Page last updated: 2024-11-11

cgp 74588

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

Description

CGP 74588: a metabolite of STI-571; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9869737
CHEMBL ID2386594
CHEMBL ID3040018
CHEBI ID169508
SCHEMBL ID846536
MeSH IDM0437794

Synonyms (39)

Synonym
404844-02-6
CHEBI:169508
n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]-4-(piperazin-1-ylmethyl)benzamide
FT-0666167
AKOS024573735
bdbm50434582
chembl2386594 ,
norimatinib
n-desmethyl imatinib
n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-4-(1-piperazinylmethyl)-benzamide
cgp-74588
n-desmethyl gleevec
SCHEMBL846536
sti-50900
unii-6goh0n63qd
cgp 74588
n-desmethylimatinib
sti-509-00
benzamide, n-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)-4-(1-piperazinylmethyl)-
n desmethyl imatinib
6goh0n63qd ,
n-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-piperazin-1-ylmethyl-benzamide
n-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-4-(piperazin-1-ylmethyl)-benzamide
BQQYXPHRXIZMDM-UHFFFAOYSA-N
n-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(piperazin-1-ylmethyl)benzamide
AC-23925
HY-G0017
CHEMBL3040018
imatinib metabolite n-desmethyl imatinib
DTXSID80193500
n-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)-4-[(piperazin-1-yl)methyl]benzamide
AS-74968
NCGC00485941-01
cgp74588
mfcd07369291
n-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)-4-(1-piperazinylmethyl)benzamide
AMY38986
Q27264884
cgp-74588 (n-desmethyl imatinib)

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" iT with IM is a feasible and safe strategy for short-time 'bridging' management of patients with significant hematologic toxicity after standard daily dosing."( Intermittent dosage of imatinib mesylate in CML patients with a history of significant hematologic toxicity after standard dosing.
Divoký, V; Egorin, MJ; Faber, E; Holzerová, M; Indrák, K; Jarosová, M; Maresová, I; Nausová, J; Rozmanová, S, 2006
)
0.33
" We here describe the correlation of imatinib trough plasma concentrations (C(mins)) with clinical responses, event-free survival (EFS), and adverse events (AEs)."( Imatinib pharmacokinetics and its correlation with response and safety in chronic-phase chronic myeloid leukemia: a subanalysis of the IRIS study.
Druker, BJ; Gathmann, I; Guilhot, F; Krahnke, T; Larson, RA; O'Brien, SG; Riviere, GJ; Wang, Y, 2008
)
0.35

Pharmacokinetics

ExcerptReferenceRelevance
"Despite the remarkable clinical response rates to imatinib in the treatment of bcr-abl leukemic patients, pharmacokinetic data on this relatively novel substance are needed to improve our understanding of the emergence of resistance, the interindividual variations of clinical response and the clinical and biologic relevance of its main metabolite N-desmethyl-imatinib."( Pharmacokinetics and cellular uptake of imatinib and its main metabolite CGP74588.
Baskaynak, G; Bonin, Mv; Bornhäuser, M; Dörken, B; Ehninger, G; Jenke, A; Kreuzer, KA; le Coutre, P; Leopold, T; Ottmann, O; Pursche, S; Schleyer, E, 2004
)
0.32
" Imatinib and CGP74588 (main metabolite of imatinib) concentrations were measured using LC/MS/MS method and pharmacokinetic parameters were estimated by a non-compartmental analysis."( Pharmacokinetic interaction between ketoconazole and imatinib mesylate (Glivec) in healthy subjects.
Capdeville, R; Dutreix, C; Hayes, M; Mehring, G; Peng, B; Pokorny, R; Seiberling, M, 2004
)
0.32
"The pharmacokinetic values for imatinib and CGP74588, respectively, were: maximum concentration (3,340 and 781 ng/ml), time to maximum concentration (2 h), half-life (18."( Pharmacokinetics of imatinib mesylate in end stage renal disease. A case study.
Briasoulis, E; Karavasilis, V; Marselos, M; Pappas, P; Pavlidis, N, 2005
)
0.33
" Population pharmacokinetic (PPK) studies evaluating the effect of population covariates on the pharmacokinetics of imatinib and its active metabolite have been developed in adults with chronic myeloid leukemia (CML) and gastrointestinal stromal tumor (GIST)."( Population pharmacokinetics of imatinib mesylate and its metabolite in children and young adults.
Barrett, JS; Bernstein, M; Blaney, SM; Bond, M; Champagne, M; Fossler, MJ; Jayaraman, B; Menon-Andersen, D; Mondick, JT; Thompson, PA, 2009
)
0.35
" Plasma imatinib and CGP74588 concentrations observed on day 1 and at steady-state were analyzed by a population pharmacokinetic method (NONMEM) to evaluate the effect of age, body weight, age, sex, albuminemia, plasma alpha1-acid glycoprotein (AGP), and eight polymorphisms corresponding to ABCB1, ABCG2, CYP3A4, CYP3A5, and AGP (pharmacogenetic data available for 46 of 67 patients)."( Population pharmacokinetics and pharmacogenetics of imatinib in children and adults.
Azard, J; Barrois, M; Chatelut, E; Delbaldo, C; Geoerger, B; Kattygnarath, D; LeCesne, A; Petain, A; Séronie-Vivien, S; Vassal, G, 2008
)
0.35
" When co-administered with voriconazole, pharmacokinetic parameters of imatinib were not significantly altered except for a 36."( Differential effects of ketoconazole, itraconazole and voriconazole on the pharmacokinetics of imatinib and its main metabolite GCP74588 in rat.
Han, A; Hu, G; Kan, X; Lin, G; Qiu, X; Wang, C; Wang, Z; Xu, T, 2014
)
0.4
" Future studies should focus on other pharmacokinetic processes so as to identify the major contributor to patient variability in imatinib plasma concentrations."( In Vivo Cytochrome P450 3A Isoenzyme Activity and Pharmacokinetics of Imatinib in Relation to Therapeutic Outcome in Patients With Chronic Myeloid Leukemia.
Aagesen, J; Alsenhed, J; Aluthgedara, W; Bergquist, J; Gréen, H; Hägg, S; Johnsson, A; Lotfi, K; Olsson-Strömberg, U; Peterson, C; Richter, J; Sandstedt, A; Skoglund, K; Söderlund, S; Svedberg, A; Ubhayasekera, SJ; Vikingsson, S, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" Although the bioavailability of imatinib mesylate is more than 97%, the exact gastrointestinal site of its absorption is unknown."( Disposition of imatinib and its metabolite CGP74588 in a patient with chronic myelogenous leukemia and short-bowel syndrome.
Beumer, JH; Egorin, MJ; Lagattuta, TF; Natale, JJ; Raptis, A, 2006
)
0.33
"The aim of the study was to investigate the bioavailability of a generic product of 100 mg and 400 mg imatinib film-coated tablets (test) as compared to that of a branded product (reference) at the same strength to determine bioequivalence."( Bioequivalence study of 400 and 100 mg imatinib film-coated tablets in healthy volunteers.
Boguradzki, P; Mikołajczak, PL; Ostrowicz, A; Wierzbicka, M,
)
0.13
"32-fold, and the bioavailability was greatly decreased about 30."( Effects of aprepitant on the pharmacokinetics of imatinib and its main metabolite in rats.
Darbalaei, S; Han, X; Lu, Y; Qin, Y; Rang, Y; Wang, N; Zhai, X; Zhang, X, 2018
)
0.48
"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

Dosage Studied

ExcerptRelevanceReference
" This study introduced a novel approach using intermittent dosage of IM in order to avoid prolonged interruptions in therapy, to allow spontaneous recovery in blood count and, simultaneously, to achieve intermittently therapeutic plasma drug levels."( Intermittent dosage of imatinib mesylate in CML patients with a history of significant hematologic toxicity after standard dosing.
Divoký, V; Egorin, MJ; Faber, E; Holzerová, M; Indrák, K; Jarosová, M; Maresová, I; Nausová, J; Rozmanová, S, 2006
)
0.33
" Blood samples were drawn prior to dosing and over 24-48 h on days 1 and 8 of the studies."( Population pharmacokinetics of imatinib mesylate and its metabolite in children and young adults.
Barrett, JS; Bernstein, M; Blaney, SM; Bond, M; Champagne, M; Fossler, MJ; Jayaraman, B; Menon-Andersen, D; Mondick, JT; Thompson, PA, 2009
)
0.35
"Current imatinib dosing guidelines in pediatrics is based on the achievement of exposures consistent with doses known to be safe and efficacious in adults."( Population pharmacokinetics of imatinib mesylate and its metabolite in children and young adults.
Barrett, JS; Bernstein, M; Blaney, SM; Bond, M; Champagne, M; Fossler, MJ; Jayaraman, B; Menon-Andersen, D; Mondick, JT; Thompson, PA, 2009
)
0.35
" administration, whereas the AUC after oral dosing was unaltered."( The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib.
Beijnen, JH; Buckle, T; Oostendorp, RL; Schellens, JH; van Tellingen, O, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzamides
[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]

Pathways (1)

PathwayProteinsCompounds
Imatinib Pathway, Pharmacokinetics/Pharmacodynamics122

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency41.54370.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency41.54370.00339.158239.8107AID1347411
[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)3.95000.00040.39438.3000AID1233362; AID1233363
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (122)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (32)

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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (43)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID1233362Inhibition of wild type LRRK2 (unknown origin) assessed as inhibition of LRRKtide phosphorylation after 120 mins by radiometric assay in presence of [gamma-33P]-ATP2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.
AID1233363Inhibition of LRRK2 G2019S mutant (unknown origin)2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.
AID1233367Competitive inhibition of wild type LRRK2 (unknown origin) using LRRKtide as substrate after 150 mins in presence of [gamma-33P]-ATP2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.
AID1233365Selectivity ratio of IC50 for wild type LRRK2 (unknown origin) to IC50 for LRRK2 G2019S mutant (unknown origin)2015Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's20 (51.28)29.6817
2010's16 (41.03)24.3611
2020's3 (7.69)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 (%)
Trials9 (22.50%)5.53%
Reviews2 (5.00%)6.00%
Case Studies6 (15.00%)4.05%
Observational0 (0.00%)0.25%
Other23 (57.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]