMBL4783695
5.20	IC50	6300	nM	CHEMBL4780586
5.15	IC50	7100	nM	CHEMBL4785280
5.14	IC50	7200	nM	CHEMBL4780306
5.08	IC50	8400	nM	CHEMBL4800446
5.06	IC50	8800	nM	CHEMBL4783089

PubChem BioAssay actives

11 with measured affinity, of 53 total; 11 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
5-(dimethylamino)-3-phenylmethoxy-N-[[3-(thiophene-2-carbonylamino)phenyl]methyl]-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	2.4000	uM
5-(ethylamino)-3-phenylmethoxy-N-[[3-(thiophene-2-carbonylamino)phenyl]methyl]-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	3.0000	uM
N-[[3-(1-benzothiophene-2-carbonylamino)phenyl]methyl]-3-phenylmethoxy-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	3.2000	uM
5-(methylamino)-3-phenylmethoxy-N-[[3-(thiophene-2-carbonylamino)phenyl]methyl]-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	4.6000	uM
N-[(3-benzamidophenyl)methyl]-3-phenylmethoxy-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	5.4000	uM
5-[(2-chloroacetyl)amino]-3-phenylmethoxy-N-[[3-(thiophene-2-carbonylamino)phenyl]methyl]-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	5.7000	uM
5-amino-3-phenylmethoxy-N-[[3-(thiophene-2-carbonylamino)phenyl]methyl]-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	6.3000	uM
N-[[3-(naphthalene-2-carbonylamino)phenyl]methyl]-3-phenylmethoxy-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	7.1000	uM
N-[[3-[(2-methoxybenzoyl)amino]phenyl]methyl]-3-phenylmethoxy-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	7.2000	uM
N-[[3-[(3,4-dichlorobenzoyl)amino]phenyl]methyl]-3-phenylmethoxy-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	8.4000	uM
N-[[3-(butanoylamino)phenyl]methyl]-3-phenylmethoxy-1-benzothiophene-2-carboxamide	1741435: Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining based SDS-PAGE analysis	ic50	8.8000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation	2
Aflatoxin B1	increases methylation	2
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
trichostatin A	affects expression	1
sodium arsenite	increases expression	1
benzo(e)pyrene	increases methylation	1
aflatoxin B2	decreases methylation	1
(4-amino-1,4-dihydro-3-(2-pyridyl)-5-thioxo-1,2,4-triazole)copper(II)	increases expression	1
PCI 5002	affects cotreatment, increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Sunitinib	increases expression	1
Caffeine	increases phosphorylation	1
Doxorubicin	decreases expression	1
Estradiol	increases expression	1
Methapyrilene	increases methylation	1
Methyl Methanesulfonate	decreases expression	1
Phenobarbital	affects expression	1
Plant Extracts	affects cotreatment, increases expression	1
Plant Oils	increases expression	1
Smoke	decreases expression	1
Dronabinol	decreases expression	1
Thiram	increases expression	1
Tretinoin	decreases expression	1
Valproic Acid	increases expression	1
Zinc	affects cotreatment, increases expression	1
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	increases expression	1
Oxyquinoline	decreases expression	1
Cyclosporine	increases expression	1
Copper Sulfate	increases 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
CHEMBL4772835	Binding	Inhibition of recombinant human SNEP5 (567 to 755 residues) expressed in Escherichia coli (DE3) cells using RanGAP-SUMO2 substrate preincubated for 10 mins followed by substrate addition and measured after 25 min by Coomassie blue staining	Benzothiophene-2-carboxamide derivatives as SENPs inhibitors with selectivity within SENPs family. — Eur J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B2F0	Abcam HeLa SENP5 KO	Cancer cell line	Female
CVCL_TK61	HAP1 SENP5 (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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