Page last updated: 2024-11-11

vuf 2274

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Description

VUF 2274: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

5-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-2,2-diphenylpentanenitrile: an inverse agonist of human cytomegalovirus; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID56972186
MeSH IDM0448660
PubMed CID9889700
CHEMBL ID34166
SCHEMBL ID8891715
MeSH IDM0448660

Synonyms (33)

Synonym
bx 513 hydrochloride
193542-65-3
4-(4-chlorophenyl)-4-hydroxy-?,?-diphenyl-1-piperidinepentanenitrile hydrochloride
vuf 2274
1216540-18-9
AKOS024457285
5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylpentanenitrile--hydrogen chloride (1/1)
DTXSID30719335
bx-513 hydrochloride
1-piperidinepentanenitrile,4-(4-chlorophenyl)-4-hydroxy-a,a-diphenyl-,hcl
BCP27909
vuf 2274;vuf2274; bx513 hydrochloride; bx-513 hydrochloride
bx 513 hcl
bx-513
5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylpentanenitrile hydrochloride
AS-57268
bx-513 hcl
5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylpentanenitrile;hydrochloride
bx513hydrochloride
5-[4-(4-chlorophenyl)-4-hydroxy-1-piperidyl]-2,2-diphenyl-pentanenitrile
CHEMBL34166 ,
vuf-2274
1-piperidinepentanenitrile, 4-(4-chlorophenyl)-4-hydroxy-a,a-diphenyl-
L000124
bdbm50027216
5-(4-(4-chlorophenyl)-4-hydroxy-piperidin-1-yl)-2,2-diphenylpentanenitrile
5-[4-(4-chloro-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-pentanenitrile
SCHEMBL8891715
A1-01967
NCGC00378719-01
5-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-2,2-diphenylpentanenitrile
5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylpentanenitrile
berlex compound

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]

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.50920.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency23.91850.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.53550.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency23.91850.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency23.91850.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency23.91850.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency23.91850.01238.964839.8107AID1645842
[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)
C-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)1.05930.00070.20022.5000AID223365; AID52700; AID82371
C-C chemokine receptor type 1Homo sapiens (human)Ki0.05200.00100.03300.0740AID44615
C-C chemokine receptor type 1Mus musculus (house mouse)IC50 (µMol)5.00000.00580.91425.0000AID221355
C-C chemokine receptor type 3Homo sapiens (human)IC50 (µMol)9.00000.00060.60419.0000AID52703
G-protein coupled receptor homolog US28Human herpesvirus 5 strain AD169IC50 (µMol)9.30009.30009.30009.3000AID255096
[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)
G-protein coupled receptor homolog US28Human herpesvirus 5 strain AD169EC50 (µMol)4.09030.35002.59514.5709AID1185299; AID255657
G protein-coupled receptorHuman betaherpesvirus 5EC50 (µMol)10.00000.33000.33060.3311AID1185301
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
D(2) dopamine receptorHomo sapiens (human)Activity2.00000.00970.58492.0000AID616715
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (166)

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)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
temperature homeostasisD(2) dopamine receptorHomo sapiens (human)
response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein phosphorylationD(2) dopamine receptorHomo sapiens (human)
response to amphetamineD(2) dopamine receptorHomo sapiens (human)
nervous system process involved in regulation of systemic arterial blood pressureD(2) dopamine receptorHomo sapiens (human)
regulation of heart rateD(2) dopamine receptorHomo sapiens (human)
regulation of sodium ion transportD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(2) dopamine receptorHomo sapiens (human)
positive regulation of neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
positive regulation of receptor internalizationD(2) dopamine receptorHomo sapiens (human)
autophagyD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
neuron-neuron synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
neuroblast proliferationD(2) dopamine receptorHomo sapiens (human)
axonogenesisD(2) dopamine receptorHomo sapiens (human)
synapse assemblyD(2) dopamine receptorHomo sapiens (human)
sensory perception of smellD(2) dopamine receptorHomo sapiens (human)
long-term memoryD(2) dopamine receptorHomo sapiens (human)
grooming behaviorD(2) dopamine receptorHomo sapiens (human)
locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
adult walking behaviorD(2) dopamine receptorHomo sapiens (human)
protein localizationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell population proliferationD(2) dopamine receptorHomo sapiens (human)
associative learningD(2) dopamine receptorHomo sapiens (human)
visual learningD(2) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(2) dopamine receptorHomo sapiens (human)
response to light stimulusD(2) dopamine receptorHomo sapiens (human)
response to toxic substanceD(2) dopamine receptorHomo sapiens (human)
response to iron ionD(2) dopamine receptorHomo sapiens (human)
response to inactivityD(2) dopamine receptorHomo sapiens (human)
Wnt signaling pathwayD(2) dopamine receptorHomo sapiens (human)
striatum developmentD(2) dopamine receptorHomo sapiens (human)
orbitofrontal cortex developmentD(2) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(2) dopamine receptorHomo sapiens (human)
adenohypophysis developmentD(2) dopamine receptorHomo sapiens (human)
negative regulation of cell migrationD(2) dopamine receptorHomo sapiens (human)
peristalsisD(2) dopamine receptorHomo sapiens (human)
auditory behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of synaptic transmission, GABAergicD(2) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(2) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
response to histamineD(2) dopamine receptorHomo sapiens (human)
response to nicotineD(2) dopamine receptorHomo sapiens (human)
positive regulation of urine volumeD(2) dopamine receptorHomo sapiens (human)
positive regulation of renal sodium excretionD(2) dopamine receptorHomo sapiens (human)
positive regulation of multicellular organism growthD(2) dopamine receptorHomo sapiens (human)
response to cocaineD(2) dopamine receptorHomo sapiens (human)
negative regulation of circadian sleep/wake cycle, sleepD(2) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(2) dopamine receptorHomo sapiens (human)
drinking behaviorD(2) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(2) dopamine receptorHomo sapiens (human)
response to morphineD(2) dopamine receptorHomo sapiens (human)
pigmentationD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(2) dopamine receptorHomo sapiens (human)
negative regulation of innate immune responseD(2) dopamine receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IID(2) dopamine receptorHomo sapiens (human)
negative regulation of insulin secretionD(2) dopamine receptorHomo sapiens (human)
acid secretionD(2) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(2) dopamine receptorHomo sapiens (human)
behavioral response to ethanolD(2) dopamine receptorHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityD(2) dopamine receptorHomo sapiens (human)
response to axon injuryD(2) dopamine receptorHomo sapiens (human)
branching morphogenesis of a nerveD(2) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(2) dopamine receptorHomo sapiens (human)
epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of epithelial cell proliferationD(2) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(2) dopamine receptorHomo sapiens (human)
release of sequestered calcium ion into cytosolD(2) dopamine receptorHomo sapiens (human)
dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
positive regulation of dopamine uptake involved in synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
regulation of synapse structural plasticityD(2) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(2) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(2) dopamine receptorHomo sapiens (human)
excitatory postsynaptic potentialD(2) dopamine receptorHomo sapiens (human)
positive regulation of growth hormone secretionD(2) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(2) dopamine receptorHomo sapiens (human)
negative regulation of dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeD(2) dopamine receptorHomo sapiens (human)
regulation of locomotion involved in locomotory behaviorD(2) dopamine receptorHomo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(2) dopamine receptorHomo sapiens (human)
negative regulation of cellular response to hypoxiaD(2) dopamine receptorHomo sapiens (human)
positive regulation of glial cell-derived neurotrophic factor productionD(2) dopamine receptorHomo sapiens (human)
positive regulation of long-term synaptic potentiationD(2) dopamine receptorHomo sapiens (human)
hyaloid vascular plexus regressionD(2) dopamine receptorHomo sapiens (human)
negative regulation of neuron migrationD(2) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(2) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(2) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(2) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(2) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(2) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(2) dopamine receptorHomo sapiens (human)
dendritic cell chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
monocyte chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
calcium ion transportC-C chemokine receptor type 1Homo sapiens (human)
intracellular calcium ion homeostasisC-C chemokine receptor type 1Homo sapiens (human)
exocytosisC-C chemokine receptor type 1Homo sapiens (human)
chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
immune responseC-C chemokine receptor type 1Homo sapiens (human)
cell adhesionC-C chemokine receptor type 1Homo sapiens (human)
cell surface receptor signaling pathwayC-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 1Homo sapiens (human)
cell-cell signalingC-C chemokine receptor type 1Homo sapiens (human)
response to woundingC-C chemokine receptor type 1Homo sapiens (human)
negative regulation of gene expressionC-C chemokine receptor type 1Homo sapiens (human)
cytokine-mediated signaling pathwayC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cell migrationC-C chemokine receptor type 1Homo sapiens (human)
negative regulation of bone mineralizationC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of osteoclast differentiationC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of calcium ion transportC-C chemokine receptor type 1Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of monocyte chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 1Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 1Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 1Homo sapiens (human)
positive regulation of endothelial cell proliferationC-C chemokine receptor type 3Homo sapiens (human)
chemotaxisC-C chemokine receptor type 3Homo sapiens (human)
cellular defense responseC-C chemokine receptor type 3Homo sapiens (human)
cell adhesionC-C chemokine receptor type 3Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayC-C chemokine receptor type 3Homo sapiens (human)
positive regulation of angiogenesisC-C chemokine receptor type 3Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 3Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 3Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 3Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 3Homo sapiens (human)
immune responseC-C chemokine receptor type 3Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 3Homo 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 (32)

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)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(2) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(2) dopamine receptorHomo sapiens (human)
protein bindingD(2) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(2) dopamine receptorHomo sapiens (human)
dopamine bindingD(2) dopamine receptorHomo sapiens (human)
ionotropic glutamate receptor bindingD(2) dopamine receptorHomo sapiens (human)
identical protein bindingD(2) dopamine receptorHomo sapiens (human)
heterocyclic compound bindingD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(2) dopamine receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityC-C chemokine receptor type 1Homo sapiens (human)
chemokine receptor activityC-C chemokine receptor type 1Homo sapiens (human)
protein bindingC-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 1Homo sapiens (human)
chemokine (C-C motif) ligand 7 bindingC-C chemokine receptor type 1Homo sapiens (human)
chemokine (C-C motif) ligand 5 bindingC-C chemokine receptor type 1Homo sapiens (human)
chemokine receptor activityC-C chemokine receptor type 3Homo sapiens (human)
protein bindingC-C chemokine receptor type 3Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 3Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 3Homo 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 (41)

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)
Golgi membraneD(2) dopamine receptorHomo sapiens (human)
acrosomal vesicleD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
ciliumD(2) dopamine receptorHomo sapiens (human)
lateral plasma membraneD(2) dopamine receptorHomo sapiens (human)
endocytic vesicleD(2) dopamine receptorHomo sapiens (human)
axonD(2) dopamine receptorHomo sapiens (human)
dendriteD(2) dopamine receptorHomo sapiens (human)
synaptic vesicle membraneD(2) dopamine receptorHomo sapiens (human)
sperm flagellumD(2) dopamine receptorHomo sapiens (human)
dendritic spineD(2) dopamine receptorHomo sapiens (human)
perikaryonD(2) dopamine receptorHomo sapiens (human)
axon terminusD(2) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(2) dopamine receptorHomo sapiens (human)
ciliary membraneD(2) dopamine receptorHomo sapiens (human)
non-motile ciliumD(2) dopamine receptorHomo sapiens (human)
dopaminergic synapseD(2) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(2) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(2) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(2) dopamine receptorHomo sapiens (human)
presynaptic membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneD(2) dopamine receptorHomo sapiens (human)
plasma membraneC-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 1Homo sapiens (human)
cytoplasmC-C chemokine receptor type 1Homo sapiens (human)
plasma membraneC-C chemokine receptor type 3Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 3Homo sapiens (human)
cytoplasmC-C chemokine receptor type 3Homo 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 (30)

Assay IDTitleYearJournalArticle
AID616715Binding affinity to dopamine D2L receptor2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Identification of novel allosteric modulators for the G-protein coupled US28 receptor of human cytomegalovirus.
AID1185301Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
AID458777Activity at HCMV US28 receptor assessed as receptor-mediated inositol phosphate response2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.
AID1185302Allosteric modulatory activity at FLAG-tagged human cytomegalovirus US28 receptor delta300 mutant expressed in HEK293T cells by PathDetectElk1 assay relative to basal level2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
AID1360732Modulation of basal activity of HCMV US28 expressed in tetracyclin-induced HEK293 cells assessed as change in inositol phosphate accumulation at 10 uM using [3H]-myo-inositol by scintillation proximity assay relative to control2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID1360734Displacement of [125I]-CCL2 from HCMV US28 expressed in HEK293 cells at 10 uM after 3 hrs by gamma counting method relative to control2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID52703Inhibitory activity against recombinant human Chemokine receptor type 3 (CCR3) expressed in chinese hamster ovary cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.
AID1185299Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
AID616711Inverse agonist activity at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by luciferase reporter gene assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Identification of novel allosteric modulators for the G-protein coupled US28 receptor of human cytomegalovirus.
AID52700Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Discovery and structure-activity relationship of N-(ureidoalkyl)-benzyl-piperidines as potent small molecule CC chemokine receptor-3 (CCR3) antagonists.
AID221355Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Design, synthesis, and discovery of a novel CCR1 antagonist.
AID1185300Allosteric modulatory activity at FLAG-tagged wild type human cytomegalovirus US28 receptor expressed in HEK293T cells by PathDetectElk1 assay relative to basal level2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
AID82371Inhibition of MIP-1-alpha-induced intracellular calcium mobilization in HEK293 cells expressing human CCR1 receptor1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
Discovery of novel non-peptide CCR1 receptor antagonists.
AID616714Efficacy at HCMV TB40/E US28 expressed in human HEK cells assessed as Elk-1 activation preincubated for 1 hrs measured after 20 to 24 hrs by PathDetect trans Elk-1 reporter gene assay relative to control2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Identification of novel allosteric modulators for the G-protein coupled US28 receptor of human cytomegalovirus.
AID1360735Displacement of [125I]-CCL4 from HCMV US28 expressed in HEK293 cells at 10 uM after 3 hrs by gamma counting method relative to control2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID1360731Modulation of basal activity of HCMV US28 expressed in tetracyclin-induced HEK293 cells assessed as change in inositol phosphate accumulation using [3H]-myo-inositol by scintillation proximity assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID458776Displacement of [125I]CCL5 from HCMV US28 receptor2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.
AID44615Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
Discovery of novel non-peptide CCR1 receptor antagonists.
AID1360733Displacement of [125I]-CX3CL1 from HCMV US28 expressed in HEK293 cells at 10 uM after 3 hrs by gamma counting method relative to control2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID223365Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Design, synthesis, and discovery of a novel CCR1 antagonist.
AID255657Effective concentration against US28-mediated inositol phosphate production in COS-7 cells2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.
AID255096Inhibitory concentration against chemokine receptor US28 expressed in COS-7 cells using [125I]-CCL52005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28.
AID1360738Modulation of basal activity of HCMV US28 delta300 mutant expressed in tetracyclin-induced HEK293 cells assessed as change in inositol phosphate accumulation using [3H]-myo-inositol by scintillation proximity assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID1360729Inverse agonist activity at HCMV US28 expressed in African green monkey COS7 cells assessed as inhibition of inositol phosphate accumulation using [3H]-myo-inositol by liquid scintillation counting method2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
AID1360739Modulation of basal activity of HCMV US28 delta300 mutant expressed in tetracyclin-induced HEK293 cells assessed as change in inositol phosphate accumulation at 10 uM using [3H]-myo-inositol by scintillation proximity assay relative to control2018European journal of medicinal chemistry, Jul-15, Volume: 155Ligand-selective small molecule modulators of the constitutively active vGPCR US28.
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.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (6.67)18.2507
2000's4 (26.67)29.6817
2010's8 (53.33)24.3611
2020's2 (13.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]