Page last updated: 2024-08-07 23:49:34

Serine/threonine-protein kinase ATR

A serine/threonine-protein kinase ATR that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13535]

Synonyms

EC 2.7.11.1;
Ataxia telangiectasia and Rad3-related protein;
FRAP-related protein 1

Research

Bioassay Publications (22)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (22.73)29.6817
2010's13 (59.09)24.3611
2020's4 (18.18)2.80

Compounds (116)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
caffeineHomo sapiens (human)IC501,100.000011
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-oneHomo sapiens (human)IC5070.000033
schizandrin bHomo sapiens (human)IC507.250022
nu 6027Homo sapiens (human)IC506.700011
thioureaHomo sapiens (human)IC500.200011
ku 55933Homo sapiens (human)IC5065.000022
cgk 733Homo sapiens (human)IC500.200011
nu 7026Homo sapiens (human)IC50100.000044
nu 7441Homo sapiens (human)IC5055.000022
ku-0060648Homo sapiens (human)IC5010.000011
ku 60019Homo sapiens (human)IC5021.000011
ku 0063794Homo sapiens (human)IC5010.000011
PP121Homo sapiens (human)IC501.420011
cp 466722Homo sapiens (human)IC5030.000011
(3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholineHomo sapiens (human)IC500.030866
ve 821Homo sapiens (human)IC500.026011
byl719Homo sapiens (human)IC509.100011
vx-970Homo sapiens (human)IC500.015544
vx-970Homo sapiens (human)Ki0.000211
etp-46464Homo sapiens (human)IC500.014011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
lestaurtinibHomo sapiens (human)Kd30.000011
ruboxistaurinHomo sapiens (human)Kd30.000011
enzastaurinHomo sapiens (human)Kd30.000011
erlotinibHomo sapiens (human)Kd30.000011
lapatinibHomo sapiens (human)Kd30.000011
sorafenibHomo sapiens (human)Kd30.000011
xl147Homo sapiens (human)Kd30.000011
ha 1100Homo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd30.000011
imd 0354Homo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd30.000011
bosutinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd30.000011
temsirolimusHomo sapiens (human)Kd30.000011
on 01910Homo sapiens (human)Kd30.000011
av 412Homo sapiens (human)Kd30.000011
telatinibHomo sapiens (human)Kd30.000011
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000012
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd30.000011
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
tofacitinibHomo sapiens (human)Kd30.000011
cediranibHomo sapiens (human)Kd30.000011
masitinibHomo sapiens (human)Kd30.000011
ly-2157299Homo sapiens (human)Kd30.000011
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000012
aee 788Homo sapiens (human)Kd30.000012
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
tg100-115Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd30.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd30.000011
brivanibHomo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd30.000011
inno-406Homo sapiens (human)Kd30.000011
azd 1152Homo sapiens (human)Kd30.000011
ch 4987655Homo sapiens (human)Kd30.000011
cc-930Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
fostamatinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd30.000011
ly2603618Homo sapiens (human)Kd30.000011
tg100801Homo sapiens (human)Kd30.000011
dactolisibHomo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd30.000011
gdc-0973Homo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd30.000011
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaeneHomo sapiens (human)Kd30.000011
pf 04217903Homo sapiens (human)Kd30.000011
icotinibHomo sapiens (human)Kd30.000011
cx 4945Homo sapiens (human)Kd30.000011
bms 754807Homo sapiens (human)Kd30.000011
bms 777607Homo sapiens (human)Kd30.000011
mk-1775Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000012
lucitanibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd30.000011
entrectinibHomo sapiens (human)Kd30.000011
TAK-580Homo sapiens (human)Kd30.000011
gsk 2126458Homo sapiens (human)Kd30.000011
emd1214063Homo sapiens (human)Kd30.000011
pf 3758309Homo sapiens (human)Kd30.000011
azd2014Homo sapiens (human)Kd30.000011
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanolHomo sapiens (human)Kd30.000011
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd30.000011
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000011
bay 869766Homo sapiens (human)Kd30.000011
baricitinibHomo sapiens (human)Kd30.000011
pki 587Homo sapiens (human)Kd30.000011
n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamideHomo sapiens (human)Kd30.000011
ribociclibHomo sapiens (human)Kd30.000012
mk-8033Homo sapiens (human)Kd30.000011
abemaciclibHomo sapiens (human)Kd30.000011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
alectinibHomo sapiens (human)Kd30.000012
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd30.000011
bms-911543Homo sapiens (human)Kd30.000011
torin 2Homo sapiens (human)EC500.035011
azd8186Homo sapiens (human)Kd30.000011
byl719Homo sapiens (human)Kd30.000011
rociletinibHomo sapiens (human)Kd30.000011
ceritinibHomo sapiens (human)Kd30.000011
volitinibHomo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd30.000011
bay 80-6946Homo sapiens (human)Kd30.000012

Enables

This protein enables 9 target(s):

TargetCategoryDefinition
DNA bindingmolecular functionAny molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw]
protein kinase activitymolecular functionCatalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640]
protein serine/threonine kinase activitymolecular functionCatalysis 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 bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
MutLalpha complex bindingmolecular functionBinding to a MutLalpha mismatch repair complex. [GOC:vk]
MutSalpha complex bindingmolecular functionBinding to a MutSalpha mismatch repair complex. [GOC:vk]
histone H2AXS139 kinase activitymolecular functionCatalysis of the reaction: histone H2AX-serine (position 139) + ATP = histone H2AX-phosphoserine (position 139) + ADP. This reaction is the addition of a phosphate group to the serine residue at position 139 of histone variant H2AX. [GOC:yaf, PMID:11893489, PMID:16061642]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 5 target(s):

TargetCategoryDefinition
nucleuscellular componentA 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]
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
chromosomecellular componentA structure composed of a very long molecule of DNA and associated proteins (e.g. histones) that carries hereditary information. [ISBN:0198547684]
Golgi apparatuscellular componentA membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732]
PML bodycellular componentA class of nuclear body; they react against SP100 auto-antibodies (PML, promyelocytic leukemia); cells typically contain 10-30 PML bodies per nucleus; alterations in the localization of PML bodies occurs after viral infection. [GOC:ma, PMID:10944585]

Active In

This protein is active in 4 target(s):

TargetCategoryDefinition
nuclear envelopecellular componentThe double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684]
site of DNA damagecellular componentA region of a chromosome at which DNA damage has occurred. DNA damage signaling and repair proteins accumulate at the lesion to respond to the damage and repair the DNA to form a continuous DNA helix. [GOC:pg]
nucleuscellular componentA 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]
chromosomecellular componentA structure composed of a very long molecule of DNA and associated proteins (e.g. histones) that carries hereditary information. [ISBN:0198547684]

Part Of

This protein is part of 1 target(s):

TargetCategoryDefinition
ATR-ATRIP complexcellular componentA protein complex that contains the protein kinase ATR and ATR-interacting protein (ATRIP) and binds single-stranded DNA; ssDNA binding affinity is increased in the presence of replication protein A. [GOC:mah, PMID:14724280]

Involved In

This protein is involved in 28 target(s):

TargetCategoryDefinition
DNA damage checkpoint signalingbiological processA signal transduction process that contributes to a DNA damage checkpoint. [GOC:mah]
nucleobase-containing compound metabolic processbiological processAny cellular metabolic process involving nucleobases, nucleosides, nucleotides and nucleic acids. [GOC:ai]
DNA replicationbiological processThe cellular metabolic process in which a cell duplicates one or more molecules of DNA. DNA replication begins when specific sequences, known as origins of replication, are recognized and bound by the origin recognition complex, and ends when the original DNA molecule has been completely duplicated and the copies topologically separated. The unit of replication usually corresponds to the genome of the cell, an organelle, or a virus. The template for replication can either be an existing DNA molecule or RNA. [GOC:mah]
double-strand break repairbiological processThe repair of double-strand breaks in DNA via homologous and nonhomologous mechanisms to reform a continuous DNA helix. [GOC:elh]
chromatin remodelingbiological processA dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820]
DNA damage responsebiological processAny 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]
negative regulation of DNA replicationbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of DNA replication. [GOC:go_curators]
response to xenobiotic stimulusbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc]
response to mechanical stimulusbiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a mechanical stimulus. [GOC:hb]
peptidyl-serine phosphorylationbiological processThe phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]
replication fork processingbiological processThe process in which a DNA replication fork that has stalled is restored to a functional state and replication is restarted. The stalling may be due to DNA damage, DNA secondary structure, bound proteins, dNTP shortage, or other causes. [GOC:vw, PMID:11459955, PMID:15367656, PMID:17660542]
positive regulation of telomere maintenance via telomerasebiological processAny process that activates or increases the frequency, rate or extent of the addition of telomeric repeats by telomerase. [GOC:mah]
cellular response to UVbiological processAny 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 ultraviolet radiation (UV light) stimulus. Ultraviolet radiation is electromagnetic radiation with a wavelength in the range of 10 to 380 nanometers. [GOC:mah]
interstrand cross-link repairbiological processRemoval of a DNA interstrand crosslink (a covalent attachment of DNA bases on opposite strands of the DNA) and restoration of the DNA. DNA interstrand crosslinks occur when both strands of duplex DNA are covalently tethered together (e.g. by an exogenous or endogenous agent), thus preventing the strand unwinding necessary for essential DNA functions such as transcription and replication. [GOC:vw, PMID:16464006, PMID:22064477]
positive regulation of DNA damage response, signal transduction by p53 class mediatorbiological processAny process that activates, maintains or increases the rate of the cascade of processes induced by the cell cycle regulator phosphoprotein p53, or an equivalent protein, in response to the detection of DNA damage. [GOC:jl]
mitotic G2/M transition checkpointbiological processA cell cycle checkpoint that detects and negatively regulates progression from G2 to M phase as part of a mitotic cell cycle. [GOC:mtg_cell_cycle]
response to arsenic-containing substancebiological processAny process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an arsenic stimulus from compounds containing arsenic, including arsenates, arsenites, and arsenides. [GOC:hjd, ISBN:0721662544]
protein autophosphorylationbiological processThe phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732]
protein localization to chromosome, telomeric regionbiological processAny process in which a protein is transported to, or maintained at, the telomeric region of a chromosome. [GOC:BHF, GOC:mah]
cellular response to gamma radiationbiological processAny 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 gamma radiation stimulus. Gamma radiation is a form of electromagnetic radiation (EMR) or light emission of a specific frequency produced from sub-atomic particle interaction, such as electron-positron annihilation and radioactive decay. Gamma rays are generally characterized as EMR having the highest frequency and energy, and also the shortest wavelength, within the electromagnetic radiation spectrum. [GOC:mah]
replicative senescencebiological processA cell aging process associated with the dismantling of a cell as a response to telomere shortening and/or cellular aging. [GOC:BHF]
establishment of RNA localization to telomerebiological processThe directed movement of RNA to a specific location in the telomeric region of a chromosome. [GOC:BHF, GOC:BHF_telomere, GOC:rph, PMID:26586433]
establishment of protein-containing complex localization to telomerebiological processThe directed movement of a protein-containing macromolecular complex to a specific location in the telomeric region of a chromosome. [GOC:BHF, GOC:BHF_telomere, GOC:rph, PMID:26586433]
regulation of cellular response to heatbiological processAny process that modulates the frequency, rate or extent of cellular response to heat. [GOC:TermGenie, GOC:yaf]
positive regulation of telomerase catalytic core complex assemblybiological processAny process that activates or increases the frequency, rate or extent of telomerase catalytic core complex assembly. [GO_REF:0000058, GOC:BHF, GOC:BHF_telomere, GOC:rph, GOC:TermGenie, PMID:26586433]
regulation of double-strand break repairbiological processAny process that modulates the frequency, rate or extent of double-strand break repair. [GOC:BHF]
DNA repairbiological processThe process of restoring DNA after damage. Genomes are subject to damage by chemical and physical agents in the environment (e.g. UV and ionizing radiations, chemical mutagens, fungal and bacterial toxins, etc.) and by free radicals or alkylating agents endogenously generated in metabolism. DNA is also damaged because of errors during its replication. A variety of different DNA repair pathways have been reported that include direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [PMID:11563486]
telomere maintenancebiological processAny process that contributes to the maintenance of proper telomeric length and structure by affecting and monitoring the activity of telomeric proteins, the length of telomeric DNA and the replication and repair of the DNA. These processes includes those that shorten, lengthen, replicate and repair the telomeric DNA sequences. [GOC:BHF, GOC:BHF_telomere, GOC:elh, GOC:rl, PMID:11092831]