STK32A
gene geneOn this page
Also known as MGC22688YANK1
Summary
STK32A (serine/threonine kinase 32A, HGNC:28317) is a protein-coding gene on chromosome 5q32, encoding Serine/threonine-protein kinase 32A (Q8WU08).
Predicted to enable protein serine/threonine kinase activity. Predicted to be involved in intracellular signal transduction. Predicted to be located in plasma membrane.
Source: NCBI Gene 202374 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 73 total
- Druggable target: yes — 8 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001112724
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:28317 |
| Approved symbol | STK32A |
| Name | serine/threonine kinase 32A |
| Location | 5q32 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | MGC22688, YANK1 |
| Ensembl gene | ENSG00000169302 |
| Ensembl biotype | protein_coding |
| OMIM | 621310 |
| Entrez | 202374 |
Gene structure
Transcript identifiers
Ensembl transcripts: 10 — 6 retained_intron, 3 protein_coding, 1 nonsense_mediated_decay
ENST00000306304, ENST00000397936, ENST00000398523, ENST00000503384, ENST00000503975, ENST00000506091, ENST00000510953, ENST00000515832, ENST00000626951, ENST00000648628
RefSeq mRNA: 3 — MANE Select: NM_001112724
NM_001112724, NM_001287740, NM_145001
CCDS: CCDS47299, CCDS54931, CCDS75351
Canonical transcript exons
ENST00000397936 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001533450 | 147383441 | 147383505 |
| ENSE00001533452 | 147375090 | 147375218 |
| ENSE00002057341 | 147383890 | 147387855 |
| ENSE00003506691 | 147323898 | 147324071 |
| ENSE00003526815 | 147239539 | 147239686 |
| ENSE00003532739 | 147279247 | 147279398 |
| ENSE00003544570 | 147343006 | 147343043 |
| ENSE00003599143 | 147278124 | 147278179 |
| ENSE00003602055 | 147373169 | 147373294 |
| ENSE00003609964 | 147361517 | 147361614 |
| ENSE00003628208 | 147370654 | 147370770 |
| ENSE00003668573 | 147351065 | 147351154 |
| ENSE00003846187 | 147235026 | 147235199 |
Expression profiles
Bgee: expression breadth ubiquitous, 187 present calls, max score 83.04.
FANTOM5 (CAGE): breadth broad, TPM avg 2.3322 / max 146.3959, expressed in 473 samples.
FANTOM5 promoters (4 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 59234 | 1.6928 | 354 |
| 59238 | 0.3530 | 151 |
| 59235 | 0.2071 | 100 |
| 59233 | 0.0793 | 48 |
Top tissues by expression
247 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| sural nerve | UBERON:0015488 | 83.04 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 82.72 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 82.00 | gold quality |
| hypothalamus | UBERON:0001898 | 81.97 | gold quality |
| left adrenal gland | UBERON:0001234 | 81.88 | gold quality |
| right adrenal gland | UBERON:0001233 | 81.27 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 80.81 | gold quality |
| adrenal cortex | UBERON:0001235 | 79.64 | gold quality |
| tibial nerve | UBERON:0001323 | 79.27 | gold quality |
| substantia nigra | UBERON:0002038 | 78.97 | gold quality |
| tibia | UBERON:0000979 | 78.89 | gold quality |
| adrenal gland | UBERON:0002369 | 78.36 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 77.59 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 77.06 | gold quality |
| ascending aorta | UBERON:0001496 | 76.94 | gold quality |
| thoracic aorta | UBERON:0001515 | 76.78 | gold quality |
| midbrain | UBERON:0001891 | 76.39 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 76.35 | gold quality |
| cerebellar cortex | UBERON:0002129 | 76.29 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 76.03 | gold quality |
| cerebellum | UBERON:0002037 | 75.67 | gold quality |
| adenohypophysis | UBERON:0002196 | 75.26 | gold quality |
| medial globus pallidus | UBERON:0002477 | 75.08 | gold quality |
| spinal cord | UBERON:0002240 | 74.91 | gold quality |
| gall bladder | UBERON:0002110 | 74.15 | gold quality |
| islet of Langerhans | UBERON:0000006 | 73.70 | gold quality |
| calcaneal tendon | UBERON:0003701 | 73.48 | gold quality |
| amygdala | UBERON:0001876 | 73.10 | gold quality |
| pituitary gland | UBERON:0000007 | 72.91 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 72.82 | gold quality |
Single-cell (SCXA)
Detected in 3 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ENAD-20 | yes | 395.55 |
| E-ANND-3 | yes | 5.46 |
| E-MTAB-9543 | no | 1.22 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
22 targeting STK32A, 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-548AW | 99.99 | 72.57 | 3559 |
| HSA-MIR-1468-3P | 99.96 | 72.74 | 3797 |
| HSA-MIR-450B-5P | 99.92 | 71.48 | 3175 |
| HSA-MIR-548AJ-5P | 99.78 | 71.12 | 3085 |
| HSA-MIR-548F-5P | 99.78 | 71.02 | 3093 |
| HSA-MIR-548G-5P | 99.78 | 71.12 | 3085 |
| HSA-MIR-548X-5P | 99.78 | 71.12 | 3085 |
| HSA-MIR-19A-5P | 99.36 | 66.93 | 1675 |
| HSA-MIR-19B-1-5P | 99.36 | 67.07 | 1669 |
| HSA-MIR-19B-2-5P | 99.36 | 67.07 | 1669 |
| HSA-MIR-2115-3P | 99.31 | 69.68 | 2026 |
| HSA-MIR-661 | 99.09 | 65.94 | 2062 |
| HSA-MIR-939-3P | 98.97 | 65.07 | 2347 |
| HSA-MIR-361-5P | 98.95 | 70.16 | 1340 |
| HSA-MIR-374A-3P | 98.87 | 67.82 | 1531 |
| HSA-MIR-31-5P | 98.58 | 68.35 | 1239 |
| HSA-MIR-548AO-5P | 98.55 | 69.57 | 1362 |
| HSA-MIR-548AX | 98.55 | 69.58 | 1362 |
| HSA-MIR-1271-3P | 97.56 | 64.85 | 865 |
| HSA-MIR-550A-3-5P | 97.56 | 65.35 | 823 |
| HSA-MIR-550A-5P | 97.56 | 65.35 | 823 |
| HSA-MIR-4800-3P | 88.42 | 63.07 | 35 |
Cross-species orthologs
8 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Stk32a | ENSMUSG00000039954 |
| rattus_norvegicus | Stk32a | ENSRNOG00000027066 |
| drosophila_melanogaster | CG32944 | FBGN0052944 |
| drosophila_melanogaster | dop | FBGN0267390 |
| caenorhabditis_elegans | WBGENE00002192 | |
| caenorhabditis_elegans | wts-1 | WBGENE00007047 |
| caenorhabditis_elegans | WBGENE00010838 | |
| caenorhabditis_elegans | WBGENE00011992 |
Paralogs (13): MAST4 (ENSG00000069020), MAST2 (ENSG00000086015), MAST3 (ENSG00000099308), SGK2 (ENSG00000101049), SGK3 (ENSG00000104205), DMPK (ENSG00000104936), MAST1 (ENSG00000105613), SGK1 (ENSG00000118515), MASTL (ENSG00000120539), LATS1 (ENSG00000131023), LATS2 (ENSG00000150457), STK32B (ENSG00000152953), STK32C (ENSG00000165752)
Protein
Protein identifiers
Serine/threonine-protein kinase 32A — Q8WU08 (reviewed: Q8WU08)
Alternative names: Yet another novel kinase 1
All UniProt accessions (3): Q8WU08, A0A3B3IS85, B7Z9H7
UniProt curated annotations — full annotation on UniProt →
Subcellular location. Cell membrane.
Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q8WU08-1 | 1 | yes |
| Q8WU08-2 | 2 | |
| Q8WU08-3 | 3 |
RefSeq proteins (3): NP_001106195, NP_001274669, NP_659438 (=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 |
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 (40 total): helix 16, strand 7, splice variant 4, sequence variant 3, binding site 2, initiator methionine 1, chain 1, mutagenesis site 1, turn 1, domain 1, region of interest 1, active site 1, lipid moiety-binding region 1
Structure
Experimental structures (PDB)
1 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 4FR4 | X-RAY DIFFRACTION | 2.29 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q8WU08-F1 | 87.61 | 0.68 |
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): 146 (proton acceptor)
Ligand- & substrate-binding residues (2): 29–37; 52
Post-translational modifications (1): 2
Mutagenesis-validated functional residues (1):
| Position | Phenotype |
|---|---|
| 2 | localizes to cytoplasm. |
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 61 (showing top):
TGACCTY_ERR1_Q2, TGACCTTG_SF1_Q6, chr5q32, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY, GOMF_PROTEIN_SERINE_THREONINE_KINASE_ACTIVITY, GOMF_ADENYL_NUCLEOTIDE_BINDING, GOMF_TRANSFERASE_ACTIVITY_TRANSFERRING_PHOSPHORUS_CONTAINING_GROUPS, MEISSNER_NPC_HCP_WITH_H3_UNMETHYLATED, MEISSNER_BRAIN_HCP_WITH_H3K4ME3_AND_H3K27ME3, FOSTER_KDM1A_TARGETS_UP, ZNF618_TARGET_GENES, MIR1468_3P, MIR656_3P, MIR128_3P
GO Biological Process (2): intracellular signal transduction (GO:0035556), protein phosphorylation (GO:0006468)
GO Molecular Function (9): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), metal ion binding (GO:0046872), 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 (2): plasma membrane (GO:0005886), membrane (GO:0016020)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein kinase activity | 2 |
| intracellular anatomical structure | 1 |
| signal transduction | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| cation 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 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
940 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| STK32A | DPYSL3 | Q14195 | 651 |
| STK32A | JAKMIP2 | Q96AA8 | 479 |
| STK32A | RABGGTA | Q92696 | 474 |
| STK32A | STAC2 | Q6ZMT1 | 472 |
| STK32A | GPR149 | Q86SP6 | 461 |
| STK32A | PLEKHG1 | Q9ULL1 | 455 |
| STK32A | RUNX2 | Q13950 | 453 |
| STK32A | ARHGAP25 | P42331 | 449 |
| STK32A | FAM131C | Q96AQ9 | 433 |
| STK32A | CCER2 | I3L3R5 | 433 |
| STK32A | DOCK5 | Q9H7D0 | 425 |
| STK32A | GULP1 | Q9UBP9 | 414 |
| STK32A | ING2 | Q9H160 | 412 |
| STK32A | VARS1 | P26640 | 410 |
| STK32A | PPP2R2B | Q00005 | 410 |
IntAct
3 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CDKL3 | psi-mi:“MI:0914”(association) | 0.350 | |
| STK32A | HSP90AA1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (19): STK32A (Synthetic Growth Defect), CST7 (Affinity Capture-MS), STK32A (Two-hybrid), STK32A (Affinity Capture-MS), HSP90AA1 (Affinity Capture-MS), HSP90AB1 (Affinity Capture-MS), TCP1 (Affinity Capture-MS), CCT6A (Affinity Capture-MS), CCT5 (Affinity Capture-MS), CCT3 (Affinity Capture-MS), CCT8 (Affinity Capture-MS), CCT4 (Affinity Capture-MS), CCT2 (Affinity Capture-MS), PRKCE (Affinity Capture-MS), FKBP5 (Affinity Capture-MS)
ESM2 similar proteins: A2VDV2, A8XJL7, O13310, O75582, O97627, P00518, P07934, P13286, P18652, P18653, P18654, P21146, P23443, P26817, P26818, P26819, P35626, P51812, P54645, P67998, P67999, Q09639, Q12706, Q15208, Q21734, Q2L6W9, Q2LZZ7, Q39030, Q3UYH7, Q54IH8, Q5F3L1, Q5R4K3, Q5R8M1, Q64682, Q6PFQ0, Q6TGC6, Q6TJY3, Q7TPS0, Q7TSE6, Q8BGW6
Diamond homologs: A0A078CGE6, A1A5Q6, A2QHV0, A4K2M3, A4K2P5, A4K2Q5, A4K2S1, A4K2T0, A4K2W5, A4K2Y1, B0WAU8, B3DL84, B3NKK1, B4IMC3, B4J3F1, B4KYX8, B4LDJ6, B4MXR8, B4NSS9, D3ZHP7, F1M7Y5, F4HPN2, F4HYG2, F4IRW0, F4J6F6, F4JBP3, F4JY37, J9W0G9, O22042, O54748, O61122, O64629, O74426, O75011, P0C8M8, P18652, P23647, P34102, P38692, P41743
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
73 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 65 |
| Likely benign | 0 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2949 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 5:147239683:GATG:G | donor_gain | 1.0000 |
| 5:147278122:A:AG | acceptor_gain | 1.0000 |
| 5:147278123:G:GA | acceptor_gain | 1.0000 |
| 5:147278123:GTC:G | acceptor_gain | 1.0000 |
| 5:147278123:GTCA:G | acceptor_gain | 1.0000 |
| 5:147278123:GTCAA:G | acceptor_gain | 1.0000 |
| 5:147279396:GTG:G | donor_gain | 1.0000 |
| 5:147279399:G:A | donor_loss | 1.0000 |
| 5:147279400:TGA:T | donor_loss | 1.0000 |
| 5:147279401:GAG:G | donor_loss | 1.0000 |
| 5:147323890:A:AG | acceptor_gain | 1.0000 |
| 5:147323891:A:G | acceptor_gain | 1.0000 |
| 5:147323896:A:AG | acceptor_gain | 1.0000 |
| 5:147323896:AG:A | acceptor_gain | 1.0000 |
| 5:147323897:G:GA | acceptor_gain | 1.0000 |
| 5:147323897:GG:G | acceptor_gain | 1.0000 |
| 5:147323897:GGT:G | acceptor_gain | 1.0000 |
| 5:147323897:GGTA:G | acceptor_gain | 1.0000 |
| 5:147323897:GGTAT:G | acceptor_gain | 1.0000 |
| 5:147348838:C:G | donor_gain | 1.0000 |
| 5:147351061:GCA:G | acceptor_loss | 1.0000 |
| 5:147351063:A:AT | acceptor_loss | 1.0000 |
| 5:147351063:AG:A | acceptor_gain | 1.0000 |
| 5:147351063:AGG:A | acceptor_gain | 1.0000 |
| 5:147351064:GG:G | acceptor_gain | 1.0000 |
| 5:147351064:GGG:G | acceptor_gain | 1.0000 |
| 5:147351064:GGGC:G | acceptor_gain | 1.0000 |
| 5:147361621:T:TA | donor_gain | 1.0000 |
| 5:147361622:A:AA | donor_gain | 1.0000 |
| 5:147370652:A:G | acceptor_gain | 1.0000 |
AlphaMissense
2680 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 5:147278139:T:C | F23S | 1.000 |
| 5:147278160:G:A | G30E | 1.000 |
| 5:147278165:G:C | G32R | 1.000 |
| 5:147278171:T:A | F34I | 1.000 |
| 5:147278171:T:C | F34L | 1.000 |
| 5:147278173:T:A | F34L | 1.000 |
| 5:147278173:T:G | F34L | 1.000 |
| 5:147278174:G:A | G35R | 1.000 |
| 5:147278174:G:C | G35R | 1.000 |
| 5:147278174:G:T | G35W | 1.000 |
| 5:147278175:G:A | G35E | 1.000 |
| 5:147278175:G:T | G35V | 1.000 |
| 5:147279287:C:A | A50E | 1.000 |
| 5:147279292:A:C | K52Q | 1.000 |
| 5:147279292:A:G | K52E | 1.000 |
| 5:147279294:G:C | K52N | 1.000 |
| 5:147279294:G:T | K52N | 1.000 |
| 5:147279306:A:C | K56N | 1.000 |
| 5:147279306:A:T | K56N | 1.000 |
| 5:147323905:T:C | F90L | 1.000 |
| 5:147323907:C:A | F90L | 1.000 |
| 5:147323907:C:G | F90L | 1.000 |
| 5:147343008:A:C | D146A | 1.000 |
| 5:147343008:A:T | D146V | 1.000 |
| 5:147351082:G:C | D164H | 1.000 |
| 5:147351083:A:C | D164A | 1.000 |
| 5:147351083:A:G | D164G | 1.000 |
| 5:147351083:A:T | D164V | 1.000 |
| 5:147351084:T:A | D164E | 1.000 |
| 5:147351084:T:G | D164E | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000026849 (5:147321337 C>T), RS1000054251 (5:147240365 A>G), RS1000065445 (5:147325519 T>C), RS1000066855 (5:147305342 C>A,G,T), RS1000070910 (5:147234506 G>T), RS1000095579 (5:147239316 T>C), RS1000101867 (5:147283534 G>A), RS1000103907 (5:147245861 C>G,T), RS1000104536 (5:147298262 T>C), RS1000135429 (5:147277821 T>C), RS1000162362 (5:147379755 T>C), RS1000183667 (5:147251836 G>A), RS1000185465 (5:147234831 G>C), RS1000208574 (5:147315307 A>T), RS1000216315 (5:147252085 T>C)
Disease associations
OMIM: gene MIM:621310 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003542_162 | Night sleep phenotypes | 7.000000e-06 |
| GCST008759_50 | Intake of total sugars | 4.000000e-07 |
| GCST009218_12 | Lateral ventricle temporal horn volume | 5.000000e-06 |
| GCST010397_73 | Gut microbiota (bacterial taxa, rank normal transformation method) | 5.000000e-06 |
| GCST011494_25 | Daytime nap | 6.000000e-26 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0010158 | sugar consumption measurement |
| EFO:0007874 | gut microbiome measurement |
| EFO:0007828 | daytime rest measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL6150 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
8 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 94,834 (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 |
|---|---|---|---|
| CHEMBL24828 | VANDETANIB | 4 | 42,230 |
| CHEMBL288441 | BOSUTINIB | 4 | 12,255 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL428690 | ALVOCIDIB | 3 | 27,781 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| 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 — YANK family
ChEMBL bioactivities
18 potent at pChembl≥5 of 18 total, top 18 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.89 | Kd | 13 | nM | TAE-684 |
| 7.89 | Kd | 13 | nM | STAUROSPORINE |
| 6.19 | Kd | 640 | nM | LINIFANIB |
| 6.16 | Kd | 690 | nM | CHEMBL1241674 |
| 6.00 | IC50 | 1000 | nM | TP-030-1 |
| 6.00 | IC50 | 1000 | nM | TP-030-2 |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 5.89 | Kd | 1300 | nM | SB-203580 |
| 5.81 | Kd | 1544 | nM | CHEMBL4465866 |
| 5.76 | Kd | 1749 | nM | CHEMBL4576489 |
| 5.75 | Kd | 1800 | nM | BOSUTINIB |
| 5.68 | Kd | 2100 | nM | LESTAURTINIB |
| 5.64 | Kd | 2300 | nM | R-406 |
| 5.62 | Kd | 2400 | nM | MIDOSTAURIN |
| 5.60 | Kd | 2500 | nM | CHEMBL386051 |
| 5.36 | Kd | 4400 | nM | KW-2449 |
| 5.30 | Kd | 5000 | nM | VANDETANIB |
| 5.26 | Kd | 5500 | nM | ALVOCIDIB |
PubChem BioAssay actives
15 with measured affinity, of 128 total; 15 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 5-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 | 624821: Binding constant for YANK1 kinase domain | kd | 0.0130 | 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 | 624821: Binding constant for YANK1 kinase domain | kd | 0.0130 | uM |
| 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea | 624821: Binding constant for YANK1 kinase domain | kd | 0.6400 | uM |
| 2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol | 624821: Binding constant for YANK1 kinase domain | kd | 0.6900 | uM |
| 4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine | 624821: Binding constant for YANK1 kinase domain | kd | 1.3000 | 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 | 1526220: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged STK32A (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 1.5440 | 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 | 1526220: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged STK32A (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay | kd | 1.7490 | uM |
| Bosutinib | 624821: Binding constant for YANK1 kinase domain | kd | 1.8000 | 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 | 624821: Binding constant for YANK1 kinase domain | kd | 2.1000 | 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 | 624821: Binding constant for YANK1 kinase domain | kd | 2.3000 | uM |
| Midostaurin | 624821: Binding constant for YANK1 kinase domain | kd | 2.4000 | uM |
| 6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one | 624821: Binding constant for YANK1 kinase domain | kd | 2.5000 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624821: Binding constant for YANK1 kinase domain | kd | 4.4000 | uM |
| Vandetanib | 624821: Binding constant for YANK1 kinase domain | kd | 5.0000 | uM |
| 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one | 624821: Binding constant for YANK1 kinase domain | kd | 5.5000 | uM |
CTD chemical–gene interactions
29 total (human), top 29 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, decreases expression, increases expression | 5 |
| trichostatin A | decreases expression, affects cotreatment | 3 |
| Benzo(a)pyrene | decreases expression, increases expression, increases methylation | 3 |
| sodium arsenite | increases expression | 2 |
| mercuric bromide | decreases expression, affects cotreatment | 2 |
| entinostat | decreases expression, affects cotreatment | 2 |
| Vorinostat | affects cotreatment, decreases expression | 2 |
| Panobinostat | affects cotreatment, decreases expression | 2 |
| Nickel | decreases expression | 2 |
| Phenylmercuric Acetate | affects cotreatment, decreases expression | 2 |
| Tobacco Smoke Pollution | decreases expression, increases methylation | 2 |
| p-Chloromercuribenzoic Acid | decreases expression, affects cotreatment | 2 |
| methylmercuric chloride | decreases expression | 1 |
| caffeic acid | decreases expression, affects cotreatment | 1 |
| perfluoro-n-nonanoic acid | increases expression | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, decreases expression | 1 |
| belinostat | decreases expression | 1 |
| dorsomorphin | affects cotreatment, decreases expression | 1 |
| bisphenol S | decreases methylation | 1 |
| NSC 689534 | affects binding, increases expression | 1 |
| Zoledronic Acid | decreases expression | 1 |
| Troglitazone | increases expression | 1 |
| Acetaminophen | increases expression | 1 |
| Copper | affects binding, increases expression | 1 |
| Diethylhexyl Phthalate | decreases expression | 1 |
| N-Nitrosopyrrolidine | increases expression | 1 |
| Cyclosporine | increases expression | 1 |
| Thapsigargin | affects cotreatment, decreases expression | 1 |
| Acrylamide | increases expression | 1 |
ChEMBL screening assays
85 unique, capped per target: 85 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1045672 | Binding | Binding affinity to YANK1 assessed as percentage of kinase remaining bound to the bead at 1 uM by T7 phage display based binding assay | Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). — J Med Chem |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.