Page last updated: 2024-11-13

EG00229

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

Cross-References

ID SourceID
PubMed CID44631827
CHEMBL ID1078974
CHEBI ID166820
SCHEMBL ID4569813

Synonyms (21)

Synonym
n(2)-({3-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]thiophen-2-yl}carbonyl)-l-arginine
CHEBI:166820
1018927-63-3
eg 00229
eg-00229
n(2)-[[3-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-l-arginine
(s)-2-(3-(benzo[c][1,2,5]thiadiazole-4-sulfonamido)thiophene-2-carboxamido)-5-guanidinopentanoic acid
8dr ,
bdbm50313491
CHEMBL1078974 ,
SCHEMBL4569813
AKOS025142031
n2-[[3-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-l-arginine
eg00229, >=98% (hplc)
NCGC00387214-02
n~2~-({3-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]thiophen-2-yl}carbonyl)-l-arginine
l-arginine, n2-[[3-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-
Q27456878
(2s)-2-[[3-(2,1,3-benzothiadiazol-4-ylsulfonylamino)thiophene-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid
gtpl11335
compound 2 [pmid: 20151671]

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
neuropilin receptor antagonistAn antagonist that binds to and deactivates neuropilin receptors.
angiogenesis inhibitorAn agent and endogenous substances that antagonize or inhibit the development of new blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (6)

ClassDescription
benzothiadiazole
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
thiophenesCompounds containing at least one thiophene ring.
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
L-arginine derivativeA proteinogenic amino acid derivative resulting from reaction of L-arginine at the amino group, the carboxy group, or the guanidyl group, or from the replacement of any hydrogen of L-arginine by a heteroatom.
dicarboxylic acid monoamide
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency26.83700.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency26.83700.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuropilin-1Homo sapiens (human)IC50 (µMol)9.18333.00005.25008.0000AID1650060; AID466773; AID466774; AID466775; AID466776; AID466777
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (122)

Processvia Protein(s)Taxonomy
substrate-dependent cell migration, cell extensionNeuropilin-1Homo sapiens (human)
angiogenesisNeuropilin-1Homo sapiens (human)
branching involved in blood vessel morphogenesisNeuropilin-1Homo sapiens (human)
neuron migrationNeuropilin-1Homo sapiens (human)
positive regulation of endothelial cell proliferationNeuropilin-1Homo sapiens (human)
sprouting angiogenesisNeuropilin-1Homo sapiens (human)
cell migration involved in sprouting angiogenesisNeuropilin-1Homo sapiens (human)
outflow tract septum morphogenesisNeuropilin-1Homo sapiens (human)
signal transductionNeuropilin-1Homo sapiens (human)
integrin-mediated signaling pathwayNeuropilin-1Homo sapiens (human)
cell-cell signalingNeuropilin-1Homo sapiens (human)
axon guidanceNeuropilin-1Homo sapiens (human)
axonal fasciculationNeuropilin-1Homo sapiens (human)
motor neuron axon guidanceNeuropilin-1Homo sapiens (human)
animal organ morphogenesisNeuropilin-1Homo sapiens (human)
positive regulation of endothelial cell migrationNeuropilin-1Homo sapiens (human)
positive regulation of smooth muscle cell migrationNeuropilin-1Homo sapiens (human)
facial nerve structural organizationNeuropilin-1Homo sapiens (human)
trigeminal nerve structural organizationNeuropilin-1Homo sapiens (human)
vestibulocochlear nerve structural organizationNeuropilin-1Homo sapiens (human)
branchiomotor neuron axon guidanceNeuropilin-1Homo sapiens (human)
gonadotrophin-releasing hormone neuronal migration to the hypothalamusNeuropilin-1Homo sapiens (human)
retinal ganglion cell axon guidanceNeuropilin-1Homo sapiens (human)
regulation of Cdc42 protein signal transductionNeuropilin-1Homo sapiens (human)
cellular response to hepatocyte growth factor stimulusNeuropilin-1Homo sapiens (human)
endothelial cell chemotaxisNeuropilin-1Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusNeuropilin-1Homo sapiens (human)
ventral trunk neural crest cell migrationNeuropilin-1Homo sapiens (human)
neuropilin signaling pathwayNeuropilin-1Homo sapiens (human)
VEGF-activated neuropilin signaling pathwayNeuropilin-1Homo sapiens (human)
negative regulation of neuron apoptotic processNeuropilin-1Homo sapiens (human)
positive regulation of angiogenesisNeuropilin-1Homo sapiens (human)
symbiont entry into host cellNeuropilin-1Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayNeuropilin-1Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayNeuropilin-1Homo sapiens (human)
hepatocyte growth factor receptor signaling pathwayNeuropilin-1Homo sapiens (human)
positive regulation of axon extension involved in axon guidanceNeuropilin-1Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceNeuropilin-1Homo sapiens (human)
artery morphogenesisNeuropilin-1Homo sapiens (human)
axon extension involved in axon guidanceNeuropilin-1Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationNeuropilin-1Homo sapiens (human)
positive chemotaxisNeuropilin-1Homo sapiens (human)
positive regulation of filopodium assemblyNeuropilin-1Homo sapiens (human)
positive regulation of stress fiber assemblyNeuropilin-1Homo sapiens (human)
positive regulation of focal adhesion assemblyNeuropilin-1Homo sapiens (human)
axonogenesis involved in innervationNeuropilin-1Homo sapiens (human)
regulation of vesicle-mediated transportNeuropilin-1Homo sapiens (human)
dichotomous subdivision of terminal units involved in salivary gland branchingNeuropilin-1Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisNeuropilin-1Homo sapiens (human)
coronary artery morphogenesisNeuropilin-1Homo sapiens (human)
retina vasculature morphogenesis in camera-type eyeNeuropilin-1Homo sapiens (human)
renal artery morphogenesisNeuropilin-1Homo sapiens (human)
sympathetic ganglion developmentNeuropilin-1Homo sapiens (human)
trigeminal ganglion developmentNeuropilin-1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuropilin-1Homo sapiens (human)
semaphorin-plexin signaling pathwayNeuropilin-1Homo sapiens (human)
commissural neuron axon guidanceNeuropilin-1Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisNeuropilin-1Homo sapiens (human)
endothelial tip cell fate specificationNeuropilin-1Homo sapiens (human)
sensory neuron axon guidanceNeuropilin-1Homo sapiens (human)
motor neuron migrationNeuropilin-1Homo sapiens (human)
sympathetic neuron projection extensionNeuropilin-1Homo sapiens (human)
sympathetic neuron projection guidanceNeuropilin-1Homo sapiens (human)
postsynapse organizationNeuropilin-1Homo sapiens (human)
basal dendrite developmentNeuropilin-1Homo sapiens (human)
basal dendrite arborizationNeuropilin-1Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingNeuropilin-1Homo sapiens (human)
neural crest cell migration involved in autonomic nervous system developmentNeuropilin-1Homo sapiens (human)
protein localization to early endosomeNeuropilin-1Homo sapiens (human)
facioacoustic ganglion developmentNeuropilin-1Homo sapiens (human)
dorsal root ganglion morphogenesisNeuropilin-1Homo sapiens (human)
otic placode developmentNeuropilin-1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayNeuropilin-1Homo sapiens (human)
neural crest cell migrationNeuropilin-1Homo sapiens (human)
regulation of vascular endothelial growth factor receptor signaling pathwayNeuropilin-1Homo sapiens (human)
vasculogenesisNeuropilin-1Homo sapiens (human)
response to woundingNeuropilin-1Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
vascular endothelial growth factor receptor activityNeuropilin-1Homo sapiens (human)
GTPase activator activityNeuropilin-1Homo sapiens (human)
protein bindingNeuropilin-1Homo sapiens (human)
heparin bindingNeuropilin-1Homo sapiens (human)
coreceptor activityNeuropilin-1Homo sapiens (human)
semaphorin receptor activityNeuropilin-1Homo sapiens (human)
growth factor bindingNeuropilin-1Homo sapiens (human)
protein kinase bindingNeuropilin-1Homo sapiens (human)
cytokine bindingNeuropilin-1Homo sapiens (human)
vascular endothelial growth factor bindingNeuropilin-1Homo sapiens (human)
metal ion bindingNeuropilin-1Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
extracellular spaceNeuropilin-1Homo sapiens (human)
early endosomeNeuropilin-1Homo sapiens (human)
cytosolNeuropilin-1Homo sapiens (human)
neurofilamentNeuropilin-1Homo sapiens (human)
plasma membraneNeuropilin-1Homo sapiens (human)
focal adhesionNeuropilin-1Homo sapiens (human)
axonNeuropilin-1Homo sapiens (human)
cytoplasmic vesicleNeuropilin-1Homo sapiens (human)
mitochondrial membraneNeuropilin-1Homo sapiens (human)
neuron projectionNeuropilin-1Homo sapiens (human)
postsynaptic membraneNeuropilin-1Homo sapiens (human)
sorting endosomeNeuropilin-1Homo sapiens (human)
glutamatergic synapseNeuropilin-1Homo sapiens (human)
semaphorin receptor complexNeuropilin-1Homo sapiens (human)
receptor complexNeuropilin-1Homo sapiens (human)
focal adhesionNeuropilin-1Homo sapiens (human)
plasma membraneNeuropilin-1Homo sapiens (human)
axonNeuropilin-1Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
AID466784Inhibition of VEGF-A-induced chemotaxis in HUVEC assessed as reduction in cell migration2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466785Cytotoxicity against human A549 cells after 48 hrs by XTT method2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466781Displacement of biotinylated-VEGF-A125 from human VEGFR2 expressed in human A549 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466780Displacement of biotinylated-VEGF-A125 from human VEGFR1 expressed in human A549 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466778Displacement of biotinylated-VEGF-A125 from human VEGFR1 expressed in human DU145 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466783Inhibition of VEGF-A-induced VEGFR2 phosphorylation in HUVEC at 100 uM by ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466776Displacement of biotinylated-VEGF-A125 from human NRP1 expressed in human DU145 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID1650062Inhibition of recombinant human biotinylated VEGF-165A expressed in HEK293 cells binding to immobilized recombinant full length human FC-tagged NRP1 (chimera active) expressed in HEK293 cells at 11 uM using TMB as substrate incubated for 2 hrs followed by2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification.
AID466774Displacement of biotinylated-VEGF-A125 from NRP1 b1 domain by cell-free assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466773Displacement of [125I]VEGF-A from human NRP1 expressed in pig aortic endothelial cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466772Displacement of [125I]VEGF-A from human NRP1 expressed in pig aortic endothelial cells at 100 uM2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID466782Inhibition of VEGF-A-induced VEGFR2 phosphorylation in HUVEC by ELISA2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID1650065Inhibition of recombinant human biotinylated VEGF-165A expressed in HEK293 cells binding to FC-tagged VEGFR2 (unknown origin) using TMB as substrate incubated for 2 hrs followed by substrate addition by competitive ELISA2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification.
AID466779Displacement of biotinylated-VEGF-A125 from human VEGFR2 expressed in human DU145 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID1369557Half life in mouse at 2.5 mg/kg, iv2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells.
AID466777Displacement of biotinylated-VEGF-A125 from human NRP1 expressed in HUVEC2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID1650060Inhibition of recombinant human biotinylated VEGF-165A expressed in HEK293 cells binding to immobilized recombinant full length human FC-tagged NRP1 (chimera active) expressed in HEK293 cells using TMB as substrate incubated for 2 hrs followed by substrat2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification.
AID466775Displacement of [125I]VEGF-A from human NRP1 expressed in human A549 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (50.00)24.3611
2020's3 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.85

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 Index23.85 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index5.21 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.85)

All Compounds (24.57)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]