Page last updated: 2024-11-10

sb 290157

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

Description

SB 290157: an anaphylatoxin C3a receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311120
CHEMBL ID389348
SCHEMBL ID1568736
MeSH IDM0394788
PubMed CID24906270
CHEBI ID197424
MeSH IDM0394788

Synonyms (23)

Synonym
sb290157
CHEMBL389348 ,
n2-[(2,2-diphenylethoxy)acetyl]-l-arginine
bdbm50322650
(s)-2-(2-(2,2-diphenylethoxy)acetamido)-5-guanidinopentanoic acid
(2s)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid
sb-290157
(2s)-5-(diaminomethylideneamino)-2-[[2-[2,2-di(phenyl)ethoxy]acetyl]amino]pentanoic acid
gtpl3529
SCHEMBL1568736
AKOS030260728
Q27088720
259218-28-5
STARBLD0022778
(2-(2,2-diphenylethoxy)acetyl)-l-arginine
sb 290157
n(2)-[(2,2-diphenylethoxy)acetyl]-l-arginine trifluoroacetate
n2-[2-(2,2-diphenylethoxy)acetyl]-l-arginine, 2,2,2-trifluoroacetate
n(2)-[2-(2,2-diphenylethoxy)acetyl]-l-arginine trifluoroacetate salt
CHEBI:197424
zjrmppvjaqwgeg-uhfffaoysa-n
5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid;2,2,2-trifluoroacetic acid
HMS3749C21

Research Excerpts

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C3a anaphylatoxin chemotactic receptorHomo sapiens (human)IC50 (µMol)0.76060.00130.76063.9811AID1166388; AID1166389; AID1393258; AID1393259; AID1582628; AID1582636; AID290701; AID491629; AID491630
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (13)

Processvia Protein(s)Taxonomy
calcium-mediated signalingC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
complement receptor mediated signaling pathwayC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
chemotaxisC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
blood circulationC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
positive regulation of macrophage chemotaxisC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
complement component C5a signaling pathwayC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
positive regulation of angiogenesisC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
positive regulation of neutrophil chemotaxisC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
inflammatory responseC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
complement component C3a receptor activityC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
G protein-coupled receptor activityC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
complement component C5a receptor activityC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
azurophil granule membraneC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
specific granule membraneC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
plasma membraneC3a anaphylatoxin chemotactic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay IDTitleYearJournalArticle
AID1582636Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
AID1582626Agonist activity at C3a receptor in human MDM cells assessed as induction of intracellular calcium release measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
AID491631Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release at 10 uM2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Selective hexapeptide agonists and antagonists for human complement C3a receptor.
AID491629Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Selective hexapeptide agonists and antagonists for human complement C3a receptor.
AID1393258Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Chemical Approaches to Modulating Complement-Mediated Diseases.
AID491630Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Selective hexapeptide agonists and antagonists for human complement C3a receptor.
AID1393259Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Chemical Approaches to Modulating Complement-Mediated Diseases.
AID1166395Competitive antagonist activity against C3AR in HMDMs assessed as inhibition of (2-Benzhydryl-4-methyl-1H-imidazole-5-carbonyl)-L-arginine-induced intracellular calcium release by Schild plot2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Potent heterocyclic ligands for human complement c3a receptor.
AID1582628Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
AID491624Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release at 1 mM2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Selective hexapeptide agonists and antagonists for human complement C3a receptor.
AID1166391Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release up to 100 uM by Fluo-3 AM dye based FLIPR assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Potent heterocyclic ligands for human complement c3a receptor.
AID1166389Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Potent heterocyclic ligands for human complement c3a receptor.
AID1166388Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Potent heterocyclic ligands for human complement c3a receptor.
AID290701Inhibition of human C3a receptor expressed on HMC1 cells by SPA assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Discovery of new C3aR ligands. Part 1: arginine derivatives.
AID1582647Antiinflammatory activity in Wistar rat model of BR103-induced paw edema assessed as reduction in hind paw swelling at <30 mg/kg, po administered via gavage pretreated for 2 hrs followed by BR103 challenge and measured after 0.5 to 2 hrs by digital calipe2020Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
AID491623Displacement of [125IC-5a] from C5a receptor in human PBMC at 1 mM by scintillation counting2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Selective hexapeptide agonists and antagonists for human complement C3a receptor.
AID1346363Human C3a receptor (Complement peptide receptors)2001Journal of immunology (Baltimore, Md. : 1950), May-15, Volume: 166, Issue:10
Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (40)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (35.00)29.6817
2010's18 (45.00)24.3611
2020's8 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.74

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 Index17.74 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Reviews3 (8.11%)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 (83.33%)84.16%
Other34 (91.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]