Page last updated: 2024-11-11

sch 527123

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID9865554
CHEMBL ID216981
SCHEMBL ID184744
MeSH IDM0506183

Synonyms (28)

Synonym
HY-10198
SCH 527123,CAS:473727-83-2
sch-527123
navarixin
(r)-2-hydroxy-n,n-dimethyl-3-(2-(1-(5-methylfuran-2-yl)propylamino)-3,4-dioxocyclobut-1-enylamino)benzamide
2-hydroxy-n,n-dimethyl-3-{2-[[(r)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide
bdbm50200880
sch527123
CHEMBL216981 ,
sch 527123
473727-83-2
(r)-2-hydroxy-n,n-dimethyl-3-((2-((1-(5-methylfuran-2-yl)propyl)amino)-3,4-dioxocyclobut-1-en-1-yl)amino)benzamide
AKOS016003539
CS-0609
S8506
SCHEMBL184744
AC-33600
gtpl8497
2-hydroxy-n,n-dimethyl-3-[[2-[[(1r)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxo-1-cyclobutenyl]amino]benzamide
NCGC00390675-01
2-hydroxy-n,n-dimethyl-3-[[2-[[(1r)-1-(5-methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobuten-1-yl]amino]benzamide
BS-17324
Q27087854
EX-A4879
YTA72783
cxcr2 antagonist iv, sch527123
AT10795
A917603

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity."( Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Aki, C; Baldwin, J; Bian, H; Biju, P; Bond, R; Chao, J; Dwyer, MP; Fan, X; Fine, J; Fossetta, J; Girijavallabhan, V; Gonsiorek, W; Hipkin, RW; Jakway, J; Kaiser, B; Li, G; Lundell, D; Mayer-Ezel, R; Merritt, JR; Ozgur, L; Rindgen, D; Rokosz, LL; Stauffer, T; Taveras, AG; Terminelli, C; Wang, W; Yu, Y, 2006
)
0.77
"A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various fluoroalkyl groups as alpha side chain were prepared and found to show significant improvements in the binding affinities towards both CXCR2 and CXCR1 receptors."( Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
Biju, P; Chao, J; Dwyer, MP; Fan, X; Fine, J; Hipkin, RW; Lundell, D; Rindgen, D; Taveras, AG; Yu, Y, 2009
)
0.35
"A series of potent and orally bioavailable 3,4-diaminocyclobutenediones with various amide modifications and substitution on the left side phenyl ring were prepared and found to show significant inhibitory activities towards both CXCR2 and CXCR1 receptors."( Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Aki, C; Biju, P; Chao, J; Dwyer, MP; Fan, X; Ferreira, JA; Fine, J; Fosseta, J; Gonsiorek, W; Hipkin, RW; Lai, G; Lundell, D; Merritt, RJ; Rindgen, D; Taveras, AG; Wu, M; Yu, Y, 2009
)
0.35
"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 (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.68400.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency2.39190.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency37.90830.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency2.39190.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.39190.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.39190.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.39190.01238.964839.8107AID1645842
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)10.00000.11007.190310.0000AID1449628
Prostaglandin G/H synthase 1Homo sapiens (human)Ki0.00500.00301.37704.0000AID432705
C-X-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)0.10210.00102.022710.0000AID1702400; AID1710068; AID1742061; AID274659; AID274662; AID707880
C-X-C chemokine receptor type 1Homo sapiens (human)Ki0.01900.01800.01900.0200AID307570; AID418196
C-X-C chemokine receptor type 2Homo sapiens (human)IC50 (µMol)0.11830.00000.30296.0130AID1455190; AID1710067; AID274658; AID274662; AID274663; AID707879
C-X-C chemokine receptor type 2Homo sapiens (human)Ki0.00470.00401.05584.2090AID307569; AID418195; AID432705
C-X-C chemokine receptor type 2Mus musculus (house mouse)IC50 (µMol)0.00810.00810.00810.0081AID1455185
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
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)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
dendritic cell chemotaxisC-X-C chemokine receptor type 1Homo sapiens (human)
cell surface receptor signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
receptor internalizationC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8-mediated signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
chemokine-mediated signaling pathwayC-X-C chemokine receptor type 1Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 1Homo sapiens (human)
immune responseC-X-C chemokine receptor type 1Homo sapiens (human)
neutrophil chemotaxisC-X-C chemokine receptor type 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 1Homo sapiens (human)
dendritic cell chemotaxisC-X-C chemokine receptor type 2Homo sapiens (human)
chemotaxisC-X-C chemokine receptor type 2Homo sapiens (human)
inflammatory responseC-X-C chemokine receptor type 2Homo sapiens (human)
cellular defense responseC-X-C chemokine receptor type 2Homo sapiens (human)
signal transductionC-X-C chemokine receptor type 2Homo sapiens (human)
cell surface receptor signaling pathwayC-X-C chemokine receptor type 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayC-X-C chemokine receptor type 2Homo sapiens (human)
positive regulation of cell population proliferationC-X-C chemokine receptor type 2Homo sapiens (human)
neutrophil chemotaxisC-X-C chemokine receptor type 2Homo sapiens (human)
receptor internalizationC-X-C chemokine receptor type 2Homo sapiens (human)
interleukin-8-mediated signaling pathwayC-X-C chemokine receptor type 2Homo sapiens (human)
neutrophil activationC-X-C chemokine receptor type 2Homo sapiens (human)
chemokine-mediated signaling pathwayC-X-C chemokine receptor type 2Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 2Homo sapiens (human)
immune responseC-X-C chemokine receptor type 2Homo 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 (36)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
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)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
interleukin-8 receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
G protein-coupled receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
chemokine receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8 bindingC-X-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 1Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 1Homo sapiens (human)
interleukin-8 receptor activityC-X-C chemokine receptor type 2Homo sapiens (human)
G protein-coupled receptor activityC-X-C chemokine receptor type 2Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 2Homo sapiens (human)
C-X-C chemokine receptor activityC-X-C chemokine receptor type 2Homo sapiens (human)
interleukin-8 bindingC-X-C chemokine receptor type 2Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 2Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 2Homo 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 (35)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
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)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
plasma membraneC-X-C chemokine receptor type 1Homo sapiens (human)
secretory granule membraneC-X-C chemokine receptor type 1Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 1Homo sapiens (human)
nucleoplasmC-X-C chemokine receptor type 2Homo sapiens (human)
plasma membraneC-X-C chemokine receptor type 2Homo sapiens (human)
cell surfaceC-X-C chemokine receptor type 2Homo sapiens (human)
microtubule cytoskeletonC-X-C chemokine receptor type 2Homo sapiens (human)
membraneC-X-C chemokine receptor type 2Homo sapiens (human)
secretory granule membraneC-X-C chemokine receptor type 2Homo sapiens (human)
mast cell granuleC-X-C chemokine receptor type 2Homo sapiens (human)
mitotic spindleC-X-C chemokine receptor type 2Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 2Homo 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 (51)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID307570Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPA2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
AID432705Displacement of human [125I]IL-8 from human CXCR22009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
AID1710097Antimigratory activity in human A-375 cells assessed as reduction in wound closure at 10 uM incubated for 42 hrs by wound healing assay2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Discovery of 1,5-Dihydro-4
AID707908Lipophilicity, log P of the compound2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID314911AUC (0 to 24 hrs) in monkey at 3 mg/kg, po2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID314904Oral bioavailability in rat at 10 mg/kg2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID1528083Antitumor activity against human A375SM cells xenografted in athymic nude mice assessed as reduction in tumor volume at 100 mg/kg, po for 21 days2020European journal of medicinal chemistry, Jan-01, Volume: 185Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead.
AID274666Inhibition of CCR5 receptor at 2 to 20 uM2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID274667Inhibition of C5a-induced human neutrophil chemotaxis2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID418197AUC in po dosed rat2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
AID1710067Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM 2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Discovery of 1,5-Dihydro-4
AID707879Binding affinity to CXCR22012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID314910Mean residence time in monkey at 3 mg/kg, po2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID1742061Antagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins b
AID1811230Cytotoxicity against human Caco2 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists.
AID274659Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID707880Binding affinity to CXCR12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID274660AUC (0-6h) in rat at 10 mg/kg, po2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1455190Antagonist activity at CXCR2 in human whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation preincubated for 15 mins followed by GROalpha stimulation measured after 15 mins by FITC-staining based FACS analysis2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
AID307569Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists.
AID1710069Selectivity index, ratio of IC50 for CXCR1 (unknown origin) expressed in human HEK293 cells to IC50 for CXCR2 (unknown origin) expressed in human HEK293 cells2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Discovery of 1,5-Dihydro-4
AID1702400Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM based fl2020European journal of medicinal chemistry, Feb-01, Volume: 187Structural optimization of aminopyrimidine-based CXCR4 antagonists.
AID314906Mean residence time in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID274663Inhibition of CXCL1-induced human neutrophil chemotaxis2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1455185Antagonist activity at CXCR2 in C57 mouse whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation preincubated for 1 hr followed by GROalpha stimulation measured after 10 mins by FITC-staining based FACS analysis2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
AID1455276Antagonist activity at CXCR2 in C57 mouse whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation at 10 uM preincubated for 1 hr followed by GROalpha stimulation measured after 10 mins by FITC-staining based FACS analysis2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
AID314908Oral bioavailability in monkey at 3 mg/kg2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID1710068Antagonist activity in CXCR1 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM 2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Discovery of 1,5-Dihydro-4
AID1528084Antitumor activity against human A375SM cells xenografted in athymic nude mice assessed as reduction in blood vessels formation at 100 mg/kg, po for 21 days and measured on day 50 by immunohistochemistry relative to control2020European journal of medicinal chemistry, Jan-01, Volume: 185Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead.
AID274665Inhibition of CXCR3 receptor at 2 to 20 uM2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID418196Binding affinity to CXCR12009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
AID314909Half life in monkey at 3 mg/kg, po2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID1710099Antiinvasive activity in human A-375 cells assessed as reduction in invasive number cells at 10 uM incubated for overnight by transwell assay2021ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5
Discovery of 1,5-Dihydro-4
AID274668Inhibition of fMLP-induced human neutrophil chemotaxis2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1173699Antagonist activity at CXCR2 in human whole blood by CD11b assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.
AID274664Inhibition of CXCL1-induced human neutrophil chemotaxis at 2 nM2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID314907AUC (0 to 24 hrs) in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID314905Half life in rat at 10 mg/kg, po2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
AID418195Binding affinity to CXCR22009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
AID274658Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID274662Inhibition of CXCL8-induced human neutrophil chemotaxis2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1346925Human CXCR1 (Chemokine receptors)2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1346925Human CXCR1 (Chemokine receptors)2014Pharmacological reviews, , Volume: 66, Issue:1
International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors.
AID1346826Human CXCR2 (Chemokine receptors)2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
AID1346826Human CXCR2 (Chemokine receptors)2014Pharmacological reviews, , Volume: 66, Issue:1
International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (27.78)29.6817
2010's6 (33.33)24.3611
2020's7 (38.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 24.21

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 Index24.21 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.79 (4.65)
Search Engine Demand Index17.79 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]