SRPK2

Summary

SRPK2 (SRSF protein kinase 2, HGNC:11306) is a protein-coding gene on chromosome 7q22.3, encoding SRSF protein kinase 2 (P78362). Serine/arginine-rich protein-specific kinase which specifically phosphorylates its substrates at serine residues located in regions rich in arginine/serine dipeptides, known as RS domains and is involved in the phosphorylation of SR splicing factors and the regulation of splicin….

Enables ATP binding activity; magnesium ion binding activity; and protein serine/threonine kinase activity. Involved in several processes, including R-loop processing; peptidyl-serine phosphorylation; and regulation of viral genome replication. Located in chromatin; cytosol; and nuclear lumen.

Source: NCBI Gene 6733 — RefSeq curated summary.

At a glance

• GWAS associations: 21
• Clinical variants (ClinVar): 93 total — 1 pathogenic, 1 likely-pathogenic
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_182692

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11306
Approved symbol	SRPK2
Name	SRSF protein kinase 2
Location	7q22.3
Locus type	gene with protein product
Status	Approved
Aliases	SFRSK2
Ensembl gene	ENSG00000135250
Ensembl biotype	protein_coding
OMIM	602980
Entrez	6733

Gene structure

Transcript identifiers

Ensembl transcripts: 19 — 11 protein_coding, 3 protein_coding_CDS_not_defined, 3 nonsense_mediated_decay, 2 retained_intron

ENST00000357311, ENST00000393651, ENST00000460391, ENST00000462282, ENST00000465072, ENST00000465112, ENST00000466917, ENST00000474770, ENST00000476117, ENST00000477925, ENST00000482862, ENST00000482897, ENST00000485455, ENST00000489828, ENST00000493638, ENST00000885296, ENST00000936068, ENST00000936069, ENST00000936070

RefSeq mRNA: 12 — MANE Select: NM_182692 NM_001278273, NM_001350738, NM_001350739, NM_001350740, NM_001350741, NM_001350742, NM_001350743, NM_001350744, NM_001350745, NM_001350746, NM_182691, NM_182692

CCDS: CCDS34724, CCDS5735, CCDS94171, CCDS94172

Canonical transcript exons

ENST00000393651 — 16 exons

Exon	Start	End
ENSE00001882149	105142008	105142490
ENSE00001922776	105203628	105203785
ENSE00001947146	105116374	105118022
ENSE00003474950	105388791	105388921
ENSE00003508060	105388648	105388702
ENSE00003574748	105132791	105132898
ENSE00003584336	105133004	105133104
ENSE00003620434	105126248	105126340
ENSE00003673512	105126993	105127062
ENSE00003993938	105168008	105168095
ENSE00003993939	105167377	105167464
ENSE00003993941	105160507	105160613
ENSE00003993942	105145283	105145308
ENSE00003993943	105143084	105143330
ENSE00003993944	105146493	105146658
ENSE00003995356	105169157	105169265

Expression profiles

Bgee: expression breadth ubiquitous, 293 present calls, max score 99.77.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 49.8335 / max 2052.5668, expressed in 1824 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
85434	32.5604	1820
85426	13.9063	1389
85435	1.9694	850
85433	0.5317	289
85432	0.3104	150
85431	0.1851	62
85424	0.1444	59
85436	0.0873	4
85423	0.0824	23
85430	0.0560	11

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sperm	CL:0000019	99.77	gold quality
male germ cell	CL:0000015	99.52	gold quality
pons	UBERON:0000988	98.86	gold quality
secondary oocyte	CL:0000655	98.85	gold quality
middle temporal gyrus	UBERON:0002771	98.64	gold quality
lateral nuclear group of thalamus	UBERON:0002736	98.28	gold quality
entorhinal cortex	UBERON:0002728	98.26	gold quality
parietal lobe	UBERON:0001872	98.21	gold quality
postcentral gyrus	UBERON:0002581	98.18	gold quality
left testis	UBERON:0004533	98.16	gold quality
right testis	UBERON:0004534	98.10	gold quality
substantia nigra pars compacta	UBERON:0001965	98.07	gold quality
oocyte	CL:0000023	98.05	gold quality
substantia nigra pars reticulata	UBERON:0001966	98.03	gold quality
lateral globus pallidus	UBERON:0002476	98.00	gold quality
ventral tegmental area	UBERON:0002691	97.98	gold quality
Brodmann (1909) area 23	UBERON:0013554	97.95	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	97.89	gold quality
inferior vagus X ganglion	UBERON:0005363	97.85	gold quality
superior vestibular nucleus	UBERON:0007227	97.85	gold quality
inferior olivary complex	UBERON:0002127	97.83	gold quality
cortical plate	UBERON:0005343	97.81	gold quality
globus pallidus	UBERON:0001875	97.74	gold quality
corpus callosum	UBERON:0002336	97.71	gold quality
medulla oblongata	UBERON:0001896	97.69	gold quality
medial globus pallidus	UBERON:0002477	97.64	gold quality
superior frontal gyrus	UBERON:0002661	97.43	gold quality
occipital lobe	UBERON:0002021	97.40	gold quality
subthalamic nucleus	UBERON:0001906	97.28	gold quality
adult organism	UBERON:0007023	97.25	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	7.83
E-MTAB-7381	no	236.96

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
CCND1	Activation

Upstream regulators (CollecTRI, top): CREB1

miRNA regulators (miRDB)

158 targeting SRPK2, 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-4668-3P	100.00	68.74	2635
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-4776-3P	100.00	68.73	1340
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-32-5P	99.98	75.21	1964
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-3692-3P	99.98	70.27	2139
HSA-MIR-499A-5P	99.98	70.79	1323
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-367-3P	99.98	74.83	1819
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-493-5P	99.96	72.47	2382

Literature-anchored findings (GeneRIF, showing 25)

• Both SRPK1 and SRPK2 are most likely the cellular protein kinases mediating HBV core protein phosphorylation during viral infection and therefore represent important host cell targets for therapeutic intervention in HBV infection. (PMID:12134018)
• negative role of SRPK1 and SRPK2 in the regulation of HBV replication through a mechanism not involving the phosphorylation of the core protein (PMID:16122776)
• SRPK2 knock down results in hypophosphorylation of the arginine-serine (RS) domain-containing human PRP28 protein (PRP28, also known as DDX23), and destabilizes PRP28 association with the tri-snRNP. (PMID:18425142)
• overexpression of SRPK2 is associated with phosphorylating acinus and regulating its stimulatory effects on cyclin A1 expression, contributing to leukemia cell proliferation (PMID:18559500)
• Interaction of Akt-phosphorylated SRPK2 with 14-3-3 mediates cell cycle and cell death in neurons. (PMID:19592491)
• Short-term exercise resulted in a significant increase of mRNA expression of genes encoding proteins involved in the formation of precatalytic splisosome: SRPK2. (PMID:19902070)
• Our results demonstrate that SRPK1 and SRPK2 are host factors essential for Hepatitis C virus replication. (PMID:20498328)
• the BLRF2 RS motif is phosphorylated by SRPK2 and is important for viral replication. (PMID:23326445)
• A conserved electronegative docking groove in SRPK2 is responsible for substrate binding. (PMID:24444330)
• Data indicate serine/arginine-rich protein kinases SRPK1/2/SRPIN340 complexes by molecular docking and molecular dynamics. (PMID:26244849)
• Our results indicate that phosphorylation of SRPK2 plays a crucial role in the regulation of splicing process in head and neck squamous cell carcinoma (HNSCC), and that splicing kinases can be developed as a new class of therapeutic target in HNSCC. (PMID:26853621)
• In this study, it was found that the expression of SRPK2 was up-regulated in the clinical colon cancer samples. Overexpression of SRPK2 promoted the growth and migration of colon cancer cells, while knocking down the expression of SRPK2 inhibited the growth, migration and tumorigenecity of colon cancer cells. (PMID:27041240)
• ten candidate variants were prioritised. Of these, SRPK2 (c.2044C>T[p.Arg682Trp]) and NOTCH1 (c.3835C>T[p.Arg1279Cys]), co-segregated with disease in the family; however, previous functional analyses on SRPK2 make this an unlikely candidate. Functional analyses in the variant (c.3835C>T[p.Arg1279Cys]) of the known CHD gene NOTCH1 demonstrated a non-significant decrease in signalling activity. (PMID:27989580)
• pausing of RNA polymerase II (RNA Pol II) initiates a signaling cascade whereby the serine/arginine protein kinase 2 (SRPK2) phosphorylates the DDX23 helicase, culminating in the suppression of R-loops. (PMID:28076779)
• Delta-secretase phosphorylation by SRPK2 plays a critical role in aggravating Alzheimer disease pathogenesis. (PMID:28826672)
• SRPK2 may play an important role in the progression and metastasis of prostate cancer. (PMID:29587239)
• The conserved SRPK-specific substrate-docking groove in SRPK2 impacts the binding and phosphorylation of both SR proteins, and the localization of SRSF3. (PMID:30478176)
• SRPK2 expression was upregulated in pancreatic cancer tissues, positively correlated with stage, and associated with decreased overall survival in pancreatic cancer patients. In pancreatic cancer cells, SRPK2 overexpression promoted cell invasion and migration, and decreased chemosensitivity to gemcitabine or oxaliplatin. SRPK2 silencing decreased cell invasion and migration and increased chemosensitivity. (PMID:30724469)
• Serine-Arginine Protein Kinase SRPK2 Modulates the Assembly of the Active Zone Scaffolding Protein CAST1/ERC2. (PMID:31671734)
• Cooperation of SRPK2, Numb and p53 in the malignant biology and chemosensitivity of colorectal cancer. (PMID:31898732)
• Inhibition of Long Noncoding RNA Linc-Pint by Hepatitis C Virus in Infected Hepatocytes Enhances Lipogenesis. (PMID:33236406)
• SRPK1/2 and PP1alpha exert opposite functions by modulating SRSF1-guided MKNK2 alternative splicing in colon adenocarcinoma. (PMID:33602301)
• Stress Granules Determine the Development of Obesity-Associated Pancreatic Cancer. (PMID:35674408)
• The pre-mRNA alternative splicing regulated by SRPK2: A new player in alcohol-associated liver disease? (PMID:37183907)
• SRPK2 Mediates HBV Core Protein Phosphorylation and Capsid Assembly via Docking Interaction. (PMID:38324561)

Cross-species orthologs

16 orthologs

Organism	Symbol	Gene ID
danio_rerio		ENSDARG00000110142
danio_rerio	srpk2	ENSDARG00000110485
danio_rerio	srpk2	ENSDARG00000114874
mus_musculus	Srpk2	ENSMUSG00000062604
rattus_norvegicus	Srpk2	ENSRNOG00000010601
drosophila_melanogaster	nmo	FBGN0011817
drosophila_melanogaster	CG8565	FBGN0030697
drosophila_melanogaster	SRPK	FBGN0286813
caenorhabditis_elegans		WBGENE00002187
caenorhabditis_elegans		WBGENE00002188
caenorhabditis_elegans		WBGENE00003048
caenorhabditis_elegans		WBGENE00004055
caenorhabditis_elegans		WBGENE00004056
caenorhabditis_elegans		WBGENE00004980
caenorhabditis_elegans	gskl-2	WBGENE00007977
caenorhabditis_elegans	Y106G6E.1	WBGENE00013705

Paralogs (19): MAPK9 (ENSG00000050748), MAPK6 (ENSG00000069956), MOK (ENSG00000080823), NLK (ENSG00000087095), SRPK1 (ENSG00000096063), MAPK1 (ENSG00000100030), MAPK3 (ENSG00000102882), MAPK8 (ENSG00000107643), MAPK10 (ENSG00000109339), MAK (ENSG00000111837), MAPK14 (ENSG00000112062), CILK1 (ENSG00000112144), MAPK4 (ENSG00000141639), MAPK13 (ENSG00000156711), MAPK7 (ENSG00000166484), MAPK15 (ENSG00000181085), SRPK3 (ENSG00000184343), MAPK11 (ENSG00000185386), MAPK12 (ENSG00000188130)

Protein

Protein identifiers

SRSF protein kinase 2 — P78362 (reviewed: P78362)

Alternative names: SFRS protein kinase 2, Serine/arginine-rich protein-specific kinase 2

All UniProt accessions (8): A0A994J591, C9J2M4, C9JWF7, P78362, F8WAV6, F8WBW4, H7C521, H7C5L6

UniProt curated annotations — full annotation on UniProt →

Function. Serine/arginine-rich protein-specific kinase which specifically phosphorylates its substrates at serine residues located in regions rich in arginine/serine dipeptides, known as RS domains and is involved in the phosphorylation of SR splicing factors and the regulation of splicing. Promotes neuronal apoptosis by up-regulating cyclin-D1 (CCND1) expression. This is done by the phosphorylation of SRSF2, leading to the suppression of p53/TP53 phosphorylation thereby relieving the repressive effect of p53/TP53 on cyclin-D1 (CCND1) expression. Phosphorylates ACIN1, and redistributes it from the nuclear speckles to the nucleoplasm, resulting in cyclin A1 but not cyclin A2 up-regulation. Plays an essential role in spliceosomal B complex formation via the phosphorylation of DDX23/PRP28. Probably by phosphorylating DDX23, leads to the suppression of incorrect R-loops formed during transcription; R-loops are composed of a DNA:RNA hybrid and the associated non-template single-stranded DNA. Can mediate hepatitis B virus (HBV) core protein phosphorylation. Plays a negative role in the regulation of HBV replication through a mechanism not involving the phosphorylation of the core protein but by reducing the packaging efficiency of the pregenomic RNA (pgRNA) without affecting the formation of the viral core particles. Phosphorylates the N-terminus of ERC1.

Subunit / interactions. Associates with U4/U6-U5 tri-small nuclear ribonucleoproteins (U4/U6-U5 tri-snRNPs). Interacts with PKB/AKT1 in a phosphorylation-dependent manner. The phosphorylated form (by PKB/AKT1) interacts with YWHAB and YWHAE. Interaction with YWHAB suppresses its cleavage by caspases and inhibits the release of its N-terminal pro-apoptotic fragment. Interacts with SFN. Interacts with ACIN1. Interacts with POLR2A/RNA polymerase II; the interaction occurs during the co-transcriptional formation of inappropriate R-loops. Interacts (via kinase domain) with ERC1 (via N-terminus); the interaction is direct and may be involved in SRPK protein localization.

Subcellular location. Cytoplasm. Nucleus. Nucleoplasm. Nucleus speckle. Chromosome.

Tissue specificity. Highly expressed in brain, moderately expressed in heart and skeletal muscle and at low levels in lung, liver, and kidney.

Post-translational modifications. Phosphorylation at Thr-492 by PKB/AKT1 enhances its stimulatory activity in triggering cyclin-D1 (CCND1) expression and promoting apoptosis in neurons, which can be blocked by YWHAB. It also enhances its protein kinase activity toward ACIN1 and SRSF2, promotes its nuclear translocation and prevents its proteolytic cleavage. Proteolytically cleaved at Asp-139 and Asp-403 by caspase-3 during apoptotic cell death. Cleavage at Asp-139 which is the major site of cleavage, produces a small N-terminal fragment that translocates into nucleus and promotes VP16-induced apoptosis.

Activity regulation. Activated by phosphorylation on Ser-52 and Ser-588.

Similarity. Belongs to the protein kinase superfamily. CMGC Ser/Thr protein kinase family.

Isoforms (2)

UniProt ID	Names	Canonical?
P78362-1	1	yes
P78362-2	2

RefSeq proteins (12): NP_001265202, NP_001337667, NP_001337668, NP_001337669, NP_001337670, NP_001337671, NP_001337672, NP_001337673, NP_001337674, NP_001337675, NP_872633, NP_872634* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR051334

Pfam: PF00069

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (78 total): helix 20, modified residue 11, sequence conflict 10, strand 8, sequence variant 7, compositionally biased region 5, region of interest 4, chain 3, turn 3, binding site 2, site 2, active site 1, splice variant 1, domain 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
7ZKX	X-RAY DIFFRACTION	2.06
2X7G	X-RAY DIFFRACTION	2.5
5MYV	X-RAY DIFFRACTION	2.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P78362-F1	72.62	0.50

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): 214 (proton acceptor); 139–140 (cleavage; by caspase-3); 403–404 (cleavage; by caspase-3)

Ligand- & substrate-binding residues (2): 87–95; 110

Post-translational modifications (11): 52, 380, 475, 478, 484, 486, 490, 492, 494, 497, 588

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-9694631	Maturation of nucleoprotein
R-HSA-1643685	Disease
R-HSA-5663205	Infectious disease
R-HSA-9679506	SARS-CoV Infections
R-HSA-9694516	SARS-CoV-2 Infection
R-HSA-9694635	Translation of Structural Proteins
R-HSA-9772573	Late SARS-CoV-2 Infection Events
R-HSA-9824446	Viral Infection Pathways

MSigDB gene sets: 312 (showing top): BORCZUK_MALIGNANT_MESOTHELIOMA_UP, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GCANCTGNY_MYOD_Q6, GOBP_PEPTIDYL_SERINE_MODIFICATION, GOBP_NEGATIVE_REGULATION_OF_VIRAL_PROCESS, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_POSITIVE_REGULATION_OF_VIRAL_GENOME_REPLICATION, TATTATA_MIR374, THEILGAARD_NEUTROPHIL_AT_SKIN_WOUND_DN, LHX3_01, RODRIGUES_NTN1_TARGETS_DN, EVI1_05, PAX8_B, AP1_Q4_01, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM

GO Biological Process (21): spliceosomal complex assembly (GO:0000245), angiogenesis (GO:0001525), protein phosphorylation (GO:0006468), positive regulation of cell population proliferation (GO:0008284), RNA splicing (GO:0008380), positive regulation of gene expression (GO:0010628), peptidyl-serine phosphorylation (GO:0018105), cell differentiation (GO:0030154), nuclear speck organization (GO:0035063), intracellular signal transduction (GO:0035556), phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0043491), positive regulation of neuron apoptotic process (GO:0043525), positive regulation of viral genome replication (GO:0045070), negative regulation of viral genome replication (GO:0045071), innate immune response (GO:0045087), positive regulation of cell cycle (GO:0045787), regulation of mRNA splicing, via spliceosome (GO:0048024), regulation of mRNA processing (GO:0050684), R-loop processing (GO:0062176), mRNA processing (GO:0006397), regulation of gene expression (GO:0010468)

GO Molecular Function (11): magnesium ion binding (GO:0000287), RNA binding (GO:0003723), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), 14-3-3 protein binding (GO:0071889), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (11): chromatin (GO:0000785), acrosomal vesicle (GO:0001669), nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730), cytoplasm (GO:0005737), cytosol (GO:0005829), nuclear speck (GO:0016607), sperm end piece (GO:0097229), presynapse (GO:0098793), chromosome (GO:0005694)

Reactome top-level categories

Rollup of top-7 pathways:

Category	Pathways
Translation of Structural Proteins	1
Disease	1
Viral Infection Pathways	1
SARS-CoV Infections	1
Late SARS-CoV-2 Infection Events	1
SARS-CoV-2 Infection	1
Infectious disease	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	6
mRNA splicing, via spliceosome	2
positive regulation of cellular process	2
RNA processing	2
intracellular anatomical structure	2
viral genome replication	2
regulation of viral genome replication	2
protein kinase activity	2
nuclear lumen	2
intracellular membraneless organelle	2
protein-RNA complex assembly	1
blood vessel morphogenesis	1
anatomical structure formation involved in morphogenesis	1
phosphorylation	1
protein modification process	1
cell population proliferation	1
regulation of cell population proliferation	1
gene expression	1
regulation of gene expression	1
positive regulation of macromolecule biosynthetic process	1
protein phosphorylation	1
peptidyl-serine modification	1
cellular developmental process	1
nuclear body organization	1
signal transduction	1
intracellular signaling cassette	1
positive regulation of apoptotic process	1
regulation of neuron apoptotic process	1
neuron apoptotic process	1
positive regulation of viral process	1
negative regulation of viral process	1
immune response	1
defense response to symbiont	1
cell cycle	1
regulation of cell cycle	1
regulation of RNA splicing	1
regulation of mRNA processing	1
mRNA processing	1
regulation of mRNA metabolic process	1
chromatin remodeling	1

Protein interactions and networks

STRING

2346 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SRPK2	DDX23	Q9BUQ8	955
SRPK2	SRSF1	Q07955	841
SRPK2	SRSF2	Q01130	798
SRPK2	LUC7L3	O95232	723
SRPK2	LUC7L	Q9NQ29	579
SRPK2	SRSF4	Q08170	564
SRPK2	SRSF6	Q13247	561
SRPK2	KMT2E	Q8IZD2	555
SRPK2	SRSF5	Q13243	537
SRPK2	SRSF9	Q13242	535
SRPK2	SRSF3	P23152	530
SRPK2	SRSF7	Q16629	491
SRPK2	SNRNP70	P08621	489
SRPK2	SF3A3	Q12874	482
SRPK2	U2AF2	P26368	479

IntAct

452 interactions, top by confidence:

A	B	Type	Score
SRPK2	RBM39	psi-mi:“MI:0915”(physical association)	0.910
RBM39	SRPK2	psi-mi:“MI:0915”(physical association)	0.910
PRPF38A	SRPK2	psi-mi:“MI:0915”(physical association)	0.890
SRPK2	PRPF38A	psi-mi:“MI:0915”(physical association)	0.890
SRPK2	RNPS1	psi-mi:“MI:0915”(physical association)	0.890
ZRSR2	SRPK2	psi-mi:“MI:0915”(physical association)	0.880
SRPK2	ZRSR2	psi-mi:“MI:0915”(physical association)	0.880
U2AF1	SRPK2	psi-mi:“MI:0915”(physical association)	0.830
SRPK2	U2AF1	psi-mi:“MI:0915”(physical association)	0.830
SRPK2	CLK3	psi-mi:“MI:0915”(physical association)	0.810
TRA2B	SRPK2	psi-mi:“MI:0915”(physical association)	0.760
SNRNP27	SRPK2	psi-mi:“MI:0915”(physical association)	0.750
SRPK2	ZSCAN9	psi-mi:“MI:0915”(physical association)	0.720
ZSCAN9	SRPK2	psi-mi:“MI:0915”(physical association)	0.720
FXR2	SRPK2	psi-mi:“MI:0915”(physical association)	0.670
SRPK2	FXR2	psi-mi:“MI:0915”(physical association)	0.670

BioGRID (1041): SRPK2 (Two-hybrid), SRPK2 (Two-hybrid), SRPK2 (Two-hybrid), SRPK2 (Two-hybrid), U2AF1 (Two-hybrid), ZSCAN9 (Two-hybrid), ZRSR2 (Two-hybrid), FXR2 (Two-hybrid), RBM39 (Two-hybrid), RNPS1 (Two-hybrid), SNRNP27 (Two-hybrid), LUZP4 (Two-hybrid), PRPF38A (Two-hybrid), SRPK2 (Affinity Capture-MS), SRPK2 (Biochemical Activity)

ESM2 similar proteins: A2X6X1, A2XUW1, A9RVK2, B9FMJ3, F4HRJ4, F4I114, F4ICB6, O08678, O08679, O45818, P21127, P24788, P27448, P78362, Q03141, Q05512, Q08DZ2, Q09437, Q13523, Q23357, Q39008, Q40541, Q5R814, Q5RKH1, Q5Z9J0, Q5ZCI1, Q61136, Q6K5F8, Q6L5D4, Q6L5F7, Q6Z829, Q7KZI7, Q7XUF4, Q8H0U8, Q8RX66, Q8VHF0, Q8VHJ5, Q96VK3, Q9C9U4, Q9C9U5

Diamond homologs: B0Y8Y4, B8Y466, O54781, O70551, P78362, Q03563, Q45FA5, Q4WW94, Q5RD27, Q5UQ24, Q61IS6, Q93VK0, Q96SB4, Q9UPE1, Q9Z0G2, A0A509AHB6, A8WJR8, B2MVY4, E2RTQ7, G5EBT1, G5EDB2, O35492, O35493, O43781, O59853, O76039, O93982, P11802, P14680, P14681, P30285, P32350, P35426, P36616, P46551, P49657, P49761, P51137, P51566, P51568

SIGNOR signaling

10 interactions.

A	Effect	B	Mechanism
SRPK2	up-regulates	ACIN1	phosphorylation
AKT1	up-regulates	SRPK2	phosphorylation
SRPK2	“up-regulates quantity by expression”	CCND1	“transcriptional regulation”
YWHAB	down-regulates	SRPK2	binding
AKT	up-regulates	SRPK2	phosphorylation
RPS6KB1	“up-regulates activity”	SRPK2	phosphorylation
CSNK1A1	“up-regulates activity”	SRPK2	phosphorylation
SRPK2	“up-regulates activity”	SRSF1	phosphorylation
SRPK2	“up-regulates activity”	LGMN	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 154 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
Transport of Mature Transcript to Cytoplasm	9	32.0×	1e-10
mRNA 3’-end processing	13	23.9×	1e-13
RNA Polymerase II Transcription Termination	11	22.6×	3e-11
Peptide chain elongation	16	19.0×	7e-15
Viral mRNA Translation	16	19.0×	7e-15
PELO:HBS1L and ABCE1 dissociate a ribosome on a non-stop mRNA	16	18.8×	7e-15
Selenocysteine synthesis	16	18.0×	1e-14
Eukaryotic Translation Termination	16	18.0×	1e-14

GO biological processes:

GO term	Partners	Fold	FDR
mRNA splice site recognition	6	33.4×	2e-06
negative regulation of mRNA splicing, via spliceosome	5	26.6×	7e-05
cytoplasmic translation	18	23.1×	4e-17
regulation of alternative mRNA splicing, via spliceosome	10	17.0×	6e-08
ribosomal large subunit biogenesis	5	15.4×	8e-04
mRNA splicing, via spliceosome	20	12.7×	3e-14
ribosomal small subunit biogenesis	8	12.7×	2e-05
translation	17	12.1×	1e-11

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	1
Uncertain significance	61
Likely benign	15
Benign	5

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
1098306	GRCh37/hg19 7q22.3(chr7:104730300-104791108)	Pathogenic
563407	GRCh37/hg19 7q22.1-22.3(chr7:102910570-105104800)x1	Likely pathogenic

SpliceAI

3707 predictions. Top by Δscore:

Variant	Effect	Δscore
7:105110768:TA:T	acceptor_loss	1.0000
7:105110769:A:AG	acceptor_gain	1.0000
7:105110770:G:GA	acceptor_gain	1.0000
7:105110770:GA:G	acceptor_gain	1.0000
7:105110770:GAC:G	acceptor_gain	1.0000
7:105110770:GACC:G	acceptor_gain	1.0000
7:105110770:GACCC:G	acceptor_gain	1.0000
7:105110865:CAAGG:C	donor_loss	1.0000
7:105110866:AAGGT:A	donor_loss	1.0000
7:105110869:GT:G	donor_loss	1.0000
7:105110870:T:A	donor_loss	1.0000
7:105111823:A:AG	acceptor_gain	1.0000
7:105111823:AGCCT:A	acceptor_gain	1.0000
7:105111824:G:GG	acceptor_gain	1.0000
7:105111824:GC:G	acceptor_gain	1.0000
7:105111824:GCCT:G	acceptor_gain	1.0000
7:105111824:GCCTG:G	acceptor_gain	1.0000
7:105118018:TTCTC:T	acceptor_gain	1.0000
7:105118020:CTC:C	acceptor_gain	1.0000
7:105118021:TC:T	acceptor_gain	1.0000
7:105118022:CC:C	acceptor_gain	1.0000
7:105118022:CCTAC:C	acceptor_loss	1.0000
7:105118023:C:CC	acceptor_gain	1.0000
7:105118024:T:G	acceptor_loss	1.0000
7:105118027:A:T	acceptor_gain	1.0000
7:105125895:A:T	acceptor_gain	1.0000
7:105132785:CCTTA:C	donor_loss	1.0000
7:105132786:CTTAC:C	donor_loss	1.0000
7:105132787:TTACC:T	donor_loss	1.0000
7:105132788:TAC:T	donor_loss	1.0000

AlphaMissense

4625 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:105117852:A:G	W685R	1.000
7:105117852:A:T	W685R	1.000
7:105117865:G:C	C680W	1.000
7:105117867:A:G	C680R	1.000
7:105117875:G:T	A677D	1.000
7:105117905:A:G	L667S	1.000
7:105117917:A:G	L663P	1.000
7:105117920:A:G	F662S	1.000
7:105117929:A:G	F659S	1.000
7:105117954:A:G	W651R	1.000
7:105117954:A:T	W651R	1.000
7:105117971:A:G	L645P	1.000
7:105117971:A:T	L645H	1.000
7:105117974:A:T	V644E	1.000
7:105117988:C:A	W639C	1.000
7:105117988:C:G	W639C	1.000
7:105117990:A:G	W639R	1.000
7:105117990:A:T	W639R	1.000
7:105118007:A:C	I633S	1.000
7:105118007:A:T	I633N	1.000
7:105118016:A:T	L630Q	1.000
7:105126259:A:G	F624S	1.000
7:105126280:C:A	G617V	1.000
7:105126280:C:T	G617E	1.000
7:105126281:C:G	G617R	1.000
7:105126281:C:T	G617R	1.000
7:105126289:G:T	A614D	1.000
7:105126316:A:G	L605P	1.000
7:105126316:A:T	L605Q	1.000
7:105126318:C:A	E604D	1.000

dbSNP variants (sampled 300 via entrez): RS1000008197 (7:105163078 T>C), RS1000010597 (7:105165343 T>C), RS1000012176 (7:105327086 A>T), RS1000022010 (7:105258356 A>G), RS1000042638 (7:105362711 A>T), RS1000049455 (7:105367862 C>G), RS1000053325 (7:105332662 G>A,T), RS1000064968 (7:105161665 C>G), RS1000067944 (7:105211225 T>A,C), RS1000069297 (7:105132275 G>A,C), RS1000073759 (7:105296108 A>C), RS1000090091 (7:105301481 A>C,G), RS1000098875 (7:105210958 T>C,G), RS1000105843 (7:105250695 G>A,T), RS1000110367 (7:105219165 A>G)

Disease associations

OMIM: gene MIM:602980 | disease phenotypes: MIM:618512

GenCC curated gene-disease

Mondo (1): O’Donnell-Luria-Rodan syndrome (MONDO:0032793)

Orphanet (0):

HPO phenotypes

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

GWAS associations

21 associations (top):

Study	Trait	p-value
GCST001712_15	Myopia (pathological)	2.000000e-07
GCST002539_67	Schizophrenia	1.000000e-09
GCST003219_47	Advanced age-related macular degeneration	1.000000e-09
GCST004063_124	Waist circumference adjusted for body mass index	3.000000e-08
GCST004500_119	Waist circumference adjusted for BMI (adjusted for smoking behaviour)	5.000000e-06
GCST004521_190	Autism spectrum disorder or schizophrenia	3.000000e-10
GCST004521_221	Autism spectrum disorder or schizophrenia	5.000000e-11
GCST004946_4	Schizophrenia	2.000000e-12
GCST006269_781	General cognitive ability	2.000000e-09
GCST006269_804	General cognitive ability	7.000000e-09
GCST006618_2	Uterine fibroid size (maximum dimension)	4.000000e-07
GCST006803_102	Schizophrenia	7.000000e-11
GCST006922_16	Regular attendance at a religious group	8.000000e-10
GCST007201_218	Schizophrenia	2.000000e-09
GCST007201_75	Schizophrenia	3.000000e-12
GCST007556_45	Autism spectrum disorder	3.000000e-08
GCST008103_107	Bipolar disorder	4.000000e-06
GCST008103_9	Bipolar disorder	1.000000e-09
GCST009600_53	Anorexia nervosa, attention-deficit/hyperactivity disorder, autism spectrum disorder, bipolar disorder, major depression, obsessive-compulsive disorder, schizophrenia, or Tourette syndrome (pleiotropy)	4.000000e-10
GCST011011_73	Youthful appearance (self-reported)	8.000000e-11
GCST012465_5	Bipolar disorder	3.000000e-09

EFO canonical traits (7, from GWAS)

EFO ID	Trait name
EFO:0004207	pathological myopia
EFO:1001492	atrophic macular degeneration
EFO:0007789	BMI-adjusted waist circumference
EFO:0004318	smoking behavior
EFO:0004337	intelligence
EFO:0009410	uterine fibroid measurement
EFO:0009592	social interaction measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5668 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 114,113 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1738797	ALECTINIB	4	6,731
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3	77
CHEMBL1721885	SU-014813	2	363
CHEMBL572878	TOZASERTIB	2	2,998
CHEMBL1908397	KW-2449	1	622

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — SRPK family

Binding affinities (BindingDB)

6 measured of 6 human assays (6 total across all organisms); most potent 6 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Staurosporine	KD	1.7 nM
PKC-412	KD	190 nM
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril	KD	520 nM
N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide	KD	1100 nM
5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide	KD	2600 nM
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	KD	3500 nM

ChEMBL bioactivities

71 potent at pChembl≥5 of 71 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.60	IC50	2.54	nM	CHEMBL4468747
8.18	IC50	6.6	nM	CHEMBL3746522
8.13	IC50	7.46	nM	CHEMBL3747611
8.07	IC50	8.57	nM	CHEMBL3746960
7.91	IC50	12.4	nM	CHEMBL3747406
7.90	IC50	12.5	nM	CHEMBL3747301
7.88	IC50	13.2	nM	CHEMBL3746627
7.84	IC50	14.5	nM	CHEMBL3746395
7.82	Kd	15	nM	KW-2449
7.63	IC50	23.6	nM	CHEMBL3747108
7.55	IC50	28.2	nM	ALECTINIB
7.44	Kd	36	nM	NINTEDANIB
7.29	Kd	51	nM	LESTAURTINIB
7.17	Kd	67	nM	STAUROSPORINE
7.10	IC50	80	nM	CHEMBL5085558
7.09	IC50	81	nM	CHEMBL5085558
7.01	IC50	98	nM	CHEMBL4468747
7.00	Kd	100	nM	FEDRATINIB
6.83	IC50	149	nM	CHEMBL5085558
6.83	IC50	147	nM	CHEMBL5435975
6.83	IC50	147	nM	CHEMBL5397100
6.83	EC50	149	nM	CHEMBL5085558
6.77	IC50	171	nM	STAUROSPORINE
6.73	IC50	185	nM	STAUROSPORINE
6.72	Kd	190	nM	SUNITINIB
6.70	Kd	200	nM	SU-014813
6.69	IC50	203	nM	CHEMBL4787157
6.68	IC50	210	nM	CHEMBL5405335
6.64	IC50	227	nM	STAUROSPORINE
6.59	IC50	256	nM	CHEMBL5074274
6.58	IC50	260	nM	CHEMBL5439515
6.54	Kd	290	nM	DOVITINIB
6.52	IC50	300	nM	CHEMBL5416930
6.48	Kd	330	nM	MIDOSTAURIN
6.47	IC50	340	nM	CHEMBL5437009
6.34	IC50	460	nM	CHEMBL5409896
6.30	Kd	500	nM	PHA-665752
6.29	IC50	510	nM	CHEMBL5407046
6.20	IC50	626	nM	CHEMBL5409387
6.19	EC50	648	nM	CHEMBL5074274
6.18	IC50	660	nM	CHEMBL5398076
6.17	IC50	670	nM	CHEMBL5399262
6.17	Kd	680	nM	TOZASERTIB
6.12	IC50	750	nM	CHEMBL5433267
6.06	IC50	870	nM	CHEMBL5422948
6.05	IC50	900	nM	CHEMBL5403164
6.00	IC50	1000	nM	TP-030-1
6.00	IC50	1000	nM	TP-030-2
6.00	IC50	1000	nM	TP-030n
5.97	IC50	1080	nM	CHEMBL5416263

PubChem BioAssay actives

55 with measured affinity, of 687 total; 38 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
3-(3-cyano-9-ethyl-6,6-dimethyl-11-oxo-5H-benzo[b]carbazol-8-yl)benzenesulfonyl fluoride	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.0025	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	624768: Binding constant for SRPK2 kinase domain	kd	0.0150	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	624768: Binding constant for SRPK2 kinase domain	kd	0.0360	uM
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one	508092: Binding affinity to SRPK2	kd	0.0510	uM
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	435196: Binding constant for full-length SRPK2	kd	0.0670	uM
N-[3-[[[2-(5-chloro-4-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.0800	uM
Fedratinib	624768: Binding constant for SRPK2 kinase domain	kd	0.1000	uM
N-[3-[[[6-(6-chloro-1H-benzimidazol-2-yl)-2-pyridinyl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.1470	uM
N-[3-[[[2-(5-chloro-1-methylbenzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.1470	uM
Sunitinib	435196: Binding constant for full-length SRPK2	kd	0.1900	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	435196: Binding constant for full-length SRPK2	kd	0.2000	uM
5-amino-6-[(E)-(3-methoxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-2-(trifluoromethyl)-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one	1851165: Inhibition of SRPK2 (unknown origin) incubated for 10 mins in presence of ATP by Kinase-Glo assay	ic50	0.2030	uM
N-[3-[[6-(6-chloro-1H-benzimidazol-2-yl)pyrrolo[3,2-c]pyridin-1-yl]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.2100	uM
5-pyridin-4-yl-N-[2-[4-(pyridin-2-ylmethyl)piperazin-1-yl]-5-(trifluoromethyl)phenyl]furan-2-carboxamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.2560	uM
N-[3-[[[2-(6-chloro-4-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.2600	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	435196: Binding constant for full-length SRPK2	kd	0.2900	uM
N-[3-[[2-(6-chloro-1H-benzimidazol-2-yl)pyrrolo[2,3-d]pyrimidin-7-yl]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.3000	uM
Midostaurin	435196: Binding constant for full-length SRPK2	kd	0.3300	uM
N-[3-[[2-(6-chloro-1H-benzimidazol-2-yl)-6-methylpyrrolo[2,3-d]pyrimidin-7-yl]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.3400	uM
N-[3-[[[5-bromo-2-(6-chloro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.4600	uM
(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one	624768: Binding constant for SRPK2 kinase domain	kd	0.5000	uM
N-[3-[[[2-(6-chloro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.5100	uM
N-[3-[[[2-(6-chloro-1H-benzimidazol-2-yl)pyrimidin-4-yl]-methylamino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.6260	uM
N-[3-[[[2-(4-chloro-6-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.6600	uM
N-[3-[[[2-(5-chloro-6-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.6700	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	435196: Binding constant for full-length SRPK2	kd	0.6800	uM
N-methyl-N-[3-[[[2-(6-propan-2-yl-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]methanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.7500	uM
N-[3-[[[2-(4,6-difluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.8700	uM
N-methyl-N-[3-[[[2-[6-(1-methylpyrazol-4-yl)-1H-benzimidazol-2-yl]pyrimidin-4-yl]amino]methyl]-2-pyridinyl]methanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	0.9000	uM
N-[3-[[[2-(5,6-difluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	1.0800	uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine	624768: Binding constant for SRPK2 kinase domain	kd	1.1000	uM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione	624768: Binding constant for SRPK2 kinase domain	kd	1.1000	uM
N-[2-piperidin-1-yl-5-(trifluoromethyl)phenyl]pyridine-4-carboxamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	1.5100	uM
N-[3-[[[2-(6-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	1.9900	uM
N-methyl-N-[3-[[[2-(6-methyl-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]methanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	2.0900	uM
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride	624768: Binding constant for SRPK2 kinase domain	kd	2.2000	uM
N-[3-[[[2-(6-methoxy-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	3.5000	uM
N-[3-[[[2-(6-cyano-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide	1968976: Inhibition of human SRPK2 using GRSRSRSRSR as substrate in presence of [gamma-33p]-ATP by radiometric hotspot kinase assay	ic50	3.7700	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases abundance, affects cotreatment, increases expression, affects binding (+1 more)	4
Valproic Acid	affects expression, decreases methylation, increases expression	4
Arsenic	increases abundance, increases expression, affects methylation, affects cotreatment	2
Benzo(a)pyrene	decreases expression	2
Cisplatin	increases phosphorylation, affects localization	2
aristolochic acid I	decreases expression	1
testosterone enanthate	affects expression	1
triphenyl phosphate	affects expression	1
bisphenol A	affects cotreatment, affects methylation, decreases methylation	1
arsenite	decreases methylation	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
manganese chloride	increases abundance, increases expression, affects cotreatment	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
coumarin	affects phosphorylation	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
di-n-butylphosphoric acid	affects expression	1
monomethylarsonous acid	increases expression	1
14-deoxy-11,12-didehydroandrographolide	increases expression	1
Fulvestrant	affects cotreatment, affects methylation	1
Acetaminophen	increases expression	1
Caffeine	increases phosphorylation	1
Diethylnitrosamine	decreases expression	1
Drugs, Chinese Herbal	increases expression	1
Enzyme Inhibitors	increases O-linked glycosylation, decreases activity	1
Ivermectin	decreases expression	1
Lead	affects expression	1
Manganese	increases abundance, increases expression, affects cotreatment	1
Methotrexate	increases expression	1
Naphthoquinones	increases expression	1
Paraquat	increases phosphorylation, affects reaction, affects localization	1

ChEMBL screening assays

221 unique, capped per target: 221 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1043819	Binding	Residual activity of SRPK2 at 1 uM by microplate scintillation counting	Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization. — Bioorg Med Chem

Cellosaurus cell lines

3 cell lines: 2 hybrid cell line, 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_TQ48	HAP1 SRPK2 (-)	Cancer cell line	Male
CVCL_YT54	CNE1 SRPK2 KO	Hybrid cell line
CVCL_YT55	CNE1 SRPK1/2 KO	Hybrid cell line

Clinical trials (associated diseases)

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