Compounds > gne-9605
Page last updated: 2024-11-13

gne-9605

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 CID76328936
CHEMBL ID3122117
SCHEMBL ID23373288
MeSH IDM0593379

Synonyms (24)

Synonym
CHEMBL3122117 ,
bdbm50448110
S7368
gtpl7919
gne9605
gne 9605
2-n-[5-chloro-1-[(3s,4s)-3-fluoro-1-(oxetan-3-yl)piperidin-4-yl]pyrazol-4-yl]-4-n-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
HY-12282
gne-9605
CS-3297
1536200-31-3
NCGC00386367-04
NCGC00386367-02
rel-n2-(5-chloro-1-((3s,4s)-3-fluoro-1-(oxetan-3-yl)piperidin-4-yl)-1h-pyrazol-4-yl)-n4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine
AKOS032947345
BS-15967
Q27077825
BCP10209
CCG-269231
EX-A2064
NCGC00386367-03
SCHEMBL23373288
puxpeqjknawnqa-aaeuagobsa-n
cid 76328936

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)Potency13.45040.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency2.68370.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency2.68370.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.68370.01238.964839.8107AID1645842
[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)0.01880.00040.39438.3000AID1071299; AID1912877
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)Ki0.00200.00061.13536.7150AID1071300; AID1913080
[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 (36)

Assay IDTitleYearJournalArticle
AID1071265Drug metabolism in human liver microsomes in presence of potassium cyanide2014Journal 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.
AID1071277Induction of CYP3A4 in human hepatocytes2014Journal 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.
AID1071261In vivo inhibition of human LRRK2 G2019S Parkinson's disease mutant expressed in BAC mouse assessed as inhibition of autophosphorylation at Ser1292 in brain at 10 to 50 mg/kg, ip after 1 to 6 hrs2014Journal 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.
AID1071256Unbound clearance in cynomolgus monkey at 1 mg/kg, po and 0.5 mg/kg, iv2014Journal 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.
AID1071257Half life in cynomolgus monkey at 0.5 mg/kg, iv2014Journal 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.
AID1071267Activity at BCRP transporter (unknown origin) transfected in MDCK cells assessed as efflux ratio of permeability2014Journal 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.
AID1071262Selectivity ratio of Ki for TAK1/TAB1 (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.
AID1071299Inhibition of LRRK2 (unknown origin) phosphorylation by cell-based assay2014Journal 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.
AID1071260Plasma protein binding in cynomolgus monkey at 5 uM after 4 hrs by equilibrium dialysis technique2014Journal 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.
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.
AID1071294Clearance in Sprague-Dawley rat at 1 mg/kg, po and 0.5 mg/kg, iv2014Journal 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.
AID1071272Oral bioavailability in Sprague-Dawley rat at 1 mg/kg2014Journal 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.
AID1071266Drug metabolism in human liver microsomes in presence of glutathione2014Journal 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.
AID1071276Induction of CYP1A2 in human hepatocytes2014Journal 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.
AID1071254Oral bioavailability in cynomolgus monkey at 1 mg/kg2014Journal 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.
AID1071258Clearance in cynomolgus monkey at 1 mg/kg, po and 0.5 mg/kg, iv2014Journal 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.
AID1071300Inhibition of 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.
AID1071295Unbound clearance in Sprague-Dawley rat at 1 mg/kg, po and 0.5 mg/kg, iv2014Journal 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.
AID1071263Inhibition of TAK1/TAB1 (unknown origin) at 0.1 uM relative to control2014Journal 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.
AID1071269Time dependent inhibition of CYP in human liver microsomes by HPLC-MS analysis2014Journal 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.
AID1071297Clearance in human hepatocytes at 1 uM by LC-MS/MS analysis2014Journal 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.
AID1071281Ratio of unbound drug level in brain to plasma in Sprague-Dawley rat2014Journal 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.
AID1071303Activity at human MDR1 transfected in MDCK cells assessed as efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side at 5 uM2014Journal 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.
AID1071296Clearance in rat hepatocytes at 1 uM by LC-MS/MS analysis2014Journal 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.
AID1071264Drug metabolism in human liver microsomes in presence of methoxyamine2014Journal 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.
AID1071274Reversible inhibition of CYP in human liver microsomes by mass spectrophotometric analysis2014Journal 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.
AID1071275Induction of CYP2B6 in human hepatocytes2014Journal 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.
AID1071259Clearance in cynomolgus monkey hepatocytes at 1 uM by LC-MS/MS analysis2014Journal 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.
AID1071255Ratio of drug level in CSF to unbound drug level in plasma in cynomolgus monkey2014Journal 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.
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.
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.
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.
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.
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 (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's2 (40.00)24.3611
2020's3 (60.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.72

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.72 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.72)

All Compounds (24.57)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gne-7915
[no description available]		2.110
gne-0877
2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile: a leucine-rich repeat kinase 2 (LRRK2) inhibitor; structure in first source		2.110
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510