STK17B
gene geneOn 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
| Field | Value |
|---|---|
| HGNC ID | HGNC:11396 |
| Approved symbol | STK17B |
| Name | serine/threonine kinase 17b |
| Location | 2q32.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | DRAK2 |
| Ensembl gene | ENSG00000081320 |
| Ensembl biotype | protein_coding |
| OMIM | 604727 |
| Entrez | 9262 |
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
| Exon | Start | End |
|---|---|---|
| ENSE00001159995 | 196171333 | 196171578 |
| ENSE00001692887 | 196163262 | 196163427 |
| ENSE00004023932 | 196156439 | 196156651 |
| ENSE00004023933 | 196145911 | 196146055 |
| ENSE00004023934 | 196133583 | 196137729 |
| ENSE00004023935 | 196139620 | 196139799 |
| ENSE00004023936 | 196143560 | 196143686 |
| ENSE00004023937 | 196141249 | 196141297 |
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 ID | TPM avg | Samples expressed |
|---|---|---|
| 32997 | 70.1593 | 1805 |
| 32996 | 28.4180 | 1658 |
| 32995 | 3.4758 | 514 |
| 32998 | 2.0968 | 900 |
| 33002 | 0.1585 | 82 |
| 33001 | 0.0596 | 21 |
| 32999 | 0.0553 | 27 |
| 33000 | 0.0040 | 1 |
Top tissues by expression
287 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| epithelium of nasopharynx | UBERON:0001951 | 98.32 | gold quality |
| nasopharynx | UBERON:0001728 | 98.30 | gold quality |
| monocyte | CL:0000576 | 98.23 | gold quality |
| mononuclear cell | CL:0000842 | 98.03 | gold quality |
| leukocyte | CL:0000738 | 97.93 | gold quality |
| jejunal mucosa | UBERON:0000399 | 97.51 | gold quality |
| calcaneal tendon | UBERON:0003701 | 96.60 | gold quality |
| tonsil | UBERON:0002372 | 96.51 | gold quality |
| blood | UBERON:0000178 | 96.30 | gold quality |
| lymph node | UBERON:0000029 | 96.22 | gold quality |
| bone marrow | UBERON:0002371 | 95.80 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 95.31 | gold quality |
| lower lobe of lung | UBERON:0008949 | 95.20 | gold quality |
| granulocyte | CL:0000094 | 94.80 | gold quality |
| colonic epithelium | UBERON:0000397 | 94.20 | gold quality |
| mammary duct | UBERON:0001765 | 94.18 | gold quality |
| vermiform appendix | UBERON:0001154 | 94.13 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 93.77 | gold quality |
| bone marrow cell | CL:0002092 | 93.39 | gold quality |
| caecum | UBERON:0001153 | 93.23 | gold quality |
| adrenal tissue | UBERON:0018303 | 92.79 | gold quality |
| tibia | UBERON:0000979 | 92.23 | gold quality |
| amniotic fluid | UBERON:0000173 | 92.09 | gold quality |
| visceral pleura | UBERON:0002401 | 91.80 | gold quality |
| spleen | UBERON:0002106 | 91.74 | gold quality |
| parietal pleura | UBERON:0002400 | 91.70 | gold quality |
| pleura | UBERON:0000977 | 91.09 | gold quality |
| epithelium of mammary gland | UBERON:0003244 | 90.92 | gold quality |
| oral cavity | UBERON:0000167 | 90.45 | gold quality |
| upper leg skin | UBERON:0004262 | 90.40 | gold quality |
Single-cell (SCXA)
Detected in 13 experiment(s), a significant marker in 12.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-5061 | yes | 188.27 |
| E-MTAB-6701 | yes | 101.96 |
| E-MTAB-8142 | yes | 54.30 |
| E-MTAB-10287 | yes | 37.03 |
| E-MTAB-6678 | yes | 36.66 |
| E-CURD-122 | yes | 35.73 |
| E-GEOD-135922 | yes | 33.13 |
| E-MTAB-9543 | yes | 18.66 |
| E-CURD-119 | yes | 5.35 |
| E-MTAB-9067 | yes | 4.62 |
| E-CURD-112 | yes | 3.89 |
| E-CURD-10 | no | 386.94 |
| E-ANND-3 | no | 0.00 |
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):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-340-5P | 100.00 | 72.50 | 4437 |
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| 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-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-4795-3P | 100.00 | 74.62 | 4024 |
| HSA-MIR-126-5P | 100.00 | 72.71 | 3180 |
| HSA-MIR-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-5692B | 100.00 | 71.32 | 2622 |
| HSA-MIR-5692C | 100.00 | 71.32 | 2622 |
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-186-5P | 99.99 | 70.83 | 3707 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-302C-5P | 99.97 | 72.56 | 3642 |
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
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | stk17b | ENSDARG00000014348 |
| mus_musculus | Stk17b | ENSMUSG00000026094 |
| rattus_norvegicus | Stk17b | ENSRNOG00000012502 |
| drosophila_melanogaster | Drak | FBGN0052666 |
Paralogs (1): STK17A (ENSG00000164543)
Protein
Protein identifiers
Serine/threonine-protein kinase 17B — O94768 (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)
| 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 |
| IPR042763 | ST17B_STKc | Domain |
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), 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.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6ZJF | X-RAY DIFFRACTION | 1.75 |
| 6Y6H | X-RAY DIFFRACTION | 1.95 |
| 6Y6F | X-RAY DIFFRACTION | 1.98 |
| 7AKG | X-RAY DIFFRACTION | 2.08 |
| 3LM5 | X-RAY DIFFRACTION | 2.29 |
| 3LM0 | X-RAY DIFFRACTION | 2.35 |
| 6QF4 | X-RAY DIFFRACTION | 2.5 |
| 7Q7D | X-RAY DIFFRACTION | 2.6 |
| 7Q7C | X-RAY DIFFRACTION | 2.85 |
| 7Q7E | X-RAY DIFFRACTION | 2.85 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O94768-F1 | 81.31 | 0.67 |
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):
| Position | Phenotype |
|---|---|
| 62 | loss 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:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| signal transduction | 2 |
| protein kinase activity | 2 |
| intracellular membrane-bounded organelle | 2 |
| phosphorylation | 1 |
| protein modification process | 1 |
| programmed cell death | 1 |
| apoptotic signaling pathway | 1 |
| execution phase of apoptosis | 1 |
| intracellular anatomical structure | 1 |
| apoptotic process | 1 |
| regulation of apoptotic process | 1 |
| positive regulation of programmed cell death | 1 |
| protein phosphorylation | 1 |
| positive regulation of apoptotic process | 1 |
| fibroblast apoptotic process | 1 |
| regulation of fibroblast apoptotic process | 1 |
| cell death | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| nuclear lumen | 1 |
| cytoplasm | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cytoskeleton | 1 |
| midbody | 1 |
Protein interactions and networks
STRING
1717 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| STK17B | DAP | P51397 | 581 |
| STK17B | CHP1 | Q99653 | 567 |
| STK17B | PRKD3 | O94806 | 453 |
| STK17B | PRKD2 | Q9BZL6 | 452 |
| STK17B | PRKD1 | Q15139 | 451 |
| STK17B | HECW2 | Q9P2P5 | 437 |
| STK17B | PLEKHF1 | Q96S99 | 428 |
| STK17B | SPRR2G | Q9BYE4 | 414 |
| STK17B | RMP24 | Q32NC0 | 409 |
| STK17B | NME5 | P56597 | 401 |
| STK17B | CDC7 | O00311 | 393 |
| STK17B | NUP35 | Q8NFH5 | 389 |
| STK17B | DRC11 | Q86XH1 | 387 |
| STK17B | ITPR1 | Q14643 | 383 |
| STK17B | TMEM101 | Q96IK0 | 359 |
IntAct
37 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| EPHA1 | EXOC5 | psi-mi:“MI:0914”(association) | 0.530 |
| FAM174A | BLTP3B | psi-mi:“MI:0914”(association) | 0.530 |
| LAMP1 | FZD7 | psi-mi:“MI:0914”(association) | 0.530 |
| STK17B | KCNIP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| STK17B | UBA52 | psi-mi:“MI:0915”(physical association) | 0.400 |
| STK17B | RPS24 | psi-mi:“MI:0915”(physical association) | 0.370 |
| STK17B | SCAMP3 | psi-mi:“MI:0914”(association) | 0.350 |
| STK17B | REV3L | psi-mi:“MI:0914”(association) | 0.350 |
| TMEM30A | UPK3BL1 | psi-mi:“MI:0914”(association) | 0.350 |
| P2RX5 | NOP56 | psi-mi:“MI:0914”(association) | 0.350 |
| CHRM4 | GEMIN2 | psi-mi:“MI:0914”(association) | 0.350 |
| LPAR6 | DEGS1 | psi-mi:“MI:0914”(association) | 0.350 |
| LAMP1 | ORC4 | psi-mi:“MI:0914”(association) | 0.350 |
| CHSY3 | STK17B | psi-mi:“MI:0914”(association) | 0.350 |
| STK17B | TPM2 | psi-mi:“MI:0914”(association) | 0.350 |
| STK17B | H2AZ1 | psi-mi:“MI:0914”(association) | 0.350 |
| IGHM | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| AVPR2 | GXYLT2 | psi-mi:“MI:0914”(association) | 0.350 |
| GPR17 | TMEM120B | psi-mi:“MI:0914”(association) | 0.350 |
| HCST | TMEM120B | psi-mi:“MI:0914”(association) | 0.350 |
| HIDE1 | TMEM120B | psi-mi:“MI:0914”(association) | 0.350 |
| MLNR | NBAS | psi-mi:“MI:0914”(association) | 0.350 |
| CD80 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| TACSTD2 | RIMOC1 | psi-mi:“MI:0914”(association) | 0.350 |
| FAXC | METTL15 | psi-mi:“MI:0914”(association) | 0.350 |
| FPR1 | GPR89A | psi-mi:“MI:0914”(association) | 0.350 |
| P2RX5 | TNPO2 | psi-mi:“MI:0914”(association) | 0.350 |
| CHRM4 | TNPO2 | psi-mi:“MI:0914”(association) | 0.350 |
| COMTD1 | TARS3 | psi-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.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PRKD1 | “up-regulates activity” | STK17B | phosphorylation |
| PRKCG | “down-regulates activity” | STK17B | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
40 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 28 |
| Likely benign | 2 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1628 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:196139614:A:AC | donor_gain | 1.0000 |
| 2:196139615:C:CC | donor_gain | 1.0000 |
| 2:196139615:CTTA:C | donor_gain | 1.0000 |
| 2:196139616:TTAC:T | donor_loss | 1.0000 |
| 2:196139617:TACTC:T | donor_loss | 1.0000 |
| 2:196139618:A:AC | donor_gain | 1.0000 |
| 2:196139618:A:T | donor_loss | 1.0000 |
| 2:196139618:ACT:A | donor_gain | 1.0000 |
| 2:196139619:C:CC | donor_gain | 1.0000 |
| 2:196139619:CT:C | donor_gain | 1.0000 |
| 2:196139619:CTC:C | donor_gain | 1.0000 |
| 2:196139619:CTCT:C | donor_gain | 1.0000 |
| 2:196139619:CTCTG:C | donor_gain | 1.0000 |
| 2:196139795:TATTC:T | acceptor_gain | 1.0000 |
| 2:196139797:TTC:T | acceptor_gain | 1.0000 |
| 2:196139798:TC:T | acceptor_gain | 1.0000 |
| 2:196139799:CC:C | acceptor_gain | 1.0000 |
| 2:196139800:C:CA | acceptor_loss | 1.0000 |
| 2:196139800:C:CC | acceptor_gain | 1.0000 |
| 2:196139801:T:C | acceptor_loss | 1.0000 |
| 2:196141248:CCA:C | donor_gain | 1.0000 |
| 2:196141255:T:C | donor_gain | 1.0000 |
| 2:196141297:GC:G | acceptor_loss | 1.0000 |
| 2:196141298:C:CA | acceptor_loss | 1.0000 |
| 2:196141298:C:CC | acceptor_gain | 1.0000 |
| 2:196141299:T:A | acceptor_loss | 1.0000 |
| 2:196143554:TCTTA:T | donor_loss | 1.0000 |
| 2:196143555:CTTA:C | donor_loss | 1.0000 |
| 2:196143556:TTAC:T | donor_loss | 1.0000 |
| 2:196143557:TACC:T | donor_loss | 1.0000 |
AlphaMissense
2453 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:196137723:T:A | R281S | 0.999 |
| 2:196137723:T:G | R281S | 0.999 |
| 2:196137724:C:G | R281T | 0.999 |
| 2:196139791:C:T | G222D | 0.999 |
| 2:196139792:C:G | G222R | 0.999 |
| 2:196141250:A:G | W219R | 0.999 |
| 2:196141250:A:T | W219R | 0.999 |
| 2:196143630:A:C | D179E | 0.999 |
| 2:196143630:A:T | D179E | 0.999 |
| 2:196143631:T:A | D179V | 0.999 |
| 2:196156588:T:A | K62N | 0.999 |
| 2:196156588:T:G | K62N | 0.999 |
| 2:196156595:G:T | A60D | 0.999 |
| 2:196139751:A:C | F235L | 0.998 |
| 2:196139751:A:T | F235L | 0.998 |
| 2:196139753:A:G | F235L | 0.998 |
| 2:196139791:C:A | G222V | 0.998 |
| 2:196139799:C:A | W219C | 0.998 |
| 2:196139799:C:G | W219C | 0.998 |
| 2:196143631:T:G | D179A | 0.998 |
| 2:196143632:C:G | D179H | 0.998 |
| 2:196145918:T:A | D158V | 0.998 |
| 2:196145958:C:G | G145R | 0.998 |
| 2:196145958:C:T | G145R | 0.998 |
| 2:196156523:A:G | L84P | 0.998 |
| 2:196156590:T:C | K62E | 0.998 |
| 2:196156590:T:G | K62Q | 0.998 |
| 2:196156592:G:T | A61E | 0.998 |
| 2:196156593:C:G | A61P | 0.998 |
| 2:196156624:A:C | C50W | 0.998 |
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):
| Study | Trait | p-value |
|---|---|---|
| GCST90002381_55 | Eosinophil count | 9.000000e-11 |
| GCST90002382_81 | Eosinophil percentage of white cells | 3.000000e-12 |
| GCST90002396_178 | Mean reticulocyte volume | 1.000000e-09 |
| GCST90002397_455 | Mean spheric corpuscular volume | 3.000000e-14 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004842 | eosinophil count |
| EFO:0007991 | eosinophil percentage of leukocytes |
| EFO:0010701 | mean 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).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1789941 | RUXOLITINIB | 4 | 11,547 |
| CHEMBL180022 | NERATINIB | 4 | 9,404 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL553 | ERLOTINIB | 4 | 108,300 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL939 | GEFITINIB | 4 | 117,814 |
| CHEMBL31965 | CANERTINIB | 3 | 8,083 |
| CHEMBL428690 | ALVOCIDIB | 3 | 27,781 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL475251 | R-406 | 2 | 762 |
| CHEMBL607707 | PELITINIB | 2 | 6,340 |
| CHEMBL1908397 | KW-2449 | 1 | 622 |
| CHEMBL259084 | MLN-8054 | 1 | 2,430 |
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.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| Staurosporine | KD | 1.7 nM | |
| PKC-412 | KD | 190 nM | |
| 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid | KD | 300 nM | |
| (3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril | KD | 520 nM | |
| GEFITINIB | IC50 | 2300 nM | US-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-carboxamide | KD | 2600 nM | |
| (E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)but-2-enamide | KD | 3500 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 | |
| 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-one | KD | 5300 nM |
ChEMBL bioactivities
216 potent at pChembl≥5 of 235 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
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.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]pentanamide | 1298205: Competitive inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by Lineweaver-Burk plot analysis in presence of ATP | ki | 0.0003 | uM |
| 2-[6-(4-methylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assay | kd | 0.0038 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624942: Binding constant for DRAK2 kinase domain | kd | 0.0048 | 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 | 507904: Binding affinity to DRAK2 | kd | 0.0050 | uM |
| 2-[6-(1-benzothiophen-2-yl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assay | kd | 0.0056 | uM |
| 2-[6-(4-methylsulfinylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0070 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]cyclopropanecarboxamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.0080 | uM |
| 5-(3-amino-5-thiophen-3-ylthieno[2,3-b]pyridin-2-yl)-3H-1,3,4-oxadiazole-2-thione | 1966671: Binding affinity to DRAK2 (unknown origin) assessed as dissociation constant | kd | 0.0080 | uM |
| 4-[[9-chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid | 435401: Binding constant for full-length DRAK2 | kd | 0.0081 | uM |
| N-[5-(3,4-dimethoxyphenyl)thieno[2,3-b]pyridin-3-yl]cyclohexanecarboxamide | 1162292: Binding affinity to DRAK2 (unknown origin) ATP site | kd | 0.0090 | 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 | 624942: Binding constant for DRAK2 kinase domain | kd | 0.0092 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]butanamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.0100 | uM |
| 4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-5-methoxy-2-N-[4-(methylsulfonylmethyl)phenyl]pyrimidine-2,4-diamine | 1966670: Inhibition of DRAK2 (unknown origin) | ic50 | 0.0100 | uM |
| 2-[6-(4-carbamoylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assay | kd | 0.0110 | uM |
| 2-[6-(4-acetylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0130 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-3-methylbut-2-enamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.0140 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-3,3-dimethylbutanamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.0140 | uM |
| 2-[6-(4-morpholin-4-ylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0140 | uM |
| 2-[6-(3-fluoro-4-methoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0180 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-2,2-dimethylpropanamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.0210 | 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 | 435401: Binding constant for full-length DRAK2 | kd | 0.0210 | uM |
| 2-[6-(4-acetamidophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0230 | uM |
| N-[2-(3,4-dimethoxyphenyl)thieno[2,3-b]pyrazin-7-yl]cyclohexanecarboxamide | 1162292: Binding affinity to DRAK2 (unknown origin) ATP site | kd | 0.0270 | uM |
| 2-[6-(3-fluoro-4-methylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0270 | uM |
| 2-[6-(4-ethenylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0280 | uM |
| 2-[6-(1H-indazol-5-yl)thieno[3,2-d]pyrimidin-4-yl]oxyacetic acid | 1718368: Binding affinity to N-terminal His-tagged STK17B kinase domain (25 to 329 residues) (unknown origin) expressed in Escherichia coli by KINOMEscan scanMAX assay | kd | 0.0300 | uM |
| N-[5-(3,4-dimethoxyphenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]cyclohexanecarboxamide | 1162292: Binding affinity to DRAK2 (unknown origin) ATP site | kd | 0.0330 | uM |
| 2-[6-[4-(trifluoromethyl)phenyl]thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0330 | uM |
| 2-[6-(3-acetamidophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0350 | uM |
| 2-[6-(4-cyanophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0350 | uM |
| 2-[6-(6-acetyl-3-pyridinyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0370 | uM |
| 2-[6-(4-chlorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0390 | uM |
| 2-[6-(4-ethoxycarbonylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0400 | uM |
| 2-[6-(4-ethylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0410 | uM |
| Fedratinib | 624942: Binding constant for DRAK2 kinase domain | kd | 0.0450 | uM |
| 2-[6-(4-propan-2-ylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0490 | uM |
| 2-[6-(3-fluorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0490 | uM |
| 2-[6-(3-methylsulfanylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0490 | uM |
| 2-[6-(4-propan-2-ylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0590 | uM |
| 2-[6-(2-fluorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0600 | uM |
| 2-[6-(4-cyclopropylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0620 | uM |
| 2-(6-thiophen-2-ylthieno[3,2-d]pyrimidin-4-yl)sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0630 | uM |
| 2-[6-(3,4-difluorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0740 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]-3,5-dinitrobenzamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.0770 | uM |
| 2-[6-(3-morpholin-4-ylphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0830 | uM |
| 2-[6-(3,4-dichlorophenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.0920 | uM |
| 2-[6-(2-methoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.1100 | uM |
| 2-[6-(4-phenylmethoxyphenyl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid | 1718373: 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 assay | ic50 | 0.1100 | uM |
| Sunitinib | 435401: Binding constant for full-length DRAK2 | kd | 0.1100 | uM |
| N-[2-hydroxy-3-(3-nitroso-1H-indol-2-yl)-1H-indol-5-yl]cyclohexanecarboxamide | 1298193: Inhibition of DRAK2 (unknown origin) using MRLC3 peptide as substrate incubated for 2 hrs by ADP-Glo kinase assay | ic50 | 0.1200 | uM |
CTD chemical–gene interactions
64 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Arsenic | affects expression, affects methylation | 2 |
| Dexamethasone | increases expression, affects cotreatment | 2 |
| Nickel | increases expression | 2 |
| Tobacco Smoke Pollution | decreases expression, increases expression | 2 |
| 3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide | decreases expression | 1 |
| bisphenol F | affects cotreatment, increases expression | 1 |
| TL8-506 | affects cotreatment, increases expression | 1 |
| methylmercuric chloride | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| trichostatin A | affects expression | 1 |
| butyraldehyde | increases expression | 1 |
| sulindac sulfide | increases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| resorcinol | decreases expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | increases expression, affects response to substance | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| erucylphospho-N,N,N-trimethylpropylammonium | increases expression | 1 |
| abrine | increases expression | 1 |
| jinfukang | affects cotreatment, decreases expression | 1 |
| NSC 689534 | affects binding, increases expression | 1 |
| Resveratrol | decreases expression | 1 |
| Decitabine | affects cotreatment, increases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Arsenic Trioxide | affects cotreatment, decreases expression | 1 |
| Fulvestrant | increases methylation | 1 |
| Vorinostat | increases expression | 1 |
| Leflunomide | increases expression | 1 |
| Acetaminophen | increases expression | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Ascorbic Acid | affects cotreatment, increases expression | 1 |
ChEMBL screening assays
179 unique, capped per target: 179 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1034105 | Binding | Inhibition of DRAK2 at 3 uM | Discovery 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):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D1QT | Abcam K-562 STK17B KO | Cancer cell line | Female |
| CVCL_D2ME | Abcam Raji STK17B KO | Cancer cell line | Male |
| CVCL_TQ76 | HAP1 STK17B (-) 1 | Cancer cell line | Male |
| CVCL_TQ77 | HAP1 STK17B (-) 2 | Cancer cell line | Male |
| CVCL_WQ62 | Abcam Jurkat STK17B KO | Cancer cell line | Male |
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.