Compounds > crt 0066101
Page last updated: 2024-10-15

crt 0066101

Description

CRT 0066101: protein kinase D inhibitor with antineoplastic activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID136189563
CHEMBL ID4515390
SCHEMBL ID4514713
MeSH IDM0549143

Synonyms (14)

Synonym
gtpl8048
2-[4-[[(2r)-2-aminobutyl]amino]pyrimidin-2-yl]-4-(1-methyl-1h-pyrazol-4-yl)phenol dihydrochloride
SCHEMBL4514713
crt 0066101
CHEMBL4515390 ,
NCGC00387217-01
956123-34-5
Q27076919
(r)-2-(4-((2-aminobutyl)amino)pyrimidin-2-yl)-4-(1-methyl-1h-pyrazol-4-yl)phenol
crt0066101 hcl
2-[4-[[(2r)-2-aminobutyl]amino]pyrimidin-2-yl]-4-(1-methylpyrazol-4-yl)phenol
bdbm50565693
EN300-7426907
2-(4-{[(2r)-2-aminobutyl]amino}pyrimidin-2-yl)-4-(1-methyl-1h-pyrazol-4-yl)phenol

Bioavailability

ExcerptReference
"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)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency15.09160.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency13.45040.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency9.52210.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency13.45040.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase D3Homo sapiens (human)IC50 (µMol)0.00600.00011.170110.0000AID1742911
Serine/threonine-protein kinase D1Homo sapiens (human)IC50 (µMol)0.01600.00011.231910.0000AID1742909
Serine/threonine-protein kinase D2Homo sapiens (human)IC50 (µMol)0.00900.00130.16820.7860AID1742910
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (108)

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)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
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)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein 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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein 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 (28)

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)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
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 (21)

Assay IDTitleYearJournalArticle
AID1742922Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742921Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742909Inhibition of recombinant FLAG-tagged PKD1 (unknown origin) expressed in HEK293T cells using Syntide-2 as substrate measured after 15 mins by ADP-Glo assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742910Inhibition of recombinant FLAG-tagged PKD2 (unknown origin) expressed in HEK293T cells using Syntide-2 as substrate measured after 15 mins by ADP-Glo assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742927Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742924Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742928Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742923Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742925Antiproliferative activity against human DND41 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742926Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by IncuCyte live-cell automated imaging analysis2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742911Inhibition of recombinant FLAG-tagged PKD3 (unknown origin) expressed in HEK293T cells using Syntide-2 as substrate measured after 15 mins by ADP-Glo assay2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742916Inhibition of recombinant FLAG-tagged PKD2 (unknown origin) expressed in human PANC-1 cells co-transfected with Myc-CTTN assessed as reduction in PDBu-stimulated CTTN phosphorylation at S298 residues at 20 uM preincubated for 1 hr followed PDBu stimulatio2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
AID1742915Inhibition of recombinant FLAG-tagged PKD1 (unknown origin) expressed in human PANC-1 cells co-transfected with Myc-CTTN assessed as reduction in PDBu-stimulated CTTN phosphorylation at S298 residues at 20 uM preincubated for 1 hr followed PDBu stimulatio2020European journal of medicinal chemistry, Nov-01, Volume: 205Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.
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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1345351Human protein kinase D1 (Protein kinase D (PKD) family)2010Molecular cancer therapeutics, May, Volume: 9, Issue:5
A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
AID1345867Human protein kinase D2 (Protein kinase D (PKD) family)2010Molecular cancer therapeutics, May, Volume: 9, Issue:5
A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
AID1345845Human protein kinase D3 (Protein kinase D (PKD) family)2010Molecular cancer therapeutics, May, Volume: 9, Issue:5
A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer growth in vitro and in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's17 (70.83)24.3611
2020's7 (29.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
go 6976
[no description available]		2.0610indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.0610ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
xanthenes
Xanthenes: Compounds with three aromatic rings in linear arrangement with an OXYGEN in the center ring.		2.5720xanthene
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.2510taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
gallein
gallein: do not confuse with gallin; structure. gallein : A xanthene dye that is fluoran carrying four hydroxy substituents at positions 3', 4', 5' and 6'.		2.57202-benzofurans;
gamma-lactone;
organic heteropentacyclic compound;
oxaspiro compound;
polyphenol;
xanthene dye		fluorochrome;
G-protein-coupled receptor antagonist;
histological dye
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		2.2510
cid755673
CID755673: a potent and selective inhibitor of protein kinase D; structure in first source		2.2510benzofurans
1-tert-butyl-3-naphthalen-1-ylmethyl-1h-pyrazolo(3,4-d)pyrimidin-4-ylemine
[no description available]		2.2510pyrazolopyrimidinetyrosine kinase inhibitor
sphingosine
sphing-4-enine : A sphingenine in which the C=C double bond is located at the 4-position.. sphingenine : A 2-aminooctadecene-1,3-diol having (2S,3R)-configuration.. sphingoid : Sphinganine, its homologs and stereoisomers, and the hydroxy and unsaturated derivatives of these compounds.. 2-aminooctadec-4-ene-1,3-diol : A 2-aminooctadecene-1,3-diol having its double bond at position 4.		2.0810sphing-4-eninehuman metabolite;
mouse metabolite
sphingosine 1-phosphate
sphingosine 1-phosphate: RN given refers to (R-(R*,S*-(E)))-isomer; RN for cpd without isomeric designation not available 8/89. sphingosine 1-phosphate : A phosphosphingolipid that consists of sphingosine having a phospho group attached at position 1		2.0810sphingoid 1-phosphatemouse metabolite;
signalling molecule;
sphingosine-1-phosphate receptor agonist;
T-cell proliferation inhibitor;
vasodilator agent
lysophosphatidic acid
lysophosphatidic acid: RN given refers to parent cpd. 1-oleoyl-sn-glycerol 3-phosphate : A 1-acyl-sn-glycerol 3-phosphate having oleoyl as the 1-O-acyl group.. lysophosphatidic acid : A member of the class of lysophosphatidic acids obtained by hydrolytic removal of one of the two acyl groups of any phosphatidic acid. A 'closed' class.		2.15101-acyl-sn-glycerol 3-phosphate
cholecystokinin
Cholecystokinin: A peptide, of about 33 amino acids, secreted by the upper INTESTINAL MUCOSA and also found in the central nervous system. It causes gallbladder contraction, release of pancreatic exocrine (or digestive) enzymes, and affects other gastrointestinal functions. Cholecystokinin may be the mediator of satiety.		2.0610
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		2.0610
kb-nb142-70
kb-NB142-70: inhibitor of protein kinase D; structure in first source		2.1310
ConditionIndicatedRelationship StrengthStudiesTrials
Cancer of Pancreas
[description not available]		02.4620
Carcinoma, Ductal, Pancreatic
[description not available]		02.4620
Pancreatic Neoplasms
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).		02.4620
Carcinoma, Pancreatic Ductal
Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.		02.4620
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Lung Injury, Acute
[description not available]		02.610
Cytokine Release Syndrome
A severe immune reaction characterized by excessive release of CYTOKINES. Symptoms include DYSPNEA; FEVER; HEADACHE; HYPOTENSION; NAUSEA; RASH; TACHYCARDIA; HYPOXIA; HYPERFERRITINEMIA, and MULTIPLE ORGAN FAILURE. It is associated with viral infections, SEPSIS; AUTOIMMUNE DISEASES and a variety of factors used in IMMUNOTHERAPY.		02.610
2019 Novel Coronavirus Disease
[description not available]		02.610
Innate Inflammatory Response
[description not available]		02.7220
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		02.610
Acute Respiratory Distress Syndrome
[description not available]		02.610
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.7220
Pneumonia
Infection of the lung often accompanied by inflammation.		02.610
Respiratory Distress Syndrome
A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.		02.610
Acute Lung Injury
A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).		02.610
Arteriosclerosis, Coronary
[description not available]		02.2110
Cardiovascular Stroke
[description not available]		02.2110
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.2110
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		02.2110
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		02.2110
ER-Negative PR-Negative HER2-Negative Breast Cancer
[description not available]		02.6320
Triple Negative Breast Neoplasms
Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.		02.6320
Arthritis, Degenerative
[description not available]		02.2110
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		02.2110
Bone Loss, Osteoclastic
[description not available]		02.2510
Bladder Cancer
[description not available]		02.1710
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		02.1710
Allodynia
[description not available]		02.2110
Benign Neoplasms, Brain
[description not available]		02.0810
Astrocytoma, Grade IV
[description not available]		02.0810
Invasiveness, Neoplasm
[description not available]		02.7830
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		02.0810
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		02.0810
Breast Cancer
[description not available]		02.1110
Cancer of Lung
[description not available]		02.1110
Lymph Node Metastasis
[description not available]		02.1110
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.1110
Lung Neoplasms
Tumors or cancer of the LUNG.		02.1110
Angiogenesis, Pathologic
[description not available]		02.0610
Acute Edematous Pancreatitis
[description not available]		02.0610
Pancreatitis
INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.		02.0610