Page last updated: 2024-11-13

lrrk2-in1

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

Description

LRRK2-IN1: inhibits leucine-rich repeat kinase 2; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46843906
CHEMBL ID2012582
CHEBI ID78413
SCHEMBL ID616761
MeSH IDM0586961

Synonyms (46)

Synonym
lrrk2-in-1 ,
HY-10875
BRD-K01436366-001-01-6
2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenyl)amino)-5,11-dimethyl-5h-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11h)-one
smr001913505
MLS003230940
chebi:78413 ,
CHEMBL2012582 ,
bdbm50379529
HMS3265P18
HMS3265O17
HMS3265O18
HMS3265P17
NCGC00346807-01
CS-0246
S7584
1234480-84-2
BRD-K01436366-001-14-9
SCHEMBL616761
lrrk2in1
lrrk2-in1
2-[(2-methoxy-4-{[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}phenyl)amino]-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one
4k4 ,
2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one
5,11-dihydro-2-[[2-methoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dimethyl-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one
2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenylamino)-5,11-dimethyl-5h-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11h)-one
AC-35378
gtpl9396
lrrk-2in1
AKOS024458067
J-004944
2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino}-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one
DTXSID70676751
EX-A644
lrrk2-tn-1
NCGC00346807-04
2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenyl)-amino)-5,11-dimethyl-5h-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11h)-one
FT-0700139
Q27147815
BCP14860
lrrk2-in 1
SB18523
2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenyl)amino)-5,11-dimethyl-5,11-dihydro-6h-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one
CCG-270098
AS-56177
bdbm482157

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Two LRRK2IN1 analogues 1 and 2 were synthesised which retained LRRK2 inhibitory activity (1: IC50 = 72 nM; 2: IC50 = 51 nM), were predicted to have improved bioavailability and were efficacious in cell-based models of neuroinflammation."( Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
Chen, EJ; Doddareddy, MR; Dzamko, N; Guillemin, GJ; Heng, B; Kassiou, M; Kavanagh, ME; Munoz, L; Phoa, AF, 2015
)
0.42
"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]

Roles (2)

RoleDescription
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of non-specific serine/threonine protein kinase (EC 2.7.11.1), a kinase enzyme involved in phosphorylation of hydroxy group of serine or threonine.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (7)

ClassDescription
N-acylpiperidine
N-alkylpiperazine
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
pyrimidobenzodiazepineAny three-ring heterocyclic compound with a skeleton consisting of a pyrimidine ring fused to a benzodiazepine bicycle.
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (14)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency23.36170.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency33.78580.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency7.85460.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency26.83700.01238.964839.8107AID1645842
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency24.23050.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
[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)0.43420.00040.39438.3000AID1164094; AID1198809; AID1198815; AID1239652; AID1377746; AID1377747; AID1673903; AID653133; AID653134; AID653135; AID653189; AID756065; AID756066
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)Ki0.00600.00061.13536.7150AID756066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bromodomain-containing protein 4Homo sapiens (human)Kd0.10970.00100.36918.9300AID1807750; AID1807751; AID1807752
Bromodomain testis-specific proteinHomo sapiens (human)Kd0.93000.02201.00834.8360AID1807754; AID1807755; AID1807756
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
serine/threonine-protein kinase 33 isoform aHomo sapiens (human)AC506.45000.12203.372112.6000AID588632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (155)

Processvia Protein(s)Taxonomy
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo 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)
positive regulation of gene expressionBromodomain testis-specific proteinHomo sapiens (human)
chromatin remodelingBromodomain testis-specific proteinHomo sapiens (human)
regulation of DNA-templated transcriptionBromodomain testis-specific proteinHomo sapiens (human)
mRNA processingBromodomain testis-specific proteinHomo sapiens (human)
male meiotic nuclear divisionBromodomain testis-specific proteinHomo sapiens (human)
male meiosis IBromodomain testis-specific proteinHomo sapiens (human)
RNA splicingBromodomain testis-specific proteinHomo sapiens (human)
sperm DNA condensationBromodomain testis-specific proteinHomo sapiens (human)
regulation of RNA splicingBromodomain testis-specific proteinHomo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain testis-specific proteinHomo 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 (56)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo 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)
transcription coactivator activityBromodomain testis-specific proteinHomo sapiens (human)
histone bindingBromodomain testis-specific proteinHomo sapiens (human)
lysine-acetylated histone bindingBromodomain testis-specific proteinHomo sapiens (human)
histone reader activityBromodomain testis-specific proteinHomo 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 (57)

Processvia Protein(s)Taxonomy
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo 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)
nucleusBromodomain testis-specific proteinHomo 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 (95)

Assay IDTitleYearJournalArticle
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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS 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.
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.
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.
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.
AID1377747Inhibition of recombinant catalytic human GST-tagged LLRK2 G2019S mutant (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate after 1 hr by alexaFluor-ADP-based FRET assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
AID715064Inhibition of GFP-tagged LRRK2 G2019S mutant expressed in HEK293 cells assessed as inhibition of Ser935 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblotting method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
AID700626Inhibition of LRRK2 autophosphorylation at Ser910 and Ser935 expressed in HEK293 cells at 1 uM after 90 mins by immunoblotting analysis2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Brain Penetrant LRRK2 Inhibitor.
AID653135Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1239652Inhibition of LRRK2 (unknown origin)2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.
AID1673903Inhibition of GST-LRRK2 (1326 to 2527 residues) G2019S mutant (unknown origin) expressed in HEK293 cells incubated for 15 mins by cerenkov counting method2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Monomeric Targeted Protein Degraders.
AID1807749Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature by DSF assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID756065Inhibition of wild type GST-tagged LRRK2 ((1326 to 2517 amino acids) (unknown origin)2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
The development of CNS-active LRRK2 inhibitors using property-directed optimisation.
AID653230Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse spleen at 100 mg/kg, po administered for 8 hrs followed by 2 hrs dosing2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1807755Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1239653Clearance in mouse at 1 mg/kg, iv2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.
AID700648Inhibition of LRRK2 in C57BL/6 mouse brain at 100 mg/kg, ip by ADP-acylphosphate probe-based mass spectrometry relative to vehicle-treated control2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Brain Penetrant LRRK2 Inhibitor.
AID1198813Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human U87 cells compound pretreated for 30 mins before stimulation measured after 24 hrs by ELISA2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID1807751Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807759Inhibition of PLK1 in HEK293T cells assessed as reduction in phosphorylation of TCTP at S46 residue at 30 to 100 nM incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID715065Inhibition of GFP-tagged LRRK2 G2019S mutant expressed in HEK293 cells assessed as inhibition of Ser910 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblotting method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
AID1807760Inhibition of PLK1 in human MM1.S cells assessed as reduction in c-Myc levels incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807754Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID654031Inhibition of wild-type LRRK2 phosphorylation at Ser910 expressed in HEK293 cells at 0.03 to 3 uM after 90 mins by immunoblot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID653205Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID700630Inhibition of LRRK2 autophosphorylation at Ser910 and Ser935 human EBV immortalized primary lymphoblastoid cells after 90 mins by immunoblotting analysis2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Brain Penetrant LRRK2 Inhibitor.
AID1198816Oral bioavailability in mouse2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID654030Inhibition of wild-type LRRK2 phosphorylation at Ser935 expressed in HEK293 cells at 0.03 to 3 uM after 90 mins by immunoblot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1807758Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1164145Inhibition of recombinant LRRK2 (unknown origin) using gamma-32P-ATP assessed as LRRKtide substrate phosphorylation level at 1 uM by autoradiography2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.
AID1807753Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature by DSF assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID715055Inhibition of LRRK2 in human lymphoblastoid cells assessed as inhibition of Ser910 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblot method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
AID1198815Inhibition of wild-type GST-tagged LRRK2 (1326 to 2527 aa)(unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID1198812Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human U87 cells compound pretreated at 10 uM for 30 mins before stimulation measured after 24 hrs by ELISA2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID756066Inhibition of GST-tagged LRRK2 (1326 to 2527 amino acids) G2019S mutant (unknown origin)2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
The development of CNS-active LRRK2 inhibitors using property-directed optimisation.
AID653189Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1198814Biochemical index, ratio of IC50 for LRRK2 G2019S mutant (unknown origin) to EC50 for IL6 secretion in LPS/IL-1beta-stimulated human primary microglia2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID653229Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse kidney at 100 mg/kg, po administered for 8 hrs followed by 2 hrs dosing2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID653203Inhibition of wild type LRRK2 phosphorylation at Ser935 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1164094Inhibition of recombinant LRRK2 (unknown origin) using gamma-32P-ATP assessed as LRRKtide substrate phosphorylation level by autoradiography2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.
AID1807756Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1198809Inhibition of LRRK2 G2019S mutant (1326 to 252 aa) (unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID715066Inhibition of GFP-tagged LRRK2 expressed in HEK293 cells assessed as inhibition of Ser935 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblotting method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
AID654032Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 expressed in HEK293 cells at 0.03 to 3 uM after 90 mins by immunoblot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1807750Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1198810Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human primary microglia compound pretreated at 10 uM for 30 mins before stimulation measured after 24 hrs by ELISA2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID654033Inhibition of LRRK2 G2019S mutant phosphorylation at Ser935 expressed in HEK293 cells at 0.03 to 3 uM after 90 mins by immunoblot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID715067Inhibition of GFP-tagged LRRK2 expressed in HEK293 cells assessed as inhibition of Ser910 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblotting method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
AID1807763Inhibition of PLK1 in HEK293T cells assessed as increase in p21 levels at 0.0001 to 10 uM incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID653133Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1198811Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human primary microglia compound pretreated for 30 mins before stimulation measured after 24 hrs by ELISA2015European journal of medicinal chemistry, May-05, Volume: 95Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation.
AID653204Inhibition of LRRK2 G2019S mutant phosphorylation at Ser910 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1164144Inhibition of recombinant LRRK2 (unknown origin) using gamma-32P-ATP assessed as LRRKtide substrate phosphorylation level at 10 uM by autoradiography2014Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19
Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond.
AID1807761Inhibition of PLK1 in human MM1.S cells assessed as increase in p21 levels incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID653228Inhibition of LRRK2 phosphorylation at Ser910 in C57BL/6 mouse kidney at 100 mg/kg, po administered for 8 hrs followed by 2 hrs dosing2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID715054Inhibition of LRRK2 in human lymphoblastoid cells assessed as inhibition of Ser935 autophosphorylation at 0.03 to 3 uM after 90 mins by immunoblot method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor.
AID653134Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID653202Inhibition of wild type LRRK2 phosphorylation at Ser910 in human lymphoblastoid cells at 0.03 to 3 uM after 90 mins by Western blot analysis2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID653231Inhibition of LRRK2 phosphorylation at Ser935 in C57BL/6 mouse spleen at 100 mg/kg, po administered for 8 hrs followed by 2 hrs dosing2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
AID1807752Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807757Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1377746Inhibition of recombinant catalytic human GST-tagged LLRK2 (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate after 1 hr by alexaFluor-ADP-based FRET assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
AID700631Inhibition of LRRK2 G2019S mutant autophosphorylation at Ser910 and Ser935 Parkinson's patient EBV immortalized primary lymphoblastoid cells after 90 mins by immunoblotting analysis2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Brain Penetrant LRRK2 Inhibitor.
AID700627Inhibition of LRRK2 G2019S mutant autophosphorylation at Ser910 and Ser935 expressed in HEK293 cells at 1 uM after 90 mins by immunoblotting analysis2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Brain Penetrant LRRK2 Inhibitor.
AID1347154Primary screen GU AMC 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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1345739Human leucine rich repeat kinase 2 (Leucine-rich repeat kinase (LRRK) family)2011Nature chemical biology, Apr, Volume: 7, Issue:4
Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.
AID1345739Human leucine rich repeat kinase 2 (Leucine-rich repeat kinase (LRRK) family)2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
The development of CNS-active LRRK2 inhibitors using property-directed optimisation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's27 (77.14)24.3611
2020's8 (22.86)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%
Reviews1 (2.86%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (97.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]