Page last updated: 2024-08-07 23:59:40
Dual serine/threonine and tyrosine protein kinase
A dual serine/threonine and tyrosine protein kinase that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q6XUX3]
Synonyms
EC 2.7.12.1;
Dusty protein kinase;
Dusty PK;
RIP-homologous kinase;
Receptor-interacting serine/threonine-protein kinase 5;
Sugen kinase 496;
SgK496
Research
Bioassay Publications (5)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 4 (80.00) | 24.3611 |
| 2020's | 1 (20.00) | 2.80 |
Compounds (70)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| staurosporine | Homo sapiens (human) | IC50 | 0.0552 | 3 | 3 |
| dabrafenib | Homo sapiens (human) | IC50 | 29.3500 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | Kd | 0.0110 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.0053 | 1 | 1 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| canertinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| enzastaurin | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pd 173955 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| s 1033 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms 387032 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| dasatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 4.2000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 0.3800 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 1.3000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pd 184352 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bms345541 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| midostaurin | Homo sapiens (human) | Kd | 4.7000 | 1 | 1 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| hki 272 | Homo sapiens (human) | Kd | 6.4000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cediranib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| masitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pazopanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 0.9300 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 0.3600 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | Kd | 0.6600 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| crizotinib | Homo sapiens (human) | Kd | 0.4500 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| motesanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| GDC-0879 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 461364 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 3.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 0.0570 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 1.7000 | 1 | 1 |
| gsk690693 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gdc 0941 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| plx 4720 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sgx 523 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| quizartinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 4.3000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 0.5100 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 0.5100 | 1 | 1 |
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|---|---|
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| protein serine/threonine/tyrosine kinase activity | molecular function | Catalysis of the reactions: ATP + a protein serine = ADP + protein serine phosphate; ATP + a protein threonine = ADP + protein threonine phosphate; and ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [GOC:mah] |
| protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| protein serine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|---|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| anchoring junction | cellular component | A cell junction that mechanically attaches a cell (and its cytoskeleton) to neighboring cells or to the extracellular matrix. [ISBN:0815332181] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 5 target(s):
| Target | Category | Definition |
|---|---|---|
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| cellular response to fibroblast growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an fibroblast growth factor stimulus. [GOC:jl, GOC:yaf] |
| positive regulation of fibroblast growth factor receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of fibroblast growth factor receptor signaling pathway activity. [GOC:go_curators] |
| positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |