STK17B

gene
On this page

Also known as DRAK2

Summary

STK17B (serine/threonine kinase 17b, HGNC:11396) is a protein-coding gene on chromosome 2q32.3, encoding Serine/threonine-protein kinase 17B (O94768). Phosphorylates myosin light chains.

Enables ATP binding activity and protein serine/threonine kinase activity. Involved in intracellular signal transduction; positive regulation of fibroblast apoptotic process; and protein phosphorylation. Located in Flemming body and nucleoplasm.

Source: NCBI Gene 9262 — RefSeq curated summary.

At a glance

  • GWAS associations: 4
  • Clinical variants (ClinVar): 40 total
  • Druggable target: yes — 17 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_004226

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:11396
Approved symbolSTK17B
Nameserine/threonine kinase 17b
Location2q32.3
Locus typegene with protein product
StatusApproved
AliasesDRAK2
Ensembl geneENSG00000081320
Ensembl biotypeprotein_coding
OMIM604727
Entrez9262

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 13 protein_coding, 3 nonsense_mediated_decay

ENST00000263955, ENST00000409228, ENST00000420683, ENST00000449152, ENST00000606789, ENST00000714417, ENST00000714419, ENST00000714420, ENST00000714421, ENST00000714422, ENST00000714423, ENST00000879796, ENST00000879797, ENST00000879798, ENST00000879799, ENST00000915456

RefSeq mRNA: 1 — MANE Select: NM_004226 NM_004226

CCDS: CCDS2315

Canonical transcript exons

ENST00000263955 — 8 exons

ExonStartEnd
ENSE00001159995196171333196171578
ENSE00001692887196163262196163427
ENSE00004023932196156439196156651
ENSE00004023933196145911196146055
ENSE00004023934196133583196137729
ENSE00004023935196139620196139799
ENSE00004023936196143560196143686
ENSE00004023937196141249196141297

Expression profiles

Bgee: expression breadth ubiquitous, 252 present calls, max score 98.32.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 104.4272 / max 5066.3275, expressed in 1816 samples.

FANTOM5 promoters (8 alternative TSS)

Promoter IDTPM avgSamples expressed
3299770.15931805
3299628.41801658
329953.4758514
329982.0968900
330020.158582
330010.059621
329990.055327
330000.00401

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
epithelium of nasopharynxUBERON:000195198.32gold quality
nasopharynxUBERON:000172898.30gold quality
monocyteCL:000057698.23gold quality
mononuclear cellCL:000084298.03gold quality
leukocyteCL:000073897.93gold quality
jejunal mucosaUBERON:000039997.51gold quality
calcaneal tendonUBERON:000370196.60gold quality
tonsilUBERON:000237296.51gold quality
bloodUBERON:000017896.30gold quality
lymph nodeUBERON:000002996.22gold quality
bone marrowUBERON:000237195.80gold quality
mucosa of paranasal sinusUBERON:000503095.31gold quality
lower lobe of lungUBERON:000894995.20gold quality
granulocyteCL:000009494.80gold quality
colonic epitheliumUBERON:000039794.20gold quality
mammary ductUBERON:000176594.18gold quality
vermiform appendixUBERON:000115494.13gold quality
trabecular bone tissueUBERON:000248393.77gold quality
bone marrow cellCL:000209293.39gold quality
caecumUBERON:000115393.23gold quality
adrenal tissueUBERON:001830392.79gold quality
tibiaUBERON:000097992.23gold quality
amniotic fluidUBERON:000017392.09gold quality
visceral pleuraUBERON:000240191.80gold quality
spleenUBERON:000210691.74gold quality
parietal pleuraUBERON:000240091.70gold quality
pleuraUBERON:000097791.09gold quality
epithelium of mammary glandUBERON:000324490.92gold quality
oral cavityUBERON:000016790.45gold quality
upper leg skinUBERON:000426290.40gold quality

Single-cell (SCXA)

Detected in 13 experiment(s), a significant marker in 12.

ExperimentMarker?Max mean expression
E-MTAB-5061yes188.27
E-MTAB-6701yes101.96
E-MTAB-8142yes54.30
E-MTAB-10287yes37.03
E-MTAB-6678yes36.66
E-CURD-122yes35.73
E-GEOD-135922yes33.13
E-MTAB-9543yes18.66
E-CURD-119yes5.35
E-MTAB-9067yes4.62
E-CURD-112yes3.89
E-CURD-10no386.94
E-ANND-3no0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MYB

miRNA regulators (miRDB)

195 targeting STK17B, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3163100.0077.238605
HSA-MIR-340-5P100.0072.504437
HSA-MIR-7110-3P100.0073.182486
HSA-MIR-30A-5P100.0076.313233
HSA-MIR-30B-5P100.0076.293248
HSA-MIR-30C-5P100.0076.293248
HSA-MIR-30D-5P100.0076.323233
HSA-MIR-30E-5P100.0076.323242
HSA-MIR-8485100.0077.574731
HSA-MIR-4795-3P100.0074.624024
HSA-MIR-126-5P100.0072.713180
HSA-MIR-3613-3P100.0076.367965
HSA-MIR-5692B100.0071.322622
HSA-MIR-5692C100.0071.322622
HSA-LET-7A-3P100.0074.033932
HSA-LET-7B-3P100.0074.083913
HSA-LET-7F-1-3P100.0074.023928
HSA-MIR-98-3P100.0074.083907
HSA-MIR-186-5P99.9970.833707
HSA-MIR-428299.9975.366408
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-371B-5P99.9975.344759
HSA-MIR-366299.9973.825684
HSA-MIR-1213699.9872.815713
HSA-MIR-373-5P99.9875.364753
HSA-MIR-616-5P99.9875.584775
HSA-MIR-477599.9875.006394
HSA-MIR-569699.9872.364487
HSA-MIR-60799.9773.625593
HSA-MIR-302C-5P99.9772.563642

Literature-anchored findings (GeneRIF, showing 11)

  • DRAK2 kinase activity is regulated in a calcium-dependent manner and that Ser(12) phosphorylation is necessary for optimal suppression of T cell activation by this kinase (PMID:17182616)
  • Strong suppression of T cell receptor signals during thymic selection caused by ectopic DRAK2 expression in a DRAK2 transgenic mouse model of autoimmune encephalomyelitis alters the responsiveness of peripheral T cells. (PMID:19542440)
  • Regulation of the apoptosis-inducing kinase DRAK2 by cyclooxygenase-2 in colorectal cancer. (PMID:19638987)
  • DRAK2 and protein kinase D form a novel signaling module that controls calcium homeostasis following T cell activation. (PMID:21148796)
  • DRAK2 protein directly binds to the type I TGF-beta receptor and Knockdown of DRAK2 suppresses the tumorigenic ability of breast cancer cells. (PMID:23122956)
  • ChIP assays showed that in U937 cells MYB binds to a conserved element upstream of the DRAK2 transcription start site. (PMID:23398943)
  • A significant interaction between variants in STK17B and PAX8, in papillary thyroid cancer susceptibility, is reported. (PMID:24086368)
  • STK17B promotes carcinogenesis and metastasis via AKT/GSK-3beta/Snail signaling in hepatocellular carcinoma. (PMID:29445189)
  • DAP Kinase-Related Apoptosis-Inducing Protein Kinase 2 (DRAK2) Is a Key Regulator and Molecular Marker in Chronic Lymphocytic Leukemia. (PMID:33081245)
  • DRAK2 aggravates nonalcoholic fatty liver disease progression through SRSF6-associated RNA alternative splicing. (PMID:34614409)
  • DRAK2 suppresses autophagy by phosphorylating ULK1 at Ser[56] to diminish pancreatic beta cell function upon overnutrition. (PMID:38324636)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_reriostk17bENSDARG00000014348
mus_musculusStk17bENSMUSG00000026094
rattus_norvegicusStk17bENSRNOG00000012502
drosophila_melanogasterDrakFBGN0052666

Paralogs (1): STK17A (ENSG00000164543)

Protein

Protein identifiers

Serine/threonine-protein kinase 17BO94768 (reviewed: O94768)

Alternative names: DAP kinase-related apoptosis-inducing protein kinase 2

All UniProt accessions (7): O94768, A0AAQ5BHY2, A0AAQ5BI08, A0AAQ5BI73, C9JZJ1, Q53QE7, U3KQF8

UniProt curated annotations — full annotation on UniProt →

Function. Phosphorylates myosin light chains. Acts as a positive regulator of apoptosis.

Subunit / interactions. Interacts with CHP1; the interaction induces CHP1 to translocate from the Golgi to the nucleus.

Subcellular location. Nucleus. Cell membrane. Endoplasmic reticulum-Golgi intermediate compartment.

Tissue specificity. Highly expressed in placenta, lung, pancreas. Lower levels in heart, brain, liver, skeletal muscle and kidney.

Post-translational modifications. Autophosphorylated.

Similarity. Belongs to the protein kinase superfamily. CAMK Ser/Thr protein kinase family. DAP kinase subfamily.

RefSeq proteins (1): NP_004217* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000719Prot_kinase_domDomain
IPR008271Ser/Thr_kinase_ASActive_site
IPR011009Kinase-like_dom_sfHomologous_superfamily
IPR017441Protein_kinase_ATP_BSBinding_site
IPR042763ST17B_STKcDomain

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.

SubstrateKm (mM)Measurements
ATP0.0007–0.6411
KKRAARATSNVFA0.013–0.0453
PAH1 PHOSPHATIDATE PHOSPHATASE0.00022
RRRLSSLRA0.0036–0.00372
GTP0.461
KKRAARASSNVFA0.021
LYS-LYS-PHE-ASN-ARG-THR-LEU-SER-VAL-ALA0.00931
MYELIN BASIC PROTEIN0.1451

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 (36 total): helix 18, strand 7, turn 2, binding site 2, chain 1, domain 1, region of interest 1, compositionally biased region 1, active site 1, sequence variant 1, mutagenesis site 1

Structure

Experimental structures (PDB)

10 structures.

PDBMethodResolution (Å)
6ZJFX-RAY DIFFRACTION1.75
6Y6HX-RAY DIFFRACTION1.95
6Y6FX-RAY DIFFRACTION1.98
7AKGX-RAY DIFFRACTION2.08
3LM5X-RAY DIFFRACTION2.29
3LM0X-RAY DIFFRACTION2.35
6QF4X-RAY DIFFRACTION2.5
7Q7DX-RAY DIFFRACTION2.6
7Q7CX-RAY DIFFRACTION2.85
7Q7EX-RAY DIFFRACTION2.85

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O94768-F181.310.67

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): 158 (proton acceptor)

Ligand- & substrate-binding residues (2): 39–47; 62

Mutagenesis-validated functional residues (1):

PositionPhenotype
62loss of activity and of apoptotic function.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 323 (showing top): BEGUM_TARGETS_OF_PAX3_FOXO1_FUSION_UP, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, WALLACE_PROSTATE_CANCER_RACE_UP, TGCACTT_MIR519C_MIR519B_MIR519A, ENK_UV_RESPONSE_KERATINOCYTE_UP, TTTGTAG_MIR520D, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, IVANOVA_HEMATOPOIESIS_MATURE_CELL, GRANDVAUX_IRF3_TARGETS_DN, RODRIGUES_NTN1_TARGETS_DN, WANG_ESOPHAGUS_CANCER_VS_NORMAL_DN, FINETTI_BREAST_CANCER_KINOME_GREEN, FISCHER_G2_M_CELL_CYCLE, MODULE_206

GO Biological Process (7): protein phosphorylation (GO:0006468), apoptotic process (GO:0006915), intracellular signal transduction (GO:0035556), positive regulation of apoptotic process (GO:0043065), protein autophosphorylation (GO:0046777), positive regulation of fibroblast apoptotic process (GO:2000271), programmed cell death (GO:0012501)

GO Molecular Function (7): protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (7): nucleus (GO:0005634), nucleoplasm (GO:0005654), endoplasmic reticulum-Golgi intermediate compartment (GO:0005793), plasma membrane (GO:0005886), actin cytoskeleton (GO:0015629), Flemming body (GO:0090543), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
signal transduction2
protein kinase activity2
intracellular membrane-bounded organelle2
phosphorylation1
protein modification process1
programmed cell death1
apoptotic signaling pathway1
execution phase of apoptosis1
intracellular anatomical structure1
apoptotic process1
regulation of apoptotic process1
positive regulation of programmed cell death1
protein phosphorylation1
positive regulation of apoptotic process1
fibroblast apoptotic process1
regulation of fibroblast apoptotic process1
cell death1
kinase activity1
phosphotransferase activity, alcohol group as acceptor1
catalytic activity, acting on a protein1
adenyl ribonucleotide binding1
purine ribonucleoside triphosphate binding1
nucleoside phosphate binding1
heterocyclic compound binding1
transferase activity, transferring phosphorus-containing groups1
catalytic activity1
nuclear lumen1
cytoplasm1
membrane1
cell periphery1
cytoskeleton1
midbody1

Protein interactions and networks

STRING

1717 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
STK17BDAPP51397581
STK17BCHP1Q99653567
STK17BPRKD3O94806453
STK17BPRKD2Q9BZL6452
STK17BPRKD1Q15139451
STK17BHECW2Q9P2P5437
STK17BPLEKHF1Q96S99428
STK17BSPRR2GQ9BYE4414
STK17BRMP24Q32NC0409
STK17BNME5P56597401
STK17BCDC7O00311393
STK17BNUP35Q8NFH5389
STK17BDRC11Q86XH1387
STK17BITPR1Q14643383
STK17BTMEM101Q96IK0359

IntAct

37 interactions, top by confidence:

ABTypeScore
EPHA1EXOC5psi-mi:“MI:0914”(association)0.530
FAM174ABLTP3Bpsi-mi:“MI:0914”(association)0.530
LAMP1FZD7psi-mi:“MI:0914”(association)0.530
STK17BKCNIP2psi-mi:“MI:0915”(physical association)0.400
STK17BUBA52psi-mi:“MI:0915”(physical association)0.400
STK17BRPS24psi-mi:“MI:0915”(physical association)0.370
STK17BSCAMP3psi-mi:“MI:0914”(association)0.350
STK17BREV3Lpsi-mi:“MI:0914”(association)0.350
TMEM30AUPK3BL1psi-mi:“MI:0914”(association)0.350
P2RX5NOP56psi-mi:“MI:0914”(association)0.350
CHRM4GEMIN2psi-mi:“MI:0914”(association)0.350
LPAR6DEGS1psi-mi:“MI:0914”(association)0.350
LAMP1ORC4psi-mi:“MI:0914”(association)0.350
CHSY3STK17Bpsi-mi:“MI:0914”(association)0.350
STK17BTPM2psi-mi:“MI:0914”(association)0.350
STK17BH2AZ1psi-mi:“MI:0914”(association)0.350
IGHMESYT2psi-mi:“MI:0914”(association)0.350
AVPR2GXYLT2psi-mi:“MI:0914”(association)0.350
GPR17TMEM120Bpsi-mi:“MI:0914”(association)0.350
HCSTTMEM120Bpsi-mi:“MI:0914”(association)0.350
HIDE1TMEM120Bpsi-mi:“MI:0914”(association)0.350
MLNRNBASpsi-mi:“MI:0914”(association)0.350
CD80POTEFpsi-mi:“MI:0914”(association)0.350
TACSTD2RIMOC1psi-mi:“MI:0914”(association)0.350
FAXCMETTL15psi-mi:“MI:0914”(association)0.350
FPR1GPR89Apsi-mi:“MI:0914”(association)0.350
P2RX5TNPO2psi-mi:“MI:0914”(association)0.350
CHRM4TNPO2psi-mi:“MI:0914”(association)0.350
COMTD1TARS3psi-mi:“MI:0914”(association)0.350

BioGRID (68): STK17B (Affinity Capture-MS), STK17B (Affinity Capture-MS), AFMID (Affinity Capture-MS), KCNIP2 (Affinity Capture-MS), REV3L (Affinity Capture-MS), SLC2A1 (Affinity Capture-MS), TOX4 (Affinity Capture-MS), SCAMP3 (Affinity Capture-MS), TRIB1 (Affinity Capture-MS), ATXN2L (Affinity Capture-MS), MDN1 (Affinity Capture-MS), FAF2 (Affinity Capture-MS), WBP11 (Affinity Capture-MS), UBAC2 (Affinity Capture-MS), STK17B (Affinity Capture-MS)

ESM2 similar proteins: D4A7V9, F1QGZ6, O15530, O54785, O54863, O94768, O96017, P53351, P53666, P53670, P53671, P92958, Q14680, Q20443, Q28GW8, Q32L23, Q38997, Q3SZW1, Q5HZ38, Q5RBJ6, Q5SUV5, Q61241, Q61846, Q6DE87, Q6SA08, Q7RTN6, Q7TNJ7, Q7TNZ6, Q852Q2, Q86YV6, Q8BG48, Q8C1R0, Q8NG66, Q8VDF3, Q8WNU8, Q91821, Q91VB2, Q91XS8, Q93V58, Q96NX5

Diamond homologs: A0A509AFG4, A0A5K1K8H0, A2AAJ9, A2ZVI7, A4IFM7, A8C984, A8WXF6, B9FKW9, C0HKC8, C0HKC9, E9PT87, O02827, O43293, O44997, O54784, O62305, O70150, O75147, O80673, O88764, O94768, P07313, P08414, P11801, P13234, P15735, P18653, P20689, P29294, P31325, P34101, P43292, P53355, P53681, Q00168, Q00771, Q0KHT7, Q0V7M1, Q10KY3, Q14012

SIGNOR signaling

2 interactions.

AEffectBMechanism
PRKD1“up-regulates activity”STK17Bphosphorylation
PRKCG“down-regulates activity”STK17Bphosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance28
Likely benign2
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1628 predictions. Top by Δscore:

VariantEffectΔscore
2:196139614:A:ACdonor_gain1.0000
2:196139615:C:CCdonor_gain1.0000
2:196139615:CTTA:Cdonor_gain1.0000
2:196139616:TTAC:Tdonor_loss1.0000
2:196139617:TACTC:Tdonor_loss1.0000
2:196139618:A:ACdonor_gain1.0000
2:196139618:A:Tdonor_loss1.0000
2:196139618:ACT:Adonor_gain1.0000
2:196139619:C:CCdonor_gain1.0000
2:196139619:CT:Cdonor_gain1.0000
2:196139619:CTC:Cdonor_gain1.0000
2:196139619:CTCT:Cdonor_gain1.0000
2:196139619:CTCTG:Cdonor_gain1.0000
2:196139795:TATTC:Tacceptor_gain1.0000
2:196139797:TTC:Tacceptor_gain1.0000
2:196139798:TC:Tacceptor_gain1.0000
2:196139799:CC:Cacceptor_gain1.0000
2:196139800:C:CAacceptor_loss1.0000
2:196139800:C:CCacceptor_gain1.0000
2:196139801:T:Cacceptor_loss1.0000
2:196141248:CCA:Cdonor_gain1.0000
2:196141255:T:Cdonor_gain1.0000
2:196141297:GC:Gacceptor_loss1.0000
2:196141298:C:CAacceptor_loss1.0000
2:196141298:C:CCacceptor_gain1.0000
2:196141299:T:Aacceptor_loss1.0000
2:196143554:TCTTA:Tdonor_loss1.0000
2:196143555:CTTA:Cdonor_loss1.0000
2:196143556:TTAC:Tdonor_loss1.0000
2:196143557:TACC:Tdonor_loss1.0000

AlphaMissense

2453 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
2:196137723:T:AR281S0.999
2:196137723:T:GR281S0.999
2:196137724:C:GR281T0.999
2:196139791:C:TG222D0.999
2:196139792:C:GG222R0.999
2:196141250:A:GW219R0.999
2:196141250:A:TW219R0.999
2:196143630:A:CD179E0.999
2:196143630:A:TD179E0.999
2:196143631:T:AD179V0.999
2:196156588:T:AK62N0.999
2:196156588:T:GK62N0.999
2:196156595:G:TA60D0.999
2:196139751:A:CF235L0.998
2:196139751:A:TF235L0.998
2:196139753:A:GF235L0.998
2:196139791:C:AG222V0.998
2:196139799:C:AW219C0.998
2:196139799:C:GW219C0.998
2:196143631:T:GD179A0.998
2:196143632:C:GD179H0.998
2:196145918:T:AD158V0.998
2:196145958:C:GG145R0.998
2:196145958:C:TG145R0.998
2:196156523:A:GL84P0.998
2:196156590:T:CK62E0.998
2:196156590:T:GK62Q0.998
2:196156592:G:TA61E0.998
2:196156593:C:GA61P0.998
2:196156624:A:CC50W0.998

dbSNP variants (sampled 300 via entrez): RS1000012000 (2:196141128 T>C), RS1000074930 (2:196169305 T>C), RS1000085688 (2:196162560 A>G), RS1000122190 (2:196169604 T>C), RS1000151141 (2:196177190 C>T), RS1000221199 (2:196162852 T>C,G), RS1000388486 (2:196157270 A>G), RS1000445284 (2:196151439 G>A), RS1000480932 (2:196134649 G>A), RS1000497218 (2:196151631 T>A), RS1000539371 (2:196139305 T>C), RS1000639401 (2:196147619 A>G), RS1000642993 (2:196145589 A>G), RS1000659767 (2:196138719 G>A), RS1000795301 (2:196138935 A>G)

Disease associations

OMIM: gene MIM:604727 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

StudyTraitp-value
GCST90002381_55Eosinophil count9.000000e-11
GCST90002382_81Eosinophil percentage of white cells3.000000e-12
GCST90002396_178Mean reticulocyte volume1.000000e-09
GCST90002397_455Mean spheric corpuscular volume3.000000e-14

EFO canonical traits (3, from GWAS)

EFO IDTrait name
EFO:0004842eosinophil count
EFO:0007991eosinophil percentage of leukocytes
EFO:0010701mean reticulocyte volume

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3980 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 396,768 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL1287853FEDRATINIB43,554
CHEMBL1789941RUXOLITINIB411,547
CHEMBL180022NERATINIB49,404
CHEMBL502835NINTEDANIB48,545
CHEMBL535SUNITINIB479,020
CHEMBL553ERLOTINIB4108,300
CHEMBL608533MIDOSTAURIN47,259
CHEMBL939GEFITINIB4117,814
CHEMBL31965CANERTINIB38,083
CHEMBL428690ALVOCIDIB327,781
CHEMBL522892DOVITINIB34,944
CHEMBL603469LESTAURTINIB3
CHEMBL1721885SU-0148132363
CHEMBL475251R-4062762
CHEMBL607707PELITINIB26,340
CHEMBL1908397KW-24491622
CHEMBL259084MLN-805412,430

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Death-associated kinase (DAPK) family

Binding affinities (BindingDB)

9 measured of 10 human assays (10 total across all organisms); most potent 9 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
StaurosporineKD1.7 nM
PKC-412KD190 nM
4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acidKD300 nM
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyrilKD520 nM
GEFITINIBIC502300 nMUS-9416123: Kinase modulators for the treatment of cancer
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-carboxamideKD2600 nM
(E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)but-2-enamideKD3500 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-carboxamideKD3500 nM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-oneKD5300 nM

ChEMBL bioactivities

216 potent at pChembl≥5 of 235 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.59Ki0.26nMCHEMBL3797480
8.52IC503nMCHEMBL3797480
8.42Kd3.8nMCHEMBL1836719
8.32Kd4.8nMKW-2449
8.30Kd5nMLESTAURTINIB
8.25Kd5.6nMCHEMBL4752776
8.15IC507nMCHEMBL4796519
8.10IC508nMCHEMBL3799389
8.10Kd8nMCHEMBL4060481
8.09Kd8.1nMMLN-8054
8.05Kd9nMCHEMBL3334979
8.04Kd9.2nMR-406
8.00IC5010nMCHEMBL3799585
8.00IC5010nMCHEMBL5433785
7.96Kd11nMCHEMBL1836721
7.89IC5013nMCHEMBL4760126
7.85IC5014nMCHEMBL3797466
7.85IC5014nMCHEMBL3799505
7.85IC5014nMCHEMBL4753926
7.75IC5018nMCHEMBL4763132
7.70IC5020nMCHEMBL1836719
7.68IC5021nMCHEMBL513703
7.68Kd21nMSTAUROSPORINE
7.64IC5023nMCHEMBL1836724
7.59IC5025.8nMSTAUROSPORINE
7.58Kd26nMSTAUROSPORINE
7.57Kd27nMCHEMBL3334980
7.57IC5027nMCHEMBL4754748
7.55IC5028nMCHEMBL4794509
7.54IC5029nMCHEMBL4060481
7.52Kd30nMCHEMBL1836641
7.52IC5030nMCHEMBL6005757
7.48Kd33nMCHEMBL3334981
7.48IC5033nMCHEMBL4788024
7.47IC5034nMCHEMBL4752776
7.46IC5035nMCHEMBL1836717
7.46IC5035nMCHEMBL4747753
7.43IC5037nMCHEMBL4740090
7.41IC5039nMCHEMBL1836714
7.40IC5040nMCHEMBL4783516
7.40IC5040nMCHEMBL5831473
7.39IC5041nMCHEMBL4753625
7.35Kd45nMFEDRATINIB
7.31IC5049nMCHEMBL4745018
7.31IC5049nMCHEMBL4740604
7.31IC5049nMCHEMBL4789685
7.23IC5059nMCHEMBL4748440
7.22IC5060nMCHEMBL4788886
7.21IC5062nMCHEMBL4739879
7.20IC5063nMCHEMBL4792541

PubChem BioAssay actives

188 with measured affinity, of 655 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.

CompoundAssayTypeValueUnit
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]pentanamide1298205: Competitive inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by Lineweaver-Burk plot analysis in presence of ATPki0.0003uM
2-[6-(4-methylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assaykd0.0038uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone624942: Binding constant for DRAK2 kinase domainkd0.0048uM
(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-one507904: Binding affinity to DRAK2kd0.0050uM
2-[6-(1-benzothiophen-2-yl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assaykd0.0056uM
2-[6-(4-methylsulfinylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0070uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]cyclopropanecarboxamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.0080uM
5-(3-amino-5-thiophen-3-ylthieno[2,3-b]pyridin-2-yl)-3H-1,3,4-oxadiazole-2-thione1966671: Binding affinity to DRAK2 (unknown origin) assessed as dissociation constantkd0.0080uM
4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid435401: Binding constant for full-length DRAK2kd0.0081uM
N-[5-(3,4-dimethoxyphenyl)thieno[2,3-b]pyridin-3-yl]cyclohexanecarboxamide1162292: Binding affinity to DRAK2 (unknown origin) ATP sitekd0.0090uM
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one624942: Binding constant for DRAK2 kinase domainkd0.0092uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]butanamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.0100uM
4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-5-methoxy-2-N-[4-(methylsulfonylmethyl)phenyl]pyrimidine-2,4-diamine1966670: Inhibition of DRAK2 (unknown origin)ic500.0100uM
2-[6-(4-carbamoylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assaykd0.0110uM
2-[6-(4-acetylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0130uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-3-methylbut-2-enamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.0140uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-3,3-dimethylbutanamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.0140uM
2-[6-(4-morpholin-4-ylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0140uM
2-[6-(3-fluoro-4-methoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0180uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-2,2-dimethylpropanamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.0210uM
(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-one435401: Binding constant for full-length DRAK2kd0.0210uM
2-[6-(4-acetamidophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0230uM
N-[2-(3,4-dimethoxyphenyl)thieno[2,3-b]pyrazin-7-yl]cyclohexanecarboxamide1162292: Binding affinity to DRAK2 (unknown origin) ATP sitekd0.0270uM
2-[6-(3-fluoro-4-methylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0270uM
2-[6-(4-ethenylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0280uM
2-[6-(1H-indazol-5-yl)thieno[3,2-d]pyrimidin-4-yl]oxyacetic acid1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assaykd0.0300uM
N-[5-(3,4-dimethoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]cyclohexanecarboxamide1162292: Binding affinity to DRAK2 (unknown origin) ATP sitekd0.0330uM
2-[6-[4-(trifluoromethyl)phenyl]thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0330uM
2-[6-(3-acetamidophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0350uM
2-[6-(4-cyanophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0350uM
2-[6-(6-acetyl-3-pyridinyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0370uM
2-[6-(4-chlorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0390uM
2-[6-(4-ethoxycarbonylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0400uM
2-[6-(4-ethylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0410uM
Fedratinib624942: Binding constant for DRAK2 kinase domainkd0.0450uM
2-[6-(4-propan-2-ylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0490uM
2-[6-(3-fluorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0490uM
2-[6-(3-methylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0490uM
2-[6-(4-propan-2-ylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0590uM
2-[6-(2-fluorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0600uM
2-[6-(4-cyclopropylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0620uM
2-(6-thiophen-2-ylthieno[3,2-d]pyrimidin-4-yl)sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0630uM
2-[6-(3,4-difluorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0740uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-3,5-dinitrobenzamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.0770uM
2-[6-(3-morpholin-4-ylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0830uM
2-[6-(3,4-dichlorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.0920uM
2-[6-(2-methoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.1100uM
2-[6-(4-phenylmethoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid1718373: Inhibition of N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli incubated for 90 mins by Kinase seeker split luciferase assayic500.1100uM
Sunitinib435401: Binding constant for full-length DRAK2kd0.1100uM
N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]cyclohexanecarboxamide1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assayic500.1200uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Arsenicaffects expression, affects methylation2
Dexamethasoneincreases expression, affects cotreatment2
Nickelincreases expression2
Tobacco Smoke Pollutiondecreases expression, increases expression2
3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamidedecreases expression1
bisphenol Faffects cotreatment, increases expression1
TL8-506affects cotreatment, increases expression1
methylmercuric chloridedecreases expression1
triphenyl phosphateaffects expression1
trichostatin Aaffects expression1
butyraldehydeincreases expression1
sulindac sulfideincreases expression1
benzo(e)pyreneincreases methylation1
resorcinoldecreases expression1
S-(1,2-dichlorovinyl)cysteineincreases expression, affects response to substance1
di-n-butylphosphoric acidaffects expression1
erucylphospho-N,N,N-trimethylpropylammoniumincreases expression1
abrineincreases expression1
jinfukangaffects cotreatment, decreases expression1
NSC 689534affects binding, increases expression1
Resveratroldecreases expression1
Decitabineaffects cotreatment, increases expression1
Sunitinibdecreases expression1
Arsenic Trioxideaffects cotreatment, decreases expression1
Fulvestrantincreases methylation1
Vorinostatincreases expression1
Leflunomideincreases expression1
Acetaminophenincreases expression1
Air Pollutantsdecreases expression, increases abundance1
Ascorbic Acidaffects cotreatment, increases expression1

ChEMBL screening assays

179 unique, capped per target: 179 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1034105BindingInhibition of DRAK2 at 3 uMDiscovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — J Med Chem

Cellosaurus cell lines

5 cell lines: 5 cancer cell line

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

CellosaurusNameCategorySex
CVCL_D1QTAbcam K-562 STK17B KOCancer cell lineFemale
CVCL_D2MEAbcam Raji STK17B KOCancer cell lineMale
CVCL_TQ76HAP1 STK17B (-) 1Cancer cell lineMale
CVCL_TQ77HAP1 STK17B (-) 2Cancer cell lineMale
CVCL_WQ62Abcam Jurkat STK17B KOCancer cell lineMale

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.