Page last updated: 2024-11-12

nutlin-3a

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Description

nutlin 3: an MDM2 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11433190
CHEMBL ID191334
CHEBI ID95096
SCHEMBL ID1155752
MeSH IDM0510642

Synonyms (71)

Synonym
HY-10029
nutlin-3
nutlin 3
nutlin-3a ,
(4s,5r)-nutlin-3
4-((4s,5r)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
(rac)-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl)(piperazin-1-yl)methanone
bdbm50229787
rac-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
4-[(4s,5r)-4,5-bis-(4-chloro-phenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
nsc-732664
CHEMBL191334 ,
nsc 732664
53ia0v845c ,
unii-53ia0v845c
BCP9001003
675576-98-4
(+)-nutlin-3
4HG7
4J3E
CS-0296
(-)-nutlin 3
4-(((4s,5r)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl)carbonyl)piperazin-2-one
rebemadlin
sml-0580
rebemadlin [inn]
S8059
nutlin 3a
l7c92ioe65 ,
2-piperazinone, 4-(((4s,5r)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1h-imidazol-1-yl)carbonyl)-
unii-l7c92ioe65
SCHEMBL1155752
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)-, rel-
4-[[(4s,5r)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1h-imidazol-1-yl]carbonyl]-2-piperazinone
nutlin-3, (-)-
BDUHCSBCVGXTJM-WUFINQPMSA-N
4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4, 5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
HMS3649P17
4-[(4s,5r)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
nutlin 3b
nutlin (3a)
EX-A1359
AKOS027422740
CHEBI:95096
nutlin-3a chiral
(-)-nutlin-3
(?)-nutlin-3
4-[(4s,5r)-4,5-bis(4-chlorophenyl)-2-[4-methoxy-2-(propan-2-yloxy)phenyl]-4,5-dihydro-1h-imidazole-1-carbonyl]piperazin-2-one
AS-75148
nutlin-3a, >=98% (hplc)
AC-35379
NCGC00344347-05
nutlin3a
Q27166862
(+/-)-4-[4,5-bis-(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
548472-68-0 (4r5s, and 4s5r)
mfcd14636430
SR-01000946691-1
sr-01000946691
4-[cis-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl]piperazin-2-one
675576-98-4 (4s5r)
nsc763443
nsc-763443
nsc-756875
nsc-756876
nsc756876
nsc756875
(-)-4-(4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-2-one
DTXSID801317967
4-[(4s,5r)-4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one
Z2037279564

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Collectively, these results demonstrate that the induction of p53 peri-operatively protects bone healing from the toxic effects of CDP, while maintaining OS toxicity."( Nutlin-3 treatment spares cisplatin-induced inhibition of bone healing while maintaining osteosarcoma toxicity.
Aronson, J; Becton, DL; Bunn, RC; Liu, L; Lumpkin, CK; Montgomery, CO; Nicholas, RW; Skinner, RA; Stine, KC; Suva, LJ; Swearingen, CJ; VanderSchilden, J; Wahl, EC, 2016
)
0.43

Pharmacokinetics

ExcerptReferenceRelevance
" We used physiologically based pharmacokinetic (PBPK) modeling to characterize the disposition of nutlin-3a in the mouse."( Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
Boulos, N; Dyer, MA; Guy, RK; Lu, M; Mallari, J; Miller, L; Nemeth, K; Panetta, JC; Roussel, MF; Stewart, CF; Tagen, M; Throm, S; Williams, RT; Zhang, F; Zhang, J; Zhu, F, 2011
)
0.83

Compound-Compound Interactions

ExcerptReferenceRelevance
" Here, we explored the antitumor potential of cyclin-dependent kinase (CDK) inhibitors in combination with a small molecule inhibitor of p53-murine double minute 2 (MDM2) interaction."( Cyclin-dependent kinase inhibitors sensitize tumor cells to nutlin-induced apoptosis: a potent drug combination.
Cheok, CF; Dey, A; Lane, DP, 2007
)
0.34
" We examined the effects of the MDM2 inhibitor nutlin3a and its combination with the dual Bcl-2 and Bcl-xL inhibitor ABT-737, and the Bcr-Abl inhibitor nilotinib on BC CML patient samples."( Synergistic effects of p53 activation via MDM2 inhibition in combination with inhibition of Bcl-2 or Bcr-Abl in CD34+ proliferating and quiescent chronic myeloid leukemia blast crisis cells.
Andreeff, M; Carter, BZ; Champlin, RE; Cortes, J; Kantarjian, HM; Konopleva, M; Mak, DH; Mak, PY; McQueen, T; Ruvolo, VR; Schober, W, 2015
)
0.42
"Various cytotoxic agents were evaluated in combination with (131) I-MIP-1095 for their capacity to delay the growth of LNCaP cells cultured as multicellular tumour spheroids."( Preliminary evaluation of prostate-targeted radiotherapy using (131) I-MIP-1095 in combination with radiosensitising chemotherapeutic drugs.
Babich, JW; Mairs, RJ; Nixon, C; Rae, C; Tesson, M, 2016
)
0.43
" Nutlin-3 combined with MG-132 narrowed this between-group difference and triggered stronger inhibitory effects on the growth of schwannomas through coordinated reactivation of p53."( Synergistic effect of Nutlin-3 combined with MG-132 on schwannoma cells through restoration of merlin and p53 tumour suppressors.
Chen, H; Huang, H; Wang, H; Wang, Z; Wu, H; Xue, L; Zhang, X; Zhu, W, 2018
)
0.48
" Here we used nutlin-3 in combination with another potent anticancer drug, doxorubicin, to investigate the synergism between these drugs."( MDM2 antagonist-loaded targeted micelles in combination with doxorubicin: effective synergism against human glioblastoma via p53 re-activation.
Bilir, C; Filipczak, N; Liu, J; Porter, TM; Sarisozen, C; Shen, L; Tan, Y; Torchilin, VP,
)
0.13

Bioavailability

ExcerptReferenceRelevance
" Compound 5 has a good oral bioavailability and effectively inhibits tumor growth in the SJSA-1 xenograft model."( Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.
Chen, J; Ding, K; Kang, S; McEachern, D; Miller, R; Nikolovska-Coleska, Z; Qin, D; Qiu, S; Shangary, S; Wang, G; Wang, S; Yang, D; Yu, S, 2009
)
0.35
" To overcome the poor bioavailability of Nutlin-3, we have assessed the potential efficacy of Nutlin-3 loaded poly(lactide-co-glycolide) (PLGA) nanoparticles (NP) against hematological malignancies."( Nanoparticles loaded with Nutlin-3 display cytotoxicity towards p53(wild-type) JVM-2 but not towards p53(mutated) BJAB leukemic cells.
Caruso, L; Forni, F; Palomba, M; Ruozi, B; Secchiero, P; Vandelli, MA; Voltan, R; Zauli, G, 2013
)
0.39
" The AURKA/MDM2 combination therapy shows adequate bioavailability and low toxicity to the host."( Mdm2 and aurora kinase a inhibitors synergize to block melanoma growth by driving apoptosis and immune clearance of tumor cells.
Ayers, GD; Davis, TA; Ecsedy, JA; Essaka, DC; Hawkins, OE; Horton, LW; Johnston, JN; Kelley, MC; Liu, Y; McClain, CM; Pawlikowski, JS; Richmond, A; Smith, J; Sosman, JA; Stewart, CF; Turner, DC; Vilgelm, AE; Weller, KP, 2015
)
0.42
"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

A combination of nutlin-3a and a low dose of. aspirin provides better results than a high dose of aspirin. A comparative analysis is also tabulated with different dosing regimens.

ExcerptRelevanceReference
" The final model was used to perform simulations of unbound tissue concentrations to determine which dosing regimens are appropriate for preclinical models of several pediatric malignancies."( Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
Boulos, N; Dyer, MA; Guy, RK; Lu, M; Mallari, J; Miller, L; Nemeth, K; Panetta, JC; Roussel, MF; Stewart, CF; Tagen, M; Throm, S; Williams, RT; Zhang, F; Zhang, J; Zhu, F, 2011
)
0.61
" A 4-day dosing schedule in vivo generated a similar response in colon tumors; growth arrest without significantly increased apoptosis."( Pharmacological inhibition of Mdm2 triggers growth arrest and promotes DNA breakage in mouse colon tumors and human colon cancer cells.
Belinsky, GS; Giardina, C; Rigatti, MJ; Rosenberg, DW; Verma, R, 2012
)
0.38
"7-fold over vehicle) upon oral dosing of 27 at 300 mg/kg."( Rational design and binding mode duality of MDM2-p53 inhibitors.
Bartberger, MD; Beck, HP; Canon, J; Chen, A; Chow, D; Correll, TL; Gonzalez-Lopez de Turiso, F; Huang, X; Julian, LD; Kayser, F; Lo, MC; Long, AM; McMinn, D; Medina, JC; Oliner, JD; Olson, SH; Osgood, T; Powers, JP; Rew, Y; Saiki, AY; Schneider, S; Shaffer, P; Sun, D; Xiao, SH; Yakowec, P; Yan, X; Ye, Q; Yu, D; Zhao, X; Zhou, J, 2013
)
0.39
" Using an intermittent dosing schedule of combined carboplatin and Nutlin-3a, there was a significant reduction in primary tumor growth and lung metastases compared with vehicle and single-agent treatments."( Potentiation of Carboplatin-Mediated DNA Damage by the Mdm2 Modulator Nutlin-3a in a Humanized Orthotopic Breast-to-Lung Metastatic Model.
Bailey, BJ; Batuello, CN; Ding, J; Eischen, CM; Georgiadis, TM; Gunter, TZ; Hanenberg, H; Long, EC; Marchal, CC; Mayo, LD; Minto, RE; Peterman, KM; Pollok, KE; Saadatzadeh, MR; Safa, AR; Sandusky, GE; Shannon, HE; Silver, JM; Sinn, AL; Spragins, TK; Sprouse, AA; Territo, PR; Tonsing-Carter, E; Wang, H, 2015
)
0.89
" This fact has come to notice when a novel method for the drug dosage design is introduced using system oriented concepts."( On p53 revival using system oriented drug dosage design.
Azam, R; Azam, S; Bhatti, AI; Fazal, S; Haseeb, M; Ullah, M, 2017
)
0.46
"DNA sequencing and dosage analysis were used to identify the NF2 mutation status in sporadic schwannomas."( Synergistic effect of Nutlin-3 combined with MG-132 on schwannoma cells through restoration of merlin and p53 tumour suppressors.
Chen, H; Huang, H; Wang, H; Wang, Z; Wu, H; Xue, L; Zhang, X; Zhu, W, 2018
)
0.48
" A comparative analysis is also tabulated with different dosing regimens which shows that a combination of nutlin-3a and a low dose of aspirin provides better results than a high dose of aspirin."( Effect of pharmacodynamical interaction between nutlin-3a and aspirin in the activation of p53.
Aslam, M; Awan, MS; Bhatti, AI; Liaquat, A; Liaquat, M, 2021
)
1.09
" Azithromycin and doxycycline demonstrated MICs and MBCs equal or below their peak serum concentrations (PSC) after standard dosing in both cell types."( Clearing Chlamydia abortus infection in epithelial cells and primary human macrophages by use of antibiotics and the MDM2-p53-inhibitor nutlin-3.
Diensthuber, D; Essig, A; Hagemann, JB; Peters, S; Simnacher, U; Walther, P, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
stilbenoidAny olefinic compound characterised by a 1,2-diphenylethylene backbone.
[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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.33790.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency13.45040.00108.379861.1304AID1645840
Cellular tumor antigen p53Homo sapiens (human)Potency0.30000.002319.595674.0614AID243263
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Potency0.30000.30000.30000.3000AID243263
[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)4.62730.00933.78498.2000AID1238675; AID1285801; AID1908071; AID453615
Protein Mdm4Homo sapiens (human)Ki5.86005.86005.86005.8600AID707317
Cellular tumor antigen p53Homo sapiens (human)IC50 (µMol)3.43490.00060.88508.2000AID1238620; AID1239847; AID1285800; AID1285801; AID1285802; AID1285803; AID1300245; AID1387289; AID1632470; AID1720556; AID1872997; AID1908070; AID1908071; AID438431; AID438435; AID658338; AID706601; AID706602; AID706603; AID721248
Cellular tumor antigen p53Homo sapiens (human)Ki1.28600.00301.07365.8600AID626520; AID707317; AID707326; AID749326; AID749491
Apoptosis regulator Bcl-2Homo sapiens (human)Ki10.00000.00000.19012.9000AID1296598
E3 ubiquitin-protein ligase Mdm2Mus musculus (house mouse)Ki0.01990.01990.04290.0659AID1238646
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)0.07000.00002.398310.0000AID1300245
Death-associated protein kinase 1Homo sapiens (human)IC50 (µMol)25.00000.00052.284510.0000AID1285802
E3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)Ki0.01050.01050.01550.0205AID1238645
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)IC50 (µMol)1.45480.00060.358210.0000AID1125680; AID1195730; AID1238620; AID1239847; AID1252240; AID1285800; AID1300245; AID1387289; AID1420852; AID1421138; AID1555409; AID1632470; AID1656006; AID1659344; AID1720556; AID1872997; AID1908070; AID265956; AID318566; AID417066; AID453614; AID587349; AID587948; AID658338; AID691697; AID700922; AID706601; AID706602; AID721248; AID738689; AID739072; AID739073; AID746383; AID748501
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Ki0.08600.00090.19811.2400AID1143657; AID1152866; AID1238644; AID1296599; AID1361628; AID1415891; AID1656007; AID1908077; AID265955; AID267242; AID626520; AID684825; AID707326; AID749326; AID749491
Induced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)Ki10.00000.00101.46539.5400AID1296597
Peptidyl-prolyl cis-trans isomerase DHomo sapiens (human)IC50 (µMol)25.00000.00360.00360.0036AID1285803
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)100.00000.00010.55439.9000AID1361627
[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)
Apoptosis regulator Bcl-2Homo sapiens (human)Kd15.00000.00060.95874.8000AID1296639
Delta-type opioid receptorMus musculus (house mouse)Kd0.50000.00020.08870.5000AID362382
E3 ubiquitin-protein ligase Mdm2Homo sapiens (human)Kd0.60500.00000.25851.0000AID1296640; AID362378; AID362381; AID362382; AID362383; AID362384; AID362385
Mu-type opioid receptorCavia porcellus (domestic guinea pig)Kd0.50000.50000.50000.5000AID362385
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (348)

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)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
protein polyubiquitinationApoptosis regulator Bcl-2Homo sapiens (human)
apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
response to cytokineApoptosis regulator Bcl-2Homo sapiens (human)
B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of calcium ion transportApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
ossificationApoptosis regulator Bcl-2Homo sapiens (human)
ovarian follicle developmentApoptosis regulator Bcl-2Homo sapiens (human)
metanephros developmentApoptosis regulator Bcl-2Homo sapiens (human)
branching involved in ureteric bud morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
behavioral fear responseApoptosis regulator Bcl-2Homo sapiens (human)
B cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
release of cytochrome c from mitochondriaApoptosis regulator Bcl-2Homo sapiens (human)
regulation of cell-matrix adhesionApoptosis regulator Bcl-2Homo sapiens (human)
lymphoid progenitor cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
B cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of B cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
response to ischemiaApoptosis regulator Bcl-2Homo sapiens (human)
renal system processApoptosis regulator Bcl-2Homo sapiens (human)
melanin metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
regulation of nitrogen utilizationApoptosis regulator Bcl-2Homo sapiens (human)
autophagyApoptosis regulator Bcl-2Homo sapiens (human)
humoral immune responseApoptosis regulator Bcl-2Homo sapiens (human)
DNA damage responseApoptosis regulator Bcl-2Homo sapiens (human)
actin filament organizationApoptosis regulator Bcl-2Homo sapiens (human)
axonogenesisApoptosis regulator Bcl-2Homo sapiens (human)
female pregnancyApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of cell population proliferationApoptosis regulator Bcl-2Homo sapiens (human)
male gonad developmentApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressApoptosis regulator Bcl-2Homo sapiens (human)
response to radiationApoptosis regulator Bcl-2Homo sapiens (human)
response to xenobiotic stimulusApoptosis regulator Bcl-2Homo sapiens (human)
response to toxic substanceApoptosis regulator Bcl-2Homo sapiens (human)
post-embryonic developmentApoptosis regulator Bcl-2Homo sapiens (human)
response to iron ionApoptosis regulator Bcl-2Homo sapiens (human)
response to UV-BApoptosis regulator Bcl-2Homo sapiens (human)
response to gamma radiationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of gene expressionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of autophagyApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
regulation of glycoprotein biosynthetic processApoptosis regulator Bcl-2Homo sapiens (human)
mesenchymal cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of smooth muscle cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
cochlear nucleus developmentApoptosis regulator Bcl-2Homo sapiens (human)
gland morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
regulation of transmembrane transporter activityApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of ossificationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell growthApoptosis regulator Bcl-2Homo sapiens (human)
melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cell migrationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of B cell proliferationApoptosis regulator Bcl-2Homo sapiens (human)
hair follicle morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
axon regenerationApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein stabilityApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum calcium ion homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
glomerulus developmentApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of cellular pH reductionApoptosis regulator Bcl-2Homo sapiens (human)
regulation of protein localizationApoptosis regulator Bcl-2Homo sapiens (human)
myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of myeloid cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
T cell differentiation in thymusApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationApoptosis regulator Bcl-2Homo sapiens (human)
osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of osteoblast proliferationApoptosis regulator Bcl-2Homo sapiens (human)
response to nicotineApoptosis regulator Bcl-2Homo sapiens (human)
organ growthApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of multicellular organism growthApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to glucose starvationApoptosis regulator Bcl-2Homo sapiens (human)
response to hydrogen peroxideApoptosis regulator Bcl-2Homo sapiens (human)
neuron maturationApoptosis regulator Bcl-2Homo sapiens (human)
T cell homeostasisApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
CD8-positive, alpha-beta T cell lineage commitmentApoptosis regulator Bcl-2Homo sapiens (human)
ear developmentApoptosis regulator Bcl-2Homo sapiens (human)
regulation of viral genome replicationApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of melanocyte differentiationApoptosis regulator Bcl-2Homo sapiens (human)
retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of retinal cell programmed cell deathApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane permeabilityApoptosis regulator Bcl-2Homo sapiens (human)
focal adhesion assemblyApoptosis regulator Bcl-2Homo sapiens (human)
spleen developmentApoptosis regulator Bcl-2Homo sapiens (human)
thymus developmentApoptosis regulator Bcl-2Homo sapiens (human)
digestive tract morphogenesisApoptosis regulator Bcl-2Homo sapiens (human)
oocyte developmentApoptosis regulator Bcl-2Homo sapiens (human)
skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
positive regulation of skeletal muscle fiber developmentApoptosis regulator Bcl-2Homo sapiens (human)
pigment granule organizationApoptosis regulator Bcl-2Homo sapiens (human)
stem cell developmentApoptosis regulator Bcl-2Homo sapiens (human)
homeostasis of number of cells within a tissueApoptosis regulator Bcl-2Homo sapiens (human)
B cell receptor signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
response to glucocorticoidApoptosis regulator Bcl-2Homo sapiens (human)
neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
defense response to virusApoptosis regulator Bcl-2Homo sapiens (human)
establishment of localization in cellApoptosis regulator Bcl-2Homo sapiens (human)
regulation of mitochondrial membrane potentialApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of mitochondrial depolarizationApoptosis regulator Bcl-2Homo sapiens (human)
hematopoietic stem cell differentiationApoptosis regulator Bcl-2Homo sapiens (human)
calcium ion transport into cytosolApoptosis regulator Bcl-2Homo sapiens (human)
T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of T cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to organic substanceApoptosis regulator Bcl-2Homo sapiens (human)
cellular response to hypoxiaApoptosis regulator Bcl-2Homo sapiens (human)
reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
cell-cell adhesionApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorApoptosis regulator Bcl-2Homo sapiens (human)
epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of epithelial cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of G1/S transition of mitotic cell cycleApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of dendritic cell apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of motor neuron apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of anoikisApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayApoptosis regulator Bcl-2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageApoptosis regulator Bcl-2Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandApoptosis regulator Bcl-2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processApoptosis regulator Bcl-2Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
apoptotic processDeath-associated protein kinase 1Homo sapiens (human)
defense response to tumor cellDeath-associated protein kinase 1Homo sapiens (human)
regulation of response to tumor cellDeath-associated protein kinase 1Homo sapiens (human)
protein phosphorylationDeath-associated protein kinase 1Homo sapiens (human)
apoptotic processDeath-associated protein kinase 1Homo sapiens (human)
extrinsic apoptotic signaling pathway via death domain receptorsDeath-associated protein kinase 1Homo sapiens (human)
regulation of autophagyDeath-associated protein kinase 1Homo sapiens (human)
positive regulation of autophagyDeath-associated protein kinase 1Homo sapiens (human)
negative regulation of translationDeath-associated protein kinase 1Homo sapiens (human)
intracellular signal transductionDeath-associated protein kinase 1Homo sapiens (human)
regulation of apoptotic processDeath-associated protein kinase 1Homo sapiens (human)
positive regulation of apoptotic processDeath-associated protein kinase 1Homo sapiens (human)
negative regulation of apoptotic processDeath-associated protein kinase 1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processDeath-associated protein kinase 1Homo sapiens (human)
protein autophosphorylationDeath-associated protein kinase 1Homo sapiens (human)
cellular response to type II interferonDeath-associated protein kinase 1Homo sapiens (human)
cellular response to hydroperoxideDeath-associated protein kinase 1Homo sapiens (human)
apoptotic signaling pathwayDeath-associated protein kinase 1Homo sapiens (human)
positive regulation of autophagic cell deathDeath-associated protein kinase 1Homo sapiens (human)
regulation of NMDA receptor activityDeath-associated protein kinase 1Homo sapiens (human)
apoptotic processE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
protein ubiquitinationE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
regulation of cell cycleE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
regulation of biological qualityE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
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)
DNA damage responseInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
response to cytokineInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cell fate determinationInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of autophagyInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cellular homeostasisInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
positive regulation of apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein transmembrane transportInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
positive regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of anoikisInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial fusionInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
release of cytochrome c from mitochondriaInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
protein peptidyl-prolyl isomerizationPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
protein foldingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
apoptotic processPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
protein transportPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
viral release from host cellPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
lipid droplet organizationPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
positive regulation of apoptotic processPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
positive regulation of viral genome replicationPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
positive regulation of protein secretionPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
chaperone-mediated protein foldingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
protein-containing complex assemblyPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
cellular response to UV-APeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (92)

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)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
protease bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
channel activityApoptosis regulator Bcl-2Homo sapiens (human)
channel inhibitor activityApoptosis regulator Bcl-2Homo sapiens (human)
ubiquitin protein ligase bindingApoptosis regulator Bcl-2Homo sapiens (human)
identical protein bindingApoptosis regulator Bcl-2Homo sapiens (human)
sequence-specific DNA bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein heterodimerization activityApoptosis regulator Bcl-2Homo sapiens (human)
BH3 domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
protein phosphatase 2A bindingApoptosis regulator Bcl-2Homo sapiens (human)
molecular adaptor activityApoptosis regulator Bcl-2Homo sapiens (human)
DNA-binding transcription factor bindingApoptosis regulator Bcl-2Homo sapiens (human)
BH domain bindingApoptosis regulator Bcl-2Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
protein kinase activityDeath-associated protein kinase 1Homo sapiens (human)
protein serine/threonine kinase activityDeath-associated protein kinase 1Homo sapiens (human)
calmodulin-dependent protein kinase activityDeath-associated protein kinase 1Homo sapiens (human)
protein bindingDeath-associated protein kinase 1Homo sapiens (human)
calmodulin bindingDeath-associated protein kinase 1Homo sapiens (human)
ATP bindingDeath-associated protein kinase 1Homo sapiens (human)
GTP bindingDeath-associated protein kinase 1Homo sapiens (human)
syntaxin-1 bindingDeath-associated protein kinase 1Homo sapiens (human)
identical protein bindingDeath-associated protein kinase 1Homo sapiens (human)
protein serine kinase activityDeath-associated protein kinase 1Homo sapiens (human)
5S rRNA bindingE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
identical protein bindingE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
ribonucleoprotein complex bindingE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
ubiquitin bindingE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
metal ion bindingE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
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)
protein bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein transmembrane transporter activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
protein heterodimerization activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
BH3 domain bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
channel activityInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
BH domain bindingInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
peptidyl-prolyl cis-trans isomerase activityPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
protein bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
transcription factor bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
cyclosporin A bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
nuclear estrogen receptor bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
Hsp70 protein bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
heat shock protein bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
Hsp90 protein bindingPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
nucleusProtein Mdm4Homo sapiens (human)
nucleoplasmProtein Mdm4Homo sapiens (human)
transcription repressor complexProtein Mdm4Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulum membraneApoptosis regulator Bcl-2Homo sapiens (human)
nucleusApoptosis regulator Bcl-2Homo sapiens (human)
cytoplasmApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrionApoptosis regulator Bcl-2Homo sapiens (human)
mitochondrial outer membraneApoptosis regulator Bcl-2Homo sapiens (human)
endoplasmic reticulumApoptosis regulator Bcl-2Homo sapiens (human)
cytosolApoptosis regulator Bcl-2Homo sapiens (human)
membraneApoptosis regulator Bcl-2Homo sapiens (human)
nuclear membraneApoptosis regulator Bcl-2Homo sapiens (human)
myelin sheathApoptosis regulator Bcl-2Homo sapiens (human)
BAD-BCL-2 complexApoptosis regulator Bcl-2Homo sapiens (human)
protein-containing complexApoptosis regulator Bcl-2Homo sapiens (human)
pore complexApoptosis regulator Bcl-2Homo sapiens (human)
cytosolE3 ubiquitin-protein ligase Mdm2Mus musculus (house mouse)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
cytoplasmDeath-associated protein kinase 1Homo sapiens (human)
plasma membraneDeath-associated protein kinase 1Homo sapiens (human)
postsynaptic densityDeath-associated protein kinase 1Homo sapiens (human)
actin cytoskeletonDeath-associated protein kinase 1Homo sapiens (human)
glutamatergic synapseDeath-associated protein kinase 1Homo sapiens (human)
DAPK1-calmodulin complexDeath-associated protein kinase 1Homo sapiens (human)
cytoplasmDeath-associated protein kinase 1Homo sapiens (human)
nucleusDeath-associated protein kinase 1Homo sapiens (human)
nucleusE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
nucleoplasmE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
nucleolusE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
cytoplasmE3 ubiquitin-protein ligase Mdm2Canis lupus familiaris (dog)
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)
nucleusInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
nucleoplasmInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytoplasmInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrionInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial outer membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
cytosolInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
Bcl-2 family protein complexInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
mitochondrial outer membraneInduced myeloid leukemia cell differentiation protein Mcl-1Homo sapiens (human)
nucleusPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
nucleoplasmPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
nucleolusPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
cytosolPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
cytosolPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase DHomo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (378)

Assay IDTitleYearJournalArticle
AID756930Induction of apoptosis in human MCF7 cells assessed as early apoptotic cells at 3 uM after 24 to 72 hrs by annexin V-FITC/propidium iodide staining based FACS flow cytometry (Rvb = 4 %)2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1125680Binding affinity to HDM2 (unknown origin) by fluorescence polarization peptide displacement assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
AID1908076Displacement of 5-FAM labeled PDI peptide from MDM4 C17S mutant (14 to 111 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant incubated for 1.5 hrs by fluorescence polarization competition assay
AID756946Cytotoxicity against human HGF cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID748499Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID706602Inhibition of human MDM2-p53 interaction after 18 hrs by HTRF assay in presence of 15% human serum2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID1238620Inhibition of MDM2/p53 interaction (unknown origin) using biotinylated MDM2 and Cy5-p53 (18 to 26 amino acids) by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1285810Upregulation of p53 in human MCF7 cells after 24 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID621852Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1125677Permeability of the compound in human Caco2 cells2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
AID1908032Upregulation of p53 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis
AID1300940Decrease in procaspase-3 expression level in human p53-null HCT116 -/- cells at 10 uM after 24 hrs by western blot analysis2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID739072Inhibition of human recombinant GST-thrombin-MDM2 (1 to 188) expressed in Escherichia coli assessed as reduction of MDM2-p53 interaction incubated for 20 mins followed by p53 addition measured after 60 mins by HTRF assay in presence of 15% serum2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Rational design and binding mode duality of MDM2-p53 inhibitors.
AID541422Inhibition of human recombinant p53-MDM2 interaction assessed as p53 release by NMR spectroscopy relative to untreated control2010Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
Identification of the spiro(oxindole-3,3'-thiazolidine)-based derivatives as potential p53 activity modulators.
AID1296620Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at G1 phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 28%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID626520Inhibition of Mdm2-p53 protein interaction preincubated for 30 mins by fluorescence polarization assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction.
AID756944Inhibition of p53-MDM2 interaction (unknown origin) at 5 uM after 1 hr by ELISA2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1212290Drug uptake in C57BL/6 mouse plasma at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1366819Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID503026Antiproliferative activity against human MCF7 cells at 4 uM after 14 days by coomassie staining2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1908081Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID1155057Antiproliferative activity against human SK-UT-1 cells expressing p53 mutant protein by cell Titer-Glo assay2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
AID756938Cell cycle arrest in human MCF7 cells assessed as accumulation at G0/G1 phase at 3 uM after 24 to 72 hrs by propidium iodide staining-based FACS analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1361647Induction of apoptosis in human A549 cells assessed as viable cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 93.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID503032Induction of cell cycle arrest in human MCF7 cells 53BP1-targeting iRNA-based shRNA assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID749326Inhibition of p53-MDM2 (unknown origin) interaction expressed in Escherichia coli BL-21 (DE3) after 1 hr by fluorescence polarization assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1296639Binding affinity to 15N-labeled Bcl-2 (unknown origin) by 2D 1H-15N HSQC NMR spectroscopic method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1143658Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID738689Inhibition of MDM2 (unknown origin) assessed as activation of p532013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID415699Inhibition of interaction between human DMX(1-555) and p53 at upto 30 uM2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
Beta-peptides with improved affinity for hDM2 and hDMX.
AID1296597Displacement of FAM-Bid peptide from N-terminal 8x His-tagged MCl-1 (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1908031Upregulation of MDM2 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis
AID739073Inhibition of human recombinant GST-thrombin-MDM2 (1 to 188) expressed in Escherichia coli assessed as reduction of MDM2-p53 interaction incubated for 20 mins followed by p53 addition measured after 60 mins by HTRF assay2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Rational design and binding mode duality of MDM2-p53 inhibitors.
AID1212300Drug uptake in C57BL/6 mouse liver at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID362381Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
NMR screening for lead compounds using tryptophan-mutated proteins.
AID707326Inhibition of p53-MDM2 interaction after 1 hr by fluorescence polarization assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID265955Displacement of PMDM6-F from human recombinant MDM22006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
AID438432Induction of p21 mRNA in human HCT116 cells by RT-PCR2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID738714Antiproliferative activity against human RKO cells expressing wild type p53 after 5 days by MTS assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID587349Inhibition of human GST-tagged Mdm2 expressed in Escherichia coli harboring integrated p53-Mmd2 protein assessed as blockade of enzyme-p53 interaction by ELISA assay2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
AID1300910Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1361650Induction of apoptosis in human A549 cells assessed as necrotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 0.52%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1249875Activation of p53 in human U2OS cells assessed as increase of MDM2 expression at 2.5 uM after 12 hrs by Western blotting2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Discovery of Novel Isatin-Based p53 Inducers.
AID1212292Drug uptake in C57BL/6 mouse adrenal gland at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID749490Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID621851Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1674908Inhibition of P-gp-mediated Rhodamine-123 efflux in human p53 +/+ H1299 cells assessed as Rhodamine-123 accumulation measured after 40 mins by spectrofluorimetry2020Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
Mdm2 inhibitors as a platform for the design of P-glycoprotein inhibitors.
AID362385Binding affinity to human recombinant Mdm2 F55W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
NMR screening for lead compounds using tryptophan-mutated proteins.
AID1908078Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID1361624Growth inhibition of Saccharomyces cerevisiae expressing p53 at 10 uM after 42 hrs by Yeast-based assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID749488Inhibition of p53/MDM2 (1 to 118) (unknown origin) interaction at 10 uM after 1 hr by fluorescence polarization assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID1285800Inhibition of Flag-tagged p53/GST-tagged Mdm2 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1300908Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1361627Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1361653Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.37%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1195733Cytotoxicity against human RKO cells2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID749491Inhibition of p53/MDM2 (1 to 118) (unknown origin) interaction after 1 hr by fluorescence polarization assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID503037Induction of p53 accumulation in human MCF7 cells after 18 hrs by Western blot analysis in presence of 2.5 mM caffeine2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1296633Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID749324Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1361625Growth inhibition of Saccharomyces cerevisiae expressing MDM2 at 10 uM after 42 hrs by Yeast-based assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID1285803Inhibition of Flag-tagged p53/GST-tagged PPID (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID756857Inhibition of MDM2-P53 interaction in human SJSA1 cells assessed as p53-mediated decrease in full length PARP level at 24 hrs by Western blot analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID1212304Drug uptake in C57BL/6 mouse lung at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1659344Inhibition of MDM2 (unknown origin) by HTRF assay2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.
AID1296640Binding affinity to 15N-labeled MDM2 (unknown origin) by 2D 1H-15N HSQC NMR spectroscopic method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID736743Inhibition of human p53 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell cycle arrest at 10 uM after 42 hrs2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1285816Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as decrease in tumor growth at 150 mg/kg/day, po administered every other day until day 38 and measured on day 402016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1720556Inhibition of human MDM2-p53 interaction2020Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13
A critical update on the strategies towards modulators targeting androgen receptors.
AID1908070Inhibition of GST-tagged MDM2/Biotin-tagged p53 interaction (unknown origin) incubated for 40 mins by TR-FRET assay
AID1060451Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1155058Ratio of IC50 for human SK-UT-1 cells expressing p53 mutant protein to IC50 for human SJSA1 cells expressing wild type p53 protein2014ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.
AID1057111Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID503033Induction of p53 expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1296632Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1143671Induction of apoptosis in human HCT116 cells assessed as accumulation at G2 phase at 20 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1361637Inhibition of MDM2/P53 interaction in human A549 cells assessed as increase in MDM2 expression after 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
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.
AID1632470Inhibition of C-terminal biotin-tagged streptavidin labelled human MDM2 ( 2 to 188 residues)/Cy5-labelled p53 (18 to 26 residues)(unknown origin) interaction after 15 mins by TR-FRET assay2016Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.
AID1387292Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID588009Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of MDM2 protein at 1 to 10 uM after 6 hrs by Western blot analysis2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1296626Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at G2/M phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 35%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID756926Induction of apoptosis in human MCF7 cells assessed as increase in p21 expression level at 3 uM after 24 to 72 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1361648Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.10%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1361626Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1212302Drug uptake in C57BL/6 mouse plasma at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1238647Inhibition of rat MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1361643Cell cycle arrest in human A549 cells assessed as accumulation of cells at G2 phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 19.81%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID748501Inhibition of N-terminal human recombinant MDM2 assessed as inhibition of protein interaction with p53 by HTRF assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID738727Antiproliferative activity against human MDA-MB-435S cells harboring p53 mutant at 10 uM after 5 days by MTS assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID1060449Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1296634Inhibition of Mcl-1/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID748504Apparent half life in mouse at 100 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID1212283Ratio of drug level in blood to plasma in C57BL/6 mouse after 30 mins2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1238675Inhibition of human MDM4 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID503024Induction of cell cycle arrest in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID442457Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation at 10 uM by Western blot2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.
AID621853Growth inhibition of human A2780 cells expressing MDM2 by SRB assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1392508Cytotoxicity against human U2OS cells harboring p53-dependent EGFP reporter gene assessed as reduction in cell viability at 30 uM after 48 hrs2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, in silico prioritization and biological profiling of apoptosis-inducing lactams amenable by the Castagnoli-Cushman reaction.
AID503034Induction of p53 expression in human MCF7 cells by Western blot analysis2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID425673Inhibition of GST-tagged MDM2 (1-150) / full-length His6-tagged p53 interaction expressed in Escherichia coli by alphascreen assay2009Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.
AID1361646Cell cycle arrest in human A549 cells assessed as accumulation of cells at G2 phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 19.81%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID756948Cytotoxicity against human Calu cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID626522Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction.
AID1908079Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID1656003Solubility of compound in PBS2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
AID707325Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1361631Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1212285Fraction unbound in C57BL/6 mouse plasma at 300 uM up to 24 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1285814Increase in p53 expression in human MCF7 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1908093Induction of PARP cleavage in human RKO cells at 0.3125 to 2.5 uM incubated for 24 hrs by Western blot analysis
AID1361644Cell cycle arrest in human A549 cells assessed as accumulation of cells at G1 phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 49.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1143670Induction of apoptosis in human HCT116 cells assessed as accumulation at S phase at 20 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1908055Upregulation of p53 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis
AID1565005Induction of apoptosis in human HCT116 cells expressing wild type p53 assessed as live cells at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 83.7 %)2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1908092Downregulation of MDM4 expression in human RKO cells at 0.3125 to 2.5 uM incubated for 24 hrs by Western blot analysis
AID1060450Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID588013Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID587948Inhibition of Mdm2 -p53 protein interaction by ELISA2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1212294Drug uptake in C57BL/6 mouse muscle at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1296607Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p53 expression after 12 hrs by immunoblotting method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID438434Induction of apoptosis in human SJSA1 cells assessed as caspase 3/7 activity after 48 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID746383Antagonist activity at human GST-tagged MDM2 assessed as inhibition of binding to full length p532013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Inhibitors of the p53/hdm2 protein-protein interaction-path to the clinic.
AID1125681Antiproliferative activity against human SJSA1 cells2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
AID1212296Drug uptake in C57BL/6 mouse brain at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1143669Induction of apoptosis in human HCT116 cells assessed as accumulation at G1 phase at 20 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID588016Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1908058Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID1239847Inhibition of p53-MDM2 interaction (unknown origin) by TR-FRET assay2015Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.
AID1285811Upregulation of p21 in human MCF7 cells after 24 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID453614Binding to HDM2 expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy competition method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.
AID1908028Upregulation of p53 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis
AID1565006Induction of apoptosis in human HCT116 cells expressing wild type p53 assessed as early apoptotic cells expressing wild type p53 at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 8.8 %)2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1296623Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at S phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 42%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1296624Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at G1 phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 31%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1057102Ratio of IC50 for human H1299 cells to IC50 for human HCT116 cells2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID707311Induction of apoptosis in human A549 cells expressing wild type p53 at 20 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1908077Displacement of 5-FAM labeled PDI peptide from MDM2 (1 to 118 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant incubated for 1.5 hrs by fluorescence polarization competition assay
AID700922Inhibition of HDM2 binding to p532012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
Chemical modulators working at pharmacological interface of target proteins.
AID503039Induction of apoptosis in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1361641Cell cycle arrest in human A549 cells assessed as accumulation of cells at G1 phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 49.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID438435Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID1060441Inhibition of p53-MDM2 (unknown origin) interaction expressed in p53-deficient human HCT116 cells at 50 uM after 24 hrs by BiFC-based FACS flow cytometric analysis2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1143674Induction of apoptosis in human HCT116 cells assessed as accumulation at G2 phase at 50 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 12.7%)2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1361623Growth inhibition of Saccharomyces cerevisiae expressing empty vector at 10 uM after 42 hrs by Yeast-based assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID1192743Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID1060447Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents.
AID1212301Drug uptake in C57BL/6 mouse spleen at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1212297Drug uptake in C57BL/6 mouse bone marrow at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID621854Growth inhibition of human A2780/CP70 cells expressing isogenically paired p53 mutant by SRB assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1908053Upregulation of p21 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis
AID1361654Induction of apoptosis in human A549 cells assessed as necrotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 0.52%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID318566Binding affinity to human HDM2 assessed as inhibition of HDM2-p53 interaction2007Nature, Dec-13, Volume: 450, Issue:7172
Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.
AID503025Induction of cell cycle arrest in human MCF7 cells transfected hnRNPK-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1212295Drug uptake in C57BL/6 mouse retina at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1908027Upregulation of p21 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis
AID1565008Induction of apoptosis in human HCT116 cells expressing wild type p53 assessed as necrotic cells at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 0.7 %)2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1238650Selectivity index, ratio of Ki for rat MDM2 to Ki for human MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1872997Inhibition of recombinant human MDM2/p53 interaction by Biacore's surface plasmon resonance analysis2022European journal of medicinal chemistry, Jun-05, Volume: 236Small-molecule MDM2 inhibitors in clinical trials for cancer therapy.
AID1296625Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at S phase at 10 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 36%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1300246Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
AID1656006Inhibition of 6xHis-taged MDM2 (unknown origin) expressed in Escherichia coli Gold (DE3)2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
AID1195731Cytotoxicity against human SJSA1 cells2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID1654661Inhibition of mdm2 in human ARN8 cells assessed as induction of DNA damage by measuring increase in p53 phosphorylation at Ser15 at 2 uM incubated for 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
AID1633977Inhibition of MDM2/P53 interaction in human RKO cells assessed as ratio of p53 to GAPDH level at 20 uM after 24 hrs by Western blot analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID587354Induction of p53-dependent luciferase activity in human U2OS cells at 5 uM relative to control2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
AID1195732Cytotoxicity against human HCT116 cells2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID1143668Induction of apoptosis in human HCT116 cells assessed as accumulation at G2 phase at 10 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID362383Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
NMR screening for lead compounds using tryptophan-mutated proteins.
AID1300941Decrease in procaspase-9 expression level in human p53-null HCT116 -/- cells at 10 uM after 24 hrs by western blot analysis2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1361628Inhibition of MDM2 (unknown origin) preincubated for 30 mins by fluorescence polarization assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1212293Drug uptake in C57BL/6 mouse lung at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1555409Inhibition of p53 protein binding to MDM2 (unknown origin)2019European journal of medicinal chemistry, Aug-15, Volume: 176The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy.
AID1420852Inhibition of recombinant p53 protein binding to recombinant human MDM2 by surface plasmon resonance method2018European journal of medicinal chemistry, Oct-05, Volume: 158Role of p53 circuitry in tumorigenesis: A brief review.
AID1366814Inhibition of MDM2/p53 interaction in human U2OS cells assessed as p53 activation by measuring EGFP-positive cells at 10 uM after 24 hrs by Hoechst 33258 staining based fluorescence microscopic analysis relative to control2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID738716Antiproliferative activity against human HCT116 cells expressing wild type p53 after 5 days by MTS assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID588014Cytotoxicity against human LS cells after 72 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1387289Inhibition of human MDM2 (1 to 125 residues) and p53 (unknown origin) interaction pre-incubated for 20 mins before peptide-2-biot addition and measured after 3 hrs by HTRF assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID1296635Inhibition of Mcl-1/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1252240Inhibition of human MDM2 (17 to 125 residues) assessed as reduction in MDM2 interaction with FAM-LTFEHYWAQLTS-CONH2 peptide incubated for 30 mins by fluorescence polarisation assay2015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin.
AID1152866Binding affinity to MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by fluorescence polarization binding assay2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
Discovery of 1-arylpyrrolidone derivatives as potent p53-MDM2 inhibitors based on molecule fusing strategy.
AID1654653Inhibition of mdm2 in human ARN8 cells assessed as increase in p53 level at 2 uM incubated for 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
AID1633983Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 80 uM after 24 hrs by Western blot analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID1212284Fraction unbound in C57BL/6 mouse plasma at 0.1 uM up to 24 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID748498Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID1361619Inhibition of human MDM2-p53 interaction in Saccharomyces cerevisiae assessed as p53 induced cell growth arrest at 10 uM after 42 hrs by Yeast-based assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity.
AID756940Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reduction in p53 level bound to MDM2 after 24 hrs by immunoprecipitation assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1908080Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID503036Induction of p53 expression in human MCF7 cells assessed as increase in p21CIP1 level after 18 hrs by Western blot method in presence of 2.5 mM caffeine2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1143657Binding affinity to MDM2 (1 to 118) (unknown origin) after 30 mins by fluorescence polarization assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1366812Induction of apoptosis in human U2OS cells at 10 uM after 24 hrs by Annexin V-FITC/propidium iodide based FACS analysis (Rvb= 0.1%)2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID756860Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation after 24 hrs by Western blot analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID1212308Drug uptake in C57BL/6 mouse bone marrow at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1366818Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID438433Inhibition of human HCT116 cell proliferation after 16 hrs by BrdU assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID756953Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID658338Inhibition of p53 (18 to 26)-MDM2 (2 to 188) interaction using fluorescent dye Cy5 by TR-FRET assay2012Bioorganic & medicinal chemistry letters, May-15, Volume: 22, Issue:10
The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.
AID1372140Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay2018Bioorganic & medicinal chemistry, 03-15, Volume: 26, Issue:6
Unique arginine array improves cytosolic localization of hydrocarbon-stapled peptides.
AID736737Inhibition of human MDM2-p53 interaction expressed in Saccharomyces cerevisiae CG379 assessed as reversal of MDM2-dependent inhibition of p53-induced S-phase cell cycle arrest at 10 uM after 42 hrs by Sytox Green-based flow cytometric analysis2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1238649Selectivity index, ratio of Ki for mouse MDM2 to Ki for human MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID588017Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID756858Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as accumulation of p21 after 24 hrs by Western blot analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID1175611Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors.
AID1654654Inhibition of mdm2 in human ARN8 cells assessed as increase in p53 level at 2 uM incubated for 24 hrs in presence of 100 uM de novo pyrimidine ribonucleotide synthesis pathway inhibitor, uridine by Western blot analysis2020Journal of medicinal chemistry, 04-23, Volume: 63, Issue:8
Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.
AID503028Antiproliferative activity against human MCF7 cells transfected with p53-targeting iRNA-based shRNA assessed as effect on cellular morphology at 4 uM after 14 days by coomassie staining2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1564997Displacement of 5'FAM-LTFEHYWAQLTS from human recombinant N-terminal domain of MDM2 (1 to 118 residues) expressed in Escherichia coli BL21 (DE3) cells measured after 15 mins by fluorescence polarization assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1192744Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID706604Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID756951Cytotoxicity against human PC3 cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1908060Upregulation of p21 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis
AID1285813Increase in p53 expression in human IMR32 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1361651Induction of apoptosis in human A549 cells assessed as viable cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 93.01%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1565010Inhibition of MDM2-p53 interaction in human SJSA1 cells expressing wild-type p53 assessed as upregulation of p21 expression at 5 uM measured after 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID453615Binding to GST-tagged HDMX expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy competition method2009Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53.
AID1296609Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of MDM2 expression after 12 hrs by immunoblotting method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1296599Displacement of FAM-p53TAD peptide from N-terminal 8x His-tagged human MDM2 (25 to 108 residues) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1908071Inhibition of GST-tagged MDM4/Biotin-tagged p53 interaction (unknown origin) incubated for 40 mins by TR-FRET assay
AID503042Induction of apoptosis in human MCF7 cells co-transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1633982Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 40 uM after 24 hrs by Western blot analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID1908083Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID756952Cytotoxicity against human U937 cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID267242Binding affinity to MDM22006Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
AID1361649Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 1 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.37%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID707324Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1908090Upregulation of p21 expression in human RKO cells incubated for 24 hrs by Western blot analysis
AID684828Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay2012European journal of medicinal chemistry, Oct, Volume: 56Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID1908082Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay
AID1908089Upregulation of p53 expression in human RKO cells incubated for 24 hrs by Western blot analysis
AID362384Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
NMR screening for lead compounds using tryptophan-mutated proteins.
AID1212310Drug uptake in C57BL/6 mouse adipose tissue at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1366813Inhibition of MDM2/p53 interaction in human U2OS cells assessed as p53 activation by measuring EGFP-positive cells after 24 hrs by Hoechst 33258 staining based fluorescence microscopic analysis2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID707310Induction of apoptosis in human A549 cells expressing wild type p53 after 48 hrs using annexin V-FITC staining by flow cytometry assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID749325Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1212305Drug uptake in C57BL/6 mouse muscle at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1633968Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 20 uM after 24 hrs by Western blot analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID1057110Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID415698Inhibition of interaction between human DM2(1-549) and p532009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
Beta-peptides with improved affinity for hDM2 and hDMX.
AID1366815Inhibition of MDM2/p53 interaction in human U2OS cells by assessed as p53 activation measuring EGFP-positive cells at 5 uM after 24 hrs by Hoechst 33258 staining based fluorescence microscopic analysis relative to control2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID1057105Induction of p53 translocation in human HCT116 cells assessed as protein nuclear to cytosolic ratio at 3.3 uM after 20 hrs by immunofluorescence analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID1212306Drug uptake in C57BL/6 mouse retina at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID707312Induction of apoptosis in human A549 cells expressing wild type p53 at 10 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1212307Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID438431Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID1192746Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID503029Antiproliferative activity against human A549 cells transfected with 53BP1-targeting iRNA-based shRNA assessed as effect on cellular morphology at 4 uM after 14 days by coomassie staining2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1361659Antitumor activity against human A549 cells xenografted in BALB/C nude mouse assessed as inhibition of tumor growth at 100 mg/kg, po administered once daily for 21 days starting day 11 after tumor cells implantation2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1565009Inhibition of MDM2-p53 interaction in human SJSA1 cells expressing wild-type p53 assessed as upregulation of MDM2 expression at 5 uM measured after 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1296608Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at 2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1565011Inhibition of MDM2-p53 interaction in human U2OS cells expressing wild-type p53 assessed as upregulation of MDM2 expression at 5 uM measured after 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID755375Antitumor activity against human MV4-11 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 200 mg/kg/day, po bid administered on day 21 to 24 and day 27 to 30 measured on day 31 relative to control2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.
AID756920Induction of apoptosis in human MCF7 cells assessed as accumulation of caspase-3 cleavage product at 50 nM after 24 to 72 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1366820Inhibition of MDM2/p53 (unknown origin) complex at 10 uM by ELISA2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors.
AID1238646Inhibition of mouse MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1503133Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay
AID1421138Inhibition of Cy5-labeled p53 derived TFSDLWKLL peptide binding to C-terminal biotin-labelled human MDM2 (2 to 188 residues) by TR-FRET assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.
AID438437Inhibition of human p21 deficient HCT116 cell proliferation after 16 hrs by BrdU assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID756933Induction of apoptosis in human MCF7 cells assessed as accumulation at subG1 phase at 3 uM by propidium iodide staining-based FACS analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID684826Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay2012European journal of medicinal chemistry, Oct, Volume: 56Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID756922Induction of apoptosis in human MCF7 cells assessed as increase in Bcl-xS expression level at 3 uM after 24 to 72 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID588015Cytotoxicity against human NGP cells after 72 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID1212299Drug uptake in C57BL/6 mouse intestine at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID503027Antiproliferative activity against human MCF7 cells assessed as appearance of flattened phenotype at 4 uM after 14 days by coomassie staining2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1908026Upregulation of MDM2 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis
AID1212303Drug uptake in C57BL/6 mouse adrenal gland at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID425674Inhibition of GST-tagged MDM2/His6-tagged p53 interaction by surface plasmon resonance study2009Bioorganic & medicinal chemistry letters, Jul-15, Volume: 19, Issue:14
Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking.
AID755374Toxicity in NOD/SCID mouse xenografted with human MV4-11 cells assessed as body weight loss at 200 mg/kg/day, po bid administered on day 21 to 24 and day 27 to 30 measured every 2 days during compound administration relative to control2013Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.
AID1387293Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID707323Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID748502AUClast in mouse at 100 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID706601Inhibition of human MDM2-p53 interaction after 18 hrs by HTRF assay2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID1285802Inhibition of Flag-tagged p53/GST-tagged DAPK1 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID707317Inhibition of p53-MDMX interaction after 1 hr by fluorescence polarization assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID684829Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay2012European journal of medicinal chemistry, Oct, Volume: 56Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID1908049Downregulation of MDM4 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis
AID1143672Induction of apoptosis in human HCT116 cells assessed as accumulation at G1 phase at 50 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 62.5%)2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1503134Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay
AID749489Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay2013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.
AID1238648Selectivity index, ratio of Ki for dog MDM2 to Ki for human MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1361636Inhibition of MDM2/P53 interaction in human A549 cells assessed as increase in p53 expression after 24 hrs by Western blot analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID621850Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.
AID1212289Drug uptake in C57BL/6 mouse spleen at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1249873Stabilization of p53 in human U2OS cells assessed as intracellular p53 level at 2.5 uM after 12 hrs by Western blotting2015ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
Discovery of Novel Isatin-Based p53 Inducers.
AID1633969Inhibition of MDM2/P53 interaction in human A549 cells assessed as ratio of p53 to GAPDH level at 10 uM after 24 hrs by Western blot analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID756949Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1143673Induction of apoptosis in human HCT116 cells assessed as accumulation at S phase at 50 uM after 48 hrs by propidium iodide staining-based flow cytometry (Rvb = 24.8%)2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1285812Upregulation of Mdm2 in human MCF7 cells after 24 hrs by Western blot analysis2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1238645Inhibition of dog MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1300245Inhibition of human recombinant His-tagged MDM2 (1 to 118 residues) interaction with FAM-tagged p53-based peptide (unknown origin) incubated for 15 mins by fluorescence polarization assay2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.
AID1212287Drug uptake in C57BL/6 mouse intestine at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1143660Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID756925Induction of apoptosis in human MCF7 cells assessed as reduction in Bcl-xL expression level at 3 uM after 24 to 72 hrs by Western blotting analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1143661Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID438436Inhibition of human p53 deficient HCT116 cell proliferation after 16 hrs by BrdU assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
AID1212298Drug uptake in C57BL/6 mouse vitreous humor at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1195730Binding affinity to MDM2 (unknown origin)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID503038Induction of p21CIP1 expression in irradiated human BJ cells at 3 uM by Western blot analysis2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1212309Drug uptake in C57BL/6 mouse vitreous humor at 10 mg/kg, iv as single dose measured at 24 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID503031Induction of cell cycle arrest in human MCF7 cells p53-targeting iRNA-based shRNA assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID626521Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of thio-benzodiazepines as novel small molecule inhibitors of the p53-MDM2 protein-protein interaction.
AID1908047Effect on MDM4 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis
AID707327Induction of apoptosis in human A549 cells expressing wild type p53 at 5 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID684827Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay2012European journal of medicinal chemistry, Oct, Volume: 56Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID736742Inhibition of human MDM2 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell cycle arrest after 42 hrs2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID417066Binding affinity to MDM22008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.
AID1565007Induction of apoptosis in human HCT116 cells assessed as late apoptotic cells expressing wild type p53 at 20 uM measured after 72 hrs by annexin V-FITC/propidium iodide staining-based flow cytometry analysis (Rvb = 6.8 %)2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID684825Inhibition of MDM2 binding domain assessed as inhibition of p53 binding to MDM2 after 1 hr by fluorescence polarization assay2012European journal of medicinal chemistry, Oct, Volume: 56Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors.
AID707322Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.
AID1143665Induction of apoptosis in human HCT116 cells after 48 hrs by propidium iodide staining-based flow cytometry2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1212286Cytotoxicity against doxorubicin-resistant human UKF-NB-3 cells after 96 hrs by MTT assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID588008Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p21 protein at 1 to 10 uM after 6 hrs by Western blot analysis2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID756859Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as MDM2 accumulation after 24 hrs by Western blot analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.
AID503035Induction of CDKN1A gene expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID243263Potency against MDM2 (murine double minute-2 gene) binding to p53; Range =100-300 nM2005Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
p53 Activation by small molecules: application in oncology.
AID1908039Effect on MDM4 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis
AID503041Induction of cell cycle arrest in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1415891Inhibition of 5'-FAM-LTFEHYWAQLTS binding to N-terminal domain of recombinant human MDM2 expressed in Escherichia coli BL21(DE3) after 15 mins by fluorescence polarization assay2017MedChemComm, May-01, Volume: 8, Issue:5
Scaffold hopping via ANCHOR.QUERY: β-lactams as potent p53-MDM2 antagonists
AID1296598Displacement of FAM-Bid peptide from N-terminal 8x His-tagged Bcl-2 (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by fluorescence polarization assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID736744Inhibition of human p53 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell growth at 10 uM after 42 hrs2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1908091Upregulation of MDM2 expression in human RKO cells incubated for 24 hrs by Western blot analysis
AID706603Activity at p53 in human SJSA1 cells assessed as induction of p21 mRNA expression after 7 hrs by qRT-PCR analysis in presence of 10% human serum2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
AID748500Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID738713Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 5 days by MTS assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID503030Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID588007Inhibition of Mdm2 -p53 protein interaction in human SNJSA1 cells assessed as induction of p53 protein at 1 to 10 uM after 6 hrs by Western blot analysis2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID587350Inhibition of human GST-tagged MDMX expressed in Escherichia coli harboring integrated p53-Hmd2 protein assessed as blockade of enzyme-p53 interaction by ELISA assay2011Bioorganic & medicinal chemistry letters, Mar-01, Volume: 21, Issue:5
Synthesis of cell-permeable stapled peptide dual inhibitors of the p53-Mdm2/Mdmx interactions via photoinduced cycloaddition.
AID1212291Drug uptake in C57BL/6 mouse adipose tissue at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID721248Inhibition of human p53/MDM2 interaction2013Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
Lead optimization of novel p53-MDM2 interaction inhibitors possessing dihydroimidazothiazole scaffold.
AID1300911Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID756947Cytotoxicity against human C643 cells after 24 hrs by MTT assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis, in vitro, and in cell studies of a new series of [indoline-3,2'-thiazolidine]-based p53 modulators.
AID1387291Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID738979Antiproliferative activity against human HeLa cells harboring p53 mutant at 10 uM after 5 days by MTS assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID1296621Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at 2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1143659Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1361652Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 5 uM after 48 hrs by FITC-Annexin V/propidium iodide staining based flow cytometric analysis (Rvb = 3.10%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1656007Binding affinity to 6xHis-taged MDM2 (unknown origin) expressed in Escherichia coli Gold (DE3) assessed as inhibition constant2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.
AID1192745Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents.
AID1361629Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1238644Inhibition of human MDM2 by TR-FRET assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
AID1908059Upregulation of MDM2 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis
AID1387290Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives.
AID588018Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
AID503040Antiproliferative activity against human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA assessed as effect on cellular morphology at 4 uM after 14 days by coomassie staining2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1296610Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p21 expression after 12 hrs by immunoblotting method2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID1361645Cell cycle arrest in human A549 cells assessed as accumulation of cells at S phase at 5 uM after 48 hrs by flow cytometric analysis (Rvb = 31.18%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID1195734Antitumor activity against human SJSA1 cells xenografted in mouse assessed as tumor growth inhibition at 200 mg/kg, po bid administered for 20 days2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.
AID1296622Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs by propidium iodide staining-based flow cytometric method (Rvb = 26%)2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
AID736738Inhibition of human MDM2-p53 interaction expressed in Saccharomyces cerevisiae CG379 assessed as reversal of MDM2-dependent inhibition of p53-induced growth inhibition at 10 uM after 42 hrs2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1633978Inhibition of MDM2/P53 interaction in human RKO cells assessed as ratio of p53 to GAPDH level at 10 uM after 24 hrs by Western blot analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
2,4,5-Tris(alkoxyaryl)imidazoline derivatives as potent scaffold for novel p53-MDM2 interaction inhibitors: Design, synthesis, and biological evaluation.
AID362378Binding affinity to human wild type Mdm2 by isothermal titration calorimetry2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
NMR screening for lead compounds using tryptophan-mutated proteins.
AID1378961Inhibition of V1-p53/MDM2-V2 (unknown origin) interaction expressed in human HCT116 p53-/- cells at 10 uM after 20 hrs by biomolecular fluorescence complementation-based flow cytometric analysis2017European journal of medicinal chemistry, Oct-20, Volume: 139In vitro targeting of colon cancer cells using spiropyrazoline oxindoles.
AID1300912Inhibition of HIF-1 (unknown origin) expressed in human MCF7 cells co-transfected with hypoxia reporter plasmid p(HRE)3-Luc at 20 uM measured under hypoxia condition after 24 hrs by dual-luciferase reporter assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID1580651Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay2019Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
Enhancing the Cell Permeability of Stapled Peptides with a Cyclic Cell-Penetrating Peptide.
AID1392511Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, in silico prioritization and biological profiling of apoptosis-inducing lactams amenable by the Castagnoli-Cushman reaction.
AID1361630Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID265956Antiproliferative activity against human LnCAP cell line with wild type p532006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
AID738725Antiproliferative activity against human SW480 cells harboring p53 mutant at 10 uM after 5 days by MTS assay2013Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
AID503043Induction of p21 expression in irradiated human BJ cells at 3 uM by Western blot analysis2006Nature chemical biology, Apr, Volume: 2, Issue:4
An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors.
AID1285801Inhibition of Flag-tagged p53/GST-tagged Mdmx (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities.
AID1057104Induction of p53 translocation in human HCT116 cells assessed as protein nuclear to cytosolic ratio at 10 uM after 20 hrs by immunofluorescence analysis2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Trisubstituted and tetrasubstituted pyrazolines as a novel class of cell-growth inhibitors in tumor cells with wild type p53.
AID1361642Cell cycle arrest in human A549 cells assessed as accumulation of cells at S phase at 1 uM after 48 hrs by flow cytometric analysis (Rvb = 31.18%)2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents.
AID736735Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reversal of MDM2-dependent inhibition of p53-induced transcriptional activity at 10 uM after 16 hrs by dual-luciferase reporter gene assay2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1212288Drug uptake in C57BL/6 mouse liver at 50 to 200 mg/kg, po as single dose measured at 2 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration.
AID1143667Induction of apoptosis in human HCT116 cells assessed as accumulation at S phase at 10 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1392512Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
Design, in silico prioritization and biological profiling of apoptosis-inducing lactams amenable by the Castagnoli-Cushman reaction.
AID1143666Induction of apoptosis in human HCT116 cells assessed as accumulation at G1 phase at 10 uM after 48 hrs by propidium iodide staining-based flow cytometry relative to control2014European journal of medicinal chemistry, Jun-23, Volume: 81Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
AID1300909Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Discovery and optimization of new benzofuran derivatives against p53-independent malignant cancer cells through inhibition of HIF-1 pathway.
AID748503Cmax in mouse at 100 mg/kg, po2013ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
AID362382Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
NMR screening for lead compounds using tryptophan-mutated proteins.
AID736736Inhibition of human MDM2-p53 interaction expressed in Saccharomyces cerevisiae CG379 assessed as reversal of MDM2-dependent inhibition of p53-induced transcriptional activity at 10 uM after 16 hrs by dual-luciferase reporter gene assay2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
AID1564998Displacement of 5'FAM-LTFEHYWAQLTS from human recombinant MDMX (18 to 111 residues) expressed in Escherichia coli BL21 (DE3) cells measured after 30 mins by fluorescence polarization assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID749323Selectivity ratio of IC50 for human p53-null PC3 cells to IC50 for human A549 cells expressing wild type p532013Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 1.
AID1565012Inhibition of MDM2-p53 interaction in human U2OS cells expressing wild-type p53 assessed as upregulation of p21 expression at 5 uM measured after 24 hrs by Western blot analysis2019European journal of medicinal chemistry, Nov-15, Volume: 182Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine 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.
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.
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.
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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2013Acta crystallographica. Section D, Biological crystallography, Aug, Volume: 69, Issue:Pt 8
The structure of an MDM2-Nutlin-3a complex solved by the use of a validated MDM2 surface-entropy reduction mutant.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (696)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's135 (19.40)29.6817
2010's501 (71.98)24.3611
2020's60 (8.62)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 35.84

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index35.84 (24.57)
Research Supply Index6.55 (2.92)
Research Growth Index4.85 (4.65)
Search Engine Demand Index52.41 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (35.84)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (0.14%)5.53%
Reviews28 (4.01%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other669 (95.85%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]