Page last updated: 2024-11-13

sr-3029

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Description

SR-3029: highly selective casein kinase 1delta/1epsilon inhibitor with potent antiproliferative properties; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60196195
CHEMBL ID4211454
SCHEMBL ID15243359
SCHEMBL ID17132207
MeSH IDM0590681

Synonyms (24)

Synonym
S6544
SCHEMBL15243359
SCHEMBL17132207
1454585-06-8
sr 3029
n-((6,7-difluoro-1h-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9h-purin-6-amine
HY-100011
AKOS030526553
CS-5672
sr-3029
n-[(6,7-difluoro-1h-1,3-benzodiazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(morpholin-4-yl)-9h-purin-6-amine
AKOS030238854
mfcd30187527
BCP20656
(6,7-difluoro-1h-benzoimidazol-2-ylmethyl)-[9-(3-fluoro-phenyl)-2-morpholin-4-yl-9h-purin-6-yl]-amine
EX-A2442
sr3029
n-[(4,5-difluoro-1h-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-morpholin-4-ylpurin-6-amine
MS-28935
n-((4,5-difluoro-1h-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9h-purin-6-amine
k0e ,
CHEMBL4211454 ,
bdbm50454220
AC-36072
[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)
PPM1D proteinHomo sapiens (human)Potency0.52300.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency0.52300.00339.158239.8107AID1347411
[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)
Cyclin-dependent kinase 4Homo sapiens (human)IC50 (µMol)0.57500.00060.570610.0000AID1747880
G1/S-specific cyclin-D1Homo sapiens (human)IC50 (µMol)0.50150.00060.54799.5000AID1747880; AID1747881
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.04400.00002.398310.0000AID1373027
Casein kinase I isoform deltaHomo sapiens (human)IC50 (µMol)0.04400.00401.127210.0000AID1373027; AID1854451
Casein kinase I isoform epsilonHomo sapiens (human)IC50 (µMol)0.26000.00401.11509.5000AID1373028; AID1854452
Cyclin-dependent kinase 6Homo sapiens (human)IC50 (µMol)0.42800.00190.86547.2000AID1747881
Cyclin-dependent kinase 13Homo sapiens (human)IC50 (µMol)0.01000.01000.44042.2000AID1747878
Cyclin-dependent kinase 12Homo sapiens (human)IC50 (µMol)0.05450.00701.01758.5000AID1747879; AID1854442
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (134)

Processvia Protein(s)Taxonomy
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)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 4Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 4Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-dependent kinase 4Homo sapiens (human)
cell divisionCyclin-dependent kinase 4Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 4Homo sapiens (human)
regulation of transcription initiation by RNA polymerase IICyclin-dependent kinase 4Homo sapiens (human)
regulation of type B pancreatic cell proliferationCyclin-dependent kinase 4Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 4Homo sapiens (human)
cellular response to interleukin-4Cyclin-dependent kinase 4Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateCyclin-dependent kinase 4Homo sapiens (human)
cellular response to ionomycinCyclin-dependent kinase 4Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 4Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
signal transductionCyclin-dependent kinase 4Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIG1/S-specific cyclin-D1Homo sapiens (human)
re-entry into mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of protein phosphorylationG1/S-specific cyclin-D1Homo sapiens (human)
DNA damage responseG1/S-specific cyclin-D1Homo sapiens (human)
lactationG1/S-specific cyclin-D1Homo sapiens (human)
response to xenobiotic stimulusG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
Wnt signaling pathwayG1/S-specific cyclin-D1Homo sapiens (human)
neuron differentiationG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of epithelial cell differentiationG1/S-specific cyclin-D1Homo sapiens (human)
endoplasmic reticulum unfolded protein responseG1/S-specific cyclin-D1Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingG1/S-specific cyclin-D1Homo sapiens (human)
mammary gland epithelial cell proliferationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of mammary gland epithelial cell proliferationG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of neuron apoptotic processG1/S-specific cyclin-D1Homo sapiens (human)
response to leptinG1/S-specific cyclin-D1Homo sapiens (human)
fat cell differentiationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
cell divisionG1/S-specific cyclin-D1Homo sapiens (human)
mammary gland alveolus developmentG1/S-specific cyclin-D1Homo sapiens (human)
response to UV-AG1/S-specific cyclin-D1Homo sapiens (human)
liver regenerationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
microtubule nucleationCasein kinase I isoform deltaHomo sapiens (human)
Golgi organizationCasein kinase I isoform deltaHomo sapiens (human)
protein localization to Golgi apparatusCasein kinase I isoform deltaHomo sapiens (human)
protein localization to ciliumCasein kinase I isoform deltaHomo sapiens (human)
protein localization to centrosomeCasein kinase I isoform deltaHomo sapiens (human)
non-motile cilium assemblyCasein kinase I isoform deltaHomo sapiens (human)
positive regulation of protein phosphorylationCasein kinase I isoform deltaHomo sapiens (human)
protein phosphorylationCasein kinase I isoform deltaHomo sapiens (human)
Wnt signaling pathwayCasein kinase I isoform deltaHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processCasein kinase I isoform deltaHomo sapiens (human)
circadian regulation of gene expressionCasein kinase I isoform deltaHomo sapiens (human)
regulation of circadian rhythmCasein kinase I isoform deltaHomo sapiens (human)
COPII vesicle coatingCasein kinase I isoform deltaHomo sapiens (human)
spindle assemblyCasein kinase I isoform deltaHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayCasein kinase I isoform deltaHomo sapiens (human)
midbrain dopaminergic neuron differentiationCasein kinase I isoform deltaHomo sapiens (human)
cellular response to nerve growth factor stimulusCasein kinase I isoform deltaHomo sapiens (human)
positive regulation of non-canonical Wnt signaling pathwayCasein kinase I isoform deltaHomo sapiens (human)
peptidyl-serine phosphorylationCasein kinase I isoform deltaHomo sapiens (human)
signal transductionCasein kinase I isoform deltaHomo sapiens (human)
non-motile cilium assemblyCasein kinase I isoform deltaHomo sapiens (human)
endocytosisCasein kinase I isoform deltaHomo sapiens (human)
DNA repairCasein kinase I isoform epsilonHomo sapiens (human)
protein phosphorylationCasein kinase I isoform epsilonHomo sapiens (human)
protein localizationCasein kinase I isoform epsilonHomo sapiens (human)
negative regulation of Wnt signaling pathwayCasein kinase I isoform epsilonHomo sapiens (human)
negative regulation of protein bindingCasein kinase I isoform epsilonHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processCasein kinase I isoform epsilonHomo sapiens (human)
regulation of protein localizationCasein kinase I isoform epsilonHomo sapiens (human)
circadian regulation of gene expressionCasein kinase I isoform epsilonHomo sapiens (human)
regulation of circadian rhythmCasein kinase I isoform epsilonHomo sapiens (human)
circadian behaviorCasein kinase I isoform epsilonHomo sapiens (human)
canonical Wnt signaling pathwayCasein kinase I isoform epsilonHomo sapiens (human)
positive regulation of amyloid-beta formationCasein kinase I isoform epsilonHomo sapiens (human)
cellular response to nerve growth factor stimulusCasein kinase I isoform epsilonHomo sapiens (human)
positive regulation of non-canonical Wnt signaling pathwayCasein kinase I isoform epsilonHomo sapiens (human)
peptidyl-serine phosphorylationCasein kinase I isoform epsilonHomo sapiens (human)
endocytosisCasein kinase I isoform epsilonHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayCasein kinase I isoform epsilonHomo sapiens (human)
signal transductionCasein kinase I isoform epsilonHomo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICyclin-dependent kinase 6Homo sapiens (human)
positive regulation of cell-matrix adhesionCyclin-dependent kinase 6Homo sapiens (human)
type B pancreatic cell developmentCyclin-dependent kinase 6Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 6Homo sapiens (human)
Notch signaling pathwayCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of cell population proliferationCyclin-dependent kinase 6Homo sapiens (human)
response to virusCyclin-dependent kinase 6Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 6Homo sapiens (human)
positive regulation of gene expressionCyclin-dependent kinase 6Homo sapiens (human)
astrocyte developmentCyclin-dependent kinase 6Homo sapiens (human)
dentate gyrus developmentCyclin-dependent kinase 6Homo sapiens (human)
lateral ventricle developmentCyclin-dependent kinase 6Homo sapiens (human)
T cell differentiation in thymusCyclin-dependent kinase 6Homo sapiens (human)
gliogenesisCyclin-dependent kinase 6Homo sapiens (human)
cell dedifferentiationCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of cell differentiationCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of myeloid cell differentiationCyclin-dependent kinase 6Homo sapiens (human)
regulation of erythrocyte differentiationCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of monocyte differentiationCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of osteoblast differentiationCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of cell cycleCyclin-dependent kinase 6Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-dependent kinase 6Homo sapiens (human)
generation of neuronsCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of epithelial cell proliferationCyclin-dependent kinase 6Homo sapiens (human)
cell divisionCyclin-dependent kinase 6Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 6Homo sapiens (human)
hematopoietic stem cell differentiationCyclin-dependent kinase 6Homo sapiens (human)
regulation of hematopoietic stem cell differentiationCyclin-dependent kinase 6Homo sapiens (human)
regulation of cell motilityCyclin-dependent kinase 6Homo sapiens (human)
negative regulation of cellular senescenceCyclin-dependent kinase 6Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 6Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 6Homo sapiens (human)
signal transductionCyclin-dependent kinase 6Homo sapiens (human)
alternative mRNA splicing, via spliceosomeCyclin-dependent kinase 13Homo sapiens (human)
regulation of signal transductionCyclin-dependent kinase 13Homo sapiens (human)
hemopoiesisCyclin-dependent kinase 13Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICyclin-dependent kinase 13Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 13Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 13Homo sapiens (human)
negative regulation of stem cell differentiationCyclin-dependent kinase 13Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 13Homo sapiens (human)
transcription by RNA polymerase IICyclin-dependent kinase 12Homo sapiens (human)
mRNA processingCyclin-dependent kinase 12Homo sapiens (human)
RNA splicingCyclin-dependent kinase 12Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICyclin-dependent kinase 12Homo sapiens (human)
regulation of MAP kinase activityCyclin-dependent kinase 12Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 12Homo sapiens (human)
protein autophosphorylationCyclin-dependent kinase 12Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 12Homo sapiens (human)
negative regulation of stem cell differentiationCyclin-dependent kinase 12Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (36)

Processvia Protein(s)Taxonomy
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)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
protein bindingCyclin-dependent kinase 4Homo sapiens (human)
ATP bindingCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-dependent kinase 4Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 4Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
transcription corepressor activityG1/S-specific cyclin-D1Homo sapiens (human)
protein kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
protein bindingG1/S-specific cyclin-D1Homo sapiens (human)
enzyme bindingG1/S-specific cyclin-D1Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-D1Homo sapiens (human)
histone deacetylase bindingG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityG1/S-specific cyclin-D1Homo sapiens (human)
proline-rich region bindingG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-D1Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo 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 2C19Homo sapiens (human)
protein kinase activityCasein kinase I isoform deltaHomo sapiens (human)
protein serine/threonine kinase activityCasein kinase I isoform deltaHomo sapiens (human)
protein bindingCasein kinase I isoform deltaHomo sapiens (human)
ATP bindingCasein kinase I isoform deltaHomo sapiens (human)
cadherin bindingCasein kinase I isoform deltaHomo sapiens (human)
tau-protein kinase activityCasein kinase I isoform deltaHomo sapiens (human)
protein serine kinase activityCasein kinase I isoform deltaHomo sapiens (human)
RNA bindingCasein kinase I isoform epsilonHomo sapiens (human)
protein kinase activityCasein kinase I isoform epsilonHomo sapiens (human)
protein serine/threonine kinase activityCasein kinase I isoform epsilonHomo sapiens (human)
protein bindingCasein kinase I isoform epsilonHomo sapiens (human)
ATP bindingCasein kinase I isoform epsilonHomo sapiens (human)
protein serine kinase activityCasein kinase I isoform epsilonHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 6Homo sapiens (human)
protein bindingCyclin-dependent kinase 6Homo sapiens (human)
ATP bindingCyclin-dependent kinase 6Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 6Homo sapiens (human)
FBXO family protein bindingCyclin-dependent kinase 6Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 6Homo sapiens (human)
RNA bindingCyclin-dependent kinase 13Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 13Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 13Homo sapiens (human)
protein bindingCyclin-dependent kinase 13Homo sapiens (human)
ATP bindingCyclin-dependent kinase 13Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 13Homo sapiens (human)
protein kinase bindingCyclin-dependent kinase 13Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 13Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 13Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 12Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 12Homo sapiens (human)
protein bindingCyclin-dependent kinase 12Homo sapiens (human)
ATP bindingCyclin-dependent kinase 12Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 12Homo sapiens (human)
protein kinase bindingCyclin-dependent kinase 12Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 12Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 4Homo sapiens (human)
nucleolusCyclin-dependent kinase 4Homo sapiens (human)
cytosolCyclin-dependent kinase 4Homo sapiens (human)
bicellular tight junctionCyclin-dependent kinase 4Homo sapiens (human)
nuclear membraneCyclin-dependent kinase 4Homo sapiens (human)
cyclin D1-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D2-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D3-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 4Homo sapiens (human)
chromatinCyclin-dependent kinase 4Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 4Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
cytoplasmCyclin-dependent kinase 4Homo sapiens (human)
nucleusG1/S-specific cyclin-D1Homo sapiens (human)
nucleoplasmG1/S-specific cyclin-D1Homo sapiens (human)
cytosolG1/S-specific cyclin-D1Homo sapiens (human)
bicellular tight junctionG1/S-specific cyclin-D1Homo sapiens (human)
nuclear membraneG1/S-specific cyclin-D1Homo sapiens (human)
cyclin D1-CDK4 complexG1/S-specific cyclin-D1Homo sapiens (human)
cyclin D1-CDK6 complexG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexG1/S-specific cyclin-D1Homo sapiens (human)
transcription repressor complexG1/S-specific cyclin-D1Homo sapiens (human)
centrosomeG1/S-specific cyclin-D1Homo sapiens (human)
cytoplasmG1/S-specific cyclin-D1Homo sapiens (human)
nucleusG1/S-specific cyclin-D1Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
nucleusCasein kinase I isoform deltaHomo sapiens (human)
nucleoplasmCasein kinase I isoform deltaHomo sapiens (human)
Golgi apparatusCasein kinase I isoform deltaHomo sapiens (human)
centrosomeCasein kinase I isoform deltaHomo sapiens (human)
spindleCasein kinase I isoform deltaHomo sapiens (human)
cytosolCasein kinase I isoform deltaHomo sapiens (human)
spindle microtubuleCasein kinase I isoform deltaHomo sapiens (human)
plasma membraneCasein kinase I isoform deltaHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartment membraneCasein kinase I isoform deltaHomo sapiens (human)
ciliary basal bodyCasein kinase I isoform deltaHomo sapiens (human)
perinuclear region of cytoplasmCasein kinase I isoform deltaHomo sapiens (human)
nucleusCasein kinase I isoform deltaHomo sapiens (human)
cytoplasmCasein kinase I isoform deltaHomo sapiens (human)
spindle microtubuleCasein kinase I isoform deltaHomo sapiens (human)
nucleusCasein kinase I isoform epsilonHomo sapiens (human)
nucleoplasmCasein kinase I isoform epsilonHomo sapiens (human)
cytoplasmCasein kinase I isoform epsilonHomo sapiens (human)
cytosolCasein kinase I isoform epsilonHomo sapiens (human)
growth coneCasein kinase I isoform epsilonHomo sapiens (human)
neuronal cell bodyCasein kinase I isoform epsilonHomo sapiens (human)
ribonucleoprotein complexCasein kinase I isoform epsilonHomo sapiens (human)
cytoplasmCasein kinase I isoform epsilonHomo sapiens (human)
nucleusCasein kinase I isoform epsilonHomo sapiens (human)
ruffleCyclin-dependent kinase 6Homo sapiens (human)
nucleusCyclin-dependent kinase 6Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 6Homo sapiens (human)
cytoplasmCyclin-dependent kinase 6Homo sapiens (human)
centrosomeCyclin-dependent kinase 6Homo sapiens (human)
cytosolCyclin-dependent kinase 6Homo sapiens (human)
cyclin D1-CDK6 complexCyclin-dependent kinase 6Homo sapiens (human)
cyclin D3-CDK6 complexCyclin-dependent kinase 6Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 6Homo sapiens (human)
cyclin D2-CDK6 complexCyclin-dependent kinase 6Homo sapiens (human)
cytoplasmCyclin-dependent kinase 6Homo sapiens (human)
nucleusCyclin-dependent kinase 6Homo sapiens (human)
cyclin K-CDK13 complexCyclin-dependent kinase 13Homo sapiens (human)
extracellular regionCyclin-dependent kinase 13Homo sapiens (human)
extracellular spaceCyclin-dependent kinase 13Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 13Homo sapiens (human)
Golgi apparatusCyclin-dependent kinase 13Homo sapiens (human)
cytosolCyclin-dependent kinase 13Homo sapiens (human)
nuclear speckCyclin-dependent kinase 13Homo sapiens (human)
ficolin-1-rich granule lumenCyclin-dependent kinase 13Homo sapiens (human)
nuclear cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 13Homo sapiens (human)
nucleusCyclin-dependent kinase 13Homo sapiens (human)
cyclin/CDK positive transcription elongation factor complexCyclin-dependent kinase 13Homo sapiens (human)
cyclin K-CDK12 complexCyclin-dependent kinase 12Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 12Homo sapiens (human)
nuclear speckCyclin-dependent kinase 12Homo sapiens (human)
nuclear cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 12Homo sapiens (human)
nucleusCyclin-dependent kinase 12Homo sapiens (human)
cyclin/CDK positive transcription elongation factor complexCyclin-dependent kinase 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

Assay IDTitleYearJournalArticle
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1373034Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate at 10 uM after 10 mins in presence of NADPH relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373029Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CellTiter-Glo assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373027Inhibition of recombinant human full length N-terminal GST-tagged CK1delta expressed in baculovirus in Sf9 insect cells using ULight-Topo-IIa(Thr1342) peptide as substrate after 10 mins by TR-FRET assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373050Oral bioavailability in C57BL6 mouse at 3 mg/kg measured up to 8 hrs by LC-MS/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1854451Inhibition of CK1 delta (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Current progress and novel strategies that target CDK12 for drug discovery.
AID1849033Induction of osteogenic differentiation in mouse C2C12 cells assessed as ALP activity preincubated with compound in the presence of BMP-4 for 72 hrs followed by substrate addition and measured after 1 hrs in the presence of PIK93 by luminescence based ass2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Phenotypic Discovery of Triazolo[1,5-
AID1373028Inhibition of recombinant human full length N-terminal GST-tagged CK1epsilon expressed in baculovirus in Sf9 insect cells using ULight-Topo-IIa(Thr1342) peptide as substrate after 10 mins by TR-FRET assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1849034Induction of osteogenic differentiation in mouse C2C12 cells assessed as ALP activity preincubated with compound in the presence of BMP-4 for 72 hrs followed by substrate addition and measured after 1 hrs in the presence of BYL719 by luminescence based as2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Phenotypic Discovery of Triazolo[1,5-
AID1373047Half life in C57BL6 mouse at 3 mg/kg, po by LC-MS/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373031Half life in human liver microsomes at 1 uM by LC/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373044AUC in C57BL6 mouse at 3 mg/kg, po up to 8 hrs by LC-MS/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373036Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate at 10 uM after 10 mins in presence of NADPH relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1849031Activation of BMP signaling in HEK293T cells expressing BRE-Vent2 luciferase reporter gene assessed as BRE activation by measuring increase in luciferase activity measured after 22 hrs in the presence of BMP-4 by dual-luciferase assay2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Phenotypic Discovery of Triazolo[1,5-
AID1375071Toxicity in HEK293T cells at 0.5 to 5 uM after 6 to 22 hrs by CellTiter-Glo assay2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε.
AID1854452Inhibition of CK1 epsilon (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Current progress and novel strategies that target CDK12 for drug discovery.
AID1373038Cmax in C57BL6 mouse at 3 mg/kg, po by LC-MS/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373037Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate at 10 uM after 10 mins in presence of NADPH relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373041Clearance in C57BL6 mouse at 3 mg/kg, po up to 8 hrs by LC-MS/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373033Half life in rat liver microsomes at 1 uM by LC/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373035Inhibition of CYP2C9 in human liver microsomes using tolbutamide as substrate at 10 uM after 10 mins in presence of NADPH relative to control2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1375076Inhibition of CK1delta/epsilon in HEK293T cells transfected with Wnt3A-expressing vector assessed as suppression of Wnt/beta-catenin signaling up to 0.1 uM after 22 hrs by Super-top flash reporter gene assay2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε.
AID1373053Apparent permeability at 5 uM after 5 hrs by PAMPA2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1849035Induction of osteogenic differentiation in mouse C2C12 cells assessed as ALP activity at 0.02 uM preincubated with compound in the presence of BMP-4 for 72 hrs followed by substrate addition and measured after 1 hrs in the presence of AS252424 by luminesc2022Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
Phenotypic Discovery of Triazolo[1,5-
AID1375075Inhibition of CK1delta/epsilon in HEK293T cells assessed as suppression of Wnt/beta-catenin signaling up to 0.1 uM after 22 hrs in presence of Wnt3A-conditioned medium by Super-top flash reporter gene assay2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε.
AID1854442Inhibition of CDK12 (unknown origin)2022European journal of medicinal chemistry, Oct-05, Volume: 240Current progress and novel strategies that target CDK12 for drug discovery.
AID1373030Aqueous solubility of the compound at pH 7.4 measured after 24 hrs by HPLC analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
AID1373032Half life in mouse liver microsomes at 1 uM by LC/MS analysis2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (66.67)24.3611
2020's3 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.93

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 Index19.93 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]