Page last updated: 2024-11-12

nutlin-3b

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

Cross-References

ID SourceID
PubMed CID16755649
CHEMBL ID2152332
CHEBI ID46742
SCHEMBL ID13233382
MeSH IDM0512519

Synonyms (43)

Synonym
HY-15335
nutlin-3, >=98% (hplc), powder
cis-4-{[4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl]carbonyl}piperazin-2-one
CHEBI:46742 ,
rel-4-{[(4r,5s)-4,5-bis(4-chlorophenyl)-2-{2-[(propan-2-yl)oxy]-4-methoxyphenyl}-4,5-dihydro-1h-imidazol-1-yl]carbonyl}piperazin-2-one
nutlin-3b
BCP9001004
675576-97-3
chembl2152332 ,
bdbm50392532
NCGC00263124-01
CS-0727
4-(((4r,5s)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1h-imidazol-1-yl)carbonyl)-2-piperazinone
S8065
MLS006010832
smr004701759
unii-fja1772cvw
fja1772cvw ,
2-piperazinone, 4-(((4r,5s)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1h-imidazol-1-yl)carbonyl)-
4-[[(4r,5s)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1h-imidazol-1-yl]carbonyl]-2-piperazinone
DTXSID3044330
SCHEMBL13233382
nutlin-3, (+)-
4-((4r,5s)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
(+/-)-4-[4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
AC-35271
AKOS024457911
4-[(4r,5s)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
DTXSID20217890
nutlin (3b)
nutlin (3)
EX-A1360
4-[(4r,5s)-4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1h-imidazole-1-carbonyl]piperazin-2-one
4-(cis-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
BCP05162
Q7070462
4-[(4r,5s)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl]piperazin-2-one
E78795
CCG-270135
AS-79867
BP-27838
AC-35940
N1195

Research Excerpts

Bioavailability

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

Roles (1)

RoleDescription
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
NutlinNutlins (for Nutley inhibitors) are a family of cis-imidazoline analogues. They are MDM2 antagonists and are named after the location (Nutley) in which they were developed.
piperazinone
[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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency37.22120.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency32.99930.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency14.29120.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency37.22120.00308.794948.0869AID1347053
tyrosine-protein kinase YesHomo sapiens (human)Potency12.24080.00005.018279.2586AID686947
Interferon betaHomo sapiens (human)Potency32.99930.00339.158239.8107AID1347411
[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)
Protein Mdm4Homo sapiens (human)IC50 (µMol)1.00000.00933.78498.2000AID1452025
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)IC50 (µMol)6.85400.00060.358210.0000AID1452024; AID691697
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Ki0.19840.00090.19811.2400AID1593981
[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)
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Kd0.15000.00000.25851.0000AID1462777
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (99)

Processvia Protein(s)Taxonomy
heart valve developmentProtein Mdm4Homo sapiens (human)
atrioventricular valve morphogenesisProtein Mdm4Homo sapiens (human)
endocardial cushion morphogenesisProtein Mdm4Homo sapiens (human)
ventricular septum developmentProtein Mdm4Homo sapiens (human)
atrial septum developmentProtein Mdm4Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIProtein Mdm4Homo sapiens (human)
negative regulation of cell population proliferationProtein Mdm4Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorProtein Mdm4Homo sapiens (human)
negative regulation of protein catabolic processProtein Mdm4Homo sapiens (human)
negative regulation of apoptotic processProtein Mdm4Homo sapiens (human)
negative regulation of DNA-templated transcriptionProtein Mdm4Homo sapiens (human)
protein stabilizationProtein Mdm4Homo sapiens (human)
regulation of cell cycleProtein Mdm4Homo sapiens (human)
protein-containing complex assemblyProtein Mdm4Homo sapiens (human)
cellular response to hypoxiaProtein Mdm4Homo sapiens (human)
protein ubiquitinationProtein Mdm4Homo 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)
regulation of cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein polyubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
blood vessel developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
blood vessel remodelingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of heart rateE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
atrioventricular valve morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
endocardial cushion morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ventricular septum developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
atrial septum developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
apoptotic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
traversing start control point of mitotic cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of cell population proliferationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to xenobiotic stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to toxic substanceE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to iron ionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of gene expressionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of protein processingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of neuron projection developmentE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein ubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein sumoylationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein destabilizationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to magnesium ionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein localization to nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to cocaineE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
establishment of protein localizationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to etherE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of DNA-templated transcriptionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of mitotic cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to antibioticE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of protein export from nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to steroid hormoneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of muscle cell differentiationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
proteolysis involved in protein catabolic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein autoubiquitinationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cardiac septum morphogenesisE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein-containing complex assemblyE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to hydrogen peroxideE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to vitamin B1E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to alkaloidE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to growth factor stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to peptide hormone stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to estrogen stimulusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to hypoxiaE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to gamma radiationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to UV-CE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
fibroblast activationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cellular response to actinomycin DE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of signal transduction by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway by p53 class mediatorE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to formaldehydeE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
amyloid fibril formationE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
response to water-immersion restraint stressE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
negative regulation of apoptotic processE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cell cycleE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
regulation of gene expressionE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
protein bindingProtein Mdm4Homo sapiens (human)
zinc ion bindingProtein Mdm4Homo sapiens (human)
enzyme bindingProtein Mdm4Homo sapiens (human)
ubiquitin-protein transferase activityProtein Mdm4Homo 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)
p53 bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin-protein transferase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
5S rRNA bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
zinc ion bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
SUMO transferase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
enzyme bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein domain specific bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin protein ligase bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
receptor serine/threonine kinase bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
identical protein bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
peroxisome proliferator activated receptor bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ribonucleoprotein complex bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
ubiquitin protein ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
NEDD8 ligase activityE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
disordered domain specific bindingE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
nucleusProtein Mdm4Homo sapiens (human)
nucleoplasmProtein Mdm4Homo sapiens (human)
transcription repressor complexProtein Mdm4Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
nuclear bodyE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleoplasmE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
nucleolusE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cytoplasmE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
cytosolE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
plasma membraneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
transcription repressor complexE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
endocytic vesicle membraneE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
protein-containing complexE3 ubiquitin-protein ligase Mdm2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (107)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID686947qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Identification of potent Yes1 kinase inhibitors using a library screening approach.
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.
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.
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.
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.
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.
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.
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.
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.
AID1593991Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1-phase at 10 uM measured after 24 hrs by DNA-staining solution based flow cytometry (Rvb = 52.92%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1450884Activation of p53 in human T24 cells assessed as decrease in MDM2 protein level at 10 uM after 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Phthalazino[1,2-b]quinazolinones as p53 Activators: Cell Cycle Arrest, Apoptotic Response and Bak-Bcl-xl Complex Reorganization in Bladder Cancer Cells.
AID1350427Inhibition of MDM2 in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs in presence of MDM4 inhibitor SJ-1722550 by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593973Induction of apoptosis in human A549 cells assessed as viable cells at 10 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 92.9%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1488990Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 3 days by SRB assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Synthesis and evaluation of modified chalcone based p53 stabilizing agents.
AID1350417Inhibition of MDM2 in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593989Cell cycle arrest in human A549 cells assessed as accumulation at S-phase at 5 uM measured after 24 hrs by DNA-staining solution based flow cytometry (Rvb = 31.43%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1450882Activation of p53 in human T24 cells assessed as increase in p21 level at 10 uM after 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Phthalazino[1,2-b]quinazolinones as p53 Activators: Cell Cycle Arrest, Apoptotic Response and Bak-Bcl-xl Complex Reorganization in Bladder Cancer Cells.
AID1350464Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs by transwell assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1452030Inhibition of MDM2 in human SH-SY5Y cells assessed as increase in PUMA mRNA levels at 1 uM after 24 hrs by RT-qPCR analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1452031Inhibition of MDM2 in human SH-SY5Y cells assessed as increase in p21 mRNA levels at 1 uM after 24 hrs by RT-qPCR analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1489003Induction of p53 stabilization in human HCT116 cells assessed as ratio of p53 expression levels to GAPDH expression levels at 10 uM after 4 hrs by immunoblot analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Synthesis and evaluation of modified chalcone based p53 stabilizing agents.
AID1292183Cell cycle arrest in human HCT116 cells assessed as accumulation at G2 phase after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 27.73 +/- 3.56%)2016European journal of medicinal chemistry, May-23, Volume: 114Design, synthesis and biological evaluation of novel benzimidazole-2-substituted phenyl or pyridine propyl ketene derivatives as antitumour agents.
AID1452027Inhibition of MDM2 in human SH-SY5Y cells assessed as accumulation of p53 at 1 uM after 24 hrs in presence of SJ-1722550 by Western blot analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1462780Induction of apoptosis in human A549 cells at 10 uM incubated for 48 hrs by annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 9.67%)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
AID1350439Inhibition of MDM2 in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of alphaVbeta3 inhibitor cilengitide by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350460Cell cycle arrest in human U87MG cells at 100 nM after 24 hrs2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350447Inhibition of MDM2 in human U87MG cells assessed as increase in p21 mRNA expression at 100 nM after 24 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1452035Inhibition of MDM2 in human SH-SY5Y cells assessed as increase in p21 mRNA levels at 1 uM after 24 hrs in presence of SJ-1722550 by RT-qPCR analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1593995Cell cycle arrest in human A549 cells assessed as decrease in accumulation at S-phase measured after 24 hrs by DNA-staining solution based flow cytometry2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1292175Cell cycle arrest in human HCT116 cells assessed as accumulation at G1 phase after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 31.72 +/- 2.21%)2016European journal of medicinal chemistry, May-23, Volume: 114Design, synthesis and biological evaluation of novel benzimidazole-2-substituted phenyl or pyridine propyl ketene derivatives as antitumour agents.
AID1462777Inhibition of PMDM6-F peptide binding to MDM2 binding domain (1 to 118 residues) (unknown origin) by fluorescence polarization binding assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
AID1350452Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs by MTS assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1452029Inhibition of MDM2 in human SH-SY5Y cells assessed as increase in MDM2 mRNA levels at 1 uM after 24 hrs by RT-qPCR analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1483339Cytotoxicity against p53 deficient human Saos2 cells assessed as cell growth inhibition after 24 hrs by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1593986Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 10 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.62%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593985Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 10 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.73%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593984Induction of apoptosis in human A549 cells assessed as necrotic cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.76%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593976Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth at 10 uM measured after 24 hrs by CCK8 assay relative to control2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1452024Inhibition of MDM2 in human U87MG cells assessed as reduction in MDM2 interaction with p53 after 10 mins by quantitative sandwich immune-enzymatic assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1350443Inhibition of MDM2 in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 and alphaVbeta3 inhibitor cilengitide by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1452021Antiproliferative activity against human U87MG cells at 1 uM after 24 hrs by MTS assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1593978Antiproliferative activity against human HCT116 cells assessed as inhibition of cell growth at 10 uM measured after 24 hrs by CCK8 assay relative to control2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1483338Cytotoxicity against wild type p53 expressing human U2OS cells assessed as cell growth inhibition after 24 hrs by MTT assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1452025Inhibition of MDM4 in human SH-SY5Y cells assessed as reduction in MDM4 interaction with p53 after 10 mins by quantitative sandwich immune-enzymatic assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1462773Induction of apoptosis in human A549 cells at 5 uM incubated for 48 hrs by annexin V-FITC and propidium iodide staining based flow cytometry (Rvb = 9.67%)2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
AID1593988Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1-phase at 5 uM measured after 24 hrs by DNA-staining solution based flow cytometry (Rvb = 52.92%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1462776Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
AID1489004Induction of p53 stabilization in human HCT116 cells assessed as ratio of p53 expression levels to GAPDH expression levels at 10 uM after 8 hrs by immunoblot analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Synthesis and evaluation of modified chalcone based p53 stabilizing agents.
AID1350455Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of alphaVbeta3 inhibitor cilengitide and MDM4 inhibitor SJ-1722550 by MTS assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1450886Effect on p53 protein expression in human T24 cells at 10 uM after 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Phthalazino[1,2-b]quinazolinones as p53 Activators: Cell Cycle Arrest, Apoptotic Response and Bak-Bcl-xl Complex Reorganization in Bladder Cancer Cells.
AID691697Inhibition of MDM2 binding to p532012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships.
AID1350420Inhibition of MDM2 in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of alphaVbeta3 inhibitor cilengitide by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350465Anti-invasive activity in human U87MG cells at 10 uM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 and alphaVbeta3 inhibitor cilengitide by transwell assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593982Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 4.62%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593983Binding affinity to MDM2 in human A549 cells assessed as reduction in p53-MDM2 interaction by measuring upregulation of p53 expression measured after 18 hrs by Western blot analysis2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1350423Inhibition of MDM2 in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 and alphaVbeta3 inhibitor cilengitide by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593974Antiproliferative activity against human A549 cells assessed as inhibition of cell growth at 10 uM measured after 24 hrs by CCK8 assay relative to control2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1350416Inhibition of MDM2 in human U87MG cells assessed as increase in p53 accumulation at 100 nM after 24 hrs by Western blot method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350429Inhibition of MDM2 in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs in presence of MDM4 inhibitor SJ-1722550 and alphaVbeta3 inhibitor cilengitide by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1462775Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
AID1593987Induction of apoptosis in human A549 cells assessed as necrotic cells at 10 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.76%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1292185Inhibition of MDM2/P53 protein interaction in human HCT116 cells at 50 uM after 24 hrs by immunoprecipitation analysis2016European journal of medicinal chemistry, May-23, Volume: 114Design, synthesis and biological evaluation of novel benzimidazole-2-substituted phenyl or pyridine propyl ketene derivatives as antitumour agents.
AID1350434Inhibition of MDM2 in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 8 to 24 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1452042Antiproliferative activity against human SH-SY5Y cells at 1 uM after 24 hrs by MTS assay relative to control2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1350453Antiproliferative activity against human U87MG cells at 100 nM after 72 hrs in presence of alphaVbeta3 inhibitor cilengitide by MTS assay2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593979Antiproliferative activity against human HCT116 cells measured after 24 hrs by CCK8 assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593977Antiproliferative activity against human MCF7 cells measured after 24 hrs by CCK8 assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1350437Inhibition of MDM2 in human U87MG cells assessed as increase in PUMA mRNA expression at 100 nM after 24 hrs in presence of MDM4 inhibitor SJ-1722550 by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593981Inhibition of PMDM6-F probe binding to MDM2 (1 to 118 residues) (unknown origin) preincubated for 30 mins followed by PMDM6-F addition and measured after 1 hr fluorescence polarization assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593971Induction of apoptosis in human A549 cells assessed as viable cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 92.9%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593992Cell cycle arrest in human A549 cells assessed as accumulation at S-phase at 10 uM measured after 24 hrs by DNA-staining solution based flow cytometry (Rvb = 31.43%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1483340Selectivity ratio of IC50 for human Saos2 cells to IC50 for human U2OS cells2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
AID1593993Cell cycle arrest in human A549 cells assessed as accumulation at G2/M-phase at 10 uM measured after 24 hrs by DNA-staining solution based flow cytometry (Rvb = 15.66%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1452026Inhibition of MDM2 in human SH-SY5Y cells assessed as accumulation of p53 at 1 uM after 24 hrs by Western blot analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1593972Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 5 uM measured after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.73%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1593994Cell cycle arrest in human A549 cells assessed as increase in accumulation at G0/G1-phase measured after 24 hrs by DNA-staining solution based flow cytometry2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1452034Inhibition of MDM2 in human SH-SY5Y cells assessed as increase in PUMA mRNA levels at 1 uM after 24 hrs in presence of SJ-1722550 by RT-qPCR analysis2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1292179Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 40.55 +/- 1.36%)2016European journal of medicinal chemistry, May-23, Volume: 114Design, synthesis and biological evaluation of novel benzimidazole-2-substituted phenyl or pyridine propyl ketene derivatives as antitumour agents.
AID1462774Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Design, synthesis and biological evaluation of novel antitumor spirotetrahydrothiopyran-oxindole derivatives as potent p53-MDM2 inhibitors.
AID1593990Cell cycle arrest in human A549 cells assessed as accumulation at G2/M-phase at 5 uM measured after 24 hrs by DNA-staining solution based flow cytometry (Rvb = 15.66%)2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1350426Inhibition of MDM2 in human U87MG cells assessed as increase in MDM2 mRNA expression at 100 nM after 8 hrs by RT-PCR method2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1350461Cell cycle arrest in human U87MG cells assessed as accumulation at G0/G1 phase at 100 nM in presence of MDM4 inhibitor SJ-1722550 after 24 hrs2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
AID1593975Antiproliferative activity against human A549 cells measured after 24 hrs by CCK8 assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.
AID1452043Antiproliferative activity against human SH-SY5Y cells at 1 uM after 24 hrs in presence of SJ-1722550 by MTS assay relative to control2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.
AID1464360Cytotoxicity against human U87 cells assessed as reduction in cell viability after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20
d-Amino acid mutation of PMI as potent dual peptide inhibitors of p53-MDM2/MDMX interactions.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's13 (68.42)24.3611
2020's6 (31.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.71

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 Index16.71 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.71)

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%
Other19 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]