Page last updated: 2024-11-13

unipr129

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

Description

UniPR129: an antiangiogenic agent that disrupts the interaction between EphA2 and ephrin-A1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID91668293
CHEMBL ID3735125
MeSH IDM000608727

Synonyms (10)

Synonym
CHEMBL3735125 ,
1639159-47-9
bdbm50234957
MS-30380
unipr129
HY-123607
CS-0083824
n-(3alpha-hydroxy-5beta-cholan-24-oyl)-l-beta-homotryptophan
EX-A7987
AKOS040747565

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Eph/ephrin system is an emerging target for cancer therapy but the lack of potent, stable and orally bioavailable compounds is impairing the development of the field."( Pharmacological evaluation of new bioavailable small molecules targeting Eph/ephrin interaction.
Ballabeni, V; Barocelli, E; Callegari, D; Chiodelli, P; Corrado, M; Ferlenghi, F; Giorgio, C; Incerti, M; Lodola, A; Rusnati, M; Russo, S; Tognolini, M, 2018
)
0.48
[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)
Ephrin type-A receptor 2Homo sapiens (human)Ki0.40000.40000.40000.4000AID1689866
Ephrin type-A receptor 2Mus musculus (house mouse)IC50 (µMol)0.91100.91000.91100.9120AID1436330
[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)
G-protein coupled bile acid receptor 1Homo sapiens (human)EC50 (µMol)4.00000.02372.52598.9000AID1260972
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
skeletal system developmentEphrin type-A receptor 2Homo sapiens (human)
vasculogenesisEphrin type-A receptor 2Homo sapiens (human)
osteoblast differentiationEphrin type-A receptor 2Homo sapiens (human)
blood vessel endothelial cell proliferation involved in sprouting angiogenesisEphrin type-A receptor 2Homo sapiens (human)
inflammatory responseEphrin type-A receptor 2Homo sapiens (human)
cell adhesionEphrin type-A receptor 2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageEphrin type-A receptor 2Homo sapiens (human)
regulation of lamellipodium assemblyEphrin type-A receptor 2Homo sapiens (human)
notochord formationEphrin type-A receptor 2Homo sapiens (human)
cell migrationEphrin type-A receptor 2Homo sapiens (human)
negative regulation of angiogenesisEphrin type-A receptor 2Homo sapiens (human)
neural tube developmentEphrin type-A receptor 2Homo sapiens (human)
neuron differentiationEphrin type-A receptor 2Homo sapiens (human)
keratinocyte differentiationEphrin type-A receptor 2Homo sapiens (human)
osteoclast differentiationEphrin type-A receptor 2Homo sapiens (human)
positive regulation of cell migrationEphrin type-A receptor 2Homo sapiens (human)
negative regulation of chemokine productionEphrin type-A receptor 2Homo sapiens (human)
mammary gland epithelial cell proliferationEphrin type-A receptor 2Homo sapiens (human)
regulation of cell adhesion mediated by integrinEphrin type-A receptor 2Homo sapiens (human)
post-anal tail morphogenesisEphrin type-A receptor 2Homo sapiens (human)
regulation of blood vessel endothelial cell migrationEphrin type-A receptor 2Homo sapiens (human)
regulation of angiogenesisEphrin type-A receptor 2Homo sapiens (human)
cAMP metabolic processEphrin type-A receptor 2Homo sapiens (human)
symbiont entry into host cellEphrin type-A receptor 2Homo sapiens (human)
bone remodelingEphrin type-A receptor 2Homo sapiens (human)
ephrin receptor signaling pathwayEphrin type-A receptor 2Homo sapiens (human)
axial mesoderm formationEphrin type-A receptor 2Homo sapiens (human)
cell motilityEphrin type-A receptor 2Homo sapiens (human)
defense response to Gram-positive bacteriumEphrin type-A receptor 2Homo sapiens (human)
notochord cell developmentEphrin type-A receptor 2Homo sapiens (human)
cell chemotaxisEphrin type-A receptor 2Homo sapiens (human)
branching involved in mammary gland duct morphogenesisEphrin type-A receptor 2Homo sapiens (human)
lens fiber cell morphogenesisEphrin type-A receptor 2Homo sapiens (human)
regulation of ERK1 and ERK2 cascadeEphrin type-A receptor 2Homo sapiens (human)
response to growth factorEphrin type-A receptor 2Homo sapiens (human)
protein localization to plasma membraneEphrin type-A receptor 2Homo sapiens (human)
activation of GTPase activityEphrin type-A receptor 2Homo sapiens (human)
negative regulation of lymphangiogenesisEphrin type-A receptor 2Homo sapiens (human)
positive regulation of protein localization to plasma membraneEphrin type-A receptor 2Homo sapiens (human)
positive regulation of bicellular tight junction assemblyEphrin type-A receptor 2Homo sapiens (human)
pericyte cell differentiationEphrin type-A receptor 2Homo sapiens (human)
positive regulation of kinase activityEphrin type-A receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEphrin type-A receptor 2Homo sapiens (human)
multicellular organism developmentEphrin type-A receptor 2Homo sapiens (human)
cell surface bile acid receptor signaling pathwayG-protein coupled bile acid receptor 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeG-protein coupled bile acid receptor 1Homo sapiens (human)
cellular response to bile acidG-protein coupled bile acid receptor 1Homo sapiens (human)
positive regulation of cholangiocyte proliferationG-protein coupled bile acid receptor 1Homo sapiens (human)
regulation of bicellular tight junction assemblyG-protein coupled bile acid receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayG-protein coupled bile acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
virus receptor activityEphrin type-A receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEphrin type-A receptor 2Homo sapiens (human)
ephrin receptor activityEphrin type-A receptor 2Homo sapiens (human)
protein bindingEphrin type-A receptor 2Homo sapiens (human)
ATP bindingEphrin type-A receptor 2Homo sapiens (human)
growth factor bindingEphrin type-A receptor 2Homo sapiens (human)
cadherin bindingEphrin type-A receptor 2Homo sapiens (human)
molecular function activator activityEphrin type-A receptor 2Homo sapiens (human)
protein bindingG-protein coupled bile acid receptor 1Homo sapiens (human)
bile acid receptor activityG-protein coupled bile acid receptor 1Homo sapiens (human)
G protein-coupled bile acid receptor activityG-protein coupled bile acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneEphrin type-A receptor 2Homo sapiens (human)
focal adhesionEphrin type-A receptor 2Homo sapiens (human)
cell surfaceEphrin type-A receptor 2Homo sapiens (human)
lamellipodiumEphrin type-A receptor 2Homo sapiens (human)
leading edge membraneEphrin type-A receptor 2Homo sapiens (human)
lamellipodium membraneEphrin type-A receptor 2Homo sapiens (human)
ruffle membraneEphrin type-A receptor 2Homo sapiens (human)
tight junctionEphrin type-A receptor 2Homo sapiens (human)
receptor complexEphrin type-A receptor 2Homo sapiens (human)
plasma membraneEphrin type-A receptor 2Homo sapiens (human)
cytoplasmG-protein coupled bile acid receptor 1Homo sapiens (human)
plasma membraneG-protein coupled bile acid receptor 1Homo sapiens (human)
receptor complexG-protein coupled bile acid receptor 1Homo sapiens (human)
plasma membraneG-protein coupled bile acid receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID1436340Drug uptake in mouse plasma at 30 mg/kg, administered as single dose via oral gavage after 120 hrs by HPLC-ESI-MS/MS analysis2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1436335Half-life in mouse liver microsomes at 1 uM in presence of NADPH by HPLC-ESI-MS/MS analysis2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1260978n-octanol-water distribution coefficient, log D of the compound at pH 7.4 after 4 hrs by shake-flask method2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1260976AUC (0 to t) in mouse at 30 mg/kg, po administered as single dose by HPLC-MS analysis2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1260979Metabolic stability in mouse liver S9 fractions assessed as compound remaining at 1 uM after 1 hr by HPLC-ESI-MS/MS analysis in presence of NADPH regenerating system2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1260975Cmax in mouse at 30 mg/kg, po administered as single dose by HPLC-MS analysis2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1436332n-Octanol-buffer partition co-efficient, log D of the compound at pH 7.4 incubated overnight by shake-flask method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1424429Cmax in mouse at 30 mg/kg, po2017European journal of medicinal chemistry, Dec-15, Volume: 142Targeting Eph/ephrin system in cancer therapy.
AID1436334Stability in mouse plasma assessed as compound remaining at 1 uM after 24 hrs by HPLC-ESI-MS/MS analysis2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1436330Displacement of biotinylated ephrin-A1-Fc from recombinant mouse EphA2 receptor preincubated for 1 hr followed by biotinylated ephrin-A1-Fc addition measured after 4 hrs by ELISA method2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1260977Metabolic stability in mouse plasma assessed as compound remaining at 1 uM after 24 hrs by HPLC-ESI-MS/MS analysis2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1436336Cmax in mouse at 30 mg/kg, administered as single dose via oral gavage by HPLC-ESI-MS/MS analysis2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1260980Kinetic solubility of the compound in NaCl solution at 25 deg C after 2 hrs by HPLC-ESI-MS/MS analysis2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1436329Drug metabolism in mouse liver microsomes assessed as (S)-3-((S)-4-((5R,8R,9S,10S,13R,14S,17R)-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)-4-(1H-indol-3-yl)butanoic acid formation by HPLC-ESI-MS/MS analysis2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
AID1424430Kinetic solubility of the compound2017European journal of medicinal chemistry, Dec-15, Volume: 142Targeting Eph/ephrin system in cancer therapy.
AID1260972Agonist activity at TGR5 (unknown origin) assessed as cAMP level2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1689866Competitive inhibition of biotinylated ephrin-A1-Fc binding to EphA2 (unknown origin)2020European journal of medicinal chemistry, Mar-01, Volume: 189Optimization of EphA2 antagonists based on a lithocholic acid core led to the identification of UniPR505, a new 3α-carbamoyloxy derivative with antiangiogenetic properties.
AID1260973Activation of human recombinant PXR up to 10 uM by alphascreen method2015European journal of medicinal chemistry, Oct-20, Volume: 103Δ(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.
AID1436333Kinetic solubility in MOPS buffer at pH 7.4 measured after 4 hrs by HPLC-ESI-MS/MS analysis2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
Metadynamics for Perspective Drug Design: Computationally Driven Synthesis of New Protein-Protein Interaction Inhibitors Targeting the EphA2 Receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (85.71)24.3611
2020's1 (14.29)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 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]