Compounds > bisindolylmaleimide iii
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bisindolylmaleimide iii

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Description

bisindolylmaleimide III: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2398
CHEMBL ID270875
CHEBI ID41059
SCHEMBL ID1680137
MeSH IDM0525453

Synonyms (29)

Synonym
3-[1-(3-aminopropyl)-1h-indol-3-yl]-4-(1h-indol-3-yl)-2,5-dihydro-1h-pyrrole-2,5-dione
bim-3
bisindolyl deriv. 19
bdbm2691
K00202
bim 8; bisindolylmaleimide viii, acetate salt
HSCI1_000292
3-[1-(3-aminopropyl)-1h-indol-3-yl]-4-(1h-indol-3-yl)-1h-pyrrole-2,5-dione
bisindolylmaleimide iii
bis-(iii) indolyl-maleimide
CHEBI:41059 ,
1UU9
inhibitor of 3-phosphoinositide dependent protein kinase-1
bisindolylmaleimide iii, hydrochloride
CHEMBL270875
DB07457
3-[1-(3-aminopropyl)indol-3-yl]-4-(1h-indol-3-yl)pyrrole-2,5-dione
SCHEMBL1680137
bim iii
HB0136
137592-43-9
c23h20n4o2
J-007043
Q27096676
683775-59-9
bisindolylmaleimideiii
HY-117393
CS-0065853
3-(1-(3-aminopropyl)-1h-indol-3-yl)-4-(1h-indol-3-yl)-1h-pyrrole-2,5-dione
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 2.7.11.13 (protein kinase C) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of protein kinase C (EC 2.7.11.13).
[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 (2)

ClassDescription
indolesAny compound containing an indole skeleton.
maleimidesCompounds containing a cyclic dicarboximide skeleton in which the two carboacyl groups on nitrogen together with the nitrogen itself form a 1H-pyrrole-2,5-dione structure.
[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 (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)IC50 (µMol)3.48570.00251.45139.0000AID1797582
cAMP-dependent protein kinase catalytic subunit alphaBos taurus (cattle)IC50 (µMol)0.02600.00201.24099.0000AID1795412
Phosphorylase b kinase regulatory subunit alpha, skeletal muscle isoformOryctolagus cuniculus (rabbit)IC50 (µMol)0.18000.18001.20753.2000AID1795414
cAMP-dependent protein kinase catalytic subunit alpha Rattus norvegicus (Norway rat)IC50 (µMol)0.50000.01801.09593.1000AID1795413
Calcium/calmodulin-dependent protein kinase type II subunit deltaHomo sapiens (human)IC50 (µMol)0.38000.00000.915710.0000AID322072; AID322222; AID322228
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (60)

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

Molecular Functions (18)

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

Ceullar Components (21)

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

Bioassays (31)

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.
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.
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.
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.
AID512342Inhibition of rat liver AMPK at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512339Inhibition of His-tagged human S6K1 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512331Inhibition of His-tagged human MAPKAPK2 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512328Inhibition of His-tagged human SAPK3/p38gamma expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512346Inhibition of His-tagged human CHK1 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512343Inhibition of His-tagged human CK2 expressed in Sf9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512344Inhibition of PHK from rabbit skeletal muscle at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512334Inhibition of bovine heart PKA at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512345Inhibition of His-tagged human LCK expressed in Sf9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512341Inhibition of rat ROCK2 expressed in Sf9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512327Inhibition of His-tagged human SAPK2b/p38b2 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512335Inhibition of His-tagged human PKCalpha expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID322228Inhibition of CaMK2delta2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.
AID512325Inhibition of His-tagged human JNK1a1/SAPK1c expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512326Inhibition of His-tagged human SAPK2a/p38 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512333Inhibition of His-tagged human PRAK expressed in Sf9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512338Inhibition of His-tagged human SGK expressed in Sf9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512329Inhibition of His-tagged human SAPK4/p38delta expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512340Inhibition of His-tagged human GSK3b expressed in Sf21 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512337Inhibition of human PKBalpha expressed in SF9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512323Inhibition of rabbit MKK1 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512336Inhibition of His-tagged human PDK1 expressed in Sf21 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID322072Inhibition of CaMK2delta2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 1: SAR of the aryl region.
AID512332Inhibition of His-tagged human MSK1 expressed in Sf9 cells at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512324Inhibition of His-tagged human MAPK2/ERK2 expressed in Escherichia coli at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
AID512330Inhibition of MAPKAPK1b from rabbit skeletal muscle at 1 uM2000The Biochemical journal, Oct-01, Volume: 351, Issue:Pt 1
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
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 (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (12.50)18.2507
2000's7 (87.50)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.67

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 Index17.67 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.67)

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
bisindolylmaleimide i
bisindolylmaleimide I: a bis(indolyl)maleimide		2.6930
2-(1-(2-(1-methylpyrrolidino)ethyl)-1h-indol-3-yl)maleimide
bisindolylmaleimide II: protein kinase C inhibitor; see also bisindolylmaleimide I		2.730
bisindolylmaleimide iv
[no description available]		2.6930indoles;
maleimides
bisindolylmaleimide v
bisindolylmaleimide V: used as a negative control compound for protein kinase C inhibition; structure in first source;		2.3920indoles
ro 31-7549
Ro 31-7549: structure		2.9440
ro 31-8425
[no description available]		210
go 6976
[no description available]		210indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor
fasudil
fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.		210isoquinolines;
N-sulfonyldiazepane		antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		2.0410aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
staurosporine aglycone
staurosporine aglycone: metabolite from culture broth of Nocardiopsis sp.; a neurotrophin antag; inhibits BDNF TrkB receptor		2.3920
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		210chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		210aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
ro 31-8220
Ro 31-8220: a protein kinase C inhibitor		210imidothiocarbamic ester;
indoles;
maleimides		EC 2.7.11.13 (protein kinase C) inhibitor
sb 202190
4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase		210imidazoles;
organofluorine compound;
phenols;
pyridines		apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
fluorescein
Fluorescein: A phthalic indicator dye that appears yellow-green in normal tear film and bright green in a more alkaline medium such as the aqueous humor.. fluorescein (lactone form) : A xanthene dye that is highly fluorescent, detectable even when present in minute quantities. Used forensically to detect traces of blood, in analytical chemistry as an indicator in silver nitrate titrations and in microscopy.		2.05102-benzofurans;
gamma-lactone;
organic heteropentacyclic compound;
oxaspiro compound;
polyphenol;
xanthene dye		fluorescent dye;
radioopaque medium
7-hydroxystaurosporine
[no description available]		2.0210
ruboxistaurin
ruboxistaurin: inhibits protein kinase C beta; structure in first source		2.0210
sb 203580
[no description available]		210imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
wortmannin
[no description available]		210acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
y 27632
Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.		210aromatic amide
h 89
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.		210N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
u 0126
U 0126: protein kinase kinase inhibitor; structure in first source		210aryl sulfide;
dinitrile;
enamine;
substituted aniline		antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent
quercetin
[no description available]		2107-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
rottlerin
rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.		210aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone		anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		210antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
kn 62
KN 62: inhibitor of Ca/calmodulin-dependent protein kinase II		210piperazines
arcyriaflavin a
arcyriaflavin A: from marine ascidian, Eudistoma sp.; structure given in first source		1.9710indolocarbazole
pd 184352
2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide: inhibits MAP kinase kinase; structure in first source		210aminobenzoic acid
flag peptide
FLAG peptide: engineered as a tag for immunoaffinity purification of genetically-engineered proteins; amino acid sequence given in first source; a polar octapeptide. FLAG peptide : An eight amino acid peptide consisting of L-aspartic acid, L-tyrosine, L-lysine, four L-aspartic acid residues, and L-lysine joined in sequence by peptide linkages. It is widely used as a fusion tag for the purification and detection of a wide variety of recombinant proteins.		2.0410peptide
ConditionIndicatedRelationship StrengthStudiesTrials