Compounds > azd2858
Page last updated: 2024-11-12

azd2858

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

Cross-References

ID SourceID
PubMed CID10138980
CHEMBL ID2177161
CHEBI ID167652
SCHEMBL ID3327702
MeSH IDM0587413

Synonyms (43)

Synonym
486424-20-8
azd-2858
3-amino-6-{4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-n-(pyridin-3-yl)pyrazine-2-carboxamide
azd 2858
CHEBI:167652
azd2858 ,
3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-n-3-pyridinyl-2-pyrazinecarboxamide
bdbm50397745
chembl2177161 ,
gr9 ,
3-amino-6-{4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl}-n-pyridin-3-ylpyrazine-2-carboxamide
S7253
CS-1672
HY-15761
SCHEMBL3327702
FHCSBLWRGCOVPT-UHFFFAOYSA-N
3-amino-6-(4-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-n-(pyridin-3-yl)pyrazine-2-carboxamide
3-amino-6-[4-(4-methylpiperazin-1-yl)sulfonylphenyl]-n-pyridin-3-ylpyrazine-2-carboxamide
gtpl8478
compound 18 [pmid: 22489897]
AC-30277
J-690306
2-(4-fluoro-phenyl)-6-methyl-4-(3-trifluoromethyl-phenyl)-1,6-dihydro-2h-1,2,5,6,7-pentaaza-as-indacen-3-one
AKOS026750282
EX-A707
HMS3653E04
3-amino-6-(4-(4-methylpiperazin-1-ylsulfonyl)phenyl)-n-(pyridin-3-yl)pyrazine-2-carboxamide
mfcd26397072
NCGC00386288-05
SW219701-1
BCP08089
gsk-3 inhibition
FT-0700316
Q27074728
SB19272
HMS3886P11
CCG-269270
AS-56005
486424-20-8 (free base)
3-amino-6-[4-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-n-3-pyridinyl-2-pyrazinecarboxamid
A871895
NCGC00386288-06
az2858

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
EC 2.7.11.26 (tau-protein kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of tau-protein kinase inhibitor (EC 2.7.11.26).
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
bone density conservation agentAn agent that inhibits bone resorption and/or favor bone mineralization and bone regeneration. Used to heal bone fractures and to treat bone diseases such as osteopenia and osteoporosis.
Wnt signalling activatorA substance that activates any of the Wnt signalling pathway, a group of signal transduction pathways made of proteins that pass signals from outside of a cell through cell surface receptors to the inside of the cell.
[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 (6)

ClassDescription
pyrazines
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
pyridinesAny organonitrogen heterocyclic compound based on a pyridine skeleton and its substituted derivatives.
N-methylpiperazine
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
[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 (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.39190.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency10.68400.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency10.68400.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
[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)
G1/S-specific cyclin-E2Homo sapiens (human)Ki0.54000.54000.54000.5400AID706597
G1/S-specific cyclin-E1Homo sapiens (human)Ki0.54000.00050.56331.4850AID706597
Cyclin-dependent kinase 2Homo sapiens (human)Ki0.54000.00050.64275.0000AID706597
Glycogen synthase kinase-3 betaHomo sapiens (human)IC50 (µMol)0.00500.00060.801310.0000AID1727768
Glycogen synthase kinase-3 betaHomo sapiens (human)Ki0.00490.00200.36681.6000AID706596
Glycogen synthase kinase-3 betaMus musculus (house mouse)IC50 (µMol)0.07600.03000.06870.1000AID706592
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (154)

Processvia Protein(s)Taxonomy
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-E2Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-E2Homo sapiens (human)
telomere maintenanceG1/S-specific cyclin-E2Homo sapiens (human)
DNA replication initiationG1/S-specific cyclin-E2Homo sapiens (human)
homologous chromosome pairing at meiosisG1/S-specific cyclin-E2Homo sapiens (human)
regulation of protein localizationG1/S-specific cyclin-E2Homo sapiens (human)
cell divisionG1/S-specific cyclin-E2Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-E2Homo 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)
protein phosphorylationG1/S-specific cyclin-E1Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-E1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIG1/S-specific cyclin-E1Homo sapiens (human)
telomere maintenanceG1/S-specific cyclin-E1Homo sapiens (human)
DNA replication initiationG1/S-specific cyclin-E1Homo sapiens (human)
homologous chromosome pairing at meiosisG1/S-specific cyclin-E1Homo sapiens (human)
Wnt signaling pathwayG1/S-specific cyclin-E1Homo sapiens (human)
regulation of protein localizationG1/S-specific cyclin-E1Homo sapiens (human)
cell divisionG1/S-specific cyclin-E1Homo sapiens (human)
positive regulation of mesenchymal stem cell proliferationG1/S-specific cyclin-E1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-E1Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-E1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICyclin-dependent kinase 2Homo sapiens (human)
DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
DNA repairCyclin-dependent kinase 2Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 2Homo sapiens (human)
DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
potassium ion transportCyclin-dependent kinase 2Homo sapiens (human)
centriole replicationCyclin-dependent kinase 2Homo sapiens (human)
Ras protein signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 2Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of heterochromatin formationCyclin-dependent kinase 2Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated DNA replication initiationCyclin-dependent kinase 2Homo sapiens (human)
telomere maintenance in response to DNA damageCyclin-dependent kinase 2Homo sapiens (human)
post-translational protein modificationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
centrosome duplicationCyclin-dependent kinase 2Homo sapiens (human)
cell divisionCyclin-dependent kinase 2Homo sapiens (human)
meiotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
cellular response to nitric oxideCyclin-dependent kinase 2Homo sapiens (human)
cellular senescenceCyclin-dependent kinase 2Homo sapiens (human)
regulation of anaphase-promoting complex-dependent catabolic processCyclin-dependent kinase 2Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 2Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
ER overload responseGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-serine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
intracellular signal transductionGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of apoptotic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein export from nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
epithelial to mesenchymal transitionGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cell-matrix adhesionGlycogen synthase kinase-3 betaHomo sapiens (human)
glycogen metabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
protein phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
mitochondrion organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
dopamine receptor signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
circadian rhythmGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of autophagyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-serine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-threonine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
viral protein processingGlycogen synthase kinase-3 betaHomo sapiens (human)
hippocampus developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
establishment of cell polarityGlycogen synthase kinase-3 betaHomo sapiens (human)
maintenance of cell polarityGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of cell migrationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of axon extensionGlycogen synthase kinase-3 betaHomo sapiens (human)
neuron projection developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein-containing complex assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein-containing complex assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein ubiquitinationGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of phosphoprotein phosphatase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule-based processGlycogen synthase kinase-3 betaHomo sapiens (human)
intracellular signal transductionGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to interleukin-3Glycogen synthase kinase-3 betaHomo sapiens (human)
regulation of circadian rhythmGlycogen synthase kinase-3 betaHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of GTPase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of osteoblast differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of glycogen biosynthetic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cilium assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
protein autophosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of protein export from nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of dendrite morphogenesisGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of axonogenesisGlycogen synthase kinase-3 betaHomo sapiens (human)
canonical Wnt signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
excitatory postsynaptic potentialGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule cytoskeleton organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeGlycogen synthase kinase-3 betaHomo sapiens (human)
superior temporal gyrus developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to retinoic acidGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of canonical Wnt signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
extrinsic apoptotic signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandGlycogen synthase kinase-3 betaHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionGlycogen synthase kinase-3 betaHomo sapiens (human)
neuron projection organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule anchoring at centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of cellular response to heatGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein localization to nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of long-term synaptic potentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein acetylationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein localization to ciliumGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of dopaminergic neuron differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to amyloid-betaGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein localization to centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin destruction complex disassemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of type B pancreatic cell developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of glycogen (starch) synthase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of mesenchymal stem cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of TOR signalingGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of neuron projection developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
insulin receptor signaling pathwayGlycogen synthase kinase-3 betaHomo 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 (40)

Processvia Protein(s)Taxonomy
protein bindingG1/S-specific cyclin-E2Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-E2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-E2Homo 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)
protein bindingG1/S-specific cyclin-E1Homo sapiens (human)
kinase activityG1/S-specific cyclin-E1Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-E1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-E1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 2Homo sapiens (human)
magnesium ion bindingCyclin-dependent kinase 2Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein bindingCyclin-dependent kinase 2Homo sapiens (human)
ATP bindingCyclin-dependent kinase 2Homo sapiens (human)
protein domain specific bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protease bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
p53 bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine/threonine kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
ATP bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
ubiquitin protein ligase bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase A catalytic subunit bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
dynactin bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
tau protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
tau-protein kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
NF-kappaB bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine kinase activityGlycogen synthase kinase-3 betaHomo 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)
protein serine/threonine kinase activityGlycogen synthase kinase-3 betaMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (45)

Processvia Protein(s)Taxonomy
nucleoplasmG1/S-specific cyclin-E2Homo sapiens (human)
cytosolG1/S-specific cyclin-E2Homo sapiens (human)
cyclin E2-CDK2 complexG1/S-specific cyclin-E2Homo sapiens (human)
nucleusG1/S-specific cyclin-E2Homo sapiens (human)
cytoplasmG1/S-specific cyclin-E2Homo sapiens (human)
centrosomeG1/S-specific cyclin-E2Homo sapiens (human)
cyclin E1-CDK2 complexG1/S-specific cyclin-E2Homo 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)
nucleusG1/S-specific cyclin-E1Homo sapiens (human)
nucleoplasmG1/S-specific cyclin-E1Homo sapiens (human)
cytosolG1/S-specific cyclin-E1Homo sapiens (human)
cyclin E1-CDK2 complexG1/S-specific cyclin-E1Homo sapiens (human)
centrosomeG1/S-specific cyclin-E1Homo sapiens (human)
nucleusG1/S-specific cyclin-E1Homo sapiens (human)
cytoplasmG1/S-specific cyclin-E1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 2Homo sapiens (human)
condensed chromosomeCyclin-dependent kinase 2Homo sapiens (human)
X chromosomeCyclin-dependent kinase 2Homo sapiens (human)
Y chromosomeCyclin-dependent kinase 2Homo sapiens (human)
male germ cell nucleusCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
nuclear envelopeCyclin-dependent kinase 2Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
endosomeCyclin-dependent kinase 2Homo sapiens (human)
centrosomeCyclin-dependent kinase 2Homo sapiens (human)
cytosolCyclin-dependent kinase 2Homo sapiens (human)
Cajal bodyCyclin-dependent kinase 2Homo sapiens (human)
cyclin A1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 2Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
glutamatergic synapseGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
mitochondrionGlycogen synthase kinase-3 betaHomo sapiens (human)
centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 betaHomo sapiens (human)
plasma membraneGlycogen synthase kinase-3 betaHomo sapiens (human)
axonGlycogen synthase kinase-3 betaHomo sapiens (human)
dendriteGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin destruction complexGlycogen synthase kinase-3 betaHomo sapiens (human)
presynapseGlycogen synthase kinase-3 betaHomo sapiens (human)
postsynapseGlycogen synthase kinase-3 betaHomo sapiens (human)
Wnt signalosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 betaHomo sapiens (human)
axonGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 betaHomo 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)
nucleoplasmGlycogen synthase kinase-3 betaMus musculus (house mouse)
cytosolGlycogen synthase kinase-3 betaMus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID1818100Binding affinity to recombinant GSK3beta (unknown origin) assessed as dissociation rate constant upto 0.00975 uM by SPR analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1818099Binding affinity to recombinant GSK3beta (unknown origin) assessed as association rate constant upto 0.00975 uM by SPR analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1818089Binding affinity to recombinant GSK3beta (unknown origin) assessed as ratio of dissociation rate constant to association rate constant by SPR analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1818113Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 6.25 to 100 uM measured after 72 hrs by CCK8 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1727768Inhibition of GSK3beta (unknown origin)2021European journal of medicinal chemistry, Jan-15, Volume: 210PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases.
AID1818127Induction of GSK3beta degradation (unknown origin) transfected in HEK-293T cells assessed as reduction on phosphorylated tau threonine 205 residue level at 62.5 to 1000 nM measured after 24 hrs by Westernblot analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1818106Protac activity at CRBN/GSKRbeta in human SH-SY5Y cells assessed as GSK3beta degradation by measuring GSK3beta protein levels at 0.1 to 1 uM measured after 24 hrs2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1818107Protac activity at CRBN/GSK3alpha in human SH-SY5Y cells assessed as GSK3alpha degradation by measuring GSK3alpha protein levels at 0.1 to 1 uM measured after 24 hrs2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID706596Inhibition of human recombinant GSK3beta using biotin- AAEELDSRAGS(PO3H2)PQL as substrate and [gamma32P]ATP after 20 mins by scintillation proximity assay2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
AID1818112Induction of human GSK3beta degradation transfected in HEK-293T cells assessed as induction of GSK3beta protein degradation at 62.5 to 1000 nM measured after 24 hrs by westernblot analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID1818082Induction of GSK3beta (unknown origin) degradation transfected in HEK-293T cells assessed as reduction on phosphorylated tau Ser396 residue level at 62.5 to 1000 nM measured after 24 hrs by Westernblot analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID706597Inhibition of CDK2/cyclin E expressed in baculovirus infected insect cells using [gamma33P]ATP after 60 mins by scintillation proximity assay2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
AID706592Inhibition of GSK3beta-mediated Tau phosphorylation in mouse 3T3 cells after 4 hrs by Western blot analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
AID1818081Induction of GSK3beta degradation (unknown origin) transfected in HEK-293T cells assessed as recovery of tau protein at 1 uM pretreated for 12 hrs followed by compound washout and measured upto 36 hrs by western blot assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID706595Selectivity ratio of Ki for CDK1/cyclin E to Ki for human recombinant GSK3beta2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
AID706591Blood brain barrier permeability in bovine endothelial cells at 5 uM after 60 mins by LC/MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
AID1818128Induction of GSK3beta degradation (unknown origin) transfected in HEK-293T cells assessed as reduction on phosphorylated tau Ser404 residue level at 62.5 to 1000 nM measured after 24 hrs by Westernblot analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Discovery of PT-65 as a highly potent and selective Proteolysis-targeting chimera degrader of GSK3 for treating Alzheimer's disease.
AID706594Thermodynamic solubility of the compound in DMSO solution after 24 hrs by shake flask method2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
AID706593Apparent permeability across human Caco2 cells at 10 um after 2 hrs by LC/MS/MS analysis2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1345633Human glycogen synthase kinase 3 beta (GSK subfamily)2012Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

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

Market Indicators

Research Demand Index: 23.00

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

MetricThis Compound (vs All)
Research Demand Index23.00 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbonyl cyanide m-chlorophenyl hydrazone
Carbonyl Cyanide m-Chlorophenyl Hydrazone: A proton ionophore. It is commonly used as an uncoupling agent and inhibitor of photosynthesis because of its effects on mitochondrial and chloroplast membranes.. CCCP : A member of the class of monochlorobenzenes that is benzene substituted by 2-(1,3-dinitrilopropan-2-ylidene)hydrazinyl and chloro groups at positions 1 and 3, respectively. It is a mitochondrial depolarizing agent that induces reactive oxygen species mediated cell death.		2.1310hydrazone;
monochlorobenzenes;
nitrile		antibacterial agent;
geroprotector;
ionophore
nsc 664704
kenpaullone: inhibits CDK1/cyclin B; structure in first source. kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta).		2.3110indolobenzazepine;
lactam;
organobromine compound		cardioprotective agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
geroprotector
thiazoles
[no description available]		2.13101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		2.5120diazine;
pyrazines		Daphnia magna metabolite
pomalidomide
3-aminophthalimidoglutarimide: structure in first source		2.3110aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
sb 216763
[no description available]		2.5420indoles;
maleimides
n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea
N-(4-methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea: structure in first source		2.0710
5-(4-ethylbenzylidene)-2-thioxothiazolidin-4-one
[no description available]		2.1310
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione: a GSK3beta inhibitor. TDZD-8 : A member of the class of thiadiazolidines that is 1,2,4-thiadiazolidine-3,5-dione which is substituted by a methyl group at position 2 and by a benzyl group at position 4. It is a non-ATP competitive inhibitor of glycogen synthase kinase 3beta (GSK3beta). An experimental compound which was being developed for the potential treatment of Alzheimer's disease.		2.7220benzenes;
thiadiazolidine		anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent
alsterpaullone
alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole.		2.3110C-nitro compound;
caprolactams;
organic heterotetracyclic compound		anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor
tws 119
[no description available]		2.3110pyrroles
chir 99021
Chir 99021: structure in first source. CHIR 99021 : A member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively.		2.3110aminopyridine;
aminopyrimidine;
cyanopyridine;
diamine;
dichlorobenzene;
imidazoles;
secondary amino compound		EC 2.7.11.26 (tau-protein kinase) inhibitor
np 031112
tideglusib: an NSAID and neuroprotective agent. tideglusib : A member of the class of thiadiazolidines that is 1,2,4-thiadiazolidine-3,5-dione which is substituted by a naphthalen-1-yl group at position 2 and by a benzyl group at position 4. It is a non-ATP competitive inhibitor of glycogen synthase kinase 3beta (GSK3beta) and has neuroprotective effects. Currently under clinical investigation for the treatment of Alzheimer's disease and progressive supranuclear palsy.		2.3110benzenes;
naphthalenes;
thiadiazolidine		anti-inflammatory agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent
mk 2206
MK 2206: a protein kinase inhibitor and antineoplastic agent		2.1310organic heterotricyclic compoundEC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Acute Confusional Senile Dementia
[description not available]		02.5420
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		02.5420
Degenerative Diseases, Central Nervous System
[description not available]		02.3110
Neurodegenerative Diseases
Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.		02.3110
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Femoral Fractures
Fractures of the femur.		02.0810