Page last updated: 2024-11-11

rwj-56110

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Description

RWJ-56110: a PAR-1 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9853822
CHEMBL ID311626
SCHEMBL ID4263176
MeSH IDM0399748

Synonyms (14)

Synonym
bdbm50129481
CHEMBL311626 ,
4-amino-n-benzyl-2-[(s)-2-{3-[1-(2,6-dichloro-benzyl)-3-pyrrolidin-1-ylmethyl-1h-indol-6-yl]-ureido}-3-(3,4-difluoro-phenyl)-propionylamino]-butyramide
rwj56110
rwj-56110
gtpl3525
(2s)-4-amino-2-[[(2s)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]-n-(phenylmethyl)butanamide
SCHEMBL4263176
252889-88-6
Q27088651
HY-108556
CS-0029156
(2s)-4-amino-n-benzyl-2-[[(2s)-2-[[1-[(2,6-dichlorophenyl)methyl]-3-(pyrrolidin-1-ylmethyl)indol-6-yl]carbamoylamino]-3-(3,4-difluorophenyl)propanoyl]amino]butanamide
AKOS040745344
[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)
Proteinase-activated receptor 1Homo sapiens (human)IC50 (µMol)0.44000.00111.006910.0000AID211943
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
connective tissue replacement involved in inflammatory response wound healingProteinase-activated receptor 1Homo sapiens (human)
negative regulation of glomerular filtrationProteinase-activated receptor 1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processProteinase-activated receptor 1Homo sapiens (human)
inflammatory responseProteinase-activated receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProteinase-activated receptor 1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
establishment of synaptic specificity at neuromuscular junctionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cell population proliferationProteinase-activated receptor 1Homo sapiens (human)
negative regulation of cell population proliferationProteinase-activated receptor 1Homo sapiens (human)
response to woundingProteinase-activated receptor 1Homo sapiens (human)
anatomical structure morphogenesisProteinase-activated receptor 1Homo sapiens (human)
platelet activationProteinase-activated receptor 1Homo sapiens (human)
regulation of blood coagulationProteinase-activated receptor 1Homo sapiens (human)
positive regulation of blood coagulationProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cell migrationProteinase-activated receptor 1Homo sapiens (human)
response to lipopolysaccharideProteinase-activated receptor 1Homo sapiens (human)
regulation of interleukin-1 beta productionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of interleukin-6 productionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of interleukin-8 productionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of collagen biosynthetic processProteinase-activated receptor 1Homo sapiens (human)
positive regulation of Rho protein signal transductionProteinase-activated receptor 1Homo sapiens (human)
dendritic cell homeostasisProteinase-activated receptor 1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processProteinase-activated receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeProteinase-activated receptor 1Homo sapiens (human)
negative regulation of neuron apoptotic processProteinase-activated receptor 1Homo sapiens (human)
positive regulation of GTPase activityProteinase-activated receptor 1Homo sapiens (human)
cell-cell junction maintenanceProteinase-activated receptor 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of vasoconstrictionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of smooth muscle contractionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATProteinase-activated receptor 1Homo sapiens (human)
regulation of synaptic plasticityProteinase-activated receptor 1Homo sapiens (human)
homeostasis of number of cells within a tissueProteinase-activated receptor 1Homo sapiens (human)
release of sequestered calcium ion into cytosolProteinase-activated receptor 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolProteinase-activated receptor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProteinase-activated receptor 1Homo sapiens (human)
positive regulation of calcium ion transportProteinase-activated receptor 1Homo sapiens (human)
regulation of sensory perception of painProteinase-activated receptor 1Homo sapiens (human)
platelet dense granule organizationProteinase-activated receptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProteinase-activated receptor 1Homo sapiens (human)
thrombin-activated receptor signaling pathwayProteinase-activated receptor 1Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionProteinase-activated receptor 1Homo sapiens (human)
negative regulation of renin secretion into blood streamProteinase-activated receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
G-protein alpha-subunit bindingProteinase-activated receptor 1Homo sapiens (human)
G protein-coupled receptor activityProteinase-activated receptor 1Homo sapiens (human)
signaling receptor bindingProteinase-activated receptor 1Homo sapiens (human)
protein bindingProteinase-activated receptor 1Homo sapiens (human)
thrombin-activated receptor activityProteinase-activated receptor 1Homo sapiens (human)
G-protein beta-subunit bindingProteinase-activated receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneProteinase-activated receptor 1Homo sapiens (human)
extracellular regionProteinase-activated receptor 1Homo sapiens (human)
early endosomeProteinase-activated receptor 1Homo sapiens (human)
late endosomeProteinase-activated receptor 1Homo sapiens (human)
Golgi apparatusProteinase-activated receptor 1Homo sapiens (human)
plasma membraneProteinase-activated receptor 1Homo sapiens (human)
caveolaProteinase-activated receptor 1Homo sapiens (human)
cell surfaceProteinase-activated receptor 1Homo sapiens (human)
platelet dense tubular networkProteinase-activated receptor 1Homo sapiens (human)
neuromuscular junctionProteinase-activated receptor 1Homo sapiens (human)
postsynaptic membraneProteinase-activated receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID161902Ability to block TRAP-6 (2 uM)-induced platelet aggregation2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.
AID211943Ability to inhibit the binding of [3H]S-(p-F-Phe)-homoarginine-L-homoarginine-KY-NH2 to thrombin receptor on the membranes of CHRF-288-11 cells2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.
AID161908Ability to block thrombin (0.15 nM)-induced platelet aggregation2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.
AID161906Ability to block collagen (3 ug/mL) induced platelet aggregation; inactive at a concentration of 50 uM2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.
AID161903Ability to block U-46,619 (0.3 uM)-induced platelet aggregation; inactive at a concentration of 50 uM2003Bioorganic & medicinal chemistry letters, Jul-07, Volume: 13, Issue:13
High-affinity thrombin receptor (PAR-1) ligands: a new generation of indole-based peptide mimetic antagonists with a basic amine at the C-terminus.
AID1346347Human PAR1 (Proteinase-activated receptors)1999Proceedings of the National Academy of Sciences of the United States of America, Oct-26, Volume: 96, Issue:22
Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (10.00)18.2507
2000's6 (60.00)29.6817
2010's3 (30.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]