Page last updated: 2024-11-13

gne-7915

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

Cross-References

ID SourceID
PubMed CID58539171
CHEMBL ID2178134
SCHEMBL ID7456100
MeSH IDM0581001

Synonyms (34)

Synonym
chembl2178134 ,
us8802674, 256
bdbm50398668
S7528
gne7915
[4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl]-morpholin-4-ylmethanone
gne 7915
gtpl8073
HY-18163
gne-7915
c19h21f4n5o3
1351761-44-8
SCHEMBL7456100
(4-(4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-2-fluoro-5-ethoxyphenyl)(morpholino)methanone
AKOS026750276
EX-A1001
HMS3653J13
NCGC00386346-05
SW219477-1
[4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoranyl-5-methoxy-phenyl]-morpholin-4-yl-methanone
a0t ,
mfcd25977005
FT-0728506
Q27077824
AS-17060
(4-((4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-2-fluoro-5-methoxyphenyl)(morpholino)methanone
BCP09873
SB19411
HMS3674E09
[4-[[4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-2-fluoro-5-methoxyphenyl](morpholino)methanone
CCG-269162
SY294194
xcflwtzsjybcpf-uhfffaoysa-n
AC-35918

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.50920.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency1.89990.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency1.89990.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.89990.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.89990.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.89990.01238.964839.8107AID1645842
[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)
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)IC50 (µMol)0.05070.00040.39438.3000AID1462812; AID1462813; AID707024
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)Ki0.00100.00061.13536.7150AID1673916; AID707026
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (137)

Processvia Protein(s)Taxonomy
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)
negative regulation of GTPase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
MAPK cascadeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein import into nucleusLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endocytosisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
autophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
response to oxidative stressLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrion organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulum organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Golgi organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
lysosome organizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
JNK cascadeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Rho protein signal transductionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
spermatogenesisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuromuscular junction developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein localizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
determination of adult lifespanLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to starvationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of autophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of autophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of protein kinase A signalingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein processingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of neuron projection developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of neuron maturationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of macroautophagyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
peptidyl-serine phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
peptidyl-threonine phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
calcium-mediated signalingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
striatum developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
olfactory bulb developmentLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
tangential migration from the subventricular zone to the olfactory bulbLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein ubiquitinationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of protein stabilityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of tumor necrosis factor productionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to oxidative stressLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to reactive oxygen speciesLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
intracellular signal transductionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of kidney sizeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
exploration behaviorLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
locomotory exploration behaviorLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of lysosomal lumen pHLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of locomotionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of membrane potentialLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of programmed cell deathLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of MAP kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTP metabolic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein autophosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
intracellular distribution of mitochondriaLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuron projection morphogenesisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrion localizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of mitochondrial depolarizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of synaptic transmission, glutamatergicLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
canonical Wnt signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
excitatory postsynaptic potentialLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of dopamine receptor signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of dopamine receptor signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of ER to Golgi vesicle-mediated transportLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of canonical Wnt signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of dendritic spine morphogenesisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein localization to mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein localization to endoplasmic reticulum exit siteLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to manganese ionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of mitochondrial fissionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of canonical Wnt signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of excitatory postsynaptic potentialLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuron projection arborizationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of synaptic vesicle endocytosisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of endoplasmic reticulum stress-induced intrinsic apoptotic signaling pathwayLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of protein autoubiquitinationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of neuroblast proliferationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of synaptic vesicle transportLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of late endosome to lysosome transportLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of autophagosome assemblyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of thioredoxin peroxidase activity by peptidyl-threonine phosphorylationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein targeting to mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
negative regulation of protein processing involved in protein targeting to mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cellular response to dopamineLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
positive regulation of microglial cell activationLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Wnt signalosome assemblyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of retrograde transport, endosome to GolgiLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of CAMKK-AMPK signaling cascadeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of branching morphogenesis of a nerveLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of synaptic vesicle exocytosisLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
regulation of reactive oxygen species metabolic processLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
signal transductionLeucine-rich repeat serine/threonine-protein kinase 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 (44)

Processvia Protein(s)Taxonomy
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)
SNARE bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
magnesium ion bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
actin bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTPase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein serine/threonine kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
JUN kinase kinase kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
MAP kinase kinase kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTPase activator activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
ATP bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTP bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
microtubule bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
tubulin bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
syntaxin-1 bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
signaling receptor complex adaptor activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
clathrin bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
small GTPase bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
GTP-dependent protein kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
peroxidase inhibitor activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
co-receptor bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
identical protein bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein homodimerization activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
transmembrane transporter bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein kinase A bindingLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
protein serine kinase activityLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
beta-catenin destruction complex bindingLeucine-rich repeat serine/threonine-protein kinase 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 (56)

Processvia Protein(s)Taxonomy
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)
Golgi membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
extracellular spaceLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoplasmLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial outer membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial inner membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial matrixLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
lysosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulumLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulum membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Golgi apparatusLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Golgi-associated vesicleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
trans-Golgi networkLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytosolLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoskeletonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
plasma membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
microvillusLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
axonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
dendriteLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
growth coneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
synaptic vesicle membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoplasmic vesicleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
mitochondrial membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
cytoplasmic side of mitochondrial outer membraneLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
dendrite cytoplasmLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuron projectionLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
neuronal cell bodyLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
terminal boutonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
perikaryonLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
intracellular membrane-bounded organelleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
amphisomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
autolysosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
extracellular exosomeLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
endoplasmic reticulum exit siteLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
multivesicular body, internal vesicleLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
postsynapseLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
glutamatergic synapseLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
caveola neckLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
presynaptic cytosolLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
ribonucleoprotein complexLeucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)
Wnt signalosomeLeucine-rich repeat serine/threonine-protein kinase 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 (43)

Assay IDTitleYearJournalArticle
AID706998Genotoxicity in Sprague-Dawley rat assessed as micronucleated polychromatic erythrocytes in bone marrow at 100 mg/kg, po qd for 2 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706993Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 100 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706994Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 50 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707004Inhibition of LRRK2 G2019S mutant phosphorylation at Ser1292 in ip dosed BAC transgenic mouse brain after 1 to 24 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706988Ratio of drug level CSF to unbound drug level in plasma in cynomolgus monkey at 10 to 65 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707015Inhibition of TTK at 0.1 uM2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706992Unbound plasma AUC (0 to 24 hrs) in cynomolgus monkey at 10 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707024Inhibition of autophosphorylation of LRRK2 in human HEK293 cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707020Clearance in rat hepatocytes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1821425Unbound brain-to-plasma concentration ratio in rat at 2.5 uM incubated for 4 hrs by equilibrium dialysis method2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
AID706990Ratio of unbound drug level in brain to plasma in cynomolgus monkey at 10 to 65 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1462813Inhibition of recombinant human wild type GST-tagged LRRK2 (970 to 2527 residues) preincubated for 30 mins followed by fluorescein-LRRKtide substrate addition after 2 hrs by TR-FRET assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.
AID707003Inhibition of LRRK2 G2019S mutant phosphorylation at Ser1292 in po dosed BAC transgenic mouse brain after 1 to 24 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707021Clearance in human hepatocytes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707008Inhibition of LRRK2 using FAM-LRRKtide as substrate at 0.1 uM after 120 mins by microfluidic capillary electrophoresis assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707006Inhibition of recombinant human 5HT2B receptor expressed in CHO cells at 10 uM2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1821470Unbound brain-to-plasma concentration ratio in non-human primates administered orally and measured after 120 mins by LC/MS/MS analysis2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
AID706989Unbound plasma AUC (0 to 24 hrs) in cynomolgus monkey at 65 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706995Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706996Toxicity in Sprague-Dawley rat assessed as mortality at 10 to 100 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1821424Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human MDR1-transfected dog MDCKII-MDR1 cells at 0.1 to 1 uM measured after 3 hrs by LC/MS/MS analysis2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
AID707012Selectivity ratio of Ki for TTK to Ki for LRRK22012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707019Plasma protein binding in rat2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1071301Selectivity ratio of Ki for JAK2 (unknown origin) to Ki for LRRK2 (unknown origin)2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707018Apparent permeability from apical to basolateral side of MDCK cells expressing human MDR12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707000Clearance in cynomolgus monkey hepatocytes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706991Unbound plasma AUC (0 to 24 hrs) in cynomolgus monkey at 25 mg/kg, po administered for 7 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707026Inhibition of LRRK2 using FAM-LRRKtide as substrate after 120 mins by microfluidic capillary electrophoresis assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707017Efflux ratio of permeability from apical to basolateral over basolateral to apical side in MDCK cells expressing human MDR12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1673916Inhibition of LRRK2 G2019S mutant (unknown origin)2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1462812Inhibition of recombinant human LRRK2 (970 to 2527 residues) G2019S mutant expressed in baculovirus preincubated for 30 mins followed by fluorescein-LRRKtide substrate addition after 2 hrs by TR-FRET assay2017Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18
The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.
AID706999Plasma protein binding in cynomolgus monkey2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707023Selectivity ratio of Ki for JAK2 to Ki for LRRK22012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1071302Thermodynamic solubility of the crystalline form of compound at pH 7.42014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID707007Inhibition of ALK at 0.1 uM2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID706997Unbound plasma AUC (0 to 24 hrs) in Sprague-Dawley rat at 100 mg/kg, po qd for 2 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
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.
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.
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.
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.
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.
AID1345801Human TTK protein kinase (TTK family)2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
AID1345739Human leucine rich repeat kinase 2 (Leucine-rich repeat kinase (LRRK) family)2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (50.00)24.3611
2020's4 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.00

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index24.00 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]