Page last updated: 2024-12-10

nih-12848

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Description

NIH-12848: inhibits phosphatidylinositol 5-phosphate 4-kinase gamma; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3235425
CHEMBL ID1529478
MeSH IDM000604708

Synonyms (23)

Synonym
NCGC00012848-02 ,
pcop-954689
NCGC00012848 ,
n-(thiophen-2-ylmethyl)-2-[2-(trifluoromethyl)phenyl]quinazolin-4-amine
S6529
n-(thiophen-2-ylmethyl)-2-(2-(trifluoromethyl)phenyl)quinazolin-4-amine
CHEMBL1529478 ,
959551-10-1
HY-101423
CS-6339
nih-12848
AKOS032960439
BCP20771
Z2017670862
bdbm50497347
nih 12848
nih12848
N16798
A902764
EX-A4544
MS-26352
n-[(thiophen-2-yl)methyl]-2-[2-(trifluoromethyl)phenyl]quinazolin-4-amine
EN300-246566

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule."( Highly predictive and interpretable models for PAMPA permeability.
Jadhav, A; Kerns, E; Nguyen, K; Shah, P; Sun, H; Xu, X; Yan, Z; Yu, KR, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (33)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID2517
USP1 protein, partialHomo sapiens (human)Potency7.94330.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency25.92900.000811.382244.6684AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency0.15850.001318.074339.8107AID926; AID938
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency25.11890.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency7.94330.00255.840031.6228AID899
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency5.01190.65619.452025.1189AID927
DNA polymerase kappa isoform 1Homo sapiens (human)Potency39.81070.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency3.98110.031610.279239.8107AID884; AID885
lamin isoform A-delta10Homo sapiens (human)Potency25.11890.891312.067628.1838AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency5.01191.584913.004325.1189AID927
GABA theta subunitRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency3.98111.000012.224831.6228AID885
[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)
Ubiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)IC50 (µMol)7.90002.00005.61258.0000AID1164708
WD repeat-containing protein 48Homo sapiens (human)IC50 (µMol)7.90002.00006.31678.0000AID1164708
Phosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)IC50 (µMol)1.50001.00001.50002.0000AID1547850; AID1823115
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (69)

Processvia Protein(s)Taxonomy
skeletal system developmentUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
DNA repairUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
regulation of DNA repairUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
proteolysisUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
response to UVUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
protein deubiquitinationUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
monoubiquitinated protein deubiquitinationUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
positive regulation of error-prone translesion synthesisUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
regulation of autophagyPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
megakaryocyte developmentPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
autophagosome-lysosome fusionPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
vesicle-mediated cholesterol transportPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
positive regulation of autophagosome assemblyPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
cell surface receptor signaling pathwayPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
regulation of autophagyPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
autophagosome-lysosome fusionPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
positive regulation of autophagosome assemblyPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
DNA damage responseWD repeat-containing protein 48Homo sapiens (human)
spermatogenesisWD repeat-containing protein 48Homo sapiens (human)
single fertilizationWD repeat-containing protein 48Homo sapiens (human)
multicellular organism growthWD repeat-containing protein 48Homo sapiens (human)
skin developmentWD repeat-containing protein 48Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATWD repeat-containing protein 48Homo sapiens (human)
embryonic organ developmentWD repeat-containing protein 48Homo sapiens (human)
skeletal system morphogenesisWD repeat-containing protein 48Homo sapiens (human)
homeostasis of number of cellsWD repeat-containing protein 48Homo sapiens (human)
positive regulation of epithelial cell proliferationWD repeat-containing protein 48Homo sapiens (human)
seminiferous tubule developmentWD repeat-containing protein 48Homo sapiens (human)
regulation of protein monoubiquitinationWD repeat-containing protein 48Homo sapiens (human)
positive regulation of double-strand break repair via homologous recombinationWD repeat-containing protein 48Homo sapiens (human)
double-strand break repair via homologous recombinationWD repeat-containing protein 48Homo sapiens (human)
regulation of autophagyPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
negative regulation of insulin receptor signaling pathwayPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
positive regulation of autophagosome assemblyPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
cysteine-type deubiquitinase activityUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
protein bindingUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
peptidase activityUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
protein bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
ATP bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 5-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
1-phosphatidylinositol-5-phosphate 4-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
protein homodimerization activityPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
protein bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
ATP bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
GTP bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 5-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
protein homodimerization activityPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
1-phosphatidylinositol-5-phosphate 4-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
DNA bindingWD repeat-containing protein 48Homo sapiens (human)
double-stranded DNA bindingWD repeat-containing protein 48Homo sapiens (human)
single-stranded DNA bindingWD repeat-containing protein 48Homo sapiens (human)
protein bindingWD repeat-containing protein 48Homo sapiens (human)
deubiquitinase activator activityWD repeat-containing protein 48Homo sapiens (human)
ubiquitin bindingWD repeat-containing protein 48Homo sapiens (human)
protein bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
ATP bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 5-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
identical protein bindingPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
1-phosphatidylinositol-5-phosphate 4-kinase activityPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
nucleusUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
nucleoplasmUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
nucleusUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
cytosolUbiquitin carboxyl-terminal hydrolase 1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
photoreceptor outer segmentPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
photoreceptor inner segmentPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
nucleoplasmPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
lysosomePhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
autophagosomePhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
cytosolPhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 alphaHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
nucleusPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
nucleoplasmPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
autophagosomePhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
endoplasmic reticulum membranePhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
cytosolPhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 betaHomo sapiens (human)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmWD repeat-containing protein 48Homo sapiens (human)
nucleusWD repeat-containing protein 48Homo sapiens (human)
nucleoplasmWD repeat-containing protein 48Homo sapiens (human)
lysosomeWD repeat-containing protein 48Homo sapiens (human)
late endosomeWD repeat-containing protein 48Homo sapiens (human)
cytosolWD repeat-containing protein 48Homo sapiens (human)
intracellular membrane-bounded organelleWD repeat-containing protein 48Homo sapiens (human)
nucleoplasmPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
autophagosomePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
endoplasmic reticulumPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
cytosolPhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
intracellular organellePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
extracellular exosomePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
plasma membranePhosphatidylinositol 5-phosphate 4-kinase type-2 gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID1164710Inhibition of human USP1/UAF1 in human HT1299 cells assessed as increase in Ub-PCNA measured after 4 hrs by Western blotting analysis2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.
AID1823102Inhibition of PI5P4Kalpha (unknown origin) by ADP-Glo assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823115Inhibition of GST-fused human recombinant PI5P4Kgamma expressed in Escherichia coli BL21 (DE3) using dipalmitoyl-PI5P and [gamma-32P]ATP as substrate incubated for 10 to 60 mins by radiometric 32P-ATP/PI5P incorporation assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823103Binding affinity to PI5P4Kgamma (unknown origin) assessed as change in melting temperature at 63 uM by thermal shift assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823100Inhibition of PI5P4Kbeta (unknown origin) by ADP-Glo assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823105Apparent permeability across apical to basolateral side in human Caco-2 cells at 10 uM after 60 mins by mass spectrometry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1164708Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assay2014Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.
AID1823107Kinetic solubility of the compound measured after 2 hrs by LC-UV analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823106Efflux ratio of apparent permeability from basolateral to apical side over apical to basolateral side in human Caco-2 cells at 10 uM after 60 mins by mass spectrometry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1547850Inhibition of PI5P4Kgamma (unknown origin)2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.
AID1823099Inhibition of GST-fused recombinant human PI5P4Kgamma harboring insertion of QAR aminoacids at 139/S132L/E133P/S134N/E135D/G136S/D141G/G142A/E156T/N198G/E199G/D200E mutant expressed in Escherichia coli BL21 (DE3) incubated for 60 mins by ADP-Glo assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823101Stability in human liver microsomes assessed as half life at 1 uM in presence of NADPH by mass spectrometry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823108Lipophilicity, logD of the compound at pH 7.4 by HPLC analysis2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823104Protein binding in mouse plasma assessed as bound fraction at 10 uM incubated for 4 hrs by mass spectrometry2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1823114Inhibition of PI5P4Kalpha (unknown origin) incubated for 1 hr by TR-FRET assay2022Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4
Development of Selective Phosphatidylinositol 5-Phosphate 4-Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1645848NCATS Kinetic Aqueous Solubility Profiling2019Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity.
AID1508612NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Highly predictive and interpretable models for PAMPA permeability.
AID1508591NCATS Rat Liver Microsome Stability Profiling2020Scientific reports, 11-26, Volume: 10, Issue:1
Retrospective assessment of rat liver microsomal stability at NCATS: data and QSAR models.
[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's4 (44.44)24.3611
2020's5 (55.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.36

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.36 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.66 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.36)

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]