Page last updated: 2024-08-08 00:22:38
Serine/threonine-protein kinase tousled-like 1
A serine/threonine-protein kinase tousled-like 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UKI8]
Synonyms
EC 2.7.11.1;
PKU-beta;
Tousled-like kinase 1
Research
Bioassay Publications (6)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (33.33) | 29.6817 |
| 2010's | 4 (66.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (75)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| staurosporine | Homo sapiens (human) | IC50 | 0.0295 | 3 | 3 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| sb 202190 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| imatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| staurosporine | Homo sapiens (human) | Kd | 0.0270 | 2 | 2 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.1100 | 2 | 2 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| ruboxistaurin | Homo sapiens (human) | Kd | 6.0500 | 2 | 2 |
| canertinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| birb 796 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| cyc 202 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sb 203580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| enzastaurin | Homo sapiens (human) | Kd | 0.5100 | 1 | 1 |
| erlotinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| 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 | 2 | 2 |
| tandutinib | Homo sapiens (human) | Kd | 10.0000 | 3 | 3 |
| vx-745 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| dasatinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| zd 6474 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamide | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| alvocidib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| bosutinib | Homo sapiens (human) | Kd | 0.5700 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.7400 | 3 | 3 |
| jnj-7706621 | Homo sapiens (human) | Kd | 1.1000 | 1 | 1 |
| vx680 | Homo sapiens (human) | Kd | 7.0000 | 2 | 2 |
| ekb 569 | 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 | 10.0000 | 3 | 3 |
| ki 20227 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| cp 724714 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pi103 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| hki 272 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 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 | 2 | 2 |
| azd 6244 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| su 14813 | Homo sapiens (human) | Kd | 0.6300 | 2 | 2 |
| 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 | 0.4900 | 1 | 1 |
| brivanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | Kd | 2.4000 | 1 | 1 |
| bi 2536 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-ast487 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| kw 2449 | Homo sapiens (human) | Kd | 2.7000 | 1 | 1 |
| abt 869 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| gw 2580 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| crizotinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| chir-265 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| motesanib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| mln8054 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 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 | 10.0000 | 2 | 2 |
| nvp-tae684 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 1.3000 | 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 | 2 | 2 |
| incb-018424 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1838705a | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| gsk 1363089 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| chir 258 | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| nintedanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
Enables
This protein enables 4 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 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 2 target(s):
| Target | Category | Definition |
|---|---|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Involved In
This protein is involved in 8 target(s):
| Target | Category | Definition |
|---|---|---|
| chromatin organization | biological process | The assembly or remodeling of chromatin composed of DNA complexed with histones, other associated proteins, and sometimes RNA. [PMID:20404130] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| intracellular protein transport | biological process | The directed movement of proteins in a cell, including the movement of proteins between specific compartments or structures within a cell, such as organelles of a eukaryotic cell. [GOC:mah] |
| DNA damage response | 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 a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| regulation of chromatin organization | biological process | Any process that modulates the frequency, rate or extent of chromatin organization. [GO_REF:0000058, GOC:bf, GOC:TermGenie, GOC:vw, PMID:18314879] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| chromosome segregation | biological process | The process in which genetic material, in the form of chromosomes, is organized into specific structures and then physically separated and apportioned to two or more sets. In eukaryotes, chromosome segregation begins with the condensation of chromosomes, includes chromosome separation, and ends when chromosomes have completed movement to the spindle poles. [GOC:jl, GOC:mah, GOC:mtg_cell_cycle, GOC:vw] |