STK10
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Also known as LOKPRO2729
Summary
STK10 (serine/threonine kinase 10, HGNC:11388) is a protein-coding gene on chromosome 5q35.1, encoding Serine/threonine-protein kinase 10 (O94804). Serine/threonine-protein kinase involved in regulation of lymphocyte migration.
This gene encodes a member of the Ste20 family of serine/threonine protein kinases, and is similar to several known polo-like kinase kinases. The protein can associate with and phosphorylate polo-like kinase 1, and overexpression of a kinase-dead version of the protein interferes with normal cell cycle progression. The kinase can also negatively regulate interleukin 2 expression in T-cells via the mitogen activated protein kinase kinase 1 pathway.
Source: NCBI Gene 6793 — RefSeq curated summary.
At a glance
- GWAS associations: 6
- Clinical variants (ClinVar): 171 total
- Druggable target: yes — 79 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_005990
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:11388 |
| Approved symbol | STK10 |
| Name | serine/threonine kinase 10 |
| Location | 5q35.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | LOK, PRO2729 |
| Ensembl gene | ENSG00000072786 |
| Ensembl biotype | protein_coding |
| OMIM | 603919 |
| Entrez | 6793 |
Gene structure
Transcript identifiers
Ensembl transcripts: 24 — 10 protein_coding, 8 retained_intron, 6 protein_coding_CDS_not_defined
ENST00000176763, ENST00000517360, ENST00000517381, ENST00000517524, ENST00000517527, ENST00000517775, ENST00000518267, ENST00000519269, ENST00000519441, ENST00000519710, ENST00000520476, ENST00000521322, ENST00000522879, ENST00000522936, ENST00000523603, ENST00000523615, ENST00000877786, ENST00000877787, ENST00000877788, ENST00000877789, ENST00000877790, ENST00000916144, ENST00000916145, ENST00000916146
RefSeq mRNA: 1 — MANE Select: NM_005990
NM_005990
CCDS: CCDS34290
Canonical transcript exons
ENST00000176763 — 19 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000769446 | 172156624 | 172156788 |
| ENSE00000812846 | 172187887 | 172188224 |
| ENSE00000973051 | 172096426 | 172096560 |
| ENSE00000973052 | 172093412 | 172093960 |
| ENSE00000973055 | 172082326 | 172082505 |
| ENSE00000973060 | 172055588 | 172055776 |
| ENSE00000973061 | 172054569 | 172054694 |
| ENSE00000973062 | 172052929 | 172053042 |
| ENSE00001003610 | 172064720 | 172064812 |
| ENSE00001003619 | 172061139 | 172061268 |
| ENSE00001003620 | 172042079 | 172045022 |
| ENSE00001507187 | 172082961 | 172083084 |
| ENSE00001507188 | 172090232 | 172090362 |
| ENSE00003484309 | 172106620 | 172106814 |
| ENSE00003494266 | 172107780 | 172107852 |
| ENSE00003494555 | 172117481 | 172117630 |
| ENSE00003560084 | 172057349 | 172057473 |
| ENSE00003589902 | 172127373 | 172127421 |
| ENSE00003645837 | 172105656 | 172105737 |
Expression profiles
Bgee: expression breadth ubiquitous, 262 present calls, max score 98.83.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 29.9293 / max 1085.8611, expressed in 1794 samples.
FANTOM5 promoters (7 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 64854 | 21.0184 | 1778 |
| 64855 | 4.6442 | 1414 |
| 64853 | 3.7660 | 1062 |
| 64852 | 0.3482 | 142 |
| 64841 | 0.0582 | 20 |
| 64856 | 0.0581 | 13 |
| 64842 | 0.0362 | 11 |
Top tissues by expression
287 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| granulocyte | CL:0000094 | 98.83 | gold quality |
| sural nerve | UBERON:0015488 | 97.36 | gold quality |
| blood | UBERON:0000178 | 97.35 | gold quality |
| leukocyte | CL:0000738 | 96.98 | gold quality |
| monocyte | CL:0000576 | 96.93 | gold quality |
| mononuclear cell | CL:0000842 | 96.88 | gold quality |
| spleen | UBERON:0002106 | 96.01 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 95.95 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 95.80 | gold quality |
| cerebellar cortex | UBERON:0002129 | 95.77 | gold quality |
| bone marrow cell | CL:0002092 | 94.70 | gold quality |
| cerebellum | UBERON:0002037 | 93.85 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 93.07 | gold quality |
| lymph node | UBERON:0000029 | 92.94 | gold quality |
| vermiform appendix | UBERON:0001154 | 92.55 | gold quality |
| upper lobe of lung | UBERON:0008948 | 92.39 | gold quality |
| right lung | UBERON:0002167 | 91.59 | gold quality |
| bone marrow | UBERON:0002371 | 91.23 | gold quality |
| tibial nerve | UBERON:0001323 | 91.20 | gold quality |
| omental fat pad | UBERON:0010414 | 90.80 | gold quality |
| peritoneum | UBERON:0002358 | 90.73 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 90.07 | gold quality |
| left testis | UBERON:0004533 | 90.00 | gold quality |
| right testis | UBERON:0004534 | 89.81 | gold quality |
| skin of leg | UBERON:0001511 | 89.61 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 89.37 | gold quality |
| bone element | UBERON:0001474 | 89.08 | gold quality |
| caecum | UBERON:0001153 | 88.76 | gold quality |
| apex of heart | UBERON:0002098 | 88.56 | gold quality |
| testis | UBERON:0000473 | 88.30 | gold quality |
Single-cell (SCXA)
Detected in 5 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-6678 | yes | 9.48 |
| E-GEOD-110499 | no | 268.00 |
| E-MTAB-6379 | no | 265.25 |
| E-CURD-112 | no | 2.57 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
92 targeting STK10, 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-4283 | 100.00 | 66.42 | 2097 |
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-4692 | 100.00 | 67.32 | 2066 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-513A-5P | 100.00 | 69.77 | 2465 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-4514 | 99.99 | 67.10 | 1870 |
| HSA-MIR-1184 | 99.99 | 68.19 | 1458 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-9985 | 99.98 | 72.11 | 2939 |
| HSA-MIR-548N | 99.98 | 71.94 | 4170 |
| HSA-MIR-568 | 99.98 | 69.86 | 2084 |
| HSA-MIR-767-5P | 99.95 | 70.85 | 993 |
| HSA-MIR-185-3P | 99.95 | 67.01 | 1743 |
| HSA-MIR-6721-5P | 99.93 | 68.92 | 2981 |
| HSA-MIR-10527-5P | 99.91 | 72.28 | 3754 |
| HSA-MIR-6783-3P | 99.89 | 67.92 | 2059 |
| HSA-MIR-95-5P | 99.89 | 72.17 | 3973 |
| HSA-MIR-1343-3P | 99.89 | 66.78 | 1815 |
| HSA-MIR-7162-3P | 99.89 | 68.16 | 1682 |
| HSA-MIR-3140-3P | 99.88 | 68.47 | 2069 |
| HSA-MIR-3919 | 99.87 | 69.45 | 2489 |
| HSA-MIR-548D-3P | 99.87 | 70.67 | 4362 |
| HSA-MIR-4492 | 99.87 | 68.25 | 3611 |
| HSA-MIR-548BB-3P | 99.86 | 70.58 | 4354 |
Literature-anchored findings (GeneRIF, showing 9)
- Opposing roles of serine/threonine kinases MEKK1 and LOK in regulating the CD28 responsive element in T-cells (PMID:11903060)
- Stk10 is a novel polo-like kinase kinase that cooperates with hSlk to regulate Plk1 function in human cells (PMID:12639966)
- These studies identify a new ERM kinase of importance in lymphocytes and confirm the role of ezrin-radixin-moesin phosphorylation in regulating cell shape and motility. (PMID:19255442)
- genetic polymorphism is associated with aspirin-intolerant asthma in a Korean population (PMID:21905501)
- It was shown that lymphocyte-oriented and STE20 kinase were sufficient to restrict ezrin function to the apical domain. Both kinases were enriched in microvilli and locally activated there. (PMID:23209304)
- STK10 functions as a tumor suppressor gene, and dysfunction of STK10 activity either through polymorphism or somatic mutations may confer anti-apoptotic effects contributing to carcinogenesis. (PMID:23842845)
- The gene signature of OPA1, CTSA, NDUFA1, STK10 and PRDX1 was able to identify patients post-implant with a sensitivity of 91% and a specificity of 86% in discrimination between post-implant group and healthy controls. (PMID:27177495)
- Binding of phosphatidylinositol 4,5-biphosphate to ezrin induces a conformational change permitting the insertion of the LOK C-terminal domain to wedge apart the membrane and F-actin-binding domains of ezrin. The N-terminal LOK kinase domain can then access a site 40 residues distal from the consensus sequence that collectively direct phosphorylation of the appropriate threonine residue. (PMID:28430576)
- Systematic analysis of prognostic significance, functional enrichment and immune implication of STK10 in acute myeloid leukemia. (PMID:35501867)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | stk10 | ENSDARG00000101894 |
| mus_musculus | Stk10 | ENSMUSG00000020272 |
| rattus_norvegicus | Stk10 | ENSRNOG00000004217 |
Paralogs (35): MAP3K14 (ENSG00000006062), MAP4K3 (ENSG00000011566), MAP4K5 (ENSG00000012983), MAP2K3 (ENSG00000034152), SLK (ENSG00000065613), MAP4K4 (ENSG00000071054), PAK3 (ENSG00000077264), STRADB (ENSG00000082146), MAP3K1 (ENSG00000095015), STK4 (ENSG00000101109), PAK5 (ENSG00000101349), STK24 (ENSG00000102572), STK3 (ENSG00000104375), MAP4K1 (ENSG00000104814), MAP3K8 (ENSG00000107968), MAP2K6 (ENSG00000108984), NEK4 (ENSG00000114904), STK25 (ENSG00000115694), NRK (ENSG00000123572), PAK4 (ENSG00000130669), STK26 (ENSG00000134602), TAOK3 (ENSG00000135090), PAK6 (ENSG00000137843), MINK1 (ENSG00000141503), PAK1 (ENSG00000149269), TAOK2 (ENSG00000149930), TNIK (ENSG00000154310), TAOK1 (ENSG00000160551), MAP4K2 (ENSG00000168067), OXSR1 (ENSG00000172939), MAP3K19 (ENSG00000176601), PAK2 (ENSG00000180370), SBK2 (ENSG00000187550), STK39 (ENSG00000198648), STRADA (ENSG00000266173)
Protein
Protein identifiers
Serine/threonine-protein kinase 10 — O94804 (reviewed: O94804)
Alternative names: Lymphocyte-oriented kinase
All UniProt accessions (2): O94804, H0YB71
UniProt curated annotations — full annotation on UniProt →
Function. Serine/threonine-protein kinase involved in regulation of lymphocyte migration. Phosphorylates MSN, and possibly PLK1. Involved in regulation of lymphocyte migration by mediating phosphorylation of ERM proteins such as MSN. Acts as a negative regulator of MAP3K1/MEKK1. May also act as a cell cycle regulator by acting as a polo kinase kinase: mediates phosphorylation of PLK1 in vitro; however such data require additional evidences in vivo.
Subunit / interactions. Homodimer; homodimerization is required for activation segment autophosphorylation.
Subcellular location. Cell membrane.
Tissue specificity. Highly expressed in rapidly proliferating tissues (spleen, placenta, and peripheral blood leukocytes). Also expressed in brain, heart, skeletal muscle, colon, thymus, kidney, liver, small intestine and lung.
Post-translational modifications. Autophosphorylates following homodimerization, leading to activation of the protein.
Disease relevance. Testicular germ cell tumor (TGCT) [MIM:273300] A common malignancy in males representing 95% of all testicular neoplasms. TGCTs have various pathologic subtypes including: unclassified intratubular germ cell neoplasia, seminoma (including cases with syncytiotrophoblastic cells), spermatocytic seminoma, embryonal carcinoma, yolk sac tumor, choriocarcinoma, and teratoma. The disease may be caused by variants affecting the gene represented in this entry.
Activity regulation. Inhibited by the pyrrole-indolinone inhibitor SU11274 (K00593): intercalates between the ATP-binding Lys-65 and alpha-C glutamate (Glu-81), resulting in a partial disordering of the lysine side chain. Also specifically inhibited by erlotinib. Slightly inhibited by gefitinib.
Miscellaneous. Inhibition by erlotinib, an orally administered EGFR tyrosine kinase inhibitor used for treatment, enhances STK10-dependent lymphocytic responses, possibly leading to the aggravation of skin inflammation observed upon treatment by erlotinib.
Similarity. Belongs to the protein kinase superfamily. STE Ser/Thr protein kinase family. STE20 subfamily.
RefSeq proteins (1): NP_005981* (*=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 |
| IPR022165 | PKK | Family |
| IPR042743 | STK10_STKc | Domain |
| IPR051585 | STE20_Ser/Thr_Kinases | Family |
Pfam: PF00069, PF12474
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 (72 total): helix 15, sequence variant 12, modified residue 10, strand 9, region of interest 7, turn 5, compositionally biased region 4, sequence conflict 3, binding site 2, chain 1, domain 1, active site 1, mutagenesis site 1, coiled-coil region 1
Structure
Experimental structures (PDB)
14 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6EIM | X-RAY DIFFRACTION | 1.43 |
| 7QGP | X-RAY DIFFRACTION | 1.9 |
| 2J7T | X-RAY DIFFRACTION | 2 |
| 4EQU | X-RAY DIFFRACTION | 2 |
| 6HXF | X-RAY DIFFRACTION | 2.09 |
| 4BC6 | X-RAY DIFFRACTION | 2.2 |
| 5AJQ | X-RAY DIFFRACTION | 2.2 |
| 6GTT | X-RAY DIFFRACTION | 2.25 |
| 5OWR | X-RAY DIFFRACTION | 2.3 |
| 4AOT | X-RAY DIFFRACTION | 2.33 |
| 6I2Y | X-RAY DIFFRACTION | 2.56 |
| 4USE | X-RAY DIFFRACTION | 2.65 |
| 5OWQ | X-RAY DIFFRACTION | 2.7 |
| 4USD | X-RAY DIFFRACTION | 3.05 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O94804-F1 | 74.82 | 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 (1): 157 (proton acceptor)
Ligand- & substrate-binding residues (2): 42–50; 65
Post-translational modifications (10): 13, 20, 191, 438, 450, 454, 485, 514, 549, 952
Mutagenesis-validated functional residues (1):
| Position | Phenotype |
|---|---|
| 65 | loss of kinase activity. |
Function
Pathways and Gene Ontology
Reactome pathways
10 pathways
| ID | Pathway |
|---|---|
| R-HSA-6798695 | Neutrophil degranulation |
| R-HSA-8980692 | RHOA GTPase cycle |
| R-HSA-9013026 | RHOB GTPase cycle |
| R-HSA-9013106 | RHOC GTPase cycle |
| R-HSA-162582 | Signal Transduction |
| R-HSA-168249 | Innate Immune System |
| R-HSA-168256 | Immune System |
| R-HSA-194315 | Signaling by Rho GTPases |
| R-HSA-9012999 | RHO GTPase cycle |
| R-HSA-9716542 | Signaling by Rho GTPases, Miro GTPases and RHOBTB3 |
MSigDB gene sets: 312 (showing top):
MODULE_97, REACTOME_INNATE_IMMUNE_SYSTEM, CHIARADONNA_NEOPLASTIC_TRANSFORMATION_KRAS_DN, YAGI_AML_WITH_INV_16_TRANSLOCATION, GNF2_CASP8, GOCC_SECRETORY_GRANULE, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_DN, MODULE_182, GGGTGGRR_PAX4_03, GOBP_REGULATION_OF_LEUKOCYTE_MIGRATION, GOBP_REGULATION_OF_MONONUCLEAR_CELL_MIGRATION, GOBP_CELL_CELL_ADHESION, GOBP_LEUKOCYTE_MIGRATION, FINETTI_BREAST_CANCER_KINOME_GREEN, XU_RESPONSE_TO_TRETINOIN_AND_NSC682994_UP
GO Biological Process (5): protein phosphorylation (GO:0006468), intracellular signal transduction (GO:0035556), protein autophosphorylation (GO:0046777), lymphocyte aggregation (GO:0071593), regulation of lymphocyte migration (GO:2000401)
GO Molecular Function (10): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), identical protein binding (GO:0042802), protein homodimerization activity (GO:0042803), 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 (8): nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), nuclear body (GO:0016604), specific granule membrane (GO:0035579), extracellular exosome (GO:0070062), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-6 pathways:
| Category | Pathways |
|---|---|
| RHO GTPase cycle | 3 |
| Innate Immune System | 1 |
| Immune System | 1 |
| Signaling by Rho GTPases, Miro GTPases and RHOBTB3 | 1 |
| Signaling by Rho GTPases | 1 |
| Signal Transduction | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 4 |
| intracellular anatomical structure | 2 |
| protein kinase activity | 2 |
| phosphorylation | 1 |
| protein modification process | 1 |
| signal transduction | 1 |
| protein phosphorylation | 1 |
| leukocyte aggregation | 1 |
| regulation of mononuclear cell migration | 1 |
| lymphocyte migration | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| protein binding | 1 |
| identical protein binding | 1 |
| protein dimerization activity | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| nuclear lumen | 1 |
| cytoplasm | 1 |
| membrane | 1 |
| cell periphery | 1 |
| nucleoplasm | 1 |
| intracellular membraneless organelle | 1 |
| secretory granule membrane | 1 |
| specific granule | 1 |
| extracellular vesicle | 1 |
Protein interactions and networks
STRING
728 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| STK10 | EZR | P15311 | 494 |
| STK10 | MSN | P26038 | 464 |
| STK10 | RDX | P35241 | 464 |
| STK10 | RHOA | P06749 | 457 |
| STK10 | PLK1 | P53350 | 434 |
| STK10 | IFNG | P01579 | 420 |
| STK10 | ERBB2 | P04626 | 397 |
| STK10 | ERVMER34-1 | Q9H9K5 | 355 |
| STK10 | NHERF1 | O14745 | 348 |
| STK10 | C5orf52 | A6NGY3 | 323 |
| STK10 | UBTD2 | Q8WUN7 | 311 |
| STK10 | NR3C1 | P04150 | 297 |
| STK10 | NHERF2 | Q15599 | 289 |
| STK10 | ARHGEF37 | A1IGU5 | 283 |
| STK10 | ARHGEF38 | Q9NXL2 | 279 |
IntAct
23 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CFTR | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.710 |
| STK10 | STK10 | psi-mi:“MI:0407”(direct interaction) | 0.620 |
| MAP1LC3A | STK10 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| STK10 | NONO | psi-mi:“MI:0915”(physical association) | 0.400 |
| STK10 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| Xpo1 | IFT56 | psi-mi:“MI:0914”(association) | 0.350 |
| TANK | CNOT1 | psi-mi:“MI:0914”(association) | 0.350 |
| RIPK2 | CNOT1 | psi-mi:“MI:0914”(association) | 0.350 |
| CAMK4 | CNOT1 | psi-mi:“MI:0914”(association) | 0.350 |
| BORCS8 | SH3PXD2B | psi-mi:“MI:0914”(association) | 0.350 |
| TBC1D9 | SH3PXD2B | psi-mi:“MI:0914”(association) | 0.350 |
| MILR1 | SBNO1 | psi-mi:“MI:0914”(association) | 0.350 |
| MRPL53 | psi-mi:“MI:0914”(association) | 0.350 | |
| TBKBP1 | psi-mi:“MI:0914”(association) | 0.350 | |
| PSMD12 | psi-mi:“MI:0914”(association) | 0.350 | |
| LAMP1 | PIPSL | psi-mi:“MI:2364”(proximity) | 0.270 |
| CFTR | UBA6 | psi-mi:“MI:2364”(proximity) | 0.270 |
| CDH5 | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.270 |
BioGRID (74): STK10 (Affinity Capture-RNA), STK10 (Affinity Capture-RNA), STK10 (Affinity Capture-RNA), STK10 (Affinity Capture-RNA), KIFC1 (Co-fractionation), STK10 (Affinity Capture-MS), STK10 (Affinity Capture-RNA), STK10 (Affinity Capture-RNA), STK10 (Affinity Capture-RNA), STK10 (Proximity Label-MS), STK10 (Proximity Label-MS), STK10 (Affinity Capture-RNA), STK10 (Affinity Capture-MS), STK10 (Affinity Capture-MS), NONO (Proximity Label-MS)
ESM2 similar proteins: A0JMA8, A5WW21, A8WVU9, B0S6J3, B7ZR30, E1BK52, E7F187, E9PTG8, F1NBT0, G5EFD2, O01583, O08815, O43150, O54874, O54988, O55092, O55098, O88664, O94804, P46549, Q08CX1, Q0IHQ8, Q22908, Q3UU96, Q4G3H4, Q53UA7, Q5F2E8, Q5R4F3, Q5U245, Q5VT25, Q5ZJB4, Q619T5, Q6DD27, Q6GPK9, Q6NU21, Q7L7X3, Q7SIG6, Q7SY52, Q7TT49, Q7TT50
Diamond homologs: A0A194VNL2, A0A1S4CGX4, A4K2M3, A4K2P5, A4K2Q5, A4K2S1, A4K2T0, A4K2W5, A4K2Y1, A8XJW8, A9RWC9, A9S5R3, A9SR33, B0XPE4, C4YLK8, E1BK52, F1NBT0, G4N6Z6, G4NEB8, G5EDF7, O00506, O09110, O14733, O54748, O80396, O94804, O95819, P06784, P08018, P0CY25, P10506, P29678, P31938, P32490, P32491, P33886, P36506, P36507, P45985, P46734
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| STK10 | “up-regulates activity” | MSN | phosphorylation |
| STK10 | “up-regulates activity” | EZR | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
171 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 136 |
| Likely benign | 5 |
| Benign | 5 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3620 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 5:172045019:GAGC:G | acceptor_gain | 1.0000 |
| 5:172045020:AGC:A | acceptor_gain | 1.0000 |
| 5:172045020:AGCC:A | acceptor_loss | 1.0000 |
| 5:172045021:GC:G | acceptor_gain | 1.0000 |
| 5:172045022:CC:C | acceptor_gain | 1.0000 |
| 5:172045022:CCT:C | acceptor_loss | 1.0000 |
| 5:172045023:C:CC | acceptor_gain | 1.0000 |
| 5:172045023:CTA:C | acceptor_loss | 1.0000 |
| 5:172052924:GTTA:G | donor_loss | 1.0000 |
| 5:172052926:TAC:T | donor_loss | 1.0000 |
| 5:172052928:CCTT:C | donor_gain | 1.0000 |
| 5:172052931:T:A | donor_gain | 1.0000 |
| 5:172053039:CATT:C | acceptor_gain | 1.0000 |
| 5:172053041:TT:T | acceptor_gain | 1.0000 |
| 5:172053041:TTCTG:T | acceptor_loss | 1.0000 |
| 5:172053042:TCTGG:T | acceptor_loss | 1.0000 |
| 5:172053043:C:CC | acceptor_gain | 1.0000 |
| 5:172053043:CTGGA:C | acceptor_loss | 1.0000 |
| 5:172053044:T:G | acceptor_loss | 1.0000 |
| 5:172053049:C:CT | acceptor_gain | 1.0000 |
| 5:172053056:C:CT | acceptor_gain | 1.0000 |
| 5:172053056:C:T | acceptor_gain | 1.0000 |
| 5:172054566:TA:T | donor_loss | 1.0000 |
| 5:172054567:AC:A | donor_loss | 1.0000 |
| 5:172054568:C:CT | donor_loss | 1.0000 |
| 5:172054690:GAGAA:G | acceptor_gain | 1.0000 |
| 5:172054691:AGAA:A | acceptor_gain | 1.0000 |
| 5:172054692:GAA:G | acceptor_gain | 1.0000 |
| 5:172054693:AA:A | acceptor_gain | 1.0000 |
| 5:172054695:C:CC | acceptor_gain | 1.0000 |
AlphaMissense
6454 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 5:172083073:A:G | L566P | 1.000 |
| 5:172090325:C:G | R531P | 1.000 |
| 5:172090326:G:T | R531S | 1.000 |
| 5:172106674:A:T | V245D | 1.000 |
| 5:172106728:A:G | L227P | 1.000 |
| 5:172106740:A:G | L223P | 1.000 |
| 5:172106745:C:A | W221C | 1.000 |
| 5:172106745:C:G | W221C | 1.000 |
| 5:172106747:A:G | W221R | 1.000 |
| 5:172106747:A:T | W221R | 1.000 |
| 5:172106753:C:G | D219H | 1.000 |
| 5:172106797:A:T | V204D | 1.000 |
| 5:172106812:A:C | M199R | 1.000 |
| 5:172106812:A:G | M199T | 1.000 |
| 5:172106812:A:T | M199K | 1.000 |
| 5:172106814:C:A | W198C | 1.000 |
| 5:172106814:C:G | W198C | 1.000 |
| 5:172107781:A:G | W198R | 1.000 |
| 5:172107781:A:T | W198R | 1.000 |
| 5:172107784:A:C | Y197D | 1.000 |
| 5:172107784:A:G | Y197H | 1.000 |
| 5:172107786:G:T | P196H | 1.000 |
| 5:172107792:C:T | G194D | 1.000 |
| 5:172107793:C:G | G194R | 1.000 |
| 5:172107797:G:C | F192L | 1.000 |
| 5:172107797:G:T | F192L | 1.000 |
| 5:172107799:A:G | F192L | 1.000 |
| 5:172107844:C:G | G177R | 1.000 |
| 5:172107848:G:C | D175E | 1.000 |
| 5:172107848:G:T | D175E | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000033992 (5:172142280 C>A), RS1000038065 (5:172056360 G>C), RS1000064835 (5:172133580 G>A), RS1000070058 (5:172177270 G>C), RS1000082564 (5:172095875 A>G), RS1000096966 (5:172133941 G>C), RS1000105369 (5:172061242 C>T), RS1000137865 (5:172061039 A>C,T), RS1000142524 (5:172145496 C>T), RS1000145432 (5:172098755 T>G), RS1000159789 (5:172173543 G>A,T), RS1000174272 (5:172055746 G>A), RS1000187145 (5:172136868 C>T), RS1000190220 (5:172101081 C>T), RS1000197703 (5:172108811 G>T)
Disease associations
OMIM: gene MIM:603919 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
6 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST006658_10 | Longevity | 9.000000e-06 |
| GCST006979_480 | Heel bone mineral density | 2.000000e-11 |
| GCST007202_15 | High density lipoprotein cholesterol levels | 6.000000e-06 |
| GCST011066_4 | Motor fluctuations in levodopa treated Parkinson’s disease | 9.000000e-06 |
| GCST011108_2 | Colorectal cancer x fine particulate matter exposure levels interaction | 2.000000e-09 |
| GCST90002404_228 | Red cell distribution width | 2.000000e-21 |
EFO canonical traits (6, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0009270 | heel bone mineral density |
| EFO:0004612 | high density lipoprotein cholesterol measurement |
| EFO:0010747 | response to levodopa |
| EFO:0010749 | motor function measurement |
| EFO:0008255 | particulate matter air pollution measurement |
| EFO:0009188 | Red cell distribution width |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL3981 (SINGLE PROTEIN), CHEMBL4888459 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
79 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 469,629 (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 |
|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4 | 15,144 |
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1289494 | TIVOZANIB | 4 | 4,455 |
| CHEMBL1289601 | LENVATINIB | 4 | 8,784 |
| CHEMBL1289926 | AXITINIB | 4 | 15,732 |
| CHEMBL1336 | SORAFENIB | 4 | 86,060 |
| CHEMBL180022 | NERATINIB | 4 | 9,404 |
| CHEMBL2035187 | PACRITINIB | 4 | 3,345 |
| CHEMBL24828 | VANDETANIB | 4 | 42,230 |
| CHEMBL255863 | NILOTINIB | 4 | 38,627 |
| CHEMBL288441 | BOSUTINIB | 4 | 12,255 |
| CHEMBL3301607 | FILGOTINIB | 4 | 2,905 |
| CHEMBL3301610 | ABEMACICLIB | 4 | 7,045 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,395 |
| CHEMBL3545311 | BRIGATINIB | 4 | 5,634 |
| CHEMBL477772 | PAZOPANIB | 4 | 15,540 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL5416410 | DASATINIB | 4 | 655 |
| CHEMBL553 | ERLOTINIB | 4 | 108,300 |
| CHEMBL554 | LAPATINIB | 4 | |
| CHEMBL576982 | QUIZARTINIB | 4 | |
| CHEMBL601719 | CRIZOTINIB | 4 | |
| CHEMBL608533 | MIDOSTAURIN | 4 | |
| CHEMBL939 | GEFITINIB | 4 | |
| CHEMBL2087361 | ICOTINIB | 3 | |
| CHEMBL2105728 | CRENOLANIB | 3 | |
| CHEMBL217092 | SARACATINIB | 3 | |
| CHEMBL223360 | LINIFANIB | 3 | |
| CHEMBL270995 | BRIVANIB ALANINATE | 3 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — SLK subfamily
Most potent curated ligand interactions (2 total), top 2:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| DDR1/2 inhibitor 5n | Inhibition | 8.0 | pKd |
| bosutinib | Inhibitor | 7.28 | pIC50 |
Binding affinities (BindingDB)
1 measured of 2 human assays (2 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 3-[2-(cyclopropanecarbonylamino)-[1,3]thiazolo[5,4-b]pyridin-5-yl]-N-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]benzamide | KD | 57 nM | US-8765747: Fused 2-aminothiazole compounds |
ChEMBL bioactivities
255 potent at pChembl≥5 of 265 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.52 | Kd | 0.03 | nM | STAUROSPORINE |
| 10.43 | Kd | 0.037 | nM | STAUROSPORINE |
| 9.28 | Kd | 0.53 | nM | FORETINIB |
| 9.04 | Kd | 0.92 | nM | AST-487 |
| 8.52 | Kd | 3 | nM | UCN-01 |
| 8.24 | Kd | 5.7 | nM | LESTAURTINIB |
| 8.23 | Kd | 5.9 | nM | BAY-826 |
| 8.16 | IC50 | 6.93 | nM | STAUROSPORINE |
| 8.15 | Kd | 7.1 | nM | DORAMAPIMOD |
| 8.15 | Kd | 7 | nM | BOSUTINIB |
| 8.04 | IC50 | 9.01 | nM | STAUROSPORINE |
| 8.02 | Kd | 9.5 | nM | CHEMBL2148124 |
| 8.00 | Kd | 10 | nM | CHEMBL4168305 |
| 8.00 | Kd | 10 | nM | CHEMBL4571241 |
| 7.92 | IC50 | 12 | nM | CHEMBL156277 |
| 7.92 | Kd | 12 | nM | DORAMAPIMOD |
| 7.89 | Kd | 13 | nM | NERATINIB |
| 7.89 | Kd | 13 | nM | KW-2449 |
| 7.85 | Kd | 14 | nM | CHEMBL3688339 |
| 7.81 | IC50 | 15.6 | nM | STAUROSPORINE |
| 7.72 | Kd | 19 | nM | ERLOTINIB |
| 7.72 | Kd | 19 | nM | SUNITINIB |
| 7.66 | Kd | 22 | nM | CHEMBL1908396 |
| 7.64 | IC50 | 23 | nM | CHEMBL4875188 |
| 7.64 | Kd | 23 | nM | CEDIRANIB |
| 7.58 | Ki | 26 | nM | CHEMBL4875188 |
| 7.49 | Kd | 32.12 | nM | CHEMBL5653589 |
| 7.46 | Ki | 35 | nM | CHEMBL4878325 |
| 7.46 | ED50 | 35.08 | nM | CHEMBL5653589 |
| 7.36 | Kd | 44 | nM | CRIZOTINIB |
| 7.34 | Ki | 46 | nM | CHEMBL156277 |
| 7.33 | Ki | 47 | nM | CHEMBL4877889 |
| 7.33 | IC50 | 47 | nM | REBASTINIB |
| 7.28 | IC50 | 52 | nM | BOSUTINIB |
| 7.24 | Kd | 57 | nM | CHEMBL5084426 |
| 7.22 | IC50 | 60 | nM | CHEMBL4878325 |
| 7.22 | Kd | 60 | nM | RAF-265 |
| 7.21 | Ki | 61 | nM | CHEMBL4856751 |
| 7.16 | Kd | 70 | nM | R-406 |
| 7.16 | Kd | 69 | nM | GSK-461364 |
| 7.15 | Kd | 71 | nM | DECERNOTINIB |
| 7.14 | Ki | 73 | nM | CHEMBL157089 |
| 7.12 | Ki | 76 | nM | CHEMBL4855513 |
| 7.11 | Kd | 77 | nM | CHEMBL1241674 |
| 7.09 | Kd | 81 | nM | VANDETANIB |
| 7.09 | Kd | 82 | nM | AT-9283 |
| 7.09 | Kd | 82 | nM | TAE-684 |
| 7.08 | Kd | 83 | nM | ERLOTINIB |
| 7.08 | Ki | 84 | nM | CHEMBL4869745 |
| 7.08 | Kd | 84 | nM | PAZOPANIB |
PubChem BioAssay actives
247 with measured affinity, of 1298 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (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 | 256604: Average Binding Constant for STK10; NA=Not Active at 10 uM | kd | <0.0001 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 625030: Binding constant for LOK kinase domain | kd | 0.0005 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 435677: Binding constant for LOK kinase domain | kd | 0.0009 | uM |
| (2S,3R,4R,6R,18S)-18-hydroxy-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 | 1425177: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0030 | 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 | 507591: Binding affinity to LOK | kd | 0.0057 | uM |
| 3-cyano-N-[2,4-dimethyl-5-(6-pyridin-3-ylimidazo[2,1-e]pyrazol-1-yl)phenyl]-5-(pentafluoro-lambda6-sulfanyl)benzamide | 2155086: Binding affinity to LOK (unknown origin) assessed as dissociation constant by KINOME scan assay | kd | 0.0059 | uM |
| Bosutinib | 625030: Binding constant for LOK kinase domain | kd | 0.0070 | uM |
| 1-[3-tert-butyl-1-(4-methylphenyl)pyrazol-5-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | 256604: Average Binding Constant for STK10; NA=Not Active at 10 uM | kd | 0.0071 | uM |
| N-[4-(6,7-dimethoxyquinazolin-4-yl)oxy-3-fluorophenyl]-6-ethyl-1,2-dimethyl-4-oxoquinoline-3-carboxamide | 1626965: Binding affinity to human LOK | kd | 0.0100 | uM |
| 3-(2-imidazo[1,2-a]pyrazin-3-ylethynyl)-N-[3-[(4-methylpiperazin-1-yl)methyl]-5-(trifluoromethyl)phenyl]-4-propan-2-ylbenzamide | 1356736: Binding affinity to human LOK | kd | 0.0100 | uM |
| N-[3-[2-[4-(2-aminoethoxy)anilino]quinazolin-6-yl]-4-methylphenyl]-3-(trifluoromethyl)benzamide | 1799897: Fluorescence Assay from Article 10.1021/cb300623a: “A Hexylchloride-Based Catch-and-Release System for Chemical Proteomic Applications.” | ic50 | 0.0100 | uM |
| 3-(3-chloroanilino)-4-(2-methoxyphenyl)pyrrole-2,5-dione | 1779843: Inhibition of STK10 (unknown origin) expressed in Sf9 cells assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method | ic50 | 0.0120 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 625030: Binding constant for LOK kinase domain | kd | 0.0130 | uM |
| Neratinib | 625030: Binding constant for LOK kinase domain | kd | 0.0130 | uM |
| 1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone | 1425177: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0140 | uM |
| Erlotinib | 435677: Binding constant for LOK kinase domain | kd | 0.0190 | uM |
| Sunitinib | 435677: Binding constant for LOK kinase domain | kd | 0.0190 | uM |
| 1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea | 625030: Binding constant for LOK kinase domain | kd | 0.0220 | uM |
| 3-[[4-(2-methoxyphenyl)-2,5-dioxopyrrol-3-yl]amino]benzonitrile | 1779843: Inhibition of STK10 (unknown origin) expressed in Sf9 cells assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method | ic50 | 0.0230 | uM |
| 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline | 625030: Binding constant for LOK kinase domain | kd | 0.0230 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2149507: Binding affinity to human STK10 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0321 | uM |
| 3-[[4-(4-bromo-2-methoxyphenyl)-2,5-dioxopyrrol-3-yl]amino]benzonitrile | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0350 | uM |
| Crizotinib | 625030: Binding constant for LOK kinase domain | kd | 0.0440 | uM |
| 3-(2-methoxyphenyl)-4-(naphthalen-1-ylamino)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0470 | uM |
| 4-[4-[(3-tert-butyl-1-quinolin-6-ylpyrazol-5-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | 2168214: Inhibition of human LOK preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis | ic50 | 0.0470 | uM |
| 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]benzimidazol-2-amine | 435677: Binding constant for LOK kinase domain | kd | 0.0600 | uM |
| 3-[[4-(5-bromo-2-methoxyphenyl)-2,5-dioxopyrrol-3-yl]amino]benzonitrile | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0610 | uM |
| 5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide | 625030: Binding constant for LOK kinase domain | kd | 0.0690 | uM |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | 625030: Binding constant for LOK kinase domain | kd | 0.0700 | uM |
| (2R)-2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-N-(2,2,2-trifluoroethyl)butanamide | 1425177: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0710 | uM |
| 3-(3-chloro-4-hydroxyanilino)-4-(2-methoxyphenyl)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0730 | uM |
| 3-(3-fluoroanilino)-4-(2-methoxyphenyl)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0760 | uM |
| 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol | 625030: Binding constant for LOK kinase domain | kd | 0.0770 | uM |
| Vandetanib | 435677: Binding constant for LOK kinase domain | kd | 0.0810 | uM |
| 1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea | 1425177: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0820 | uM |
| 5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine | 625030: Binding constant for LOK kinase domain | kd | 0.0820 | uM |
| Pazopanib | 435677: Binding constant for LOK kinase domain | kd | 0.0840 | uM |
| 3-(1,3-benzodioxol-5-ylamino)-4-(2-methoxyphenyl)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0840 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 625030: Binding constant for LOK kinase domain | kd | 0.0870 | uM |
| N-[4-[4-(3-cyanoanilino)-2,5-dioxopyrrol-3-yl]-3-methoxyphenyl]-2-methylpropanamide | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.0880 | uM |
| 5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid | 1425177: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry. | kd | 0.0960 | uM |
| 3-[3-[4-(1-methylindol-3-yl)-2,5-dioxopyrrol-3-yl]indol-1-yl]propyl carbamimidothioate | 1779843: Inhibition of STK10 (unknown origin) expressed in Sf9 cells assessed as transfer of radiolabelled phosphate group from ATP by reaction biology method | ic50 | 0.0990 | uM |
| 3-(2-methoxyphenyl)-4-(3-methylsulfanylanilino)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.1100 | uM |
| 3-(2-methoxyphenyl)-4-(quinolin-6-ylamino)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.1100 | uM |
| 3-[(4-naphthalen-1-yl-2,5-dioxopyrrol-3-yl)amino]benzonitrile | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.1100 | uM |
| 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 435677: Binding constant for LOK kinase domain | kd | 0.1100 | uM |
| (E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide | 256604: Average Binding Constant for STK10; NA=Not Active at 10 uM | kd | 0.1100 | uM |
| 3-(4-methoxyanilino)-4-(2-methoxyphenyl)pyrrole-2,5-dione | 1779840: Binding affinity human STK10 by binding displacement assay | ki | 0.1200 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 435677: Binding constant for LOK kinase domain | kd | 0.1200 | uM |
| Brigatinib | 2182831: Inhibition of human STK10 using RLGRDKYKTLRQIRQ as substrate in presence of [gamma33P]-ATP by HotSpot assay | ic50 | 0.1230 | uM |
CTD chemical–gene interactions
47 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Tobacco Smoke Pollution | decreases expression, increases expression, affects expression | 3 |
| Benzo(a)pyrene | affects methylation, decreases expression | 2 |
| Estradiol | affects cotreatment, increases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| FR900359 | decreases phosphorylation | 1 |
| bisphenol F | increases expression | 1 |
| testosterone enanthate | affects expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| arsenite | affects binding, decreases reaction | 1 |
| sodium arsenite | increases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| potassium chromate(VI) | affects cotreatment, decreases expression | 1 |
| coumarin | affects phosphorylation | 1 |
| N,N,N’,N’-tetrakis(2-pyridylmethyl)ethylenediamine | decreases expression | 1 |
| epigallocatechin gallate | affects cotreatment, decreases expression | 1 |
| azoxystrobin | decreases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| calfactant | affects cotreatment, decreases expression | 1 |
| bisphenol B | increases expression | 1 |
| abrine | increases expression | 1 |
| bisphenol S | affects cotreatment, increases methylation | 1 |
| picoxystrobin | decreases expression | 1 |
| Sunitinib | increases expression | 1 |
| Fulvestrant | affects cotreatment, increases methylation | 1 |
| Acetaminophen | increases expression | 1 |
| Aspirin | affects response to substance | 1 |
| Caffeine | decreases phosphorylation | 1 |
| Ethyl Methanesulfonate | increases expression | 1 |
| Ivermectin | decreases expression | 1 |
| Methapyrilene | increases methylation | 1 |
ChEMBL screening assays
308 unique, capped per target: 308 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1004492 | Binding | Binding affinity to human recombinant LOK expressed in Escherichia coli assessed as thermal shift by differential scanning fluorimetry | Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone. — Bioorg Med Chem |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B2HM | Abcam HeLa STK10 KO | Cancer cell line | Female |
| CVCL_TQ69 | HAP1 STK10 (-) 1 | Cancer cell line | Male |
| CVCL_TQ70 | HAP1 STK10 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Targeted by drugs: Bosutinib