Page last updated: 2024-11-13

pf 4800567

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Description

PF-4800567 : A pyrazolopyrimidine that is 1H-pyrazolo[3,4-d]pyrimidin-4-amine which is substituted at positions 1 and 3 by tetrahydro-2H-pyran-4-yl and (m-chlorophenoxy)methyl groups, respectively. It is a selective inhibitor of the epsilon isoform of casein kinase 1 (CK1epsilon). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID53472153
CHEMBL ID2069623
CHEBI ID87237
SCHEMBL ID12280136
MeSH IDM0560075

Synonyms (35)

Synonym
BRD-K43428468-003-01-6
chebi:87237 ,
pf-4800567
CHEMBL2069623 ,
3-[(3-chlorophenoxy)methyl]-1-(tetrahydro-2h-pyran-4-yl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine
16W ,
bdbm50399656
1188296-52-7
S2249
pf4800567
gtpl8050
3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine
4HNI
4HNF
SCHEMBL12280136
pf 4800567
3-((3-chlorophenoxy)methyl)-1-(tetrahydro-2h-pyran-4-yl)-1h-pyrazolo[3,4-d]pyrimidin-4-amine
pf-480
J-003896
DTXSID20703849
AKOS027449450
3-(3-chloro-phenoxymethyl)-1-(tetrahydro-pyran-4-yl)-1h-pyrazolo[3,4-d]pyrimidin-4-ylamine
NCGC00370925-02
CS-0011718
HY-12470
BS-14521
BCP28458
pf 4800567; pf-4800567
Q7119049
HMS3740I03
D83576
NCGC00370925-01
gee72drc63 ,
1h-pyrazolo[3,4-d]pyrimidin-4-amine, 3-[(3-chlorophenoxy)methyl]-1-(tetrahydro-2h-pyran-4-yl)-
3-[(3-chlorophenoxy)methyl]-1-(tetrahydro-2h-pyran-4-yl)-1h-pyrazolo[3,4-d]pyrimidin- 4-amine

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

Roles (1)

RoleDescription
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of non-specific serine/threonine protein kinase (EC 2.7.11.1), a kinase enzyme involved in phosphorylation of hydroxy group of serine or threonine.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
pyrazolopyrimidine
monochlorobenzenesAny member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
oxanesAny organic heteromonocyclic compoundthat is oxane or its substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency11.98770.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency11.98770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency11.98770.01238.964839.8107AID1645842
[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)
Chain A, Casein kinase I isoform deltaHomo sapiens (human)IC50 (µMol)0.37150.01300.25200.7110AID977608
Chain A, Casein kinase I isoform epsilonHomo sapiens (human)IC50 (µMol)0.37150.01300.25200.7110AID977608
Gonadotropin-releasing hormone receptorHomo sapiens (human)IC50 (µMol)0.03200.00010.12895.2000AID684970
Casein kinase I isoform deltaHomo sapiens (human)IC50 (µMol)0.54130.00401.127210.0000AID1337183; AID1539770; AID684969; AID711114
Casein kinase I isoform epsilonHomo sapiens (human)IC50 (µMol)0.03200.00401.11509.5000AID1337184; AID1539769; AID684970; AID711115
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (78)

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)
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)
gonadotropin secretionGonadotropin-releasing hormone receptorHomo sapiens (human)
cellular response to gonadotropin-releasing hormoneGonadotropin-releasing hormone receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayGonadotropin-releasing hormone receptorHomo sapiens (human)
cellular response to hormone stimulusGonadotropin-releasing hormone receptorHomo 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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

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)
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)
peptide bindingGonadotropin-releasing hormone receptorHomo sapiens (human)
gonadotropin-releasing hormone receptor activityGonadotropin-releasing hormone receptorHomo 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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
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)
plasma membraneGonadotropin-releasing hormone receptorHomo sapiens (human)
membraneGonadotropin-releasing hormone receptorHomo sapiens (human)
plasma membraneGonadotropin-releasing hormone receptorHomo 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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID676904Dose normalized fCmax in C57BL/6J mouse plasma at 10 mg/kg, po2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Getting the MAX out of Computational Models: The Prediction of Unbound-Brain and Unbound-Plasma Maximum Concentrations.
AID711106Binding affinity to human CK1epsilon S67T mutant assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID676906Ratio of dose normalized fCmax in brain to dose normalized fCmax in plasma in C57BL/6J mouse at 10 mg/kg, po2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Getting the MAX out of Computational Models: The Prediction of Unbound-Brain and Unbound-Plasma Maximum Concentrations.
AID1539770Inhibition of human CK1delta in presence of [gamma33P]-ATP2019European journal of medicinal chemistry, Nov-01, Volume: 181Small molecule modulators targeting protein kinase CK1 and CK2.
AID676905Dose normalized fCmax in C57BL/6J mouse brain at 10 mg/kg, po2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Getting the MAX out of Computational Models: The Prediction of Unbound-Brain and Unbound-Plasma Maximum Concentrations.
AID711113Selectivity index, ratio of IC50 for Casein kinase 1 delta to IC50 for Casein kinase 1 epsilon2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711110Binding affinity to human CK1delta T67S mutant assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711114Inhibition of Casein kinase 1 delta2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711112Binding affinity to human CK1delta I55F mutant assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711111Binding affinity to wild type human CK1delta (1-294 amino acids) assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID1337184Inhibition of human full length polyhistidine-tagged CK1epsilon expressed in Escherichia coli BL21-Codon-Plus (DE3)-RIL using PLSRTLpSVASLPGL as substrate after 2 hrs by kinase-glo assay2017Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
Non-kinase targets of protein kinase inhibitors.
AID1539769Inhibition of human CK1epsilon in presence of [gamma33P]-ATP2019European journal of medicinal chemistry, Nov-01, Volume: 181Small molecule modulators targeting protein kinase CK1 and CK2.
AID711108Binding affinity to wild type human CK1epsilon (1-294 amino acids) assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711115Inhibition of Casein kinase 1 epsilon2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711109Binding affinity to human CK1delta R69K mutant assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID684970Inhibition of CK1epsilon2012European journal of medicinal chemistry, Oct, Volume: 56Discovery of N6-phenyl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors using common-feature pharmacophore model based virtual screening and hit-to-lead optimization.
AID684969Inhibition of CK1delta2012European journal of medicinal chemistry, Oct, Volume: 56Discovery of N6-phenyl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors using common-feature pharmacophore model based virtual screening and hit-to-lead optimization.
AID711107Binding affinity to human CK1epsilon F55I mutant assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID711105Binding affinity to human CK1epsilon K69R mutant assessed as change in melting temperature by differential scanning fluorimetry2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID1337183Inhibition of human full length CK1delta1 (2 to 415 residues) using PLSRTLpSVASLPGL as substrate after 2 hrs by kinase-glo assay2017Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
Non-kinase targets of protein kinase inhibitors.
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.
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.
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.
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.
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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
AID1345666Human casein kinase 1 epsilon (Casein kinase 1 (CK1) family)2009The Journal of pharmacology and experimental therapeutics, Aug, Volume: 330, Issue:2
Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.
AID1345629Human casein kinase 1 delta (Casein kinase 1 (CK1) family)2009The Journal of pharmacology and experimental therapeutics, Aug, Volume: 330, Issue:2
Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (10.00)29.6817
2010's6 (60.00)24.3611
2020's3 (30.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.59

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 Index25.59 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index5.62 (4.65)
Search Engine Demand Index17.79 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]