Page last updated: 2024-12-10

cp 481715

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

Description

quinoxaline-2-carboxylic acid (4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyloctyl)amide: a CCR1 antagonist and NSAID; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311123
CHEMBL ID1628706
SCHEMBL ID995030
MeSH IDM0456678

Synonyms (22)

Synonym
cp-481,715
n-[(2s,3s,5r)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl]quinoxaline-2-carboxamide
cp-481715
CHEMBL1628706 ,
2-quinoxalinecarboxamide, n-((1s,2s,4r)-4-(aminocarbonyl)-1-((3-fluorophenyl)methyl)-2,7-dihydroxy-7-methyloctyl)-
cp 481715
212790-31-3
quinoxaline-2-carboxylic acid (4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyloctyl)amide
x3tda066me ,
unii-x3tda066me
bdbm50398338
n-((1s,2s,4r)-4-(aminocarbonyl)-1-((3-fluorophenyl)methyl)-2,7-dihydroxy-7-methyloctyl)-2-quinoxaline carboxamide
gtpl3497
cp481715
YEQJVHQCUDMXFG-FHZYATBESA-N ,
quinoxaline-2-carboxylic acid [4(r)-carbamoyl-1(s)-(3-fluoro-benzyl)-2(s),7-dihydroxy-7-methyl-octyl]-amide
SCHEMBL995030
DTXSID00175540
Q27076895
AT25906
n-((2s,3s,5r)-5-carbamoyl-1-(3-fluorophenyl)-3,8-dihydroxy-8-methylnonan-2-yl)quinoxaline-2-carboxamide
AKOS040751285

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacodynamic activity of CP-481,715 was detected ex vivo by demonstrating a dose-related and linear increase in the amount of macrophage inflammatory protein-1alpha, CCL3, required to induce CD11b upregulation."( Phase I evaluation of the safety, pharmacokinetics and pharmacodynamics of CP-481,715.
Chow, VF; Clucas, AT; Gladue, RP; Shah, A; Zhang, YD, 2007
)
0.34
"The safety and pharmacokinetic (PK)/pharmacodynamic (PD) profile of the novel CCR1 antagonist CCX354 was evaluated in double-blind, placebo-controlled, single- and multiple-dose phase I studies (1-300 mg/day oral doses)."( Pharmacokinetic and pharmacodynamic evaluation of the novel CCR1 antagonist CCX354 in healthy human subjects: implications for selection of clinical dose.
Bekker, P; Dairaghi, DJ; Ertl, LS; Jaen, JC; Johnson, DA; Miao, S; Pennell, AM; Powers, JP; Schall, TJ; Seitz, LC; Wang, Y; Zeng, Y; Zhang, P, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki1.32300.00000.690210.0000AID707910
C-C chemokine receptor type 1Homo sapiens (human)IC50 (µMol)0.04900.00070.20022.5000AID1573704; AID1573705
C-C chemokine receptor type 1Homo sapiens (human)Ki0.07400.00100.03300.0740AID707909
C-C chemokine receptor type 5Homo sapiens (human)Ki0.06600.00210.23060.8520AID707904
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo 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)
MAPK cascadeC-C chemokine receptor type 5Homo sapiens (human)
dendritic cell chemotaxisC-C chemokine receptor type 5Homo sapiens (human)
calcium ion transportC-C chemokine receptor type 5Homo sapiens (human)
chemotaxisC-C chemokine receptor type 5Homo sapiens (human)
cellular defense responseC-C chemokine receptor type 5Homo sapiens (human)
cell surface receptor signaling pathwayC-C chemokine receptor type 5Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-C chemokine receptor type 5Homo sapiens (human)
cell-cell signalingC-C chemokine receptor type 5Homo sapiens (human)
release of sequestered calcium ion into cytosol by sarcoplasmic reticulumC-C chemokine receptor type 5Homo sapiens (human)
calcium-mediated signalingC-C chemokine receptor type 5Homo sapiens (human)
signalingC-C chemokine receptor type 5Homo sapiens (human)
symbiont entry into host cellC-C chemokine receptor type 5Homo sapiens (human)
chemokine-mediated signaling pathwayC-C chemokine receptor type 5Homo sapiens (human)
response to cholesterolC-C chemokine receptor type 5Homo sapiens (human)
cellular response to lipopolysaccharideC-C chemokine receptor type 5Homo sapiens (human)
negative regulation of macrophage apoptotic processC-C chemokine receptor type 5Homo sapiens (human)
inflammatory responseC-C chemokine receptor type 5Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-C chemokine receptor type 5Homo sapiens (human)
immune responseC-C chemokine receptor type 5Homo sapiens (human)
cell chemotaxisC-C chemokine receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo 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)
virus receptor activityC-C chemokine receptor type 5Homo sapiens (human)
actin bindingC-C chemokine receptor type 5Homo sapiens (human)
phosphatidylinositol phospholipase C activityC-C chemokine receptor type 5Homo sapiens (human)
chemokine receptor activityC-C chemokine receptor type 5Homo sapiens (human)
protein bindingC-C chemokine receptor type 5Homo sapiens (human)
coreceptor activityC-C chemokine receptor type 5Homo sapiens (human)
C-C chemokine receptor activityC-C chemokine receptor type 5Homo sapiens (human)
C-C chemokine bindingC-C chemokine receptor type 5Homo sapiens (human)
identical protein bindingC-C chemokine receptor type 5Homo sapiens (human)
chemokine (C-C motif) ligand 5 bindingC-C chemokine receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo 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)
cell surfaceC-C chemokine receptor type 5Homo sapiens (human)
endosomeC-C chemokine receptor type 5Homo sapiens (human)
plasma membraneC-C chemokine receptor type 5Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 5Homo sapiens (human)
cell surfaceC-C chemokine receptor type 5Homo sapiens (human)
external side of plasma membraneC-C chemokine receptor type 5Homo sapiens (human)
cytoplasmC-C chemokine receptor type 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID707904Binding affinity to CCR52012Journal 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.
AID1573704Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Discovery and optimization of pyrazole amides as antagonists of CCR1.
AID707910Binding affinity to muscarinic M2 receptor2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID1573705Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Discovery and optimization of pyrazole amides as antagonists of CCR1.
AID707909Binding affinity to CCR12012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Chemokine receptor antagonists.
AID1346789Human CCR1 (Chemokine receptors)2003The Journal of biological chemistry, Oct-17, Volume: 278, Issue:42
CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (55.56)29.6817
2010's4 (44.44)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: 11.89

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 Index11.89 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.89)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (33.33%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]