Page last updated: 2024-11-09

10074-g5

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Description

10074-G5: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2836600
CHEMBL ID2312756
SCHEMBL ID2689577
MeSH IDM0529194

Synonyms (34)

Synonym
OPREA1_158245
4-nitro-n-(2-phenylphenyl)-2,1,3-benzoxadiazol-7-amine
413611-93-5
biphenyl-2-yl-(7-nitrobenzo[1,2,5]oxadiazol-4-yl)amine
10074-g5
n-2-biphenylyl-7-nitro-2,1,3-benzoxadiazol-4-amine
NCGC00346825-01
S8426
CHEMBL2312756 ,
bdbm50423921
SCHEMBL2689577
MLS006012602
smr004704145
DTXSID60385481
10074-g5, >=98% (hplc)
HY-100996
CS-6372
AKOS032946699
c-myc inhibitor ii - cas 413611-93-5
BS-16819
BCP09223
n-([1,1'-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine
HMS3743K15
CCG-267830
nsc764609
nsc-764609
C75103
EX-A4226
A935156
AC-35793
mfcd00576774
SY315430
n-(2-biphenylyl)-4-amino-7-nitrobenzo[c][1,2,5]oxadiazole
PD017807

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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency26.21230.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency33.17340.001310.157742.8575AID1259253
Interferon betaHomo sapiens (human)Potency26.21230.00339.158239.8107AID1347411
[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)
Myc proto-oncogene proteinHomo sapiens (human)IC50 (µMol)150.00001.00005.73259.6700AID1639655; AID722700
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Myc proto-oncogene proteinHomo sapiens (human)Kd50.53330.00651.12532.8000AID1425547; AID1639648; AID722702
Protein maxHomo sapiens (human)Kd146.00000.01340.01340.0134AID1639648
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (70)

Processvia Protein(s)Taxonomy
positive regulation of cell population proliferationMyc proto-oncogene proteinHomo sapiens (human)
regulation of gene expressionMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of gene expression via chromosomal CpG island methylationMyc proto-oncogene proteinHomo sapiens (human)
G1/S transition of mitotic cell cycleMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
MAPK cascadeMyc proto-oncogene proteinHomo sapiens (human)
branching involved in ureteric bud morphogenesisMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of mesenchymal cell proliferationMyc proto-oncogene proteinHomo sapiens (human)
chromatin remodelingMyc proto-oncogene proteinHomo sapiens (human)
intracellular iron ion homeostasisMyc proto-oncogene proteinHomo sapiens (human)
DNA damage responseMyc proto-oncogene proteinHomo sapiens (human)
response to xenobiotic stimulusMyc proto-oncogene proteinHomo sapiens (human)
response to gamma radiationMyc proto-oncogene proteinHomo sapiens (human)
regulation of cell cycle processMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of gene expressionMyc proto-oncogene proteinHomo sapiens (human)
regulation of telomere maintenanceMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of stress-activated MAPK cascadeMyc proto-oncogene proteinHomo sapiens (human)
protein-DNA complex disassemblyMyc proto-oncogene proteinHomo sapiens (human)
cellular response to UVMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of apoptotic processMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processMyc proto-oncogene proteinHomo sapiens (human)
fibroblast apoptotic processMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of monocyte differentiationMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of DNA-templated transcriptionMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of fibroblast proliferationMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of fibroblast proliferationMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of epithelial cell proliferationMyc proto-oncogene proteinHomo sapiens (human)
chromosome organizationMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of cell divisionMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of telomerase activityMyc proto-oncogene proteinHomo sapiens (human)
negative regulation of transcription initiation by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
ERK1 and ERK2 cascadeMyc proto-oncogene proteinHomo sapiens (human)
response to growth factorMyc proto-oncogene proteinHomo sapiens (human)
cellular response to hypoxiaMyc proto-oncogene proteinHomo sapiens (human)
cellular response to xenobiotic stimulusMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of metanephric cap mesenchymal cell proliferationMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathway by p53 class mediatorMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of miRNA transcriptionMyc proto-oncogene proteinHomo sapiens (human)
regulation of somatic stem cell population maintenanceMyc proto-oncogene proteinHomo sapiens (human)
regulation of transcription by RNA polymerase IIMyc proto-oncogene proteinHomo sapiens (human)
positive regulation of cell population proliferationMyc proto-oncogene proteinHomo 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)
negative regulation of transcription by RNA polymerase IIProtein maxHomo sapiens (human)
regulation of transcription by RNA polymerase IIProtein maxHomo sapiens (human)
positive regulation of DNA-templated transcriptionProtein maxHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIProtein maxHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificMyc proto-oncogene proteinHomo sapiens (human)
core promoter sequence-specific DNA bindingMyc proto-oncogene proteinHomo sapiens (human)
transcription coregulator bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificMyc proto-oncogene proteinHomo sapiens (human)
DNA bindingMyc proto-oncogene proteinHomo sapiens (human)
protein bindingMyc proto-oncogene proteinHomo sapiens (human)
identical protein bindingMyc proto-oncogene proteinHomo sapiens (human)
protein-containing complex bindingMyc proto-oncogene proteinHomo sapiens (human)
protein dimerization activityMyc proto-oncogene proteinHomo sapiens (human)
E-box bindingMyc proto-oncogene proteinHomo sapiens (human)
DNA-binding transcription factor bindingMyc proto-oncogene proteinHomo sapiens (human)
SCF ubiquitin ligase complex bindingMyc proto-oncogene proteinHomo 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)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingProtein maxHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificProtein maxHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificProtein maxHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificProtein maxHomo sapiens (human)
DNA bindingProtein maxHomo sapiens (human)
protein bindingProtein maxHomo sapiens (human)
identical protein bindingProtein maxHomo sapiens (human)
protein dimerization activityProtein maxHomo sapiens (human)
E-box bindingProtein maxHomo sapiens (human)
DNA-binding transcription factor bindingProtein maxHomo sapiens (human)
sequence-specific double-stranded DNA bindingProtein maxHomo sapiens (human)
DNA-binding transcription factor activityProtein maxHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
nucleusMyc proto-oncogene proteinHomo sapiens (human)
nucleoplasmMyc proto-oncogene proteinHomo sapiens (human)
nucleolusMyc proto-oncogene proteinHomo sapiens (human)
cytoplasmMyc proto-oncogene proteinHomo sapiens (human)
Myc-Max complexMyc proto-oncogene proteinHomo sapiens (human)
RNA polymerase II transcription repressor complexMyc proto-oncogene proteinHomo sapiens (human)
chromatinMyc proto-oncogene proteinHomo sapiens (human)
protein-containing complexMyc proto-oncogene proteinHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
nucleusProtein maxHomo sapiens (human)
nucleoplasmProtein maxHomo sapiens (human)
dendriteProtein maxHomo sapiens (human)
Mad-Max complexProtein maxHomo sapiens (human)
Myc-Max complexProtein maxHomo sapiens (human)
chromatinProtein maxHomo sapiens (human)
protein-DNA complexProtein maxHomo sapiens (human)
MLL1 complexProtein maxHomo sapiens (human)
RNA polymerase II transcription regulator complexProtein maxHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1377071Inhibition of self-renewal of human HuH7 cells assessed as reduction in EpCAM positive fraction at 50 uM after 20 mins by propidium iodide staining-based flow cytometric analysis2017Journal of natural products, 06-23, Volume: 80, Issue:6
Identification of BMI1 Promoter Inhibitors from Beaumontia murtonii and Eugenia operculata.
AID722695Cytotoxicity against human HL60 cells assessed as growth inhibition after 3 to 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Pharmacophore identification of c-Myc inhibitor 10074-G5.
AID1585072Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by prestoblue assay2018European journal of medicinal chemistry, Dec-05, Volume: 160Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer.
AID1205236Inhibition of human recombinant His-tagged c-Myc-Max(S) heterodimer binding to DNA at 6.3 to 50 uM after 30 mins by SPR analysis in presence of biotinylated E-box-containing oligonucleotides2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.
AID1585082Inhibition of biotin-labeled EBOX oligonucleotide binding to GST-tagged Myc (368 to 454 residues)/His-tagged Max (23 to 102 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) at 500 uM incubated up to 600 secs by biolayer interferometry as2018European journal of medicinal chemistry, Dec-05, Volume: 160Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer.
AID1205235Inhibition of heterodimerization of human recombinant His-tagged c-Myc-Max(S) compound treated for 20 mins with c-Myc and followed by added Max(S) at 6.3 to 50 uM after 30 mins by SPR analysis in presence of biotinylated E-box-containing oligonucleotides2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.
AID722700Inhibition of recombinant His6-tagged c-Myc bHLH-ZIP domain (353 to 437 amino acid residues) (unknown origin) assessed as disruption of Myc-Max dimerization by electrophoretic mobility shift assay2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Pharmacophore identification of c-Myc inhibitor 10074-G5.
AID722702Binding affinity to human c-Myc bHLH-ZIP domain (353 to 437 amino acid residues) expressed in Escherichia coli BL21 (DE3) by fluorescence polarization assay2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Pharmacophore identification of c-Myc inhibitor 10074-G5.
AID722701Inhibition of recombinant His6-tagged c-Myc bHLH-ZIP domain (353 to 437 amino acid residues) (unknown origin) assessed as disruption of Myc-Max dimerization at 100 uM by electrophoretic mobility shift assay relative to control2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Pharmacophore identification of c-Myc inhibitor 10074-G5.
AID1205266Induction of neutral lipid accumulation in human H460 cells assessed as ratio of mean florescent intensity of compound treated to control cells at 40 uM after 48 hrs by flow cytometry2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
Perturbation of the c-Myc-Max protein-protein interaction via synthetic α-helix mimetics.
AID1585078Inhibition of full length Myc-Max (unknown origin) expressed in human PC3 cells at 12.5 to 25 uM after 24 hrs by luciferase reporter gene based mammalian two-hybrid assay2018European journal of medicinal chemistry, Dec-05, Volume: 160Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer.
AID1585070Inhibition of Myc-Max (unknown origin) expressed in human LNCAP cells assessed as reduction in transcriptional activity at 25 uM after 1 day by luciferase reporter gene assay relative to control2018European journal of medicinal chemistry, Dec-05, Volume: 160Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer.
AID1585081Inhibition of Myc-Max (unknown origin) expressed in human 22rv1 cells harboring UBE2C promoter assessed as reduction in ARV7 level at 12.5 to 25 uM after 48 hrs by Western blot analysis2018European journal of medicinal chemistry, Dec-05, Volume: 160Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer.
AID1585080Inhibition of Myc-Max (unknown origin) expressed in human 22rv1 cells harboring UBE2C promoter assessed as reduction in ARV7 level after 1 day by luciferase reporter gene assay2018European journal of medicinal chemistry, Dec-05, Volume: 160Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer.
AID722694Cytotoxicity against human Daudi cells assessed as growth inhibition after 3 to 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Pharmacophore identification of c-Myc inhibitor 10074-G5.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (9.52)29.6817
2010's13 (61.90)24.3611
2020's6 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.75

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 Index22.75 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index5.26 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.75)

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%
Other21 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]