Page last updated: 2024-08-07 23:26:16
G protein-coupled receptor kinase 4
A G protein-coupled receptor kinase 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P32298]
Synonyms
EC 2.7.11.16;
G protein-coupled receptor kinase GRK4;
ITI1
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 | 1 (20.00) | 29.6817 |
| 2010's | 4 (80.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (70)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| staurosporine | Homo sapiens (human) | IC50 | 0.0914 | 2 | 2 |
| ophiocordin | Homo sapiens (human) | IC50 | 0.2600 | 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 | 0.0370 | 1 | 1 |
| gefitinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| lestaurtinib | Homo sapiens (human) | Kd | 0.0120 | 2 | 2 |
| vatalanib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| ruboxistaurin | Homo sapiens (human) | Kd | 0.5900 | 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 | 7.3000 | 1 | 1 |
| lapatinib | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| sorafenib | Homo sapiens (human) | Kd | 10.0000 | 2 | 2 |
| 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 | 2 | 2 |
| 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 | 10.0000 | 1 | 1 |
| bosutinib | Homo sapiens (human) | Kd | 4.9000 | 1 | 1 |
| su 11248 | Homo sapiens (human) | Kd | 0.1400 | 2 | 2 |
| vx680 | Homo sapiens (human) | Kd | 0.4000 | 1 | 1 |
| axitinib | Homo sapiens (human) | Kd | 2.3000 | 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 | 0.1100 | 2 | 2 |
| 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 | 10.0000 | 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 | 0.3700 | 1 | 1 |
| bibw 2992 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| tg100-115 | Homo sapiens (human) | Kd | 6.2000 | 1 | 1 |
| pha 665752 | Homo sapiens (human) | Kd | 0.4200 | 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 | 0.4500 | 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 | 10.0000 | 1 | 1 |
| kw 2449 | Homo sapiens (human) | Kd | 0.0710 | 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 | 4.2000 | 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 | 2.8000 | 1 | 1 |
| azd 1152-hqpa | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
| nvp-tae684 | Homo sapiens (human) | Kd | 3.5000 | 1 | 1 |
| fedratinib | Homo sapiens (human) | Kd | 0.1700 | 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 | 6.1000 | 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 | 0.0970 | 1 | 1 |
| nintedanib | Homo sapiens (human) | Kd | 0.0170 | 1 | 1 |
| pp242 | Homo sapiens (human) | Kd | 10.0000 | 1 | 1 |
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|---|---|
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| rhodopsin kinase activity | molecular function | Catalysis of the reaction: ATP + rhodopsin = ADP + phosphorhodopsin. [PMID:14654303] |
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|---|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell cortex | cellular component | The region of a cell that lies just beneath the plasma membrane and often, but not always, contains a network of actin filaments and associated proteins. [GOC:mah, ISBN:0815316194] |
| photoreceptor disc membrane | cellular component | Stack of disc membranes located inside a photoreceptor outer segment, and containing densely packed molecules of photoreceptor proteins that traverse the lipid bilayer. Disc membranes arise as evaginations of the ciliary membrane during the development of the outer segment and may or may not remain contiguous with the ciliary membrane. [GOC:bj, GOC:krc, GOC:pde, PMID:11826267, PMID:19501669, PMID:2537204, PMID:26574505, PMID:6771304, PMID:7507907] |
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 6 target(s):
| Target | Category | Definition |
|---|---|---|
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| regulation of G protein-coupled receptor signaling pathway | biological process | Any process that modulates the frequency, rate or extent of G protein-coupled receptor signaling pathway. [GOC:go_curators] |
| regulation of opsin-mediated signaling pathway | biological process | Any process that modulates the frequency, rate or extent of opsin-mediated signaling. [GOC:mah] |
| receptor internalization | biological process | A receptor-mediated endocytosis process that results in the movement of receptors from the plasma membrane to the inside of the cell. The process begins when cell surface receptors are monoubiquitinated following ligand-induced activation. Receptors are subsequently taken up into endocytic vesicles from where they are either targeted to the lysosome or vacuole for degradation or recycled back to the plasma membrane. [GOC:bf, GOC:mah, GOC:signaling, PMID:15006537, PMID:19643732] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| regulation of signal transduction | biological process | Any process that modulates the frequency, rate or extent of signal transduction. [GOC:sm] |