Page last updated: 2024-12-07

icrf 193

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

Description

4,4'-(1,2-dimethyl-1,2-ethanediyl)bis-2,6-piperazinedione: structure given in first source; RN given refers to cpd without isomeric designation [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ICRF-193 : An N-alkylpiperazine that is butane which is substituted by a 3,5-dioxopiperazin-1-yl group at positions 2 and 3. The meso isomer. [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]

Cross-References

ID SourceID
PubMed CID115150
CHEMBL ID275665
SCHEMBL ID729019
MeSH IDM0192851

Synonyms (30)

Synonym
CBIOL_002063
21416-68-2
BIO1_000349
BIO1_000838
BIO1_001327
PROBES2_000131
PROBES1_000163
icrf-193
2,6-piperazinedione, 4,4'-(1,2-dimethyl-1,2-ethanediyl)bis-
4,4'-(1,2-dimethyl-1,2-ethanediyl)bis-2,6-piperazinedione
icrf 193
MOLMAP_000031
4-(3-(3,5-dioxopiperazin-1-yl)butan-2-yl)piperazine-2,6-dione
bdbm50140290
4-[2-(3,5-dioxopiperazin-1-yl)-1-methylpropyl]piperazine-2,6-dione
CHEMBL275665 ,
4-[3-(3,5-dioxopiperazin-1-yl)butan-2-yl]piperazine-2,6-dione
icrf 196
BCP9000772
NCGC00346949-01
SCHEMBL729019
4-[2-(3,5-dioxo-1-piperazinyl)-1-methylpropyl]piperazine-2,6-dione
J-014041
Q5969732
DTXSID10943979
4,4'-(butane-2,3-diyl)bis(6-hydroxy-4,5-dihydropyrazin-2(3h)-one)
heparin, sodium, low molecular weight
icrf-196
HY-118590A
CS-0694709

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" A bisdioxopiperazine agent dexrazoxane (DEX) has been developed as a cardioprotective drug to prevent these adverse events, but it is uncertain whether it is the best representative of the class."( Prodrug of ICRF-193 provides promising protective effects against chronic anthracycline cardiotoxicity in a rabbit model in vivo.
Adamcová, M; Holečková, M; Jirkovská, A; Karabanovich, G; Kocúrová-Lengvarská, J; Kollárová-Brázdová, P; Kubeš, J; Lenčová-Popelová, O; Mazurová, Y; Roh, J; Šimůnek, T; Štěrba, M; Štěrbová-Kovaříková, P; Váňová, N, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
" The drug is well absorbed from small intestine."( [Topoisomerase inhibitors developing in Japan].
Furue, H, 1993
)
0.29
"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

Dosage Studied

ExcerptRelevanceReference
"DNA-damaging agents, such as radiation and chemotherapy, are common in cancer treatment, but the dosing has proven to be challenging, leading to severe side effects in some patients."( Quantification of single-strand DNA lesions caused by the topoisomerase II poison etoposide using single DNA molecule imaging.
Ekedahl, E; Hammarsten, O; Johansson, P; Lin, YL; Singh, V; Westerlund, F, 2022
)
0.72
[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)
EWS/FLI fusion proteinHomo sapiens (human)Potency0.69180.001310.157742.8575AID1259252; AID1259253; AID1259255
[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)
Prostaglandin G/H synthase 1Ovis aries (sheep)IC50 (µMol)13.90000.00032.177410.0000AID379629
DNA topoisomerase 2-alphaHomo sapiens (human)IC50 (µMol)13.90000.48004.35649.9400AID379629; AID57196
DNA topoisomerase 2-betaHomo sapiens (human)IC50 (µMol)13.90000.03002.77167.8000AID57196
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
hematopoietic progenitor cell differentiationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-alphaHomo sapiens (human)
DNA ligationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA damage responseDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome segregationDNA topoisomerase 2-alphaHomo sapiens (human)
female meiotic nuclear divisionDNA topoisomerase 2-alphaHomo sapiens (human)
apoptotic chromosome condensationDNA topoisomerase 2-alphaHomo sapiens (human)
embryonic cleavageDNA topoisomerase 2-alphaHomo sapiens (human)
regulation of circadian rhythmDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of apoptotic processDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIDNA topoisomerase 2-alphaHomo sapiens (human)
rhythmic processDNA topoisomerase 2-alphaHomo sapiens (human)
negative regulation of DNA duplex unwindingDNA topoisomerase 2-alphaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-alphaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-alphaHomo sapiens (human)
neuron migrationDNA topoisomerase 2-betaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-betaHomo sapiens (human)
axonogenesisDNA topoisomerase 2-betaHomo sapiens (human)
B cell differentiationDNA topoisomerase 2-betaHomo sapiens (human)
forebrain developmentDNA topoisomerase 2-betaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-betaHomo sapiens (human)
cellular response to hydrogen peroxideDNA topoisomerase 2-betaHomo sapiens (human)
cellular response to ATPDNA topoisomerase 2-betaHomo sapiens (human)
cellular senescenceDNA topoisomerase 2-betaHomo sapiens (human)
positive regulation of double-strand break repair via nonhomologous end joiningDNA topoisomerase 2-betaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-betaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
magnesium ion bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
RNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-alphaHomo sapiens (human)
protein kinase C bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP-dependent activity, acting on DNADNA topoisomerase 2-alphaHomo sapiens (human)
DNA binding, bendingDNA topoisomerase 2-alphaHomo sapiens (human)
protein homodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
ubiquitin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein heterodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
DNA bindingDNA topoisomerase 2-betaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-betaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-betaHomo sapiens (human)
protein bindingDNA topoisomerase 2-betaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-betaHomo sapiens (human)
ribonucleoprotein complex bindingDNA topoisomerase 2-betaHomo sapiens (human)
metal ion bindingDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
nuclear chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
centrioleDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome, centromeric regionDNA topoisomerase 2-alphaHomo sapiens (human)
condensed chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
male germ cell nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
cytoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA topoisomerase 2-alphaHomo sapiens (human)
protein-containing complexDNA topoisomerase 2-alphaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleolusDNA topoisomerase 2-betaHomo sapiens (human)
heterochromatinDNA topoisomerase 2-betaHomo sapiens (human)
nucleusDNA topoisomerase 2-betaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-betaHomo sapiens (human)
nucleolusDNA topoisomerase 2-betaHomo sapiens (human)
cytosolDNA topoisomerase 2-betaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-betaHomo sapiens (human)
nucleusDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (81)

Assay IDTitleYearJournalArticle
AID1235608Inhibition of human DNA topoisomerase IIalpha assessed as decatenation of kDNA at 15.625 uM after 90 mins by ethidium bromide staining2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235614Inhibition of human DNA topoisomerase IIalpha assessed as decatenation of kDNA at 31.5 uM after 90 mins by ethidium bromide staining2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235609Inhibition of human DNA topoisomerase IIalpha assessed as decatenation of kDNA at 62.5 uM after 90 mins by ethidium bromide staining2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1134108Mutagenicity in chinese hamster V79-4 cells assessed as mutation frequency measured per 1 x 10'5 cells per plate at 10'-3 M after 24 hrs relative to control1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134111Mutagenicity in chinese hamster V79-4 cells assessed as mutation frequency measured per 5 x 10'5 cells per plate at 10'-5 M after 24 hrs relative to control1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134105Cytotoxicity against chinese hamster V79-4 cells assessed as survival using 5 x 10'5 cells per plate at 10'-5 M after 24 hrs1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134125Induction of scheduled DNA synthesis in chinese hamster V79-4 cells assessed as DNA synthesis at 10'-3 to 10'-5 M measured at 0 to 8 hrs by [3H]thymidine uptake /autoradiography in presence of 2 x 10'-3 M hydroxyurea1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1235634Inhibition of human DNA topoisomerase IIalpha ATPase activity assessed as residual ATP hydrolysis at 31.5 uM measured up to 60 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1134110Mutagenicity in chinese hamster V79-4 cells assessed as mutation frequency measured per 1 x 10'5 cells per plate at 10'-4 M after 24 hrs relative to control1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134115Inhibition of scheduled DNA synthesis in chinese hamster V79-4 cells assessed as DNA synthesis at 10'-4 M measured at 10 hrs by [3H]thymidine uptake /autoradiography (Rvb = 80.1 %)1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1235635Inhibition of human DNA topoisomerase IIalpha ATPase activity assessed as residual ATP hydrolysis at 125 uM measured up to 60 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235615Inhibition of human DNA topoisomerase IIalpha assessed as decatenation of kDNA at 3.9 uM after 90 mins by ethidium bromide staining2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235621Inhibition of human DNA topoisomerase IIalpha assessed as reduction in enzyme-catalyzed supercoiling of relaxed circular pBR322 DNA by measuring linear DNA level at 15.625 uM after 60 mins by agarose gel electrophoresis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235638Inhibition of human DNA topoisomerase IIalpha ATPase activity assessed as residual ATP hydrolysis at 62.5 uM measured up to 60 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1134103Cytotoxicity against chinese hamster V79-4 cells assessed as survival using 5 x 10'5 cells per plate at 10'-4 M after 24 hrs1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134114Inhibition of scheduled DNA synthesis in chinese hamster V79-4 cells assessed as DNA synthesis at 10'-3 M measured at 10 hrs by [3H]thymidine uptake /autoradiography (Rvb = 80.1 %)1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134109Mutagenicity in chinese hamster V79-4 cells assessed as mutation frequency measured per 5 x 10'5 cells per plate at 10'-4 M after 24 hrs relative to control1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134101Cytotoxicity against chinese hamster V79-4 cells assessed as survival using 5 x 10'5 cells per plate at 10'-3 M after 24 hrs1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1235636Inhibition of human DNA topoisomerase IIalpha ATPase activity assessed as residual ATP hydrolysis at 500 uM measured up to 60 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1134107Mutagenicity in chinese hamster V79-4 cells assessed as mutation frequency measured per 5 x 10'5 cells per plate at 10'-3 M after 24 hrs relative to control1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1235617Inhibition of human DNA topoisomerase IIalpha assessed as reduction in enzyme-catalyzed supercoiling of relaxed circular pBR322 DNA by measuring linear DNA level at 3.9 uM after 60 mins by agarose gel electrophoresis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235618Inhibition of human DNA topoisomerase IIalpha assessed as reduction in enzyme-catalyzed supercoiling of relaxed circular pBR322 DNA by measuring linear DNA level at 31.5 uM after 60 mins by agarose gel electrophoresis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235633Inhibition of human DNA topoisomerase IIalpha ATPase activity assessed as residual ATP hydrolysis at 3.9 uM measured up to 60 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1235637Inhibition of human DNA topoisomerase IIalpha ATPase activity assessed as residual ATP hydrolysis at 15.625 uM measured up to 60 mins2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID57196Inhibitory activity against human DNA topoisomerase II2004Bioorganic & medicinal chemistry letters, Mar-08, Volume: 14, Issue:5
Novel quinazoline-quinoline alkaloids with cytotoxic and DNA topoisomerase II inhibitory activities.
AID1134104Cytotoxicity against chinese hamster V79-4 cells assessed as survival using 1 x 10'5 cells per plate at 10'-4 M after 24 hrs1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134112Mutagenicity in chinese hamster V79-4 cells assessed as mutation frequency measured per 1 x 10'5 cells per plate at 10'-5 M after 24 hrs relative to control1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID379629Inhibition of human topoisomerase 22000Journal of natural products, Mar, Volume: 63, Issue:3
Three new triterpenoids from Peganum nigellastrum.
AID1235622Inhibition of human DNA topoisomerase IIalpha assessed as reduction in enzyme-catalyzed supercoiling of relaxed circular pBR322 DNA by measuring linear DNA level at 62.5 uM after 60 mins by agarose gel electrophoresis2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site.
AID1134113Inhibition of scheduled DNA synthesis in chinese hamster V79-4 cells assessed as DNA synthesis at 10'-5 M measured at 10 hrs by [3H]thymidine uptake /autoradiography (Rvb = 80.1 %)1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1134106Cytotoxicity against chinese hamster V79-4 cells assessed as survival using 1 x 10'5 cells per plate at 10'-5 M after 24 hrs1977Journal of medicinal chemistry, May, Volume: 20, Issue:5
Study of trans-cyclopropylbis (diketopiperazine) and chelating agents related to ICRF 159. Cytotoxicity, mutagenicity, and effects on scheduled and unscheduled DNA synthesis.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, 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.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
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.
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.
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.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (151)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.66)18.7374
1990's38 (25.17)18.2507
2000's74 (49.01)29.6817
2010's25 (16.56)24.3611
2020's13 (8.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.40

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 Index27.40 (24.57)
Research Supply Index5.05 (2.92)
Research Growth Index6.66 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (0.65%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other154 (99.35%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]