Compounds > kb-nb142-70
Page last updated: 2024-11-13

kb-nb142-70

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Description

kb-NB142-70: inhibitor of protein kinase D; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID45258277
CHEMBL ID1672571
SCHEMBL ID9920595
MeSH IDM0582524

Synonyms (30)

Synonym
NCGC00241412-01
CHEMBL1672571 ,
kb-nb142-70
bdbm50336960
3,4-dihydro-9-hydroxy-[1]benzothieno[2,3-f]-1,4-thiazepin-5(2h)-one
HY-15528
CS-1091
kb nb 142-70
1233533-04-4
6-cyclopropyl-8-fluoro-2-(2-(hydroxymethyl)-3-(1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2-ylamino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2h)-
3,4-dihydro-9-hydroxy-[1]benzothieno-[2,3-f]-1,4-thiazepin-5(2h)-one
SCHEMBL9920595
9-hydroxy-3,4-dihydro-2h-[1]-benzothiolo[2,3-f][1,4]thiazepin-5-one
gtpl9369
AKOS024457899
9-hydroxy-3,4-dihydro-2h-[1]benzothiolo[2,3-f][1,4]thiazepin-5-one
J-004926
DTXSID10669824
9-hydroxy-3,4-dihydro[1]benzothieno[2,3-f][1,4]thiazepin-5(2h)-one
kb-nb142-70, >=97% (hplc)
DHUAGGSHTKPOHU-UHFFFAOYSA-N ,
4-hydroxy-8,14-dithia-11-azatricyclo[7.5.0.0^{2,7}]tetradeca-1(9),2,4,6-tetraen-10-one
BCP06729
EX-A2497
mfcd18086915
AS-16549
9-hydroxy-3,4-dihydrobenzo[4,5]thieno[2,3-f][1,4]thiazepin-5(2h)-one
HMS3740G15
NCGC00241412-08
A899022

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

Dosage Studied

ExcerptRelevanceReference
" In mice dosed with kb-NB165-09, the plasma C (max) was 61."( In vitro cytotoxicity, pharmacokinetics, tissue distribution, and metabolism of small-molecule protein kinase D inhibitors, kb-NB142-70 and kb-NB165-09, in mice bearing human cancer xenografts.
Beumer, JH; Bravo-Altamirano, K; Clausen, DM; Egorin, MJ; Eiseman, JL; Guo, J; Parise, RA; Sharlow, ER; Wang, QJ; Wipf, P, 2013)		0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase D3Homo sapiens (human)IC50 (µMol)0.04670.00011.170110.0000AID1799562
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)0.02830.00011.774010.0000AID570424
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)0.02830.00002.015110.0000AID570424
Serine/threonine-protein kinase D1Homo sapiens (human)IC50 (µMol)0.47370.00011.231910.0000AID1799562; AID570424; AID570425
Serine/threonine-protein kinase D2Homo sapiens (human)IC50 (µMol)0.04670.00130.16820.7860AID1799562
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (98)

Processvia Protein(s)Taxonomy
protein phosphorylationSerine/threonine-protein kinase D3Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D3Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D3Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D3Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
angiogenesisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell proliferationSerine/threonine-protein kinase D1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase D1Homo sapiens (human)
inflammatory responseSerine/threonine-protein kinase D1Homo sapiens (human)
Golgi organizationSerine/threonine-protein kinase D1Homo sapiens (human)
signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
integrin-mediated signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
nervous system developmentSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of autophagySerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell migrationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of keratinocyte proliferationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of neuron projection developmentSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of skeletal muscle contraction by modulation of calcium ion sensitivity of myofibrilSerine/threonine-protein kinase D1Homo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D1Homo sapiens (human)
cell differentiationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to amino acid starvationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to oxidative stressSerine/threonine-protein kinase D1Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of protein import into nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationSerine/threonine-protein kinase D1Homo sapiens (human)
innate immune responseSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of osteoblast differentiationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of angiogenesisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of cell sizeSerine/threonine-protein kinase D1Homo sapiens (human)
negative regulation of endocytosisSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine/threonine-protein kinase D1Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of protein export from nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
Golgi vesicle transportSerine/threonine-protein kinase D1Homo sapiens (human)
defense response to Gram-negative bacteriumSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySerine/threonine-protein kinase D1Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of sarcomere organizationSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to hydroperoxideSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to norepinephrine stimulusSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of peptide hormone secretionSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblySerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to angiotensinSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateSerine/threonine-protein kinase D1Homo sapiens (human)
cellular response to endothelinSerine/threonine-protein kinase D1Homo sapiens (human)
positive regulation of endothelial cell chemotaxisSerine/threonine-protein kinase D1Homo sapiens (human)
regulation of integrin-mediated signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D1Homo sapiens (human)
angiogenesisSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of endothelial cell proliferationSerine/threonine-protein kinase D2Homo sapiens (human)
adaptive immune responseSerine/threonine-protein kinase D2Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase D2Homo sapiens (human)
cell adhesionSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of endothelial cell migrationSerine/threonine-protein kinase D2Homo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase D2Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase D2Homo sapiens (human)
sphingolipid biosynthetic processSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwaySerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of interleukin-2 productionSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of interleukin-8 productionSerine/threonine-protein kinase D2Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase D2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of fibroblast growth factor receptor signaling pathwaySerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of angiogenesisSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of cell adhesionSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine/threonine-protein kinase D2Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase D2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwaySerine/threonine-protein kinase D2Homo sapiens (human)
T cell receptor signaling pathwaySerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of T cell receptor signaling pathwaySerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of DNA-binding transcription factor activitySerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySerine/threonine-protein kinase D2Homo sapiens (human)
endothelial tube morphogenesisSerine/threonine-protein kinase D2Homo sapiens (human)
regulation of T cell apoptotic processSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of DNA biosynthetic processSerine/threonine-protein kinase D2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisSerine/threonine-protein kinase D2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySerine/threonine-protein kinase D2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D3Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D3Homo sapiens (human)
kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D3Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D3Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
protein kinase C bindingSerine/threonine-protein kinase D1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D1Homo sapiens (human)
kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
heat shock protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase D1Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D1Homo sapiens (human)
phosphatidylinositol 3-kinase activator activitySerine/threonine-protein kinase D1Homo sapiens (human)
protein kinase activitySerine/threonine-protein kinase D2Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase D2Homo sapiens (human)
diacylglycerol-dependent serine/threonine kinase activitySerine/threonine-protein kinase D2Homo sapiens (human)
protein kinase C bindingSerine/threonine-protein kinase D2Homo sapiens (human)
protein bindingSerine/threonine-protein kinase D2Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase D2Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase D2Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase D2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
nucleoplasmSerine/threonine-protein kinase D3Homo sapiens (human)
cytosolSerine/threonine-protein kinase D3Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D3Homo sapiens (human)
cytosolSerine/threonine-protein kinase D3Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
autophagosome membraneSerine/threonine-protein kinase D1Homo sapiens (human)
nucleusSerine/threonine-protein kinase D1Homo sapiens (human)
trans-Golgi networkSerine/threonine-protein kinase D1Homo sapiens (human)
cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D1Homo sapiens (human)
cell-cell junctionSerine/threonine-protein kinase D1Homo sapiens (human)
cell cortexSerine/threonine-protein kinase D1Homo sapiens (human)
Z discSerine/threonine-protein kinase D1Homo sapiens (human)
perinuclear region of cytoplasmSerine/threonine-protein kinase D1Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase D1Homo sapiens (human)
cytosolSerine/threonine-protein kinase D1Homo sapiens (human)
nucleusSerine/threonine-protein kinase D2Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase D2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase D2Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase D2Homo sapiens (human)
cytosolSerine/threonine-protein kinase D2Homo sapiens (human)
plasma membraneSerine/threonine-protein kinase D2Homo sapiens (human)
cytosolSerine/threonine-protein kinase D2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1799562In Vitro Radiometric Kinase Assay from Article 10.1186/1472-6769-10-5: \\Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.\\2010BMC chemical biology, May-05, Volume: 10Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility.
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.
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.
AID570424Inhibition of human recombinant PKD1 after 10 mins by radiometric assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570435Inhibition of human recombinant CAMK2alpha at < 10 uM after 10 mins by radiometric assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570433Inhibition of human recombinant PKCbeta1 at < 10 uM after 10 mins by radiometric assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570432Inhibition of human recombinant PKCalpha at < 10 uM after 10 mins by radiometric assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570434Inhibition of human recombinant PKCdelta at < 10 uM after 10 mins by radiometric assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570431Inhibition of PLK2 at < 10 uM by TR-FRET assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570429Inhibition of CDK7 at < 10 uM by TR-FRET assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570428Inhibition of AKT at < 10 uM by IMAP assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570430Inhibition of PLK1 at < 10 uM by TR-FRET assay2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID570425Inhibition of PKD1 autophosphorylation at Ser916 in human PMA-induced LNCAP cells by Western blotting2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
AID1345351Human protein kinase D1 (Protein kinase D (PKD) family)2011ACS medicinal chemistry letters, Feb-14, Volume: 2, Issue:2
Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (100.00)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: 13.28

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 Index13.28 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.28)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pd 146626
kb-NB165-09: inhibitor of protein kinase D; structure in first source		2.7630
cid755673
CID755673: a potent and selective inhibitor of protein kinase D; structure in first source		2.4620benzofurans
crt 0066101
CRT 0066101: protein kinase D inhibitor with antineoplastic activity		2.1310
ConditionIndicatedRelationship StrengthStudiesTrials