Page last updated: 2024-11-13

sar 020106

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

SAR 020106: a CHK1 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44203948
CHEMBL ID1928705
SCHEMBL ID1396946
MeSH IDM0544522

Synonyms (30)

Synonym
(r)-5-(8-chloroisoquinolin-3-ylamino)-3-(1-(dimethylamino)propan-2-yloxy)pyrazine-2-carbonitrile
ym8 ,
bdbm50359807
CHEMBL1928705 ,
S7740
SRBJWIBAMIKCMV-GFCCVEGCSA-N ,
sar-020106
sar 020106
sar020106
SCHEMBL1396946
1184843-57-9
AC-29017
sar020106;sar 020106
NCGC00387035-01
AKOS030621761
5-[(8-chloroisoquinolin-3-yl)amino]-3-{[(2r)-1-(dimethylamino)propan-2-yl]oxy}pyrazine-2-carbonitrile
Q27467786
(r)-5-((8-chloroisoquinolin-3-yl)amino)-3-((1-(dimethylamino)propan-2-yl)oxy)pyrazine-2-carbonitrile
AS-16323
EX-A2810
AMY16632
BCP29578
sar020106; sar 020106; sar20106; sar20106; sar 20106
sar20106
sar 20106
CCG-268435
5-[(8-chloroisoquinolin-3-yl)amino]-3-[(2r)-1-(dimethylamino)propan-2-yl]oxypyrazine-2-carbonitrile
A898976
HY-100195
CS-0018190

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" A novel series of potent and orally bioavailable 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitrile CHK1 inhibitors was generated by hybridization of two lead scaffolds derived from fragment-based drug design and optimized for CHK1 potency and high selectivity using a cell-based assay cascade."( Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
Aherne, GW; Box, G; Boxall, KJ; Collins, I; de Haven Brandon, AK; Eccles, SA; Eve, PD; Garrett, MD; Hayes, A; Lainchbury, M; Matthews, TP; McHardy, T; Raynaud, FI; Reader, JC; Valenti, MR; Walton, MI, 2012
)
0.38
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency7.56370.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency9.52210.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.67410.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency9.52210.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase Chk1Homo sapiens (human)IC50 (µMol)0.02470.00010.45308.8300AID634542; AID719557; AID719559
Serine/threonine-protein kinase Chk2Homo sapiens (human)IC50 (µMol)100.00000.00300.34823.5000AID634543
Cyclin-dependent kinase 1Homo sapiens (human)IC50 (µMol)7.50000.00041.345210.0000AID719550
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)5.00000.00091.901410.0000AID719553
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (156)

Processvia Protein(s)Taxonomy
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
inner cell mass cell proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA replicationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA repairSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatin remodelingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleus organizationSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationSerine/threonine-protein kinase Chk1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of cell population proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2/M transition checkpointSerine/threonine-protein kinase Chk1Homo sapiens (human)
positive regulation of cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of gene expression, epigeneticSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of mitotic nuclear divisionSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of mitotic centrosome separationSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of G0 to G1 transitionSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to mechanical stimulusSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to caffeineSerine/threonine-protein kinase Chk1Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic process involved in developmentSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of DNA biosynthetic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk2Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk2Homo sapiens (human)
double-strand break repairSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of DNA-templated transcriptionSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein catabolic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic intra-S DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of protein catabolic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
positive regulation of DNA-templated transcriptionSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein stabilizationSerine/threonine-protein kinase Chk2Homo sapiens (human)
cell divisionSerine/threonine-protein kinase Chk2Homo sapiens (human)
thymocyte apoptotic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
cellular response to gamma radiationSerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic spindle assemblySerine/threonine-protein kinase Chk2Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of autophagosome assemblySerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organizationCyclin-dependent kinase 1Homo sapiens (human)
DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
DNA repairCyclin-dependent kinase 1Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-dependent kinase 1Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
DNA damage responseCyclin-dependent kinase 1Homo sapiens (human)
mitotic nuclear membrane disassemblyCyclin-dependent kinase 1Homo sapiens (human)
centrosome cycleCyclin-dependent kinase 1Homo sapiens (human)
pronuclear fusionCyclin-dependent kinase 1Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 1Homo sapiens (human)
response to toxic substanceCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
regulation of Schwann cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
response to amineCyclin-dependent kinase 1Homo sapiens (human)
response to activityCyclin-dependent kinase 1Homo sapiens (human)
cell migrationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
chromosome condensationCyclin-dependent kinase 1Homo sapiens (human)
epithelial cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
animal organ regenerationCyclin-dependent kinase 1Homo sapiens (human)
protein localization to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein import into nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of circadian rhythmCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
response to ethanolCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
regulation of embryonic developmentCyclin-dependent kinase 1Homo sapiens (human)
response to cadmium ionCyclin-dependent kinase 1Homo sapiens (human)
response to copper ionCyclin-dependent kinase 1Homo sapiens (human)
symbiont entry into host cellCyclin-dependent kinase 1Homo sapiens (human)
fibroblast proliferationCyclin-dependent kinase 1Homo sapiens (human)
rhythmic processCyclin-dependent kinase 1Homo sapiens (human)
response to axon injuryCyclin-dependent kinase 1Homo sapiens (human)
cell divisionCyclin-dependent kinase 1Homo sapiens (human)
ventricular cardiac muscle cell developmentCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitotic sister chromatid segregationCyclin-dependent kinase 1Homo sapiens (human)
protein-containing complex assemblyCyclin-dependent kinase 1Homo sapiens (human)
cellular response to hydrogen peroxideCyclin-dependent kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeCyclin-dependent kinase 1Homo sapiens (human)
cellular response to organic cyclic compoundCyclin-dependent kinase 1Homo sapiens (human)
Golgi disassemblyCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein localization to nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of attachment of mitotic spindle microtubules to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organization involved in mitosisCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitochondrial ATP synthesis coupled electron transportCyclin-dependent kinase 1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingCyclin-dependent kinase 1Homo sapiens (human)
protein deubiquitinationCyclin-dependent kinase 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (45)

Processvia Protein(s)Taxonomy
protein kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein domain specific bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
histone H3T11 kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein kinase bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
ubiquitin protein ligase bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein homodimerization activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
virus receptor activityCyclin-dependent kinase 1Homo sapiens (human)
chromatin bindingCyclin-dependent kinase 1Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein bindingCyclin-dependent kinase 1Homo sapiens (human)
ATP bindingCyclin-dependent kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 1Homo sapiens (human)
kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 1Homo sapiens (human)
Hsp70 protein bindingCyclin-dependent kinase 1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (43)

Processvia Protein(s)Taxonomy
chromosome, telomeric regionSerine/threonine-protein kinase Chk1Homo sapiens (human)
condensed nuclear chromosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
extracellular spaceSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
replication forkSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
centrosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytosolSerine/threonine-protein kinase Chk1Homo sapiens (human)
intracellular membrane-bounded organelleSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatinSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein-containing complexSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromosome, telomeric regionSerine/threonine-protein kinase Chk2Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk2Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase Chk2Homo sapiens (human)
PML bodySerine/threonine-protein kinase Chk2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk2Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
mitochondrial matrixCyclin-dependent kinase 1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 1Homo sapiens (human)
mitochondrionCyclin-dependent kinase 1Homo sapiens (human)
endoplasmic reticulum membraneCyclin-dependent kinase 1Homo sapiens (human)
centrosomeCyclin-dependent kinase 1Homo sapiens (human)
cytosolCyclin-dependent kinase 1Homo sapiens (human)
spindle microtubuleCyclin-dependent kinase 1Homo sapiens (human)
membraneCyclin-dependent kinase 1Homo sapiens (human)
midbodyCyclin-dependent kinase 1Homo sapiens (human)
extracellular exosomeCyclin-dependent kinase 1Homo sapiens (human)
mitotic spindleCyclin-dependent kinase 1Homo sapiens (human)
cyclin A1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin A2-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin B1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 1Homo sapiens (human)
cytoplasmCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID717051Permeability across apical to basolateral side in human Caco2 cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634556Selectivity for human CHK1 over human BRSK12011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634546Antimitotic activity in etoposide-induced human HT-29 cells assessed as induction of M-phase phosphoprotein 2 expression by ELISA2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634548Inhibition of human CHK1 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634555Selectivity for human CHK1 over human RSK12011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634558Selectivity for human CHK1 over human BRSK22011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634565Efflux ratio of permeability across apical to basolateral side over basolateral to apical side in human Caco2 cells2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719553Inhibition of human ERG overexpressed in HEK cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634569Antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 25 to 50 mg/kg, ip2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634549Inhibition of human RSK1 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719556Ratio of GI50 for human HT-29 cells to IC50 for CHK1-mediated abrogation of etoposide-induced G2 check point arrest in human HT-29 cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634563Drug metabolism in human liver microsomes after 30 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719559Inhibition of CHK1 using 5-FAM-KKKVSRSGLYRSPSMPENLNRPR-COOH as substrate after 1 hr by microfluidic assay in presence of ATP2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634562Drug metabolism in mouse liver microsomes after 30 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634564Effective permeability across apical to basolateral side in human Caco2 cells2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634545Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719554Potentiation index, ratio of IC50 for human SW620 cells to IC50 for potentiation of gemcitabine-induced cytotoxicity in human SW620 cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID719582Oral bioavailability in BALB/c mouse at 10 mg/kg2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634553Inhibition of human RSK2 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634559Selectivity for human CHK1 over human RSK22011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID717052Drug metabolism in mouse liver microsomes after 30 mins2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634554Inhibition of human NUAK1 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634551Inhibition of human IRAK1 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634561Drug metabolism in rat liver microsomes after 30 mins2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719546Inhibition of CHK1 in human SW620 cells assessed as potentiation of gemcitabine-induced cytotoxicity after 24 to 48 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634543Competitive inhibition of human CHK2 using ATP as substrate by DELFIA2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634557Selectivity for human CHK1 over human IRAK12011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634547Potentiation of SN38-induced cytotoxicity in human HT-29 cells after 96 hrs by SRB assay relative to control2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634568Potentiation of irinotecan-induced antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 40 mg/kg, ip2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719557Inhibition of CHK1 in human HT-29 cells assessed as etoposide-induced G2 check point arrest after 21 hrs by ELISA2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634550Inhibition of human BRSK1 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634567In vivo inhibition of irinotecan-induced CHK1 phosphorylation at Ser296 residue in human SW620 cells xenografted in nude SCID mouse at 40 mg/kg, ip after 24 hrs by Western blot analysis2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634566Oral bioavailability in SCID mouse at 40 mg/kg2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID634560Selectivity for human CHK1 over human NUAK12011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719550Inhibition of CDK12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634552Inhibition of human BRSK2 at 1 uM2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID719555Potentiation index, ratio of IC50 for human HT-29 cells to IC50 for potentiation of gemcitabine-induced cytotoxicity in human HT-29 cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
AID634542Competitive inhibition of human CHK1 using ATP as substrate by DELFIA2011Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24
Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (66.67)24.3611
2020's3 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]