Page last updated: 2024-12-09

LSM-42773

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

Cross-References

ID SourceID
PubMed CID568763
CHEMBL ID3589013
CHEBI ID131171
SCHEMBL ID7984580

Synonyms (41)

Synonym
OPREA1_783821
OPREA1_175199
9h-indeno[1,2-b][1,2,5]oxadiazolo[3,4-e]pyrazin-9-one
STK120842
AKOS000479457
HMS1607O01
CHEBI:131171
indeno[2,3-b]1,2,5-oxadiazolo[3,4-e]pyrazin-5-one
67200-34-4
smer3
9h-indeno-[1,2-e]-[1,2,5]-oxadiazolo-[3,4-b]-pyrazin-9-one
SCHEMBL7984580
smer 3
9h-indeno[1,2-e][1,2,5]oxadiazolo[3,4-b]pyrazin-9-one
9h-indeno[1,2-b][1,2,5]oxadiazolo[3,4-e]pyrazin-9-one #
indeno[1,2-b]furazano[3,4-e]pyrazin-9-one
indeno[1,2-b]furazano[3,4-e]pyrazin-9-one,
SFSSAKVWCKFRHE-UHFFFAOYSA-N
smer-3
CHEMBL3589013
bdbm188214
us9073941, 28
us9073941, 30
sr-01000388225
SR-01000388225-1
DTXSID40340952
smer3, >=98% (hplc)
smer3(smer 3)
FT-0701471
BCP14360
mfcd00451458
Q27224946
lsm-42773
AS-55891
HY-10949
13-oxa-10,12,14,16-tetrazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(16),2,4,6,9,11,14-heptaen-8-one
EN300-18558227
13-oxa-10,12,14,16-tetraazatetracyclo[7.7.0.0^{2,7}.0^{11,15}]hexadeca-1(16),2,4,6,9,11,14-heptaen-8-one
CS-0002970
E98654
Z2739880762
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Catenin beta-1Homo sapiens (human)Ki310.00003.00005.05936.3340AID1233174
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (152)

Processvia Protein(s)Taxonomy
positive regulation of telomere maintenance via telomeraseCatenin beta-1Homo sapiens (human)
negative regulation of apoptotic processCatenin beta-1Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionCatenin beta-1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICatenin beta-1Homo sapiens (human)
MAPK cascadeCatenin beta-1Homo sapiens (human)
protein polyubiquitinationCatenin beta-1Homo sapiens (human)
embryonic axis specificationCatenin beta-1Homo sapiens (human)
branching involved in blood vessel morphogenesisCatenin beta-1Homo sapiens (human)
osteoblast differentiationCatenin beta-1Homo sapiens (human)
branching involved in ureteric bud morphogenesisCatenin beta-1Homo sapiens (human)
in utero embryonic developmentCatenin beta-1Homo sapiens (human)
gastrulation with mouth forming secondCatenin beta-1Homo sapiens (human)
cell fate specificationCatenin beta-1Homo sapiens (human)
endodermal cell fate commitmentCatenin beta-1Homo sapiens (human)
neuron migrationCatenin beta-1Homo sapiens (human)
epithelial to mesenchymal transitionCatenin beta-1Homo sapiens (human)
neural plate developmentCatenin beta-1Homo sapiens (human)
positive regulation of neuroblast proliferationCatenin beta-1Homo sapiens (human)
positive regulation of mesenchymal cell proliferationCatenin beta-1Homo sapiens (human)
chondrocyte differentiationCatenin beta-1Homo sapiens (human)
lens morphogenesis in camera-type eyeCatenin beta-1Homo sapiens (human)
outflow tract morphogenesisCatenin beta-1Homo sapiens (human)
regulation of secondary heart field cardioblast proliferationCatenin beta-1Homo sapiens (human)
metanephros morphogenesisCatenin beta-1Homo sapiens (human)
negative regulation of mesenchymal to epithelial transition involved in metanephros morphogenesisCatenin beta-1Homo sapiens (human)
transcription by RNA polymerase IICatenin beta-1Homo sapiens (human)
cell adhesionCatenin beta-1Homo sapiens (human)
cell-matrix adhesionCatenin beta-1Homo sapiens (human)
chemical synaptic transmissionCatenin beta-1Homo sapiens (human)
ectoderm developmentCatenin beta-1Homo sapiens (human)
glial cell fate determinationCatenin beta-1Homo sapiens (human)
neuroblast proliferationCatenin beta-1Homo sapiens (human)
positive regulation of cell population proliferationCatenin beta-1Homo sapiens (human)
negative regulation of cell population proliferationCatenin beta-1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayCatenin beta-1Homo sapiens (human)
response to xenobiotic stimulusCatenin beta-1Homo sapiens (human)
anterior/posterior axis specificationCatenin beta-1Homo sapiens (human)
dorsal/ventral axis specificationCatenin beta-1Homo sapiens (human)
proximal/distal pattern formationCatenin beta-1Homo sapiens (human)
positive regulation of gene expressionCatenin beta-1Homo sapiens (human)
negative regulation of gene expressionCatenin beta-1Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionCatenin beta-1Homo sapiens (human)
positive regulation of heparan sulfate proteoglycan biosynthetic processCatenin beta-1Homo sapiens (human)
negative regulation of angiogenesisCatenin beta-1Homo sapiens (human)
stem cell population maintenanceCatenin beta-1Homo sapiens (human)
layer formation in cerebral cortexCatenin beta-1Homo sapiens (human)
hypothalamus developmentCatenin beta-1Homo sapiens (human)
central nervous system vasculogenesisCatenin beta-1Homo sapiens (human)
osteoclast differentiationCatenin beta-1Homo sapiens (human)
male genitalia developmentCatenin beta-1Homo sapiens (human)
hindbrain developmentCatenin beta-1Homo sapiens (human)
regulation of centriole-centriole cohesionCatenin beta-1Homo sapiens (human)
pancreas developmentCatenin beta-1Homo sapiens (human)
hair follicle morphogenesisCatenin beta-1Homo sapiens (human)
regulation of protein ubiquitinationCatenin beta-1Homo sapiens (human)
regulation of myelinationCatenin beta-1Homo sapiens (human)
negative regulation of chondrocyte differentiationCatenin beta-1Homo sapiens (human)
response to estradiolCatenin beta-1Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICatenin beta-1Homo sapiens (human)
T cell differentiation in thymusCatenin beta-1Homo sapiens (human)
negative regulation of protein sumoylationCatenin beta-1Homo sapiens (human)
adherens junction assemblyCatenin beta-1Homo sapiens (human)
protein localization to cell surfaceCatenin beta-1Homo sapiens (human)
embryonic heart tube developmentCatenin beta-1Homo sapiens (human)
genitalia morphogenesisCatenin beta-1Homo sapiens (human)
embryonic forelimb morphogenesisCatenin beta-1Homo sapiens (human)
embryonic hindlimb morphogenesisCatenin beta-1Homo sapiens (human)
hair cell differentiationCatenin beta-1Homo sapiens (human)
detection of muscle stretchCatenin beta-1Homo sapiens (human)
embryonic skeletal limb joint morphogenesisCatenin beta-1Homo sapiens (human)
astrocyte-dopaminergic neuron signalingCatenin beta-1Homo sapiens (human)
regulation of T cell proliferationCatenin beta-1Homo sapiens (human)
odontogenesis of dentin-containing toothCatenin beta-1Homo sapiens (human)
embryonic digit morphogenesisCatenin beta-1Homo sapiens (human)
positive regulation of apoptotic processCatenin beta-1Homo sapiens (human)
negative regulation of apoptotic processCatenin beta-1Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processCatenin beta-1Homo sapiens (human)
positive regulation of MAPK cascadeCatenin beta-1Homo sapiens (human)
positive regulation of neuron apoptotic processCatenin beta-1Homo sapiens (human)
canonical Wnt signaling pathway involved in mesenchymal stem cell differentiationCatenin beta-1Homo sapiens (human)
bone resorptionCatenin beta-1Homo sapiens (human)
positive regulation of cell differentiationCatenin beta-1Homo sapiens (human)
positive regulation of endothelial cell differentiationCatenin beta-1Homo sapiens (human)
positive regulation of osteoblast differentiationCatenin beta-1Homo sapiens (human)
negative regulation of osteoclast differentiationCatenin beta-1Homo sapiens (human)
positive regulation of fibroblast growth factor receptor signaling pathwayCatenin beta-1Homo sapiens (human)
regulation of angiogenesisCatenin beta-1Homo sapiens (human)
negative regulation of DNA-templated transcriptionCatenin beta-1Homo sapiens (human)
positive regulation of DNA-templated transcriptionCatenin beta-1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICatenin beta-1Homo sapiens (human)
negative regulation of mitotic cell cycle, embryonicCatenin beta-1Homo sapiens (human)
regulation of fibroblast proliferationCatenin beta-1Homo sapiens (human)
cell maturationCatenin beta-1Homo sapiens (human)
synaptic vesicle transportCatenin beta-1Homo sapiens (human)
thymus developmentCatenin beta-1Homo sapiens (human)
oocyte developmentCatenin beta-1Homo sapiens (human)
embryonic foregut morphogenesisCatenin beta-1Homo sapiens (human)
positive regulation of skeletal muscle tissue developmentCatenin beta-1Homo sapiens (human)
regulation of smooth muscle cell proliferationCatenin beta-1Homo sapiens (human)
neuron fate determinationCatenin beta-1Homo sapiens (human)
oligodendrocyte differentiationCatenin beta-1Homo sapiens (human)
negative regulation of oligodendrocyte differentiationCatenin beta-1Homo sapiens (human)
regulation of neurogenesisCatenin beta-1Homo sapiens (human)
synapse organizationCatenin beta-1Homo sapiens (human)
smooth muscle cell differentiationCatenin beta-1Homo sapiens (human)
myoblast proliferationCatenin beta-1Homo sapiens (human)
regulation of timing of anagenCatenin beta-1Homo sapiens (human)
regulation of synapse assemblyCatenin beta-1Homo sapiens (human)
oviduct developmentCatenin beta-1Homo sapiens (human)
canonical Wnt signaling pathwayCatenin beta-1Homo sapiens (human)
trachea formationCatenin beta-1Homo sapiens (human)
epithelial tube branching involved in lung morphogenesisCatenin beta-1Homo sapiens (human)
lung-associated mesenchyme developmentCatenin beta-1Homo sapiens (human)
lung epithelial cell differentiationCatenin beta-1Homo sapiens (human)
lung inductionCatenin beta-1Homo sapiens (human)
epithelial cell differentiation involved in prostate gland developmentCatenin beta-1Homo sapiens (human)
epithelial cell proliferation involved in prostate gland developmentCatenin beta-1Homo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland developmentCatenin beta-1Homo sapiens (human)
hair follicle placode formationCatenin beta-1Homo sapiens (human)
establishment of blood-brain barrierCatenin beta-1Homo sapiens (human)
mesenchymal cell proliferation involved in lung developmentCatenin beta-1Homo sapiens (human)
positive regulation of branching involved in lung morphogenesisCatenin beta-1Homo sapiens (human)
endothelial tube morphogenesisCatenin beta-1Homo sapiens (human)
fungiform papilla formationCatenin beta-1Homo sapiens (human)
sympathetic ganglion developmentCatenin beta-1Homo sapiens (human)
cranial ganglion developmentCatenin beta-1Homo sapiens (human)
regulation of centromeric sister chromatid cohesionCatenin beta-1Homo sapiens (human)
cellular response to growth factor stimulusCatenin beta-1Homo sapiens (human)
cellular response to indole-3-methanolCatenin beta-1Homo sapiens (human)
renal vesicle formationCatenin beta-1Homo sapiens (human)
renal inner medulla developmentCatenin beta-1Homo sapiens (human)
renal outer medulla developmentCatenin beta-1Homo sapiens (human)
nephron tubule formationCatenin beta-1Homo sapiens (human)
stem cell proliferationCatenin beta-1Homo sapiens (human)
regulation of nephron tubule epithelial cell differentiationCatenin beta-1Homo sapiens (human)
mesenchymal stem cell differentiationCatenin beta-1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayCatenin beta-1Homo sapiens (human)
regulation of calcium ion importCatenin beta-1Homo sapiens (human)
acinar cell differentiationCatenin beta-1Homo sapiens (human)
synaptic vesicle clusteringCatenin beta-1Homo sapiens (human)
apoptotic signaling pathwayCatenin beta-1Homo sapiens (human)
cell-cell adhesionCatenin beta-1Homo sapiens (human)
positive regulation of odontoblast differentiationCatenin beta-1Homo sapiens (human)
negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayCatenin beta-1Homo sapiens (human)
cranial skeletal system developmentCatenin beta-1Homo sapiens (human)
midbrain dopaminergic neuron differentiationCatenin beta-1Homo sapiens (human)
neuron projection extensionCatenin beta-1Homo sapiens (human)
embryonic brain developmentCatenin beta-1Homo sapiens (human)
dorsal root ganglion developmentCatenin beta-1Homo sapiens (human)
establishment of blood-retinal barrierCatenin beta-1Homo sapiens (human)
regulation of protein localization to cell surfaceCatenin beta-1Homo sapiens (human)
positive regulation of determination of dorsal identityCatenin beta-1Homo sapiens (human)
positive regulation of myoblast proliferationCatenin beta-1Homo sapiens (human)
positive regulation of stem cell proliferationCatenin beta-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
transcription coregulator bindingCatenin beta-1Homo sapiens (human)
transcription corepressor bindingCatenin beta-1Homo sapiens (human)
chromatin bindingCatenin beta-1Homo sapiens (human)
transcription coactivator activityCatenin beta-1Homo sapiens (human)
signaling receptor bindingCatenin beta-1Homo sapiens (human)
protein bindingCatenin beta-1Homo sapiens (human)
nuclear receptor bindingCatenin beta-1Homo sapiens (human)
enzyme bindingCatenin beta-1Homo sapiens (human)
kinase bindingCatenin beta-1Homo sapiens (human)
protein kinase bindingCatenin beta-1Homo sapiens (human)
nuclear estrogen receptor bindingCatenin beta-1Homo sapiens (human)
ubiquitin protein ligase bindingCatenin beta-1Homo sapiens (human)
transmembrane transporter bindingCatenin beta-1Homo sapiens (human)
alpha-catenin bindingCatenin beta-1Homo sapiens (human)
cadherin bindingCatenin beta-1Homo sapiens (human)
SMAD bindingCatenin beta-1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCatenin beta-1Homo sapiens (human)
I-SMAD bindingCatenin beta-1Homo sapiens (human)
disordered domain specific bindingCatenin beta-1Homo sapiens (human)
DNA-binding transcription factor bindingCatenin beta-1Homo sapiens (human)
protein phosphatase bindingCatenin beta-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (44)

Processvia Protein(s)Taxonomy
spindle poleCatenin beta-1Homo sapiens (human)
nucleusCatenin beta-1Homo sapiens (human)
nucleoplasmCatenin beta-1Homo sapiens (human)
cytoplasmCatenin beta-1Homo sapiens (human)
centrosomeCatenin beta-1Homo sapiens (human)
cytosolCatenin beta-1Homo sapiens (human)
plasma membraneCatenin beta-1Homo sapiens (human)
cell-cell junctionCatenin beta-1Homo sapiens (human)
adherens junctionCatenin beta-1Homo sapiens (human)
fascia adherensCatenin beta-1Homo sapiens (human)
bicellular tight junctionCatenin beta-1Homo sapiens (human)
focal adhesionCatenin beta-1Homo sapiens (human)
cell cortexCatenin beta-1Homo sapiens (human)
membraneCatenin beta-1Homo sapiens (human)
basolateral plasma membraneCatenin beta-1Homo sapiens (human)
apicolateral plasma membraneCatenin beta-1Homo sapiens (human)
lateral plasma membraneCatenin beta-1Homo sapiens (human)
Z discCatenin beta-1Homo sapiens (human)
lamellipodiumCatenin beta-1Homo sapiens (human)
cell junctionCatenin beta-1Homo sapiens (human)
microvillus membraneCatenin beta-1Homo sapiens (human)
presynaptic membraneCatenin beta-1Homo sapiens (human)
apical part of cellCatenin beta-1Homo sapiens (human)
synapseCatenin beta-1Homo sapiens (human)
postsynaptic membraneCatenin beta-1Homo sapiens (human)
perinuclear region of cytoplasmCatenin beta-1Homo sapiens (human)
extracellular exosomeCatenin beta-1Homo sapiens (human)
cell peripheryCatenin beta-1Homo sapiens (human)
Schaffer collateral - CA1 synapseCatenin beta-1Homo sapiens (human)
presynaptic active zone cytoplasmic componentCatenin beta-1Homo sapiens (human)
glutamatergic synapseCatenin beta-1Homo sapiens (human)
postsynaptic density, intracellular componentCatenin beta-1Homo sapiens (human)
beta-catenin-TCF complexCatenin beta-1Homo sapiens (human)
euchromatinCatenin beta-1Homo sapiens (human)
transcription regulator complexCatenin beta-1Homo sapiens (human)
catenin complexCatenin beta-1Homo sapiens (human)
flotillin complexCatenin beta-1Homo sapiens (human)
beta-catenin destruction complexCatenin beta-1Homo sapiens (human)
protein-containing complexCatenin beta-1Homo sapiens (human)
protein-DNA complexCatenin beta-1Homo sapiens (human)
Scrib-APC-beta-catenin complexCatenin beta-1Homo sapiens (human)
beta-catenin-TCF7L2 complexCatenin beta-1Homo sapiens (human)
beta-catenin-ICAT complexCatenin beta-1Homo sapiens (human)
Wnt signalosomeCatenin beta-1Homo sapiens (human)
cytoplasmCatenin beta-1Homo sapiens (human)
adherens junctionCatenin beta-1Homo sapiens (human)
nucleusCatenin beta-1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (35)

Assay IDTitleYearJournalArticle
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1612408Substrate activity at recombinant human NQO1 assessed as ratio of Kcat to Km by measuring umol of NADPH utilized per umol of enzyme at 10 uM preincubated for 3 mins followed by NADPH addition and measured at 2 secs interval for 5 mins by Michaelis-Menten 2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1612424Substrate activity at recombinant human NQO1 assessed as ROS generation by measuring umol of cytochrome c utilized per umol of enzyme at 10 uM co-incubated with DIC measured at 2 secs interval for 5 mins in presence of NADPH2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891970Inhibition of survivin-GAL4-DBD dimerization (unknown origin) expressed in human LNCaP C4-2 cells incubated for 24 hrs by SEAP reporter based mammalian two hybrid assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891974Inhibition of survivin dimerization in human PC-3 cells assessed as survivin degradation at 1 uM incubated for 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1612500Substrate activity at recombinant human NQO1 assessed as ratio of number of equivalents of consumed NADPH to number of equivalents of test compound at 10 uM preincubated for 3 mins followed by NADPH addition and measured at 2 secs interval for 5 mins in p2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891977Inhibition of survivin dimerization in human LNCaP C4-2 cells assessed as survivin degradation at 500 nM incubated for 24 hrs after 2 hrs pretreatment with proteasome inhibitor bortezomib by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1612407Substrate activity at recombinant human NQO1 assessed as ROS generation by measuring metabolic rate utilizing umol of NADPH per umol of enzyme at 10 uM preincubated for 3 mins followed by NADPH addition and measured at 2 secs interval for 5 mins2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891985Synergistic potentiation of docetaxel-induced cytotoxicity against human LNCaP C4-2 cells assessed as combination index for reduction in cell viability at docetaxel/7F1 ratios ((1:1, 3:1, and 1:3 using their cytotoxic IC50) incubated for 72 hrs by methyle2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891969Cytotoxicity against human LNCaP C4-2 cells assessed as inhibition of cell survival at 2.5 uM incubated for 72 hrs by methylene blue survival assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891980Inhibition of survivin dimerization in human PC-3 cells assessed as survivin degradation at 500 nM incubated for 24 hrs after 2 hrs pretreatment with proteasome inhibitor MG132 by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1233174Inhibition of human wild-type beta-catenin (residues 138-686)/C-terminally fluorescein labeled human wild-type Tcf4 (residues 7-51) interaction after 1.5 hrs by FP competitive inhibition assay2015Journal of medicinal chemistry, Jun-11, Volume: 58, Issue:11
Discovery of Selective Small-Molecule Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction through the Optimization of the Acyl Hydrazone Moiety.
AID1891984Induction of apoptosis in human LNCaP C4-2 cells assessed as increase in cleaved caspase-3 level at 200 nM incubated for 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1459225Inhibition of mPGES-1 in microsomes isolated from IL-1beta-stimulated human A549 cells at 10 uM using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC method relative to control2017European journal of medicinal chemistry, Jan-05, Volume: 125Identification of novel microsomal prostaglandin E
AID1612410Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1612411Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891976Inhibition of survivin dimerization in human PC-3 cells assessed as survivin degradation at 500 nM incubated for 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1612409Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891978Inhibition of survivin dimerization in human LNCaP C4-2 cells assessed as survivin degradation at 500 nM incubated for 24 hrs after 2 hrs pretreatment with proteasome inhibitor MG132 by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891981Induction of apoptosis in human PC-3 cells at 200 nM incubated for 24 hrs by annexin V-FITC and propidium iodide staining based flow cytometry2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891968Cytotoxicity against human PC-3 cells assessed as inhibition of cell survival at 2.5 uM incubated for 72 hrs by methylene blue survival assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891971Cytotoxicity against human LNCaP C4-2 cells with survivin overexpression assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891966Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891972Cytotoxicity against human LNCaP C4-2 cells with empty vector-transfection assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891973Inhibition of survivin dimerization in human LNCaP C4-2 cells assessed as survivin degradation at 1 uM incubated for 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891975Inhibition of survivin dimerization in human LNCaP C4-2 cells assessed as survivin degradation at 500 nM incubated for 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1612423Substrate activity at recombinant human NQO1 assessed as ROS generation by measuring umol of cytochrome c utilized per umol of enzyme at 10 uM measured at 2 secs interval for 5 mins in presence of NADPH2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1612412Selectivity ratio of IC50 for NQO1 deficient human L02 cells to IC50 for human A549/TR cells expressing NQO12018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891982Induction of apoptosis in human LNCaP C4-2 cells at 200 nM incubated for 24 hrs by annexin V-FITC and propidium iodide staining based flow cytometry2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1612499Substrate activity at recombinant human NQO1 assessed as ratio of number of equivalents of consumed NADPH to number of equivalents of test compound at 10 uM preincubated for 3 mins followed by NADPH addition and measured at 2 secs interval for 5 mins by M2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Discovery of Nonquinone Substrates for NAD(P)H: Quinone Oxidoreductase 1 (NQO1) as Effective Intracellular ROS Generators for the Treatment of Drug-Resistant Non-Small-Cell Lung Cancer.
AID1891983Induction of apoptosis in human PC-3 cells assessed as increase in cleaved caspase-3 level at 200 nM incubated for 24 hrs by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891986Synergistic potentiation of docetaxel-induced cytotoxicity against human PC-3 cells assessed as combination index for reduction in cell viability at docetaxel/7F1 ratios ((1:1, 3:1, and 1:3 using their cytotoxic IC50) incubated for 72 hrs by methylene blu2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891979Inhibition of survivin dimerization in human PC-3 cells assessed as survivin degradation at 500 nM incubated for 24 hrs after 2 hrs pretreatment with proteasome inhibitor bortezomib by Western blot analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
AID1891967Cytotoxicity against human LNCaP C4-2 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65A novel survivin dimerization inhibitor without a labile hydrazone linker induces spontaneous apoptosis and synergizes with docetaxel in prostate cancer cells.
[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's5 (83.33)24.3611
2020's1 (16.67)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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]