Page last updated: 2024-11-13

gsk1325756

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

Description

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

Cross-References

ID SourceID
PubMed CID24780598
CHEMBL ID3039531
SCHEMBL ID1198688
MeSH IDM0585895

Synonyms (33)

Synonym
CHEMBL3039531
gsk1325756b
gsk-1325756b
gsk-1325756
danirixin
1-(4-chloro-2-hydroxy-3-(((3s)-piperidine-3-sulfonyl)phenyl)-3-(3-fluoro-2-methylphenyl)urea
954126-98-8
gsk1325756
gsk 1325756
unii-r318pgh5vp
danirixin [usan:inn]
r318pgh5vp ,
n-(4-chloro-2-hydroxy-3-(3-piperidinylsulfonyl)phenyl)-n'-(3-fluoro-2-methylphenyl)urea
danirixin (usan/inn)
D10387
(s)-1-(4-chloro-2-hydroxy-3-(piperidin-3-ylsulfonyl)phenyl)-3-(3-fluoro-2-methylphenyl)urea
danirixin [who-dd]
danirixin [usan]
danirixin [inn]
SCHEMBL1198688
1-[4-chloro-2-hydroxy-3-[(3s)-piperidin-3-yl]sulfonylphenyl]-3-(3-fluoro-2-methylphenyl)urea
gtpl8500
HY-19768
CS-5465
EX-A1178
AKOS030527036
mfcd27987922
danirixin (gsk1325756)
DB11922
Q27076980
S6620
urea, n-[4-chloro-2-hydroxy-3-[(3s)-3-piperidinylsulfonyl]phenyl]-n'-(3-fluoro-2-methylphenyl)-
AC-36168

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" There was a 37% decrease in Cmax and a 16% decrease in AUC (0-∞) following administration of danirixin in the presence of food."( The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)--a selective CXCR2 antagonist --in healthy adult subjects.
Bloomer, JC; Carpenter, DC; Connolly, P; Cooray, H; Lazaar, AL; Miller, BE; Mistry, S; Smart, K; Tal-Singer, R, 2015
)
0.66
" This manuscript outlines a nonclinical approach comprising multiple biopharmaceutical, in vitro and physiologically based pharmacokinetic model (PBPK) modelling studies to enable selection of an alternative salt form for danirixin (DNX, GSK1325756), a pharmaceutical agent being developed for chronic obstructive pulmonary disease (COPD)."( Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations.
Ambery, C; Bloomer, JC; Connolly, P; Garden, H; Henley, N; Hodnett, N; Keel, S; Kreindler, JL; Lazaar, AL; Lloyd, RS; Matthews, W; Miller, BE; Yonchuk, J, 2017
)
0.64

Dosage Studied

ExcerptRelevanceReference
" All subjects also received omeprazole 20 mg each morning beginning 4 days prior to the first treatment period and continuing through danirixin dosing in the final treatment period."( The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers.
Ambery, CL; Bloomer, JC; Connolly, P; Lazaar, AL; Miller, BE; Mistry, S; Sanderson, D; Shreeves, T; Smart, K; Smith, R, 2014
)
0.63
" Dosed with normal/high fat food the selected formulation showed comparable exposure and a modest increase in DNX systemic PK was observed with PPI dependent on meal type."( Negative Food Effect of Danirixin: Use of PBPK Modelling to Explore the Effect of Formulation and Meal Type on Clinical PK.
Ambery, C; Bloomer, JC; Butler, JM; Charles, SJ; D'Amico, D; Donald, A; Hingle, MI; Lloyd, RS; Miller, B; Paul, A; Tal-Singer, R; Zhu, X, 2020
)
0.56
[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)30.00000.00102.022710.0000AID1341911
C-X-C chemokine receptor type 2Homo sapiens (human)IC50 (µMol)15.00250.00000.30296.0130AID1341912; AID1341914
[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 (2)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346826Human CXCR2 (Chemokine receptors)2015BMC pharmacology & toxicology, Jun-20, Volume: 16The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)--a selective CXCR2 antagonist --in healthy adult subjects.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's7 (58.33)24.3611
2020's5 (41.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.71

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 Index16.71 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.71)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (66.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (33.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]