SBK1
gene geneOn this page
Also known as Sbk
Summary
SBK1 (SH3 domain binding kinase 1, HGNC:17699) is a protein-coding gene on chromosome 16p12.1, encoding Serine/threonine-protein kinase SBK1 (Q52WX2). May be involved in signal-transduction pathways related to the control of brain development.
Predicted to enable protein serine/threonine kinase activity. Predicted to be involved in chromatin remodeling. Predicted to be located in cytoplasm.
Source: NCBI Gene 388228 — RefSeq curated summary.
At a glance
- GWAS associations: 35
- Clinical variants (ClinVar): 55 total
- Druggable target: yes — 14 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001024401
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:17699 |
| Approved symbol | SBK1 |
| Name | SH3 domain binding kinase 1 |
| Location | 16p12.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Sbk |
| Ensembl gene | ENSG00000188322 |
| Ensembl biotype | protein_coding |
| OMIM | 620212 |
| Entrez | 388228 |
Gene structure
Transcript identifiers
Ensembl transcripts: 2 — 2 protein_coding
ENST00000341901, ENST00000671413
RefSeq mRNA: 1 — MANE Select: NM_001024401
NM_001024401
CCDS: CCDS32416
Canonical transcript exons
ENST00000341901 — 4 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001374297 | 28318995 | 28319197 |
| ENSE00001384457 | 28317385 | 28317617 |
| ENSE00001386020 | 28320076 | 28323849 |
| ENSE00001486676 | 28292525 | 28293300 |
Expression profiles
Bgee: expression breadth ubiquitous, 195 present calls, max score 98.21.
FANTOM5 (CAGE): breadth broad, TPM avg 8.2244 / max 361.8318, expressed in 774 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 153364 | 6.1109 | 738 |
| 153365 | 1.5608 | 526 |
| 153363 | 0.4811 | 239 |
| 153366 | 0.0717 | 34 |
Top tissues by expression
247 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cortical plate | UBERON:0005343 | 98.21 | gold quality |
| ganglionic eminence | UBERON:0004023 | 96.34 | gold quality |
| cerebellar vermis | UBERON:0004720 | 95.23 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 91.25 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 90.99 | gold quality |
| quadriceps femoris | UBERON:0001377 | 90.41 | gold quality |
| vastus lateralis | UBERON:0001379 | 90.21 | gold quality |
| cerebellum | UBERON:0002037 | 89.93 | gold quality |
| cerebellar cortex | UBERON:0002129 | 89.88 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 89.80 | gold quality |
| ventricular zone | UBERON:0003053 | 89.10 | gold quality |
| biceps brachii | UBERON:0001507 | 88.83 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 87.98 | gold quality |
| thymus | UBERON:0002370 | 87.92 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 87.46 | gold quality |
| postcentral gyrus | UBERON:0002581 | 86.67 | gold quality |
| granulocyte | CL:0000094 | 86.48 | gold quality |
| parietal lobe | UBERON:0001872 | 86.30 | gold quality |
| secondary oocyte | CL:0000655 | 85.81 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 85.80 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 85.38 | gold quality |
| occipital lobe | UBERON:0002021 | 85.30 | gold quality |
| left ventricle myocardium | UBERON:0006566 | 85.26 | gold quality |
| body of tongue | UBERON:0011876 | 85.08 | gold quality |
| primary visual cortex | UBERON:0002436 | 85.07 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 84.33 | gold quality |
| entorhinal cortex | UBERON:0002728 | 84.33 | gold quality |
| deltoid | UBERON:0001476 | 84.30 | silver quality |
| muscle tissue | UBERON:0002385 | 84.06 | gold quality |
| tibialis anterior | UBERON:0001385 | 84.04 | silver quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 3.13 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
158 targeting SBK1, 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-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-4481 | 100.00 | 66.42 | 1669 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-6798-5P | 100.00 | 65.77 | 699 |
| HSA-MIR-6758-5P | 100.00 | 66.21 | 1470 |
| HSA-MIR-6856-5P | 100.00 | 65.47 | 1298 |
| HSA-MIR-4510 | 100.00 | 66.60 | 2050 |
| HSA-MIR-6127 | 100.00 | 66.76 | 2188 |
| HSA-MIR-6129 | 100.00 | 66.46 | 2080 |
| HSA-MIR-6130 | 100.00 | 66.69 | 2012 |
| HSA-MIR-6133 | 100.00 | 66.48 | 2064 |
| HSA-MIR-30A-5P | 100.00 | 76.31 | 3233 |
| HSA-MIR-30B-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30C-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30D-5P | 100.00 | 76.32 | 3233 |
| HSA-MIR-30E-5P | 100.00 | 76.32 | 3242 |
| HSA-MIR-4283 | 100.00 | 66.42 | 2097 |
| HSA-MIR-4747-5P | 100.00 | 67.90 | 2681 |
| HSA-MIR-5196-5P | 100.00 | 67.98 | 2761 |
| HSA-MIR-4500 | 99.99 | 72.72 | 2367 |
| HSA-MIR-4789-3P | 99.99 | 70.75 | 2484 |
| HSA-MIR-4745-5P | 99.98 | 65.95 | 1028 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-LET-7A-5P | 99.98 | 72.29 | 1790 |
| HSA-LET-7B-5P | 99.98 | 72.31 | 1790 |
| HSA-LET-7C-5P | 99.98 | 72.29 | 1790 |
| HSA-LET-7E-5P | 99.98 | 72.29 | 1790 |
| HSA-LET-7F-5P | 99.98 | 72.56 | 1784 |
| HSA-LET-7G-5P | 99.98 | 72.37 | 1784 |
Literature-anchored findings (GeneRIF, showing 2)
- Results suggest that the wide-spread expression pattern of human SBK1 may predict a broad cellular function, and its dysregulation in certain cancers suggests an involvement of the protein in the pathogenesis of human cancers. (PMID:21104019)
- SH3 domain-binding kinase 1 promotes proliferation and inhibits apoptosis of cervical cancer via activating the Wnt/beta-catenin and Raf/ERK1/2 signaling pathways. (PMID:37132991)
Cross-species orthologs
7 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | sbk1 | ENSDARG00000056294 |
| mus_musculus | Sbk1 | ENSMUSG00000042978 |
| rattus_norvegicus | Sbk1 | ENSRNOG00000067387 |
| drosophila_melanogaster | meng | FBGN0031855 |
| drosophila_melanogaster | CG4945 | FBGN0034137 |
| caenorhabditis_elegans | WBGENE00011299 | |
| caenorhabditis_elegans | WBGENE00012726 |
Paralogs (1): SBK3 (ENSG00000231274)
Protein
Protein identifiers
Serine/threonine-protein kinase SBK1 — Q52WX2 (reviewed: Q52WX2)
Alternative names: SH3 domain-binding kinase 1
All UniProt accessions (2): A0A590UK17, Q52WX2
UniProt curated annotations — full annotation on UniProt →
Function. May be involved in signal-transduction pathways related to the control of brain development.
Subcellular location. Cytoplasm.
Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family.
RefSeq proteins (1): NP_001019572* (*=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 |
| IPR016234 | Ser/Thr_kinase_Sbk1 | Family |
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 (12 total): sequence variant 4, region of interest 2, binding site 2, chain 1, domain 1, compositionally biased region 1, active site 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q52WX2-F1 | 77.87 | 0.63 |
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): 174 (proton acceptor)
Ligand- & substrate-binding residues (2): 59–67; 82
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 152 (showing top):
GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, BILD_E2F3_ONCOGENIC_SIGNATURE, TGTTTAC_MIR30A5P_MIR30C_MIR30D_MIR30B_MIR30E5P, CUI_TCF21_TARGETS_2_UP, HUANG_DASATINIB_RESISTANCE_DN, XU_GH1_AUTOCRINE_TARGETS_DN, BOYLAN_MULTIPLE_MYELOMA_C_D_UP, chr16p12, LEIN_LOCALIZED_TO_DISTAL_AND_PROXIMAL_DENDRITES, CTGAGCC_MIR24, PASQUALUCCI_LYMPHOMA_BY_GC_STAGE_DN, ATGTAGC_MIR221_MIR222, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY
GO Biological Process (1): protein phosphorylation (GO:0006468)
GO Molecular Function (7): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (1): cytoplasm (GO:0005737)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein kinase activity | 2 |
| phosphorylation | 1 |
| protein modification process | 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 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
670 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| SBK1 | RIOK3 | O14730 | 462 |
| SBK1 | TTC9B | Q8N6N2 | 451 |
| SBK1 | TANC1 | Q9C0D5 | 445 |
| SBK1 | RBM28 | Q9NW13 | 440 |
| SBK1 | IRGQ | Q8WZA9 | 433 |
| SBK1 | RGS7BP | Q6MZT1 | 430 |
| SBK1 | APOBR | Q0VD83 | 420 |
| SBK1 | PIP4K2B | P78356 | 411 |
| SBK1 | ABRACL | Q9P1F3 | 405 |
| SBK1 | RASSF3 | Q86WH2 | 402 |
| SBK1 | DMAC2 | Q9NW81 | 402 |
| SBK1 | SRC | P12931 | 388 |
| SBK1 | PLCXD2 | Q0VAA5 | 386 |
| SBK1 | LRFN3 | Q9BTN0 | 385 |
| SBK1 | INPP5A | Q14642 | 385 |
IntAct
2 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| SBK1 | FTL | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (11): SBK1 (Co-fractionation), SBK1 (Biochemical Activity), SBK1 (Affinity Capture-RNA), GFER (Affinity Capture-MS), YTHDF1 (Affinity Capture-MS), FTL (Affinity Capture-MS), SBK1 (Affinity Capture-RNA), SBK1 (Affinity Capture-MS), SBK1 (Affinity Capture-MS), SBK1 (Affinity Capture-MS), SBK1 (Affinity Capture-MS)
ESM2 similar proteins: A4II32, A7MCT6, D3ZRW8, G5E872, O35465, O54783, O55229, P50747, P61797, Q14164, Q14318, Q14CH1, Q1JP61, Q3B7U9, Q496Y0, Q497B8, Q52WX2, Q5I0I5, Q7TQC5, Q7YRZ1, Q7YRZ2, Q7Z2E3, Q7Z695, Q80WC9, Q8BNV1, Q8BYN3, Q8CGA0, Q8HXH0, Q8IYL2, Q8IZ69, Q8K4H4, Q8N371, Q8NF37, Q8NI29, Q8QZX0, Q920N2, Q96EN8, Q9BGQ0, Q9CXT6, Q9D2Q2
Diamond homologs: A1A5Q6, A2XFF4, A7MB74, A8XJQ6, A8XW88, B1WAS2, B1WBU5, B8BBT7, C0HKC8, C0HKC9, G1X456, O61661, O70150, O88866, O94806, P00517, P05131, P05132, P05383, P05986, P06244, P06245, P0C263, P0C264, P0C5K0, P0C5K1, P0DP15, P12370, P16912, P17612, P21137, P22612, P22694, P25321, P27791, P34099, P36887, P45894, P57058, P57059
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
55 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 51 |
| Likely benign | 0 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
564 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 16:28317576:GCACC:G | donor_gain | 1.0000 |
| 16:28317586:G:T | donor_gain | 1.0000 |
| 16:28317600:T:TA | donor_gain | 1.0000 |
| 16:28317601:G:GA | donor_gain | 1.0000 |
| 16:28317613:CACAG:C | donor_loss | 1.0000 |
| 16:28317617:GGTGA:G | donor_loss | 1.0000 |
| 16:28317618:GTG:G | donor_loss | 1.0000 |
| 16:28317619:T:A | donor_loss | 1.0000 |
| 16:28318991:TCAG:T | acceptor_loss | 1.0000 |
| 16:28318992:CA:C | acceptor_loss | 1.0000 |
| 16:28318993:A:AG | acceptor_gain | 1.0000 |
| 16:28318993:A:G | acceptor_loss | 1.0000 |
| 16:28318994:G:GG | acceptor_gain | 1.0000 |
| 16:28318994:GGC:G | acceptor_gain | 1.0000 |
| 16:28319152:GGA:G | donor_gain | 1.0000 |
| 16:28319153:GAG:G | donor_gain | 1.0000 |
| 16:28319196:AGG:A | donor_loss | 1.0000 |
| 16:28319197:GG:G | donor_loss | 1.0000 |
| 16:28319198:G:A | donor_loss | 1.0000 |
| 16:28319199:T:A | donor_loss | 1.0000 |
| 16:28293298:CAGGT:C | donor_loss | 0.9900 |
| 16:28293299:AG:A | donor_loss | 0.9900 |
| 16:28293300:GG:G | donor_loss | 0.9900 |
| 16:28293301:GTA:G | donor_loss | 0.9900 |
| 16:28317384:G:GC | acceptor_loss | 0.9900 |
| 16:28317562:G:GT | donor_gain | 0.9900 |
| 16:28317586:G:GT | donor_gain | 0.9900 |
| 16:28317587:A:T | donor_gain | 0.9900 |
| 16:28317591:T:TA | donor_gain | 0.9900 |
| 16:28317603:TCTAC:T | donor_gain | 0.9900 |
AlphaMissense
2713 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 16:28317575:G:A | G62S | 1.000 |
| 16:28317575:G:C | G62R | 1.000 |
| 16:28317575:G:T | G62C | 1.000 |
| 16:28317584:G:A | G65R | 1.000 |
| 16:28317584:G:C | G65R | 1.000 |
| 16:28317584:G:T | G65W | 1.000 |
| 16:28317585:G:A | G65E | 1.000 |
| 16:28317585:G:T | G65V | 1.000 |
| 16:28317597:T:C | L69P | 1.000 |
| 16:28319007:C:A | A80E | 1.000 |
| 16:28319010:T:C | L81P | 1.000 |
| 16:28319012:A:C | K82Q | 1.000 |
| 16:28319012:A:G | K82E | 1.000 |
| 16:28319013:A:T | K82M | 1.000 |
| 16:28319014:G:C | K82N | 1.000 |
| 16:28319014:G:T | K82N | 1.000 |
| 16:28319026:G:C | K86N | 1.000 |
| 16:28319026:G:T | K86N | 1.000 |
| 16:28319048:T:C | F94L | 1.000 |
| 16:28319049:T:C | F94S | 1.000 |
| 16:28319050:C:A | F94L | 1.000 |
| 16:28319050:C:G | F94L | 1.000 |
| 16:28319057:G:A | E97K | 1.000 |
| 16:28319058:A:T | E97V | 1.000 |
| 16:28319142:T:A | V125D | 1.000 |
| 16:28319175:T:C | L136P | 1.000 |
| 16:28319177:T:C | F137L | 1.000 |
| 16:28319179:T:A | F137L | 1.000 |
| 16:28319179:T:G | F137L | 1.000 |
| 16:28320080:G:A | G145E | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000013055 (16:28297609 A>T), RS1000101226 (16:28310132 C>T), RS1000181170 (16:28270913 G>T), RS1000187056 (16:28302826 C>G,T), RS1000269928 (16:28268008 G>A), RS1000296671 (16:28279321 C>G), RS1000340692 (16:28267799 A>C), RS1000384268 (16:28321109 G>A), RS1000439136 (16:28314840 A>G), RS1000445908 (16:28284808 T>C), RS1000492442 (16:28297332 A>G), RS1000501031 (16:28289487 C>A,T), RS1000555836 (16:28284138 C>T), RS1000708766 (16:28303480 T>C), RS1000772769 (16:28285190 C>T)
Disease associations
OMIM: gene MIM:620212 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
35 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002783_101 | Body mass index | 5.000000e-06 |
| GCST002783_183 | Body mass index | 2.000000e-09 |
| GCST002783_336 | Body mass index | 1.000000e-09 |
| GCST002783_586 | Body mass index | 5.000000e-06 |
| GCST003097_27 | Pediatric autoimmune diseases | 4.000000e-09 |
| GCST003435_31 | Body fat percentage | 1.000000e-08 |
| GCST003435_41 | Body fat percentage | 7.000000e-07 |
| GCST003995_17 | Tonsillectomy | 5.000000e-11 |
| GCST004065_103 | Waist circumference | 2.000000e-07 |
| GCST004065_93 | Waist circumference | 2.000000e-06 |
| GCST004065_98 | Waist circumference | 2.000000e-11 |
| GCST004066_126 | Hip circumference | 4.000000e-09 |
| GCST004066_48 | Hip circumference | 2.000000e-07 |
| GCST004495_96 | BMI (adjusted for smoking behaviour) | 3.000000e-08 |
| GCST004497_38 | Body mass index (joint analysis main effects and smoking interaction) | 4.000000e-07 |
| GCST004499_99 | BMI in non-smokers | 3.000000e-06 |
| GCST004519_9 | Body mass index (adult) | 9.000000e-06 |
| GCST004557_242 | Body mass index | 4.000000e-08 |
| GCST004557_31 | Body mass index | 3.000000e-08 |
| GCST004558_162 | Body mass index (joint analysis main effects and physical activity interaction) | 2.000000e-07 |
| GCST004558_28 | Body mass index (joint analysis main effects and physical activity interaction) | 4.000000e-08 |
| GCST004559_106 | Body mass index in physically active individuals | 5.000000e-07 |
| GCST004559_24 | Body mass index in physically active individuals | 3.000000e-07 |
| GCST005014_86 | Tonsillectomy | 5.000000e-11 |
| GCST005316_465 | Intelligence (MTAG) | 2.000000e-13 |
| GCST005316_514 | Intelligence (MTAG) | 5.000000e-08 |
| GCST005316_515 | Intelligence (MTAG) | 7.000000e-11 |
| GCST005752_47 | Systemic lupus erythematosus | 1.000000e-06 |
| GCST006269_379 | General cognitive ability | 1.000000e-10 |
| GCST008757_46 | Alcohol consumption | 1.000000e-10 |
EFO canonical traits (10, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004340 | body mass index |
| EFO:0007800 | body fat percentage |
| EFO:0007924 | tonsillectomy risk measurement |
| EFO:0004318 | smoking behavior |
| EFO:0008002 | physical activity measurement |
| EFO:0004337 | intelligence |
| EFO:0008111 | diet measurement |
| EFO:0004346 | neuroimaging measurement |
| EFO:0004530 | triglyceride measurement |
| EFO:0004533 | alkaline phosphatase measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL1163129 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
14 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 365,673 (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 |
| CHEMBL1789941 | RUXOLITINIB | 4 | 11,547 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL5416410 | DASATINIB | 4 | 655 |
| CHEMBL553 | ERLOTINIB | 4 | 108,300 |
| CHEMBL601719 | CRIZOTINIB | 4 | 14,403 |
| CHEMBL939 | GEFITINIB | 4 | 117,814 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL475251 | R-406 | 2 | 762 |
| 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 — NKF1 family
ChEMBL bioactivities
23 potent at pChembl≥5 of 23 total, top 23 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.49 | Kd | 3.2 | nM | STAUROSPORINE |
| 7.68 | Kd | 21 | nM | TAE-684 |
| 7.03 | Kd | 93 | nM | R-406 |
| 7.00 | IC50 | 99.8 | nM | STAUROSPORINE |
| 6.96 | Kd | 110 | nM | NINTEDANIB |
| 6.88 | IC50 | 133 | nM | STAUROSPORINE |
| 6.71 | IC50 | 193 | nM | STAUROSPORINE |
| 6.70 | Kd | 200 | nM | SUNITINIB |
| 6.70 | Kd | 200 | nM | LESTAURTINIB |
| 6.25 | Kd | 560 | nM | GEFITINIB |
| 6.24 | Kd | 580 | nM | KW-2449 |
| 6.21 | Kd | 620 | nM | SU-014813 |
| 6.10 | Kd | 790 | nM | FEDRATINIB |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 5.92 | Kd | 1200 | nM | DASATINIB |
| 5.92 | Kd | 1200 | nM | ERLOTINIB |
| 5.89 | Kd | 1300 | nM | CRIZOTINIB |
| 5.89 | Kd | 1300 | nM | RUXOLITINIB |
| 5.82 | Kd | 1500 | nM | DOVITINIB |
| 5.51 | Kd | 3100 | nM | CHEMBL1908395 |
| 5.32 | Kd | 4800 | nM | AFATINIB |
PubChem BioAssay actives
20 with measured affinity, of 144 total; 17 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 | 624812: Binding constant for SBK1 kinase domain | kd | 0.0032 | 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 | 624812: Binding constant for SBK1 kinase domain | kd | 0.0210 | 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 | 624812: Binding constant for SBK1 kinase domain | kd | 0.0930 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 624812: Binding constant for SBK1 kinase domain | kd | 0.1100 | 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 | 624812: Binding constant for SBK1 kinase domain | kd | 0.2000 | uM |
| Sunitinib | 624812: Binding constant for SBK1 kinase domain | kd | 0.2000 | uM |
| Gefitinib | 624812: Binding constant for SBK1 kinase domain | kd | 0.5600 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624812: Binding constant for SBK1 kinase domain | kd | 0.5800 | 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 | 624812: Binding constant for SBK1 kinase domain | kd | 0.6200 | uM |
| Fedratinib | 624812: Binding constant for SBK1 kinase domain | kd | 0.7900 | uM |
| N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate | 624812: Binding constant for SBK1 kinase domain | kd | 1.2000 | uM |
| Erlotinib | 624812: Binding constant for SBK1 kinase domain | kd | 1.2000 | uM |
| Crizotinib | 624812: Binding constant for SBK1 kinase domain | kd | 1.3000 | uM |
| Ruxolitinib | 624812: Binding constant for SBK1 kinase domain | kd | 1.3000 | uM |
| 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one | 624812: Binding constant for SBK1 kinase domain | kd | 1.5000 | uM |
| 5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride | 624812: Binding constant for SBK1 kinase domain | kd | 3.1000 | uM |
| Afatinib | 624812: Binding constant for SBK1 kinase domain | kd | 4.8000 | uM |
CTD chemical–gene interactions
42 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| methylmercuric chloride | increases expression, affects cotreatment | 3 |
| Valproic Acid | increases methylation | 3 |
| Benzo(a)pyrene | affects methylation, increases expression, increases methylation | 2 |
| 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine | decreases expression | 1 |
| lasiocarpine | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| propionaldehyde | increases expression | 1 |
| bisphenol A | increases methylation | 1 |
| butyraldehyde | increases expression | 1 |
| tobacco tar | decreases expression | 1 |
| hydroquinone | decreases expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects response to substance, increases expression, affects cotreatment, decreases expression | 1 |
| pentanal | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| nutlin 3 | increases expression, affects cotreatment | 1 |
| abrine | decreases expression | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Vorinostat | decreases expression | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Aldehydes | increases expression | 1 |
| Calcitriol | increases expression | 1 |
| Camptothecin | increases expression | 1 |
| Cisplatin | affects cotreatment, increases expression | 1 |
| Dactinomycin | affects cotreatment, increases expression | 1 |
| Estradiol | affects cotreatment, decreases expression | 1 |
ChEMBL screening assays
97 unique, capped per target: 97 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1167697 | Binding | Inhibition of SBK1 at 1 uM | Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. — 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_TK07 | HAP1 SBK1 (-) 1 | Cancer cell line | Male |
| CVCL_TK08 | HAP1 SBK1 (-) 2 | Cancer cell line | Male |
| CVCL_TK09 | HAP1 SBK1 (-) 3 | 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): ankylosing spondylitis, autoimmune disease, autoimmune thyroid disease, celiac disease, common variable immunodeficiency, juvenile idiopathic arthritis, type 1 diabetes mellitus