STK16
gene geneOn this page
Also known as MPSK1PKL12MPSK
Summary
STK16 (serine/threonine kinase 16, HGNC:11394) is a protein-coding gene on chromosome 2q35, encoding Serine/threonine-protein kinase 16 (O75716). Membrane-associated protein kinase that phosphorylates on serine and threonine residues.
Predicted to enable protein serine/threonine kinase activity. Involved in protein autophosphorylation. Located in cytosol; nuclear body; and plasma membrane.
Source: NCBI Gene 8576 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 60 total — 1 likely-pathogenic
- Druggable target: yes — 35 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001330213
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:11394 |
| Approved symbol | STK16 |
| Name | serine/threonine kinase 16 |
| Location | 2q35 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | MPSK1, PKL12, MPSK |
| Ensembl gene | ENSG00000115661 |
| Ensembl biotype | protein_coding |
| OMIM | 604719 |
| Entrez | 8576 |
Gene structure
Transcript identifiers
Ensembl transcripts: 20 — 12 protein_coding, 7 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000396738, ENST00000409260, ENST00000409516, ENST00000409638, ENST00000409743, ENST00000461417, ENST00000475342, ENST00000475696, ENST00000478018, ENST00000486813, ENST00000491697, ENST00000496443, ENST00000496800, ENST00000875262, ENST00000875263, ENST00000875264, ENST00000875265, ENST00000913739, ENST00000913740, ENST00000913741
RefSeq mRNA: 4 — MANE Select: NM_001330213
NM_001008910, NM_001330213, NM_001330214, NM_001330215
CCDS: CCDS42822, CCDS82573, CCDS86921
Canonical transcript exons
ENST00000396738 — 8 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001811654 | 219245479 | 219245796 |
| ENSE00001819845 | 219248421 | 219250337 |
| ENSE00003522107 | 219247415 | 219247535 |
| ENSE00003575220 | 219248193 | 219248314 |
| ENSE00003606757 | 219245896 | 219246085 |
| ENSE00003624428 | 219247113 | 219247246 |
| ENSE00003684484 | 219246657 | 219246876 |
| ENSE00003692589 | 219247662 | 219247757 |
Expression profiles
Bgee: expression breadth ubiquitous, 192 present calls, max score 93.11.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 15.5476 / max 133.8733, expressed in 1808 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 25433 | 15.5476 | 1808 |
Top tissues by expression
281 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| mucosa of transverse colon | UBERON:0004991 | 93.11 | gold quality |
| body of pancreas | UBERON:0001150 | 92.73 | gold quality |
| right lobe of liver | UBERON:0001114 | 92.72 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 92.20 | gold quality |
| islet of Langerhans | UBERON:0000006 | 92.18 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 92.12 | gold quality |
| granulocyte | CL:0000094 | 92.00 | gold quality |
| right adrenal gland | UBERON:0001233 | 91.99 | gold quality |
| stromal cell of endometrium | CL:0002255 | 91.93 | gold quality |
| body of stomach | UBERON:0001161 | 91.85 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 91.50 | gold quality |
| left adrenal gland | UBERON:0001234 | 91.40 | gold quality |
| right testis | UBERON:0004534 | 91.38 | gold quality |
| left testis | UBERON:0004533 | 91.34 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 90.92 | gold quality |
| transverse colon | UBERON:0001157 | 90.80 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 90.57 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 90.55 | gold quality |
| adenohypophysis | UBERON:0002196 | 90.43 | gold quality |
| metanephros cortex | UBERON:0010533 | 90.41 | gold quality |
| apex of heart | UBERON:0002098 | 90.19 | gold quality |
| rectum | UBERON:0001052 | 90.14 | gold quality |
| minor salivary gland | UBERON:0001830 | 90.02 | gold quality |
| pancreas | UBERON:0001264 | 89.93 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 89.76 | gold quality |
| prefrontal cortex | UBERON:0000451 | 89.75 | gold quality |
| lower esophagus | UBERON:0013473 | 89.72 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 89.72 | gold quality |
| gall bladder | UBERON:0002110 | 89.66 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 89.42 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 3.46 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
86 targeting STK16, 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-4476 | 100.00 | 68.18 | 2030 |
| HSA-MIR-6876-5P | 100.00 | 67.68 | 2126 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-6888-3P | 99.97 | 65.95 | 1170 |
| HSA-MIR-8075 | 99.97 | 67.20 | 962 |
| HSA-MIR-589-3P | 99.91 | 69.62 | 2088 |
| HSA-MIR-6783-3P | 99.89 | 67.92 | 2059 |
| HSA-MIR-1343-3P | 99.89 | 66.78 | 1815 |
| HSA-MIR-1321 | 99.84 | 65.30 | 1811 |
| HSA-MIR-4739 | 99.84 | 65.25 | 1832 |
| HSA-MIR-4756-5P | 99.84 | 64.98 | 1809 |
| HSA-MIR-4658 | 99.77 | 64.94 | 514 |
| HSA-MIR-6790-5P | 99.77 | 65.24 | 505 |
| HSA-MIR-1976 | 99.74 | 65.48 | 1127 |
| HSA-MIR-4755-5P | 99.71 | 70.34 | 2716 |
| HSA-MIR-5006-3P | 99.71 | 70.26 | 2728 |
| HSA-MIR-3659 | 99.70 | 67.97 | 694 |
| HSA-MIR-646 | 99.68 | 67.84 | 1645 |
| HSA-MIR-5004-5P | 99.68 | 66.63 | 1294 |
| HSA-MIR-298 | 99.63 | 67.56 | 1916 |
| HSA-MIR-4743-3P | 99.62 | 68.12 | 2095 |
| HSA-MIR-1249-5P | 99.61 | 66.55 | 2049 |
| HSA-MIR-6797-5P | 99.61 | 66.55 | 2084 |
| HSA-MIR-7106-5P | 99.53 | 67.47 | 3574 |
| HSA-MIR-4441 | 99.49 | 66.56 | 3216 |
| HSA-MIR-143-3P | 99.49 | 69.05 | 1457 |
| HSA-MIR-4770 | 99.49 | 69.09 | 1451 |
| HSA-MIR-1224-5P | 99.48 | 65.59 | 803 |
| HSA-MIR-1275 | 99.47 | 67.90 | 2749 |
| HSA-MIR-516A-3P | 99.46 | 67.96 | 1378 |
Literature-anchored findings (GeneRIF, showing 6)
- The Endogenous STK16 subcellular localization was evaluated by indirect immunofluorescence in NRK cells, demonstrating a Golgi-associated pattern that appears to be independent of signals provided by integrin pathways. (PMID:16310770)
- MAL2 and STK16 function to sort secretory soluble cargo into the constitutive secretory pathway in hepatocytes. (PMID:25084525)
- we revealed STK16 as a novel actin binding protein that resides in the Golgi, which regulates actin dynamics to control Golgi structure and participate in cell cycle progression. (PMID:28294156)
- Exosomes from M1-polarized macrophages promote apoptosis in lung adenocarcinoma via the miR-181a-5p/ETS1/STK16 axis. (PMID:35092121)
- STK16 promoted colorectal cancer progress in a c-MYC signaling-dependent manner. (PMID:38622518)
- Serine/Threonine kinase 16 phosphorylates STAT3 and confers a JAK2-Inhibition resistance phenotype in triple-negative breast cancer. (PMID:38723720)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | stk16 | ENSDARG00000037777 |
| mus_musculus | Stk16 | ENSMUSG00000026201 |
| rattus_norvegicus | Stk16 | ENSRNOG00000019294 |
| drosophila_melanogaster | CG1227 | FBGN0037491 |
Paralogs (2): AAK1 (ENSG00000115977), BMP2K (ENSG00000138756)
Protein
Protein identifiers
Serine/threonine-protein kinase 16 — O75716 (reviewed: O75716)
Alternative names: Myristoylated and palmitoylated serine/threonine-protein kinase, Protein kinase PKL12, TGF-beta-stimulated factor 1, Tyrosine-protein kinase STK16, hPSK
All UniProt accessions (4): B4DPS1, O75716, B8ZZI5, B8ZZN3
UniProt curated annotations — full annotation on UniProt →
Function. Membrane-associated protein kinase that phosphorylates on serine and threonine residues. In vitro substrates include DRG1, ENO1 and EIF4EBP1. Also autophosphorylates. May be involved in secretory vesicle trafficking or intracellular signaling. May have a role in regulating stromal-epithelial interactions that occur during ductal morphogenesis in the mammary gland. May be involved in TGF-beta signaling. Able to autophosphorylate on Tyr residue; it is however unclear whether it has tyrosine-protein kinase toward other proteins.
Subunit / interactions. Monomer. Interacts with DRG1 (via its N-terminal); the interaction phosphorylates DRG1.
Subcellular location. Cytoplasm. Perinuclear region. Membrane.
Tissue specificity. Ubiquitously expressed at very low levels.
Post-translational modifications. Mainly autophosphorylated on serine/threonine residues. Also autophosphorylated on Tyr-198. It is uncertain whether palmitoylation is on Cys-6 and/or Cys-8.
Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family.
RefSeq proteins (4): NP_001008910, NP_001317142, NP_001317143, NP_001317144 (=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 |
| IPR052239 | Ser/Thr-specific_kinases | Family |
Pfam: PF00069
Enzyme classification (BRENDA):
- EC 2.7.11.1 — non-specific serine/threonine protein kinase (BRENDA: 71 organisms, 682 substrates, 228 inhibitors, 23 Km, 6 kcat entries)
Substrate kinetics (BRENDA)
8 substrates with measured Km, best-characterized 8. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | 0.0007–0.64 | 11 |
| KKRAARATSNVFA | 0.013–0.045 | 3 |
| PAH1 PHOSPHATIDATE PHOSPHATASE | 0.0002 | 2 |
| RRRLSSLRA | 0.0036–0.0037 | 2 |
| GTP | 0.46 | 1 |
| KKRAARASSNVFA | 0.02 | 1 |
| LYS-LYS-PHE-ASN-ARG-THR-LEU-SER-VAL-ALA | 0.0093 | 1 |
| MYELIN BASIC PROTEIN | 0.145 | 1 |
Catalyzed reactions (Rhea), 3 shown:
- L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)
- 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 (52 total): helix 13, strand 11, sequence variant 5, sequence conflict 5, lipid moiety-binding region 3, mutagenesis site 3, modified residue 3, turn 2, binding site 2, initiator methionine 1, chain 1, domain 1, region of interest 1, active site 1
Structure
Experimental structures (PDB)
1 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2BUJ | X-RAY DIFFRACTION | 2.6 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O75716-F1 | 93.41 | 0.88 |
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): 148 (proton acceptor)
Ligand- & substrate-binding residues (2): 26–34; 49
Post-translational modifications (6): 2, 6, 8, 185, 197, 198
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 2 | loss of myristoylation. |
| 6 | loss of palmitoylation. |
| 8 | loss of palmitoylation. |
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 100 (showing top):
RNGTGGGC_UNKNOWN, GOBP_RESPONSE_TO_TRANSFORMING_GROWTH_FACTOR_BETA, GOCC_GOLGI_ASSOCIATED_VESICLE, CREB_Q2_01, GOBP_RESPONSE_TO_GROWTH_FACTOR, USF_02, HAMAI_APOPTOSIS_VIA_TRAIL_DN, GOBP_PROTEIN_AUTOPHOSPHORYLATION, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY, GOMF_NON_MEMBRANE_SPANNING_PROTEIN_TYROSINE_KINASE_ACTIVITY, TCANNTGAY_SREBP1_01, GOMF_PROTEIN_SERINE_THREONINE_KINASE_ACTIVITY, GOMF_SEQUENCE_SPECIFIC_DNA_BINDING, GOMF_ADENYL_NUCLEOTIDE_BINDING
GO Biological Process (4): positive regulation of transcription by RNA polymerase II (GO:0045944), protein autophosphorylation (GO:0046777), cellular response to transforming growth factor beta stimulus (GO:0071560), protein phosphorylation (GO:0006468)
GO Molecular Function (11): RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), protein serine/threonine kinase activity (GO:0004674), non-membrane spanning protein tyrosine kinase activity (GO:0004715), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein tyrosine kinase activity (GO:0004713), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (9): nucleoplasm (GO:0005654), cytoplasm (GO:0005737), Golgi apparatus (GO:0005794), Golgi-associated vesicle (GO:0005798), cytosol (GO:0005829), plasma membrane (GO:0005886), nuclear body (GO:0016604), perinuclear region of cytoplasm (GO:0048471), membrane (GO:0016020)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 5 |
| protein kinase activity | 3 |
| cytoplasm | 3 |
| regulation of transcription by RNA polymerase II | 1 |
| transcription by RNA polymerase II | 1 |
| positive regulation of DNA-templated transcription | 1 |
| protein phosphorylation | 1 |
| cellular response to growth factor stimulus | 1 |
| response to transforming growth factor beta | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| RNA polymerase II transcription regulatory region sequence-specific DNA binding | 1 |
| cis-regulatory region sequence-specific DNA binding | 1 |
| protein tyrosine kinase activity | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 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 |
| intracellular anatomical structure | 1 |
| endomembrane system | 1 |
| intracellular membrane-bounded organelle | 1 |
| cytoplasmic vesicle | 1 |
| membrane | 1 |
| cell periphery | 1 |
| nucleoplasm | 1 |
| intracellular membraneless organelle | 1 |
Protein interactions and networks
STRING
1105 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| STK16 | NPPC | P23582 | 651 |
| STK16 | UGT2B7 | P16662 | 548 |
| STK16 | DRG1 | Q9Y295 | 526 |
| STK16 | GCK | P35557 | 491 |
| STK16 | CSNK1G1 | Q9HCP0 | 467 |
| STK16 | HNF1A | P20823 | 455 |
| STK16 | FOXH1 | O75593 | 434 |
| STK16 | LHX3 | Q9UBR4 | 426 |
| STK16 | SERPINE1 | P05121 | 424 |
| STK16 | SRSF1 | Q07955 | 400 |
| STK16 | RIOK1 | Q9BRS2 | 393 |
| STK16 | GATA5 | Q9BWX5 | 389 |
| STK16 | ACIN1 | Q9UKV3 | 389 |
| STK16 | PCBD1 | P61457 | 386 |
| STK16 | SLCO1A2 | P46721 | 384 |
IntAct
435 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| STK16 | KCTD17 | psi-mi:“MI:0915”(physical association) | 0.780 |
| KCTD17 | STK16 | psi-mi:“MI:0915”(physical association) | 0.780 |
| TRIM42 | STK16 | psi-mi:“MI:0915”(physical association) | 0.720 |
| SAXO1 | STK16 | psi-mi:“MI:0915”(physical association) | 0.720 |
| EFEMP2 | STK16 | psi-mi:“MI:0915”(physical association) | 0.720 |
| KRTAP10-8 | STK16 | psi-mi:“MI:0915”(physical association) | 0.720 |
| INCA1 | STK16 | psi-mi:“MI:0915”(physical association) | 0.720 |
| STK16 | PLSCR3 | psi-mi:“MI:0915”(physical association) | 0.720 |
| STK16 | EFEMP2 | psi-mi:“MI:0915”(physical association) | 0.720 |
| STK16 | KRTAP10-8 | psi-mi:“MI:0915”(physical association) | 0.720 |
| STK16 | INCA1 | psi-mi:“MI:0915”(physical association) | 0.720 |
| PLSCR3 | STK16 | psi-mi:“MI:0915”(physical association) | 0.720 |
| RPIA | STK16 | psi-mi:“MI:0915”(physical association) | 0.670 |
| MIIP | STK16 | psi-mi:“MI:0915”(physical association) | 0.670 |
| KCTD14 | STK16 | psi-mi:“MI:0915”(physical association) | 0.670 |
| STK16 | MIIP | psi-mi:“MI:0915”(physical association) | 0.670 |
| STK16 | KCTD14 | psi-mi:“MI:0915”(physical association) | 0.670 |
| STK16 | RPIA | psi-mi:“MI:0915”(physical association) | 0.670 |
BioGRID (182): STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), STK16 (Two-hybrid), DNAJA3 (Two-hybrid), CALCOCO2 (Two-hybrid)
ESM2 similar proteins: A0A5B9GBF0, A1CPG7, A1D2C9, A1IVT7, A2BD05, A2QRF6, B0XR80, D3ZBE5, G1XJZ4, G5EDF7, G5EFM9, M1T7M3, O09110, O75716, O88697, P0CP69, P21708, P26696, P27361, P28482, P45985, P46196, P46734, P47809, P52564, P57760, P59895, P70236, Q0D0P5, Q0U4L8, Q1DUU8, Q1KTF2, Q2WFL5, Q4PC06, Q4W6D3, Q4WSF6, Q52PH6, Q56R42, Q5E9X2, Q63844
Diamond homologs: A0QNG1, A5D791, A5GFW1, A5TY84, A5U3A3, A5U3A6, A8XJQ6, B0BBT2, O14965, O75716, P0A5S5, P0DPS8, P0DPS9, P18652, P33973, P38070, P41808, P53599, P53739, P54666, P54737, P54744, P57760, P57993, P59241, P9WI70, P9WI71, P9WI74, P9WI75, P9WI76, P9WI77, P9WI78, P9WI79, P9WI80, P9WI81, Q04J43, Q0WPH8, Q255D2, Q2TA06, Q3KM61
SIGNOR signaling
4 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| STK16 | unknown | STK16 | phosphorylation |
| STK16 | unknown | DRG1 | phosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 77 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 |
|---|---|---|---|
| Keratinization | 10 | 12.7× | 1e-06 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| negative regulation of gene expression | 7 | 7.8× | 1e-02 |
| protein phosphorylation | 7 | 7.7× | 1e-02 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
60 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 47 |
| Likely benign | 1 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 2578200 | NM_006000.3(TUBA4A):c.313C>T (p.Arg105Cys) | Likely pathogenic |
SpliceAI
1346 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:219245891:TCCA:T | acceptor_loss | 1.0000 |
| 2:219245894:A:AC | acceptor_loss | 1.0000 |
| 2:219245894:A:AG | acceptor_gain | 1.0000 |
| 2:219245894:AGCAT:A | acceptor_gain | 1.0000 |
| 2:219245895:G:GG | acceptor_gain | 1.0000 |
| 2:219245895:GC:G | acceptor_gain | 1.0000 |
| 2:219245895:GCA:G | acceptor_gain | 1.0000 |
| 2:219245895:GCAT:G | acceptor_gain | 1.0000 |
| 2:219245895:GCATG:G | acceptor_gain | 1.0000 |
| 2:219246049:A:AG | donor_gain | 1.0000 |
| 2:219246081:GAGGG:G | donor_gain | 1.0000 |
| 2:219246083:GGG:G | donor_gain | 1.0000 |
| 2:219246084:GGG:G | donor_gain | 1.0000 |
| 2:219246647:T:TA | acceptor_gain | 1.0000 |
| 2:219246655:A:AG | acceptor_gain | 1.0000 |
| 2:219246655:AGT:A | acceptor_gain | 1.0000 |
| 2:219246655:AGTG:A | acceptor_gain | 1.0000 |
| 2:219246656:G:GG | acceptor_gain | 1.0000 |
| 2:219246656:GT:G | acceptor_gain | 1.0000 |
| 2:219246656:GTG:G | acceptor_gain | 1.0000 |
| 2:219246656:GTGG:G | acceptor_gain | 1.0000 |
| 2:219246835:GGTGC:G | donor_gain | 1.0000 |
| 2:219246836:GTGC:G | donor_gain | 1.0000 |
| 2:219246837:TGCT:T | donor_gain | 1.0000 |
| 2:219247411:ACAG:A | acceptor_loss | 1.0000 |
| 2:219247412:CA:C | acceptor_loss | 1.0000 |
| 2:219247413:A:AG | acceptor_gain | 1.0000 |
| 2:219247413:AG:A | acceptor_loss | 1.0000 |
| 2:219247414:G:GG | acceptor_gain | 1.0000 |
| 2:219247414:G:GT | acceptor_loss | 1.0000 |
AlphaMissense
2001 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:219246717:G:C | K49N | 1.000 |
| 2:219246717:G:T | K49N | 1.000 |
| 2:219246661:T:C | F31L | 0.999 |
| 2:219246663:C:A | F31L | 0.999 |
| 2:219246663:C:G | F31L | 0.999 |
| 2:219247417:A:C | D148A | 0.999 |
| 2:219247417:A:T | D148V | 0.999 |
| 2:219247418:C:A | D148E | 0.999 |
| 2:219247418:C:G | D148E | 0.999 |
| 2:219247424:G:C | K150N | 0.999 |
| 2:219247424:G:T | K150N | 0.999 |
| 2:219247435:T:A | I154K | 0.999 |
| 2:219247471:A:T | D166V | 0.999 |
| 2:219247472:C:A | D166E | 0.999 |
| 2:219247472:C:G | D166E | 0.999 |
| 2:219247696:G:C | R199P | 0.999 |
| 2:219247755:T:A | W219R | 0.999 |
| 2:219247755:T:C | W219R | 0.999 |
| 2:219248479:C:A | R280S | 0.999 |
| 2:219246713:T:C | L48P | 0.998 |
| 2:219246715:A:G | K49E | 0.998 |
| 2:219246716:A:T | K49M | 0.998 |
| 2:219247417:A:G | D148G | 0.998 |
| 2:219247422:A:G | K150E | 0.998 |
| 2:219247433:T:A | N153K | 0.998 |
| 2:219247433:T:G | N153K | 0.998 |
| 2:219247471:A:C | D166A | 0.998 |
| 2:219247684:C:T | T195I | 0.998 |
| 2:219247708:T:C | L203P | 0.998 |
| 2:219248200:G:A | G222D | 0.998 |
dbSNP variants (sampled 300 via entrez): RS1000543493 (2:219245719 T>A,G), RS1001526126 (2:219247436 A>G), RS1002031647 (2:219246041 C>G,T), RS1002200789 (2:219245260 C>G), RS1003527769 (2:219250272 A>G), RS1003768201 (2:219247832 T>C), RS1003784936 (2:219243539 A>C), RS1003968493 (2:219250021 ACTC>A), RS1004033258 (2:219248897 G>A,T), RS1004510956 (2:219249095 G>C), RS1004566261 (2:219244287 C>T), RS1005329205 (2:219243734 T>C), RS1005497649 (2:219249706 A>T), RS1005798711 (2:219249979 G>A,C), RS1006116968 (2:219250269 G>A)
Disease associations
OMIM: gene MIM:604719 | disease phenotypes: MIM:616208, MIM:621226
GenCC curated gene-disease
Mondo (2): amyotrophic lateral sclerosis type 22 (MONDO:0014531), spastic ataxia 11, autosomal dominant (MONDO:0979230)
Orphanet (1): Amyotrophic lateral sclerosis (Orphanet:803)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST90002385_463 | High light scatter reticulocyte count | 2.000000e-11 |
| GCST90002386_534 | High light scatter reticulocyte percentage of red cells | 2.000000e-12 |
| GCST90002405_4 | Reticulocyte count | 1.000000e-10 |
| GCST90002406_71 | Reticulocyte fraction of red cells | 4.000000e-12 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007986 | reticulocyte count |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3938 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
35 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 188,381 (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 |
|---|---|---|---|
| CHEMBL1078178 | MOMELOTINIB | 4 | 3,481 |
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1289926 | AXITINIB | 4 | 15,732 |
| CHEMBL1789941 | RUXOLITINIB | 4 | 11,547 |
| CHEMBL189963 | PALBOCICLIB | 4 | 13,102 |
| CHEMBL2035187 | PACRITINIB | 4 | 3,345 |
| CHEMBL2103830 | FOSTAMATINIB | 4 | 3,841 |
| CHEMBL3301610 | ABEMACICLIB | 4 | 7,045 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,395 |
| CHEMBL3622821 | UPADACITINIB | 4 | 2,726 |
| CHEMBL477772 | PAZOPANIB | 4 | 15,540 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL300138 | ENZASTAURIN | 3 | 3,209 |
| CHEMBL3137331 | DEFACTINIB | 3 | 1,229 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL230011 | TG100-115 | 2 | 1,504 |
| CHEMBL402548 | DANUSERTIB | 2 | |
| CHEMBL475251 | R-406 | 2 | |
| CHEMBL482968 | ENMD-2076 | 2 | |
| CHEMBL495727 | AT-9283 | 2 | |
| CHEMBL513909 | BI-2536 | 2 | |
| CHEMBL521851 | PICTILISIB | 2 | |
| CHEMBL564829 | MILCICLIB | 2 | |
| CHEMBL572878 | TOZASERTIB | 2 | |
| CHEMBL1084546 | PF-00562271 | 1 | |
| CHEMBL1908397 | KW-2449 | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — NAK family
Most potent curated ligand interactions (3 total), top 3:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| compound 13 [PMID: 34333981] | Inhibition | 7.09 | pIC50 |
| compound 6 [PMID: 34333981] | Inhibition | 7.06 | pIC50 |
| STK16-IN-1 | Inhibition | 6.53 | pIC50 |
Binding affinities (BindingDB)
7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| Staurosporine | KD | 1.7 nM |
| PKC-412 | KD | 190 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 |
| 1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b | KD | 3100 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 |
| STK16-IN-1 | IC50 | 7940 nM |
ChEMBL bioactivities
105 potent at pChembl≥5 of 109 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.77 | Kd | 1.7 | nM | R-406 |
| 8.18 | Kd | 6.6 | nM | FEDRATINIB |
| 7.96 | Kd | 11 | nM | CHEMBL5633837 |
| 7.78 | Kd | 16.67 | nM | CHEMBL5653589 |
| 7.75 | Kd | 18 | nM | CHEMBL1908395 |
| 7.75 | Kd | 18 | nM | NINTEDANIB |
| 7.72 | Kd | 19 | nM | LESTAURTINIB |
| 7.63 | ED50 | 23.15 | nM | CHEMBL5653589 |
| 7.62 | Kd | 24 | nM | CHEMBL516312 |
| 7.54 | Kd | 29 | nM | KW-2449 |
| 7.11 | Ki | 78 | nM | CHEMBL4571548 |
| 7.09 | IC50 | 82 | nM | CHEMBL5079149 |
| 7.07 | Ki | 86 | nM | CHEMBL4470026 |
| 7.06 | IC50 | 88 | nM | CHEMBL5083125 |
| 7.04 | Ki | 91 | nM | CHEMBL4534959 |
| 7.03 | Kd | 93.93 | nM | CHEMBL3752910 |
| 7.02 | Kd | 95 | nM | R-406 |
| 6.97 | IC50 | 107 | nM | CHEMBL4877883 |
| 6.96 | Kd | 110 | nM | CHEMBL4576489 |
| 6.96 | Ki | 110 | nM | CHEMBL4552310 |
| 6.88 | ED50 | 130.4 | nM | CHEMBL3752910 |
| 6.86 | Kd | 138 | nM | PF-00562271 |
| 6.85 | Kd | 140 | nM | JNJ-7706621 |
| 6.83 | IC50 | 148 | nM | CHEMBL5437375 |
| 6.82 | Ki | 150 | nM | CHEMBL4542463 |
| 6.78 | IC50 | 167 | nM | CHEMBL187139 |
| 6.75 | Ki | 180 | nM | CHEMBL4447403 |
| 6.75 | Ki | 180 | nM | CHEMBL4582326 |
| 6.73 | Kd | 186 | nM | CHEMBL3688339 |
| 6.70 | Kd | 200 | nM | STAUROSPORINE |
| 6.68 | Kd | 210 | nM | CYC-116 |
| 6.66 | Ki | 220 | nM | CHEMBL4472438 |
| 6.64 | Kd | 230 | nM | CHEMBL1082152 |
| 6.63 | IC50 | 235 | nM | STAUROSPORINE |
| 6.62 | Ki | 240 | nM | CHEMBL4535040 |
| 6.62 | IC50 | 242 | nM | STAUROSPORINE |
| 6.62 | IC50 | 241 | nM | STAUROSPORINE |
| 6.60 | Kd | 250 | nM | SUNITINIB |
| 6.57 | Ki | 270 | nM | CHEMBL4452939 |
| 6.57 | Kd | 270 | nM | STAUROSPORINE |
| 6.55 | Kd | 280 | nM | MIDOSTAURIN |
| 6.54 | Ki | 290 | nM | CHEMBL4561238 |
| 6.53 | Kd | 295 | nM | GILTERITINIB |
| 6.51 | Ki | 310 | nM | CHEMBL4531680 |
| 6.48 | Ki | 330 | nM | CHEMBL4516665 |
| 6.46 | Ki | 350 | nM | CHEMBL4452360 |
| 6.44 | Kd | 360 | nM | SUNITINIB |
| 6.44 | Kd | 365 | nM | CHEMBL4465866 |
| 6.44 | Kd | 360 | nM | PAZOPANIB |
| 6.43 | Kd | 370 | nM | AXITINIB |
PubChem BioAssay actives
99 with measured affinity, of 836 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 |
|---|---|---|---|---|
| 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 | 624775: Binding constant for STK16 kinase domain | kd | 0.0017 | uM |
| Fedratinib | 624775: Binding constant for STK16 kinase domain | kd | 0.0066 | uM |
| 2-[2-methyl-5-[3-(3,4,5-trimethoxyphenyl)-2H-pyrazolo[3,4-b]pyridin-5-yl]anilino]ethanol | 2137777: Binding affinity to human STK16 assessed as dissociation constant by Adp-glo assay | kd | 0.0110 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2149509: Binding affinity to human STK16 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0167 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 624775: Binding constant for STK16 kinase domain | kd | 0.0180 | uM |
| 5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride | 624775: Binding constant for STK16 kinase domain | kd | 0.0180 | 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 | 508094: Binding affinity to STK16 | kd | 0.0190 | uM |
| N-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide | 389039: Binding affinity to human MPSK1 | kd | 0.0240 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624775: Binding constant for STK16 kinase domain | kd | 0.0290 | uM |
| N-[6-[3-(2-methylpropylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.0780 | uM |
| N-[3-[[5-bromo-4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide | 1823769: Inhibition of human STK16 in presence of [gamma-33P-ATP] by radiometric scintillation assay | ic50 | 0.0820 | uM |
| N-[6-[3-[[[ethyl(methyl)sulfamoyl]amino]methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.0860 | uM |
| 4-[[[5-bromo-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide | 1823769: Inhibition of human STK16 in presence of [gamma-33P-ATP] by radiometric scintillation assay | ic50 | 0.0880 | uM |
| N-[6-[3-(cyclopropylmethylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.0910 | uM |
| 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2149509: Binding affinity to human STK16 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0939 | uM |
| 8-[3-chloro-5-(1-methylindazol-5-yl)-2H-pyrazolo[3,4-b]pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-one | 1769454: Inhibition of human wild type partial length STK16 (G11 to I305) expressed in bacterial expression system by Kinomescan method | ic50 | 0.1070 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526317: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged STK16 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.1100 | uM |
| N-[6-[3-(propylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.1100 | uM |
| N-methyl-N-[3-[[[2-[(2-oxo-1,3-dihydroindol-5-yl)amino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]methyl]-2-pyridinyl]methanesulfonamide | 1425179: 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 | 0.1380 | uM |
| 4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 435692: Binding constant for STK16 kinase domain | kd | 0.1400 | uM |
| 2-[5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylphenyl]-1H-benzimidazole-4-carboxamide | 1972173: Inhibition of MPSK1 (unknown origin) by Z’-Lyte kinase assay | ic50 | 0.1480 | uM |
| N-[6-[3-[(cyclopropylmethylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.1500 | uM |
| N-[6-[3-[(3,3,3-trifluoropropylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.1800 | uM |
| N-[6-[3-[(2,2,2-trifluoroethylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.1800 | uM |
| 1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]ethanone | 1425179: 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 | 0.1860 | 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 | 256606: Average Binding Constant for STK16; NA=Not Active at 10 uM | kd | 0.2000 | uM |
| 4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine | 1425179: 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 | 0.2100 | uM |
| N-[6-[3-[(diethylsulfamoylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.2200 | uM |
| 3-[3-(2,3-dihydroxypropylamino)phenyl]-4-(5-fluoro-1-methylindol-3-yl)pyrrole-2,5-dione | 465274: Inhibition of STK16 | kd | 0.2300 | uM |
| N-[6-[3-(cyclobutylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.2400 | uM |
| Sunitinib | 435692: Binding constant for STK16 kinase domain | kd | 0.2500 | uM |
| N-[6-[3-(diethylsulfamoylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.2700 | uM |
| Midostaurin | 435692: Binding constant for STK16 kinase domain | kd | 0.2800 | uM |
| N-[6-[3-[[[methyl(2,2,2-trifluoroethyl)sulfamoyl]amino]methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.2900 | uM |
| 1-(4-fluoro-3-hydroxyphenyl)-7H-pyrrolo[2,3-h][1,6]naphthyridin-2-one | 1801714: Invitrogen SelectScreen Enzymatic Assay from Article 10.1021/acschembio.6b00250: “Discovery of a Highly Selective STK16 Kinase Inhibitor.” | ic50 | 0.2950 | uM |
| Gilteritinib | 1425179: 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 | 0.2950 | uM |
| N-[6-[3-[[ethyl(methyl)sulfamoyl]amino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.3100 | uM |
| N-[6-[3-(cyclopropylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.3300 | uM |
| N-[6-[3-(dimethylsulfamoylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.3500 | uM |
| Pazopanib | 435692: Binding constant for STK16 kinase domain | kd | 0.3600 | uM |
| 3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-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-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide | 1526317: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged STK16 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 0.3650 | uM |
| Axitinib | 624775: Binding constant for STK16 kinase domain | kd | 0.3700 | uM |
| N-[6-[3-[(4-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.4300 | uM |
| N-[6-[3-[(2-methylpropylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.4500 | uM |
| (4-hydroxypiperidin-1-yl)-[4-[[4-[4-(3-methylsulfonylpropoxy)indol-1-yl]pyrimidin-2-yl]amino]cyclohexyl]methanone | 769493: Binding affinity to STK16 (unknown origin) | kd | 0.4500 | uM |
| N-[6-[3-[(2-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.4700 | uM |
| Ruxolitinib | 624775: Binding constant for STK16 kinase domain | kd | 0.4900 | uM |
| Abemaciclib | 1425179: 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 | 0.4950 | uM |
| N-[6-[3-[(3-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide | 1547796: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged STK16 kinase domain (13 to 305 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay | ki | 0.5100 | uM |
| 14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one | 256606: Average Binding Constant for STK16; NA=Not Active at 10 uM | kd | 0.5100 | uM |
CTD chemical–gene interactions
27 total (human), top 27 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | affects expression, decreases expression | 2 |
| Air Pollutants | affects cotreatment, increases abundance, increases oxidation, increases expression | 2 |
| Smoke | decreases expression, increases abundance, increases expression | 2 |
| Cadmium Chloride | increases expression, decreases expression, increases abundance | 2 |
| GSK-J4 | decreases expression | 1 |
| methylmercuric chloride | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| alpha-pinene | affects cotreatment, increases oxidation, increases abundance | 1 |
| bisphenol A | decreases expression, increases methylation | 1 |
| beta-lapachone | increases expression | 1 |
| nickel sulfate | increases expression | 1 |
| methacrylaldehyde | affects cotreatment, increases oxidation, increases abundance | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| abrine | increases expression | 1 |
| jinfukang | increases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Arsenic Trioxide | decreases response to substance | 1 |
| Acrolein | increases oxidation, increases abundance, affects cotreatment | 1 |
| Amiodarone | increases expression | 1 |
| Atrazine | increases expression | 1 |
| Cadmium | increases abundance, increases expression | 1 |
| Lead | affects expression | 1 |
| Ozone | affects cotreatment, increases oxidation, increases abundance | 1 |
| Quercetin | increases expression | 1 |
| Tetrachlorodibenzodioxin | affects expression | 1 |
| Okadaic Acid | decreases expression | 1 |
| Volatile Organic Compounds | affects cotreatment, increases oxidation | 1 |
ChEMBL screening assays
244 unique, capped per target: 244 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1020555 | Binding | Inhibition of STK16 assessed as enzyme activity relative to control | Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). — J Med Chem |
Cellosaurus cell lines
3 cell lines: 2 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B3IF | Abcam HEK293T STK16 KO | Transformed cell line | Female |
| CVCL_TQ73 | HAP1 STK16 (-) 1 | Cancer cell line | Male |
| CVCL_TQ74 | HAP1 STK16 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): amyotrophic lateral sclerosis type 22, spastic ataxia 11, autosomal dominant