Page last updated: 2024-12-04

2-(1-(2-(1-methylpyrrolidino)ethyl)-1h-indol-3-yl)maleimide

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Description

2-(1-(2-(1-methylpyrrolidino)ethyl)-1H-indol-3-yl)maleimide is a chemical compound that is a **selective and potent antagonist of the serotonin 5-HT3 receptor**. This receptor is a ligand-gated ion channel that is expressed in the central and peripheral nervous systems.

Here's why it is important for research:

* **Understanding 5-HT3 receptor function:** 5-HT3 receptors are involved in a variety of physiological processes, including **vomiting, pain, and anxiety**. By blocking the receptor, this compound helps researchers understand the role of 5-HT3 receptors in these processes.
* **Developing new drugs:** Antagonists of the 5-HT3 receptor are used to treat **nausea and vomiting**, especially those caused by chemotherapy and radiation therapy. This compound could potentially serve as a lead compound for the development of new and improved antiemetics.
* **Investigating other neurological conditions:** The compound could be used to study other neurological conditions that are affected by 5-HT3 receptors, such as **migraines, epilepsy, and irritable bowel syndrome**.

**It is important to note that this compound is a research tool and is not currently available for clinical use.**

The structural features of the compound are:

* **Maleimide group:** This group is known to be reactive and can form covalent bonds with cysteine residues in proteins. This property could be useful for targeting the 5-HT3 receptor and developing new therapeutic agents.
* **Indole ring:** This ring system is present in many biologically active compounds and can interact with other molecules in the body.
* **Pyrrolidine ring:** This ring system is found in many neuroactive compounds and contributes to the compound's pharmacological activity.

The research on 2-(1-(2-(1-methylpyrrolidino)ethyl)-1H-indol-3-yl)maleimide and other 5-HT3 receptor antagonists is essential for understanding the role of this receptor in various physiological processes and for developing new therapeutic agents.

bisindolylmaleimide II: protein kinase C inhibitor; see also bisindolylmaleimide I [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2397
CHEMBL ID218328
SCHEMBL ID7978085
MeSH IDM0298784

Synonyms (23)

Synonym
bdbm2694
chembl218328 ,
bisindolyl deriv. 22
3-(1h-indol-3-yl)-4-{1-[2-(1-methylpyrrolidin-2-yl)ethyl]-1h-indol-3-yl}-2,5-dihydro-1h-pyrrole-2,5-dione
bim-2
HSCI1_000316
2-[1-[2-(1-methylpyrrolidino)ethyl]-1h-indol-3-yl]-3-(1h-indol-3-yl)maleimide
bisindolylmaleimide ii
2-(1-[2-(1-methylpyrrolidino)ethyl]-1h-indol-3-yl-3-(1h-indol-3-yl)maleimide
2-(1-(2-(1-methylpyrrolidino)ethyl)-1h-indol-3-yl)maleimide
3-(1h-indol-3-yl)-4-[1-[2-(1-methylpyrrolidin-2-yl)ethyl]indol-3-yl]pyrrole-2,5-dione
SCHEMBL7978085
137592-45-1
3-(1h-indol-3-yl)-4-[1-[2-(1-methyl-2-pyrrolidinyl)ethyl]-1h-indol-3-yl]-1h-pyrrole-2,5-dione
c27h26n4o2
HB0135
3-(1h-indol-3-yl)-4-[1-[2-(1-methyl -2-pyrrolidinyl)ethyl]-1h-indol-3-yl]-1h-pyrrole-2 ,5-dione
AKOS024457989
J-007044
AT22838
DTXSID001314226
CS-0029291
HY-108604

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Fetal growth restriction (FGR) is associated with decreased nutrient availability and reduced insulin-line growth factor (IGF)-I bioavailability via increased IGF binding protein (IGFBP)-1 phosphorylation."( IGFBP-1 hyperphosphorylation in response to nutrient deprivation is mediated by activation of protein kinase Cα (PKCα).
Biggar, K; Chen, AW; Gupta, MB; Jansson, T; Li, C; Nathanielsz, PW; Nygard, K; Singal, S; Zhao, T, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)IC50 (µMol)14.00000.00251.45139.0000AID1797582
cAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)IC50 (µMol)0.01300.00201.24099.0000AID1795412
Phosphorylase b kinase regulatory subunit alpha, skeletal muscle isoformOryctolagus cuniculus (rabbit)IC50 (µMol)0.75000.18001.20753.2000AID1795414
cAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)IC50 (µMol)2.00000.01801.09593.1000AID1795413
Calcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)IC50 (µMol)1.89000.00000.915710.0000AID322222
NAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)IC50 (µMol)8.30000.50003.848110.0000AID274367
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (107)

Processvia Protein(s)Taxonomy
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
type B pancreatic cell development3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
hyperosmotic response3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
epidermal growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phospholipase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
calcium-mediated signaling3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
actin cytoskeleton organization3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
T cell costimulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
activation of protein kinase B activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to insulin stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of toll-like receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of mast cell degranulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein autophosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to epidermal growth factor stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
extrinsic apoptotic signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of protein localization to plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of sprouting angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
mesoderm formationcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein phosphorylationcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
peptidyl-serine phosphorylationcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cellular response to heatcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
negative regulation of TORC1 signalingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
regulation of cell growthCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of the force of heart contractionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of membrane depolarizationCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of transcription by RNA polymerase IICalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
protein phosphorylationCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of heart contractionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of cell communication by electrical couplingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
peptidyl-serine phosphorylationCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
peptidyl-threonine phosphorylationCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
endoplasmic reticulum calcium ion homeostasisCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
protein autophosphorylationCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
relaxation of cardiac muscleCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of ryanodine-sensitive calcium-release channel activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of cellular localizationCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
cellular response to calcium ionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
cardiac muscle cell contractionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of heart rate by cardiac conductionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of cardiac muscle cell action potentialCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of cardiac muscle cell action potential involved in regulation of contractionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of cell communication by electrical coupling involved in cardiac conductionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of relaxation of cardiac muscleCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
negative regulation of sodium ion transmembrane transportCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
negative regulation of sodium ion transmembrane transporter activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
rDNA heterochromatin formationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
protein deacetylationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
autophagyNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
mitotic nuclear membrane reassemblyNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
regulation of exit from mitosisNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of autophagyNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of peptidyl-threonine phosphorylationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
substantia nigra developmentNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
myelination in peripheral nervous systemNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
heterochromatin formationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
subtelomeric heterochromatin formationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
regulation of myelinationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cellular response to oxidative stressNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
peptidyl-lysine deacetylationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
epigenetic regulation of gene expressionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of protein catabolic processNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
regulation of phosphorylationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of DNA bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
post-translational protein modificationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cellular lipid catabolic processNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NLRP3 inflammasome complex assemblyNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
innate immune responseNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of fat cell differentiationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of fatty acid biosynthetic processNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of meiotic nuclear divisionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of striated muscle tissue developmentNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of DNA-templated transcriptionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cell divisionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
meiotic cell cycleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
regulation of cell cycleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
response to redox stateNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of cell divisionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of attachment of spindle microtubules to kinetochoreNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cellular response to caloric restrictionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of oligodendrocyte progenitor proliferationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cellular response to hypoxiaNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cellular response to epinephrine stimulusNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
tubulin deacetylationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of execution phase of apoptosisNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
positive regulation of oocyte maturationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of NLRP3 inflammasome complex assemblyNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of satellite cell differentiationNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
3-phosphoinositide-dependent protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
ATP binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase activator activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein serine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein serine/threonine kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
AMP-activated protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cAMP-dependent protein kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein bindingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
ATP bindingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein domain specific bindingcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein serine kinase activitycAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
protein serine/threonine kinase activitycAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
cAMP-dependent protein kinase activitycAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
protein serine/threonine kinase activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
calmodulin-dependent protein kinase activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
protein bindingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
ATP bindingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
sodium channel inhibitor activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
titin bindingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
identical protein bindingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
protein homodimerization activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
transmembrane transporter bindingCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
protein serine kinase activityCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
chromatin bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
histone deacetylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
protein bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
zinc ion bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD-dependent histone deacetylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
protein lysine deacetylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD-dependent protein lysine deacetylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
histone acetyltransferase bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
histone deacetylase bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
tubulin deacetylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
ubiquitin bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD-dependent histone H4K16 deacetylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD+ bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
DNA-binding transcription factor bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD-dependent protein demyristoylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
NAD-dependent protein depalmitoylase activityNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
transcription factor bindingNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (42)

Processvia Protein(s)Taxonomy
nucleus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasm3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
focal adhesion3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
postsynaptic density3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasmic vesicle3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell projection3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
acrosomal vesiclecAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
nucleuscAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cytoplasmcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
mitochondrioncAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
plasma membranecAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
neuromuscular junctioncAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
sperm flagellumcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
perinuclear region of cytoplasmcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
cAMP-dependent protein kinase complexcAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)
nucleoplasmcAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
cytosolcAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)
nucleusCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
nucleoplasmCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
cytoplasmCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
cytosolCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
membraneCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
endocytic vesicle membraneCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
sarcoplasmic reticulum membraneCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
sarcolemmaCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
calcium- and calmodulin-dependent protein kinase complexCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
cytoplasmCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
neuron projectionCalcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)
chromosome, telomeric regionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
chromosomeNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
nucleolusNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cytoplasmNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
mitochondrionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
centrosomeNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
centrioleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
spindleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
cytosolNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
microtubuleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
plasma membraneNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
growth coneNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
midbodyNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
paranodal junctionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
paranode region of axonNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
perikaryonNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
myelin sheathNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
lateral loopNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
Schmidt-Lanterman incisureNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
juxtaparanode region of axonNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
perinuclear region of cytoplasmNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
mitotic spindleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
meiotic spindleNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
glial cell projectionNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
heterochromatinNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
chromatin silencing complexNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1797582PDK1 Kinase Activity Assay from Article 10.1016/j.str.2004.01.005: \\Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.\\2004Structure (London, England : 1993), Feb, Volume: 12, Issue:2
Interactions of LY333531 and other bisindolyl maleimide inhibitors with PDK1.
AID1795414Phosphorylase Kinasse Assay from Article : \\The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.\\1991The Journal of biological chemistry, Aug-25, Volume: 266, Issue:24
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
AID1795412PKC assay from Article : \\The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.\\1991The Journal of biological chemistry, Aug-25, Volume: 266, Issue:24
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
AID1795413PKA assay from Article : \\The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.\\1991The Journal of biological chemistry, Aug-25, Volume: 266, Issue:24
The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.
AID274367Inhibition of human recombinant SIRT22006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition.
AID274368Inhibition of human SIRT1 at 50 uM2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition.
AID375128Inhibition of sheep brain dynamin 1 GTPase activity by malachite green GTPase assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles.
AID322222Inhibition of CaMK2delta2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 2: SAR of the amine tether.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (10.53)18.2507
2000's10 (52.63)29.6817
2010's5 (26.32)24.3611
2020's2 (10.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.08

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

MetricThis Compound (vs All)
Research Demand Index12.08 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.08)

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%
Other19 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]