Page last updated: 2024-11-12

sb 656933

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 CID10479502
CHEMBL ID2178579
SCHEMBL ID1562280
MeSH IDM0569469

Synonyms (31)

Synonym
sb-656933-aaf
sb-656933
sb656933
sb 656933
unii-mw2aij8usp
688763-64-6
elubrixin
mw2aij8usp ,
elubrixin [usan:inn]
bdbm50398333
CHEMBL2178579 ,
elubrixin (usan)
D10332
elubrixin [inn]
elubrixin [who-dd]
urea, n-(2-chloro-3-fluorophenyl)-n'-(4-chloro-2-hydroxy-3-(1- piperazinylsulfonyl)phenyl)-
elubrixin [usan]
DTXSID60218962
SCHEMBL1562280
3-(2-chloro-3-fluorophenyl)-1-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea
gtpl8499
elubirixin
DB12135
HY-18263A
Q27077175
CS-0016571
1-(4-chloro-2-hydroxy-3-(piperazin-1-ylsulfonyl)phenyl)-3-(2-chloro-3-fluorophenyl)urea
elubrixin free base
688763-64-6 (free base)
1-(2-chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea
AKOS040733091

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The most frequent adverse event was headache."( Safety and early treatment effects of the CXCR2 antagonist SB-656933 in patients with cystic fibrosis.
Kerem, E; Konstan, MW; Lazaar, AL; Mistry, SJ; Moss, RB; Pilewski, JM; Tal-Singer, R, 2013
)
0.39

Dosage Studied

ExcerptRelevanceReference
" A subsequent randomized study (placebo, 50 mg and 150 mg) was performed to explore the dose-response for ozone-induced airway inflammation, as measured by sputum biomarkers."( SB-656933, a novel CXCR2 selective antagonist, inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans.
Alexis, NE; Chen, C; Lazaar, AL; MacDonald, AJ; Sweeney, LE; Tal-Singer, R, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C-X-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)10.00000.00102.022710.0000AID707880
C-X-C chemokine receptor type 2Homo sapiens (human)IC50 (µMol)0.19210.00000.30296.0130AID707877; AID707878; AID707879
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID707878Antagonist activity at CXCR2 assessed as inhibition of neutrophil CD11b up-regulation2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID707877Antagonist activity at CXCR2 assessed as inhibition of neutrophil shape change2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID707879Binding affinity to CXCR22012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID707908Lipophilicity, log P of the compound2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID707880Binding affinity to CXCR12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
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 (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.31

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 Index12.31 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (33.33%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]