Page last updated: 2024-10-14

auy 954

Description

AUY 954: an S1P(1) receptor agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11259583
CHEMBL ID4579553
SCHEMBL ID2237377
MeSH IDM0507006

Synonyms (17)

Synonym
auy954
auy 954
3-[[2-[4-phenyl-3-(trifluoromethyl)phenyl]-1-benzothiophen-5-yl]methylamino]propanoic acid
gtpl2925
3-{[2-(2-trifluoromethyl-biphenyl-4-yl)benzo[b]thiophen-5-ylmethyl]amino}propionic acid
SCHEMBL2237377
bdbm50507187
Q27074628
n-[[2-[2-(trifluoromethyl)[1,1'-biphenyl]-4-yl]benzo[b]thien-5-yl]methyl]-beta-alanine
820240-77-5
BCP33492
nvp-auy954;auy-954;auy 954
820240-77-5 (free base)
3-(((2-(2-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)benzo[b]thiophen-5-yl)methyl)amino)propanoic acid
auy-954 free base
CHEMBL4579553 ,
AKOS040750638

Dosage Studied

ExcerptReference
" A recent provocative report indicated that low dosage of the sphingosine analog FTY720 caused lymphopenia in mice persistently infected with lymphocytic choriomeningitis virus (LCMV)-clone 13 (Cl 13) and induced viral clearance within 30 days post-treatment (Premenko-Lanier et al."( Treatment with a sphingosine analog does not alter the outcome of a persistent virus infection.
Marsolais, D; Oldstone, MB; Rosen, H; Walsh, KB; Welch, MJ, 2010
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sphingosine 1-phosphate receptor 1Homo sapiens (human)EC50 (µMol)0.00120.00000.17597.8700AID1532427
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
blood vessel maturationSphingosine 1-phosphate receptor 1Homo sapiens (human)
cardiac muscle tissue growth involved in heart morphogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell adhesionSphingosine 1-phosphate receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
brain developmentSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell population proliferationSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
transmission of nerve impulseSphingosine 1-phosphate receptor 1Homo sapiens (human)
lamellipodium assemblySphingosine 1-phosphate receptor 1Homo sapiens (human)
actin cytoskeleton organizationSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of cell adhesionSphingosine 1-phosphate receptor 1Homo sapiens (human)
neuron differentiationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of bone mineralizationSphingosine 1-phosphate receptor 1Homo sapiens (human)
leukocyte chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of bone resorptionSphingosine 1-phosphate receptor 1Homo sapiens (human)
endothelial cell differentiationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of positive chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
negative regulation of stress fiber assemblySphingosine 1-phosphate receptor 1Homo sapiens (human)
heart trabecula morphogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
T cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
angiogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
G protein-coupled receptor bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 1Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingolipid bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleoplasmSphingosine 1-phosphate receptor 1Homo sapiens (human)
endosomeSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
external side of plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
intracellular membrane-bounded organelleSphingosine 1-phosphate receptor 1Homo sapiens (human)
membrane raftSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1346185Mouse S1P4 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346234Mouse S1P5 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346190Mouse S1P1 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346142Mouse S1P2 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346199Mouse S1P3 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346242Human S1P5 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346170Human S1P1 receptor (Lysophospholipid (S1P) receptors)2006Chemistry & biology, Nov, Volume: 13, Issue:11
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model.
AID1346199Mouse S1P3 receptor (Lysophospholipid (S1P) receptors)2007Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
AID1532427Activation of human recombinant S1P1 expressed in CHO cell membranes after 120 mins by GTP-gamma-35S-binding assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
An update on sphingosine-1-phosphate receptor 1 modulators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (41.18)29.6817
2010's9 (52.94)24.3611
2020's1 (5.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (94.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]