Page last updated: 2024-11-13

hg-9-91-01

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Description

HG-9-91-01: inhibits salt-inducible kinases; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

HG-9-91-01 : A member of the class of phenylureas that is a potent inhibitor of salt-inducible kinase 2, a potential target protein for therapy in ovarian cancer. [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 CID78357808
CHEMBL ID4553284
CHEBI ID133818
SCHEMBL ID15271960
MeSH IDM0579940

Synonyms (28)

Synonym
CHEBI:133818
hg-9-91-01
n-(2,4-dimethoxyphenyl)-n'-(2,6-dimethylphenyl)-n-{6-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl}urea
S8393
gtpl8049
1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-[6-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]urea
CS-1749
HY-15776 ,
SCHEMBL15271960
bdbm192712
hg-9-91-01 (1)
1456858-58-4
EX-A1279
AKOS030526556
F20815
NCGC00378591-01
1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)urea
BCP25041
sik inhibitor 1; hg 9-91-01; hg9-91-01; hg99101; hg-99101; hg 99101
Q27077982
1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yl)urea
sik inhibitor 1
A906442
MS-30272
CHEMBL4553284
DTXSID401025699
1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)urea
AC-35525

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 (2)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
salt-inducible kinase 2 inhibitorAny protein kinase inhibitor that interferes with the action of salt-inducible kinase 2.
[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 (6)

ClassDescription
dimethoxybenzeneAny methoxybenzene that consists of a benzene skeleton substituted with two methoxy groups and its derivatives.
aminopyrimidineA member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
N-arylpiperazine
N-alkylpiperazine
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
phenylureasAny member of the class of ureas in which at least one of the nitrogens of the urea moiety is substituted by a phenyl or substituted phenyl group.
[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)Potency3.79080.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency13.45040.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency23.91850.00108.379861.1304AID1645840
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 SIK1Homo sapiens (human)IC50 (µMol)0.92000.00050.17710.9200AID1895085
Serine/threonine-protein kinase SIK2Homo sapiens (human)IC50 (µMol)148.52590.00031.24656.6000AID1801917; AID1895086; AID1895096; AID1895097
Serine/threonine-protein kinase SIK3Homo sapiens (human)IC50 (µMol)9.60000.00102.01349.6000AID1895087
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Interleukin-10Homo sapiens (human)EC50 (µMol)0.22000.22000.22000.2200AID1801918
[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)
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)
regulation of complement-dependent cytotoxicityInterleukin-10Homo sapiens (human)
negative regulation of endothelial cell apoptotic processInterleukin-10Homo sapiens (human)
positive regulation of immunoglobulin productionInterleukin-10Homo sapiens (human)
positive regulation of plasma cell differentiationInterleukin-10Homo sapiens (human)
positive regulation of B cell apoptotic processInterleukin-10Homo sapiens (human)
regulation of gene expressionInterleukin-10Homo sapiens (human)
negative regulation of B cell proliferationInterleukin-10Homo sapiens (human)
positive regulation of signaling receptor activityInterleukin-10Homo sapiens (human)
negative regulation of cytokine productionInterleukin-10Homo sapiens (human)
positive regulation of cytokine productionInterleukin-10Homo sapiens (human)
positive regulation of endothelial cell proliferationInterleukin-10Homo sapiens (human)
response to molecule of bacterial originInterleukin-10Homo sapiens (human)
chronic inflammatory response to antigenic stimulusInterleukin-10Homo sapiens (human)
negative regulation of cytokine production involved in immune responseInterleukin-10Homo sapiens (human)
negative regulation of chronic inflammatory response to antigenic stimulusInterleukin-10Homo sapiens (human)
cytoplasmic sequestering of NF-kappaBInterleukin-10Homo sapiens (human)
negative regulation of cell population proliferationInterleukin-10Homo sapiens (human)
response to xenobiotic stimulusInterleukin-10Homo sapiens (human)
negative regulation of autophagyInterleukin-10Homo sapiens (human)
response to activityInterleukin-10Homo sapiens (human)
response to inactivityInterleukin-10Homo sapiens (human)
hemopoiesisInterleukin-10Homo sapiens (human)
B cell differentiationInterleukin-10Homo sapiens (human)
leukocyte chemotaxisInterleukin-10Homo sapiens (human)
negative regulation of myeloid dendritic cell activationInterleukin-10Homo sapiens (human)
negative regulation of interferon-alpha productionInterleukin-10Homo sapiens (human)
negative regulation of type II interferon productionInterleukin-10Homo sapiens (human)
negative regulation of interleukin-1 productionInterleukin-10Homo sapiens (human)
negative regulation of interleukin-12 productionInterleukin-10Homo sapiens (human)
negative regulation of interleukin-18 productionInterleukin-10Homo sapiens (human)
negative regulation of interleukin-6 productionInterleukin-10Homo sapiens (human)
negative regulation of interleukin-8 productionInterleukin-10Homo sapiens (human)
negative regulation of tumor necrosis factor productionInterleukin-10Homo sapiens (human)
response to insulinInterleukin-10Homo sapiens (human)
negative regulation of heterotypic cell-cell adhesionInterleukin-10Homo sapiens (human)
positive regulation of heterotypic cell-cell adhesionInterleukin-10Homo sapiens (human)
response to carbon monoxideInterleukin-10Homo sapiens (human)
cellular response to hepatocyte growth factor stimulusInterleukin-10Homo sapiens (human)
type 2 immune responseInterleukin-10Homo sapiens (human)
B cell proliferationInterleukin-10Homo sapiens (human)
negative regulation of T cell proliferationInterleukin-10Homo sapiens (human)
defense response to bacteriumInterleukin-10Homo sapiens (human)
defense response to protozoanInterleukin-10Homo sapiens (human)
positive regulation of macrophage activationInterleukin-10Homo sapiens (human)
negative regulation of apoptotic processInterleukin-10Homo sapiens (human)
negative regulation of nitric oxide biosynthetic processInterleukin-10Homo sapiens (human)
regulation of isotype switchingInterleukin-10Homo sapiens (human)
negative regulation of MHC class II biosynthetic processInterleukin-10Homo sapiens (human)
positive regulation of MHC class II biosynthetic processInterleukin-10Homo sapiens (human)
positive regulation of cell cycleInterleukin-10Homo sapiens (human)
positive regulation of DNA-templated transcriptionInterleukin-10Homo sapiens (human)
negative regulation of mitotic cell cycleInterleukin-10Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterleukin-10Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATInterleukin-10Homo sapiens (human)
negative regulation of inflammatory responseInterleukin-10Homo sapiens (human)
regulation of synapse organizationInterleukin-10Homo sapiens (human)
negative regulation of membrane protein ectodomain proteolysisInterleukin-10Homo sapiens (human)
positive regulation of DNA-binding transcription factor activityInterleukin-10Homo sapiens (human)
response to glucocorticoidInterleukin-10Homo sapiens (human)
negative regulation of cytokine activityInterleukin-10Homo sapiens (human)
branching involved in labyrinthine layer morphogenesisInterleukin-10Homo sapiens (human)
cellular response to lipopolysaccharideInterleukin-10Homo sapiens (human)
cellular response to estradiol stimulusInterleukin-10Homo sapiens (human)
negative regulation of chemokine (C-C motif) ligand 5 productionInterleukin-10Homo sapiens (human)
endothelial cell apoptotic processInterleukin-10Homo sapiens (human)
liver regenerationInterleukin-10Homo sapiens (human)
interleukin-10-mediated signaling pathwayInterleukin-10Homo sapiens (human)
positive regulation of miRNA transcriptionInterleukin-10Homo sapiens (human)
regulation of response to woundingInterleukin-10Homo sapiens (human)
negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayInterleukin-10Homo sapiens (human)
positive regulation of sprouting angiogenesisInterleukin-10Homo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationInterleukin-10Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationInterleukin-10Homo sapiens (human)
regulation of sodium ion transportSerine/threonine-protein kinase SIK1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase SIK1Homo sapiens (human)
regulation of mitotic cell cycleSerine/threonine-protein kinase SIK1Homo sapiens (human)
regulation of myotube differentiationSerine/threonine-protein kinase SIK1Homo sapiens (human)
negative regulation of triglyceride biosynthetic processSerine/threonine-protein kinase SIK1Homo sapiens (human)
negative regulation of CREB transcription factor activitySerine/threonine-protein kinase SIK1Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase SIK1Homo sapiens (human)
entrainment of circadian clock by photoperiodSerine/threonine-protein kinase SIK1Homo sapiens (human)
anoikisSerine/threonine-protein kinase SIK1Homo sapiens (human)
regulation of cell differentiationSerine/threonine-protein kinase SIK1Homo sapiens (human)
negative regulation of gluconeogenesisSerine/threonine-protein kinase SIK1Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase SIK1Homo sapiens (human)
rhythmic processSerine/threonine-protein kinase SIK1Homo sapiens (human)
cardiac muscle cell differentiationSerine/threonine-protein kinase SIK1Homo sapiens (human)
positive regulation of anoikisSerine/threonine-protein kinase SIK1Homo 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)
protein phosphorylationSerine/threonine-protein kinase SIK2Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase SIK2Homo sapiens (human)
regulation of insulin receptor signaling pathwaySerine/threonine-protein kinase SIK2Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase SIK2Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase SIK3Homo sapiens (human)
positive regulation of TORC1 signalingSerine/threonine-protein kinase SIK3Homo sapiens (human)
positive regulation of TORC2 signalingSerine/threonine-protein kinase SIK3Homo sapiens (human)
microtubule cytoskeleton organizationSerine/threonine-protein kinase SIK3Homo sapiens (human)
intracellular signal transductionSerine/threonine-protein kinase SIK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

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)
cytokine activityInterleukin-10Homo sapiens (human)
interleukin-10 receptor bindingInterleukin-10Homo sapiens (human)
protein bindingInterleukin-10Homo sapiens (human)
growth factor activityInterleukin-10Homo sapiens (human)
protein dimerization activityInterleukin-10Homo sapiens (human)
magnesium ion bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase SIK1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
cAMP response element binding protein bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
protein kinase bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
histone deacetylase bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
14-3-3 protein bindingSerine/threonine-protein kinase SIK1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase SIK1Homo 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)
magnesium ion bindingSerine/threonine-protein kinase SIK2Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase SIK2Homo sapiens (human)
protein bindingSerine/threonine-protein kinase SIK2Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase SIK2Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase SIK2Homo sapiens (human)
magnesium ion bindingSerine/threonine-protein kinase SIK3Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase SIK3Homo sapiens (human)
protein bindingSerine/threonine-protein kinase SIK3Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase SIK3Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase SIK3Homo sapiens (human)
tau-protein kinase activitySerine/threonine-protein kinase SIK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

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)
extracellular spaceInterleukin-10Homo sapiens (human)
extracellular regionInterleukin-10Homo sapiens (human)
extracellular spaceInterleukin-10Homo sapiens (human)
nucleusSerine/threonine-protein kinase SIK1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase SIK1Homo sapiens (human)
nucleusSerine/threonine-protein kinase SIK1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase SIK1Homo 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)
endoplasmic reticulum membraneSerine/threonine-protein kinase SIK2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase SIK2Homo sapiens (human)
nucleusSerine/threonine-protein kinase SIK2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase SIK2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase SIK3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID1345890Human salt inducible kinase 2 (QIK subfamily)2012Proceedings of the National Academy of Sciences of the United States of America, Oct-16, Volume: 109, Issue:42
Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.
AID1345829Human salt inducible kinase 1 (QIK subfamily)2012Proceedings of the National Academy of Sciences of the United States of America, Oct-16, Volume: 109, Issue:42
Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.
AID1345848Human SIK family kinase 3 (QIK subfamily)2012Proceedings of the National Academy of Sciences of the United States of America, Oct-16, Volume: 109, Issue:42
Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages.
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.
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.
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.
AID1895086Inhibition of GST fused recombinant SIK2 (unknown origin) in human HEK293 cells assessed as effect on CRTC3 phosphorylation at Ser162 incubated for 1 hr in presence of ATP by autoradiography based immunoblotting analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895102Binding affinity to MST4 (unknown origin) assessed as change in melting temperature by thermal shift based DSF assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895099Binding affinity to MST1 (unknown origin) assessed as change in melting temperature by thermal shift based DSF assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895096Inhibition of SIK2 (unknown origin) assessed as enzyme remaining activity by scanMAX kinase assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895097Inhibition of full length N-terminal nanoLuc-tagged human SIK2 expressed in HEK293 cells using NanoBRET NanoGlo substrate incubated for 2 hrs in presence of tracer K10 by NanoBRET assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895085Inhibition of GST fused recombinant SIK1 (unknown origin) in human HEK293 cells assessed as effect on CRTC3 phosphorylation at Ser162 incubated for 1 hr in presence of ATP by autoradiography based immunoblotting analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895103Binding affinity to PAK1 (unknown origin) assessed as change in melting temperature by thermal shift based DSF assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895101Binding affinity to MST3 (unknown origin) assessed as change in melting temperature by thermal shift based DSF assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895087Inhibition of GST fused recombinant SIK3 (unknown origin) in human HEK293 cells assessed as effect on CRTC3 phosphorylation at Ser162 incubated for 1 hr in presence of ATP by autoradiography based immunoblotting analysis2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1895100Binding affinity to MST2 (unknown origin) assessed as change in melting temperature by thermal shift based DSF assay2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors.
AID1801918AlphaLISA-based IL-10 Detection from Article 10.1021/acschembio.6b00217: \\Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.\\2016ACS chemical biology, 08-19, Volume: 11, Issue:8
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.
AID1801917Caliper-based Mobility Shift Assay from Article 10.1021/acschembio.6b00217: \\Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.\\2016ACS chemical biology, 08-19, Volume: 11, Issue:8
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's11 (57.89)24.3611
2020's8 (42.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.30

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 Index23.30 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]