Page last updated: 2024-11-10

stx-0119

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

Description

STX-0119: antineoplastic; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4253236
CHEMBL ID1687979
SCHEMBL ID1899809
MeSH IDM0559737

Synonyms (23)

Synonym
AB00669077-01
CHEMBL1687979 ,
stx-0119
tdr77381
bdbm50338991
n-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-2-phenyl-4-quinoline-carboxamide
n-[5-(furan-2-yl)-1,3,4-oxadiazol-2-yl]-2-phenylquinoline-4-carboxamide
SCHEMBL1899809
AKOS015994781
NCGC00345805-01
n-[5-(2-furyl)-1,3,4-oxadiazol-2-yl]-2-phenyl-4-quinolinecarboxamide
MNPXTRXFUMGQLK-UHFFFAOYSA-N ,
851095-32-4
ME-0153
SR-01000007580-1
sr-01000007580
stx0119; stx 0119
BCP25956
n-(5-(furan-2-yl)-1,3,4-oxadiazol-2-yl)-2-phenylquinoline-4-carboxamide
tx-0119
HMS3741I13
HY-103692
CS-0032810

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]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
EWS/FLI fusion proteinHomo sapiens (human)Potency17.48600.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
[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)
Signal transducer and activator of transcription 3Homo sapiens (human)IC50 (µMol)74.00000.02304.13789.9800AID580770
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (76)

Processvia Protein(s)Taxonomy
positive regulation of vascular endothelial growth factor productionSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
temperature homeostasisSignal transducer and activator of transcription 3Homo sapiens (human)
eye photoreceptor cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of DNA-templated transcriptionSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
protein import into nucleusSignal transducer and activator of transcription 3Homo sapiens (human)
inflammatory responseSignal transducer and activator of transcription 3Homo sapiens (human)
signal transductionSignal transducer and activator of transcription 3Homo sapiens (human)
transforming growth factor beta receptor signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATSignal transducer and activator of transcription 3Homo sapiens (human)
nervous system developmentSignal transducer and activator of transcription 3Homo sapiens (human)
cell population proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of cell population proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of autophagySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of gene expressionSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of gene expressionSignal transducer and activator of transcription 3Homo sapiens (human)
phosphorylationSignal transducer and activator of transcription 3Homo sapiens (human)
cytokine-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
sexual reproductionSignal transducer and activator of transcription 3Homo sapiens (human)
cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of cell migrationSignal transducer and activator of transcription 3Homo sapiens (human)
intracellular receptor signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
response to estradiolSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-1 beta productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-10 productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-6 productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-8 productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of tumor necrosis factor productionSignal transducer and activator of transcription 3Homo sapiens (human)
cellular response to hormone stimulusSignal transducer and activator of transcription 3Homo sapiens (human)
leptin-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
somatic stem cell population maintenanceSignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-15-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-2-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-9-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-11-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
regulation of multicellular organism growthSignal transducer and activator of transcription 3Homo sapiens (human)
glucose homeostasisSignal transducer and activator of transcription 3Homo sapiens (human)
eating behaviorSignal transducer and activator of transcription 3Homo sapiens (human)
mRNA transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionSignal transducer and activator of transcription 3Homo sapiens (human)
cellular response to leptin stimulusSignal transducer and activator of transcription 3Homo sapiens (human)
response to leptinSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of erythrocyte differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of Notch signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of angiogenesisSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of glycolytic processSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of DNA-templated transcriptionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
astrocyte differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of inflammatory responseSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySignal transducer and activator of transcription 3Homo sapiens (human)
regulation of cell cycleSignal transducer and activator of transcription 3Homo sapiens (human)
radial glial cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
retinal rod cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of feeding behaviorSignal transducer and activator of transcription 3Homo sapiens (human)
growth hormone receptor signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATSignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-6-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
T-helper 17 type immune responseSignal transducer and activator of transcription 3Homo sapiens (human)
T-helper 17 cell lineage commitmentSignal transducer and activator of transcription 3Homo sapiens (human)
energy homeostasisSignal transducer and activator of transcription 3Homo sapiens (human)
cellular response to interleukin-17Signal transducer and activator of transcription 3Homo sapiens (human)
cell surface receptor signaling pathway via STATSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of inflammatory response to woundingSignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-10-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of miRNA transcriptionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of metalloendopeptidase activitySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of primary miRNA processingSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of stem cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of neuron migrationSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of cell population proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
response to peptide hormoneSignal transducer and activator of transcription 3Homo sapiens (human)
defense responseSignal transducer and activator of transcription 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingSignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificSignal transducer and activator of transcription 3Homo sapiens (human)
DNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription factor activitySignal transducer and activator of transcription 3Homo sapiens (human)
nuclear receptor activitySignal transducer and activator of transcription 3Homo sapiens (human)
signaling receptor bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein kinase bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein phosphatase bindingSignal transducer and activator of transcription 3Homo sapiens (human)
chromatin DNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
signaling adaptor activitySignal transducer and activator of transcription 3Homo sapiens (human)
identical protein bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein homodimerization activitySignal transducer and activator of transcription 3Homo sapiens (human)
protein dimerization activitySignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingSignal transducer and activator of transcription 3Homo sapiens (human)
primary miRNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
lncRNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription factor bindingSignal transducer and activator of transcription 3Homo sapiens (human)
RNA sequestering activitySignal transducer and activator of transcription 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusSignal transducer and activator of transcription 3Homo sapiens (human)
nucleusSignal transducer and activator of transcription 3Homo sapiens (human)
nucleoplasmSignal transducer and activator of transcription 3Homo sapiens (human)
cytoplasmSignal transducer and activator of transcription 3Homo sapiens (human)
cytosolSignal transducer and activator of transcription 3Homo sapiens (human)
plasma membraneSignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II transcription regulator complexSignal transducer and activator of transcription 3Homo sapiens (human)
chromatinSignal transducer and activator of transcription 3Homo sapiens (human)
transcription regulator complexSignal transducer and activator of transcription 3Homo sapiens (human)
cytoplasmSignal transducer and activator of transcription 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (63)

Assay IDTitleYearJournalArticle
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.
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.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1767177Antiproliferative activity against human MGC-803 cells2021European journal of medicinal chemistry, Oct-05, Volume: 221Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
AID1717301Cytotoxicity against human A-375 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTS assay2020European journal of medicinal chemistry, Jan-15, Volume: 186NO-releasing STAT3 inhibitors suppress BRAF-mutant melanoma growth.
AID1767176Antiproliferative activity against human MDA-MB-231 cells2021European journal of medicinal chemistry, Oct-05, Volume: 221Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
AID1717300Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation by MTS assay2020European journal of medicinal chemistry, Jan-15, Volume: 186NO-releasing STAT3 inhibitors suppress BRAF-mutant melanoma growth.
AID580781Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in survivin expression at 20 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580771Inhibition of STAT3 dimerization transfected in HEK293 cells at 50 uM after 24 hrs followed by 1 hr stimulation with 50 ng/ml IL-6 by FRET assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580914Induction of apoptosis in human MDA-MB-453 cells assessed as increase in caspase3/7 activity at 1-100 uM by fluorescence assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580788Toxicity in BALB/cA-v/v nude mouse assessed as increase in body weight relative to control2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID1717299Cytotoxicity against HFF assessed as inhibition of cell proliferation by MTS assay2020European journal of medicinal chemistry, Jan-15, Volume: 186NO-releasing STAT3 inhibitors suppress BRAF-mutant melanoma growth.
AID580913Induction of apoptosis in human MDA-MB-468 cells assessed as increase in caspase3/7 activity at 1-100 uM by fluorescence assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580777Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in cyclin D1 expression at 10 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580778Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in cyclin D1 expression at 20 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID1767291Antitumor activity against patient-derived breast cancer cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 15 mg/kg, iv administered once daily for 20 days2021European journal of medicinal chemistry, Oct-05, Volume: 221Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
AID580783Inhibition of STAT3 DNA binding activity in IL-6 stimulated human MDA-MB-468 cells at 50 uM by transcription factor ELISA2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580787Antitumor activity against human SCC-3 cells xenografted in BALB/cA-v/v nude mouse assessed as decrease in tumor volume at 160 mg/kg, po QD for 4 days measured on 4th day relative to control2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580772Inhibition of STAT3 dimerization transfected in HEK293 cells at 100 uM after 24 hrs followed by 1 hr stimulation with 50 ng/ml IL-6 by FRET assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580775Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in c-myc expression at 20 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580790Plasma concentration in CD1(ICR) mouse at 160 mg/kg, po after 8 hrs by LC-MS analysis2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580769Inhibition of STAT3 transcriptional activity in human HeLa cells at 100 uM by luciferase reporter gene assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580770Inhibition of STAT3 transcriptional activity in human HeLa cells by luciferase reporter gene assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580784Inhibition of STAT1 DNA binding activity in IL-6 stimulated human MDA-MB-468 cells at 50 uM by transcription factor ELISA2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID1767178Antiproliferative activity against human A549 cells2021European journal of medicinal chemistry, Oct-05, Volume: 221Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
AID580789Toxicity in BALB/cA-v/v nude mouse assessed as mortality2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580780Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in survivin expression at 10 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580776Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in c-myc expression at 50 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580785Inhibition of STAT5a DNA binding activity in IL-6 stimulated human MDA-MB-468 cells at 50 uM by transcription factor ELISA2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580786Inhibition of STAT5b DNA binding activity in IL-6 stimulated human MDA-MB-468 cells at 50 uM by transcription factor ELISA2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580773Inhibition of STAT3 in IL-6 stimulated human MDA-MB-468 cells assessed as reduction in amplification of c-myc promoter by CHIP assay2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580774Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in c-myc expression at 10 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580782Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in survivin expression at 50 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID580779Inhibition of STAT3 in human MDA-MB-468 cells assessed as reduction in cyclin D1 expression at 50 uM by Western blotting2010ACS medicinal chemistry letters, Nov-11, Volume: 1, Issue:8
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
AID1767301Toxicity in NOD/SCID mouse xenografted with patient-derived breast cancer cells assessed as change in body weight at 5 to 15 mg/kg, iv administered once daily for 20 days2021European journal of medicinal chemistry, Oct-05, Volume: 221Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (22)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (54.55)24.3611
2020's10 (45.45)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%
Other22 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]