Assay ID | Title | Year | Journal | Article |
AID756930 | Induction 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 %) | 2013 | Journal 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. |
AID1125680 | Binding affinity to HDM2 (unknown origin) by fluorescence polarization peptide displacement assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
| Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction. |
AID1908076 | Displacement 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 | | | |
AID756946 | Cytotoxicity against human HGF cells after 24 hrs by MTT assay | 2013 | Journal 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. |
AID748499 | Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID706602 | Inhibition of human MDM2-p53 interaction after 18 hrs by HTRF assay in presence of 15% human serum | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-based design of novel inhibitors of the MDM2-p53 interaction. |
AID1238620 | Inhibition of MDM2/p53 interaction (unknown origin) using biotinylated MDM2 and Cy5-p53 (18 to 26 amino acids) by TR-FRET assay | 2015 | Journal 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. |
AID1285810 | Upregulation of p53 in human MCF7 cells after 24 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID621852 | Growth inhibition of p53 deficient human HCT116 cells expressing MDM2 by SRB assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. |
AID1125677 | Permeability of the compound in human Caco2 cells | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
| Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction. |
AID1908032 | Upregulation of p53 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1300940 | Decrease in procaspase-3 expression level in human p53-null HCT116 -/- cells at 10 uM after 24 hrs by western blot analysis | 2016 | Bioorganic & 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. |
AID739072 | Inhibition 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% serum | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Rational design and binding mode duality of MDM2-p53 inhibitors. |
AID541422 | Inhibition of human recombinant p53-MDM2 interaction assessed as p53 release by NMR spectroscopy relative to untreated control | 2010 | Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23
| Identification of the spiro(oxindole-3,3'-thiazolidine)-based derivatives as potential p53 activity modulators. |
AID1296620 | Cell 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%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID626520 | Inhibition of Mdm2-p53 protein interaction preincubated for 30 mins by fluorescence polarization assay | 2011 | European 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. |
AID756944 | Inhibition of p53-MDM2 interaction (unknown origin) at 5 uM after 1 hr by ELISA | 2013 | Journal 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. |
AID1212290 | Drug uptake in C57BL/6 mouse plasma at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1366819 | Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID503026 | Antiproliferative activity against human MCF7 cells at 4 uM after 14 days by coomassie staining | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1908081 | Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay | | | |
AID1155057 | Antiproliferative activity against human SK-UT-1 cells expressing p53 mutant protein by cell Titer-Glo assay | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor. |
AID756938 | Cell 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 analysis | 2013 | Journal 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. |
AID1361647 | Induction 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%) | 2018 | Journal 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. |
AID503032 | Induction 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 assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID749326 | Inhibition of p53-MDM2 (unknown origin) interaction expressed in Escherichia coli BL-21 (DE3) after 1 hr by fluorescence polarization assay | 2013 | Bioorganic & 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. |
AID1296639 | Binding affinity to 15N-labeled Bcl-2 (unknown origin) by 2D 1H-15N HSQC NMR spectroscopic method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1143658 | Antiproliferative activity against human HCT116 cells expressing wild type p53 after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID738689 | Inhibition of MDM2 (unknown origin) assessed as activation of p53 | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID415699 | Inhibition of interaction between human DMX(1-555) and p53 at upto 30 uM | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
| Beta-peptides with improved affinity for hDM2 and hDMX. |
AID1296597 | Displacement 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 assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1908031 | Upregulation of MDM2 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID739073 | Inhibition 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 | 2013 | Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
| Rational design and binding mode duality of MDM2-p53 inhibitors. |
AID1212300 | Drug uptake in C57BL/6 mouse liver at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID362381 | Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| NMR screening for lead compounds using tryptophan-mutated proteins. |
AID707326 | Inhibition of p53-MDM2 interaction after 1 hr by fluorescence polarization assay | 2012 | Journal 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. |
AID265955 | Displacement of PMDM6-F from human recombinant MDM2 | 2006 | Journal 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. |
AID438432 | Induction of p21 mRNA in human HCT116 cells by RT-PCR | 2009 | Journal 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. |
AID738714 | Antiproliferative activity against human RKO cells expressing wild type p53 after 5 days by MTS assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID587349 | Inhibition of human GST-tagged Mdm2 expressed in Escherichia coli harboring integrated p53-Mmd2 protein assessed as blockade of enzyme-p53 interaction by ELISA assay | 2011 | Bioorganic & 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. |
AID1300910 | Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & 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. |
AID1361650 | Induction 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%) | 2018 | Journal 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. |
AID1249875 | Activation of p53 in human U2OS cells assessed as increase of MDM2 expression at 2.5 uM after 12 hrs by Western blotting | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| Discovery of Novel Isatin-Based p53 Inducers. |
AID1212292 | Drug uptake in C57BL/6 mouse adrenal gland at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID749490 | Cytotoxicity against human p53 deficient PC3 cells after 72 hrs by SRB assay | 2013 | Bioorganic & 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. |
AID621851 | Growth inhibition of human HCT116 cells expressing MDM2 by SRB assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. |
AID1674908 | Inhibition of P-gp-mediated Rhodamine-123 efflux in human p53 +/+ H1299 cells assessed as Rhodamine-123 accumulation measured after 40 mins by spectrofluorimetry | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| Mdm2 inhibitors as a platform for the design of P-glycoprotein inhibitors. |
AID362385 | Binding affinity to human recombinant Mdm2 F55W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| NMR screening for lead compounds using tryptophan-mutated proteins. |
AID1908078 | Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay | | | |
AID1361624 | Growth inhibition of Saccharomyces cerevisiae expressing p53 at 10 uM after 42 hrs by Yeast-based assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity. |
AID749488 | Inhibition of p53/MDM2 (1 to 118) (unknown origin) interaction at 10 uM after 1 hr by fluorescence polarization assay | 2013 | Bioorganic & 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. |
AID1285800 | Inhibition of Flag-tagged p53/GST-tagged Mdm2 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID1300908 | Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & 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. |
AID1361627 | Inhibition of human recombinant full length HDAC1 using fluorogenic substrate 3 after 30 mins by fluorescence assay | 2018 | Journal 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. |
AID1361653 | Induction 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%) | 2018 | Journal 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. |
AID1195733 | Cytotoxicity against human RKO cells | 2015 | Journal 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. |
AID749491 | Inhibition of p53/MDM2 (1 to 118) (unknown origin) interaction after 1 hr by fluorescence polarization assay | 2013 | Bioorganic & 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. |
AID503037 | Induction of p53 accumulation in human MCF7 cells after 18 hrs by Western blot analysis in presence of 2.5 mM caffeine | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1296633 | Inhibition of BCl-2/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID749324 | Cytotoxicity against human p53-null PC3 cells assessed as growth inhibition after 72 hrs by SRB assay | 2013 | Bioorganic & 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. |
AID1361625 | Growth inhibition of Saccharomyces cerevisiae expressing MDM2 at 10 uM after 42 hrs by Yeast-based assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity. |
AID1285803 | Inhibition of Flag-tagged p53/GST-tagged PPID (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID756857 | Inhibition of MDM2-P53 interaction in human SJSA1 cells assessed as p53-mediated decrease in full length PARP level at 24 hrs by Western blot analysis | 2013 | Journal 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. |
AID1212304 | Drug uptake in C57BL/6 mouse lung at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID1659344 | Inhibition of MDM2 (unknown origin) by HTRF assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases. |
AID1296640 | Binding affinity to 15N-labeled MDM2 (unknown origin) by 2D 1H-15N HSQC NMR spectroscopic method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID736743 | Inhibition of human p53 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell cycle arrest at 10 uM after 42 hrs | 2013 | Journal 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. |
AID1285816 | Antitumor 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 40 | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID1720556 | Inhibition of human MDM2-p53 interaction | 2020 | Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13
| A critical update on the strategies towards modulators targeting androgen receptors. |
AID1908070 | Inhibition of GST-tagged MDM2/Biotin-tagged p53 interaction (unknown origin) incubated for 40 mins by TR-FRET assay | | | |
AID1060451 | Antiproliferative activity against human HepG2 cells after 24 hrs by MTS assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents. |
AID1155058 | Ratio of IC50 for human SK-UT-1 cells expressing p53 mutant protein to IC50 for human SJSA1 cells expressing wild type p53 protein | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor. |
AID1057111 | Cytotoxicity against human HCT116 cells after 72 hrs by CellTiterGlo luciferase-based assay | 2013 | Bioorganic & 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. |
AID503033 | Induction of p53 expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1296632 | Inhibition of BCl-2/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1143671 | Induction 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 control | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1361637 | Inhibition of MDM2/P53 interaction in human A549 cells assessed as increase in MDM2 expression after 24 hrs by Western blot analysis | 2018 | Journal 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. |
AID691697 | Inhibition of MDM2 binding to p53 | 2012 | Bioorganic & 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. |
AID1632470 | Inhibition 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 assay | 2016 | Bioorganic & 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. |
AID1387292 | Antiproliferative activity against p53 -/- human HCT116 cells incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives. |
AID588009 | Inhibition 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 analysis | 2011 | Journal 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. |
AID1296626 | Cell 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%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID756926 | Induction of apoptosis in human MCF7 cells assessed as increase in p21 expression level at 3 uM after 24 to 72 hrs by Western blotting analysis | 2013 | Journal 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. |
AID1361648 | Induction 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%) | 2018 | Journal 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. |
AID1361626 | Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID1212302 | Drug uptake in C57BL/6 mouse plasma at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID1238647 | Inhibition of rat MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID1361643 | Cell 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%) | 2018 | Journal 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. |
AID748501 | Inhibition of N-terminal human recombinant MDM2 assessed as inhibition of protein interaction with p53 by HTRF assay | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID738727 | Antiproliferative activity against human MDA-MB-435S cells harboring p53 mutant at 10 uM after 5 days by MTS assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID1060449 | Antiproliferative activity against p53-deficient human HCT116 cells after 24 hrs by MTS assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents. |
AID1296634 | Inhibition of Mcl-1/Bim interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID748504 | Apparent half life in mouse at 100 mg/kg, po | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID1212283 | Ratio of drug level in blood to plasma in C57BL/6 mouse after 30 mins | 2011 | Drug 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. |
AID1238675 | Inhibition of human MDM4 by TR-FRET assay | 2015 | Journal 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. |
AID503024 | Induction of cell cycle arrest in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID442457 | Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation at 10 uM by Western blot | 2009 | Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
| Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction. |
AID621853 | Growth inhibition of human A2780 cells expressing MDM2 by SRB assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
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AID1361646 | Cell 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%) | 2018 | Journal 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. |
AID756948 | Cytotoxicity against human Calu cells after 24 hrs by MTT assay | 2013 | Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
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AID626522 | Antitumor activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
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AID1656003 | Solubility of compound in PBS | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR. |
AID707325 | Antiproliferative activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay | 2012 | Journal 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. |
AID1361631 | Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
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| Whole-body physiologically based pharmacokinetic model for nutlin-3a in mice after intravenous and oral administration. |
AID1285814 | Increase in p53 expression in human MCF7 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID1908093 | Induction of PARP cleavage in human RKO cells at 0.3125 to 2.5 uM incubated for 24 hrs by Western blot analysis | | | |
AID1361644 | Cell 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%) | 2018 | Journal 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. |
AID1143670 | Induction 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 control | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1908055 | Upregulation of p53 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1565005 | Induction 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 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID1908092 | Downregulation of MDM4 expression in human RKO cells at 0.3125 to 2.5 uM incubated for 24 hrs by Western blot analysis | | | |
AID1060450 | Antiproliferative activity against human HCT116 cells expressing p53 after 24 hrs by MTS assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents. |
AID588013 | Cytotoxicity against human SJSA1 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal 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. |
AID587948 | Inhibition of Mdm2 -p53 protein interaction by ELISA | 2011 | Journal 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. |
AID1212294 | Drug uptake in C57BL/6 mouse muscle at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
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AID1296607 | Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p53 expression after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
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AID438434 | Induction of apoptosis in human SJSA1 cells assessed as caspase 3/7 activity after 48 hrs | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
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AID746383 | Antagonist activity at human GST-tagged MDM2 assessed as inhibition of binding to full length p53 | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
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AID1125681 | Antiproliferative activity against human SJSA1 cells | 2014 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
| Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction. |
AID1212296 | Drug uptake in C57BL/6 mouse brain at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1143669 | Induction 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 control | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID588016 | Cytotoxicity against human p53 expressing HCT116 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal 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. |
AID1908058 | Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay | | | |
AID1239847 | Inhibition of p53-MDM2 interaction (unknown origin) by TR-FRET assay | 2015 | Bioorganic & 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. |
AID1285811 | Upregulation of p21 in human MCF7 cells after 24 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID453614 | Binding to HDM2 expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy competition method | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
| N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53. |
AID1908028 | Upregulation of p53 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1565006 | Induction 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 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID1296623 | Cell 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%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1296624 | Cell 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%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1057102 | Ratio of IC50 for human H1299 cells to IC50 for human HCT116 cells | 2013 | Bioorganic & 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. |
AID707311 | Induction of apoptosis in human A549 cells expressing wild type p53 at 20 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay | 2012 | Journal 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. |
AID1908077 | Displacement 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 | | | |
AID700922 | Inhibition of HDM2 binding to p53 | 2012 | Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
| Chemical modulators working at pharmacological interface of target proteins. |
AID503039 | Induction of apoptosis in human MCF7 cells transfected with p53-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1361641 | Cell 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%) | 2018 | Journal 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. |
AID438435 | Induction of p53-Ser15 phosphorylation in human HCT116 cells after 24 hrs | 2009 | Journal 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. |
AID1060441 | Inhibition 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 analysis | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents. |
AID1143674 | Induction 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%) | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1361623 | Growth inhibition of Saccharomyces cerevisiae expressing empty vector at 10 uM after 42 hrs by Yeast-based assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity. |
AID1192743 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
| Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents. |
AID1060447 | Antiproliferative activity against human SW620 cells expressing p53 mutant after 24 hrs by MTS assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Synthesis and evaluation of spiroisoxazoline oxindoles as anticancer agents. |
AID1212301 | Drug uptake in C57BL/6 mouse spleen at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID1212297 | Drug uptake in C57BL/6 mouse bone marrow at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID621854 | Growth inhibition of human A2780/CP70 cells expressing isogenically paired p53 mutant by SRB assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. |
AID1908053 | Upregulation of p21 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1361654 | Induction 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%) | 2018 | Journal 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. |
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AID503025 | Induction of cell cycle arrest in human MCF7 cells transfected hnRNPK-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1212295 | Drug uptake in C57BL/6 mouse retina at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1908027 | Upregulation of p21 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1565008 | Induction 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 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID1238650 | Selectivity index, ratio of Ki for rat MDM2 to Ki for human MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID1872997 | Inhibition of recombinant human MDM2/p53 interaction by Biacore's surface plasmon resonance analysis | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
AID1296625 | Cell 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%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1300246 | Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 72 hrs by CellTitre-Glo assay | 2016 | ACS 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. |
AID1656006 | Inhibition of 6xHis-taged MDM2 (unknown origin) expressed in Escherichia coli Gold (DE3) | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR. |
AID1195731 | Cytotoxicity against human SJSA1 cells | 2015 | Journal 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. |
AID1654661 | Inhibition 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 analysis | 2020 | Journal 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. |
AID1633977 | Inhibition 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 control | 2019 | Bioorganic & 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. |
AID587354 | Induction of p53-dependent luciferase activity in human U2OS cells at 5 uM relative to control | 2011 | Bioorganic & 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. |
AID1195732 | Cytotoxicity against human HCT116 cells | 2015 | Journal 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. |
AID1143668 | Induction 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 control | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID362383 | Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by NMR ligand-protein binary titration | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| NMR screening for lead compounds using tryptophan-mutated proteins. |
AID1300941 | Decrease in procaspase-9 expression level in human p53-null HCT116 -/- cells at 10 uM after 24 hrs by western blot analysis | 2016 | Bioorganic & 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. |
AID1361628 | Inhibition of MDM2 (unknown origin) preincubated for 30 mins by fluorescence polarization assay | 2018 | Journal 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. |
AID1212293 | Drug uptake in C57BL/6 mouse lung at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1555409 | Inhibition of p53 protein binding to MDM2 (unknown origin) | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy. |
AID1420852 | Inhibition of recombinant p53 protein binding to recombinant human MDM2 by surface plasmon resonance method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Role of p53 circuitry in tumorigenesis: A brief review. |
AID1366814 | Inhibition 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 control | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID738716 | Antiproliferative activity against human HCT116 cells expressing wild type p53 after 5 days by MTS assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID588014 | Cytotoxicity against human LS cells after 72 hrs by sulforhodamine B assay | 2011 | Journal 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. |
AID1387289 | Inhibition 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 assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives. |
AID1296635 | Inhibition of Mcl-1/Bax interaction in human DMS53 cells harboring p53 mutant at 5 to 10 uM after 12 hrs by immunoprecipitation method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1252240 | Inhibition 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 assay | 2015 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
| Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin. |
AID1152866 | Binding affinity to MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by fluorescence polarization binding assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Discovery of 1-arylpyrrolidone derivatives as potent p53-MDM2 inhibitors based on molecule fusing strategy. |
AID1654653 | Inhibition of mdm2 in human ARN8 cells assessed as increase in p53 level at 2 uM incubated for 24 hrs by Western blot analysis | 2020 | Journal 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. |
AID1633983 | Inhibition 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 control | 2019 | Bioorganic & 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. |
AID1212284 | Fraction unbound in C57BL/6 mouse plasma at 0.1 uM up to 24 hrs by equilibrium dialysis method | 2011 | Drug 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. |
AID748498 | Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID1361619 | Inhibition of human MDM2-p53 interaction in Saccharomyces cerevisiae assessed as p53 induced cell growth arrest at 10 uM after 42 hrs by Yeast-based assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Targeting the MDM2-p53 protein-protein interaction with prenylchalcones: Synthesis of a small library and evaluation of potential antitumor activity. |
AID756940 | Inhibition of MDM2-p53 interaction in human MCF7 cells assessed as reduction in p53 level bound to MDM2 after 24 hrs by immunoprecipitation assay | 2013 | Journal 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. |
AID1908080 | Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay | | | |
AID503036 | Induction 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 caffeine | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1143657 | Binding affinity to MDM2 (1 to 118) (unknown origin) after 30 mins by fluorescence polarization assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1366812 | Induction of apoptosis in human U2OS cells at 10 uM after 24 hrs by Annexin V-FITC/propidium iodide based FACS analysis (Rvb= 0.1%) | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID756860 | Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as p53 activation after 24 hrs by Western blot analysis | 2013 | Journal 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. |
AID1212308 | Drug uptake in C57BL/6 mouse bone marrow at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID1366818 | Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID438433 | Inhibition of human HCT116 cell proliferation after 16 hrs by BrdU assay | 2009 | Journal 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. |
AID756953 | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay | 2013 | Journal 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. |
AID658338 | Inhibition of p53 (18 to 26)-MDM2 (2 to 188) interaction using fluorescent dye Cy5 by TR-FRET assay | 2012 | Bioorganic & 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. |
AID1372140 | Cytotoxicity in human SJSA1 cells over expressing human DM2 after 24 hrs by CellTiter-Glo assay | 2018 | Bioorganic & medicinal chemistry, 03-15, Volume: 26, Issue:6
| Unique arginine array improves cytosolic localization of hydrocarbon-stapled peptides. |
AID736737 | Inhibition 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 analysis | 2013 | Journal 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. |
AID1238649 | Selectivity index, ratio of Ki for mouse MDM2 to Ki for human MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID588017 | Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal 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. |
AID756858 | Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as accumulation of p21 after 24 hrs by Western blot analysis | 2013 | Journal 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. |
AID1175611 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
| Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors. |
AID1654654 | Inhibition 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 analysis | 2020 | Journal 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. |
AID503028 | Antiproliferative 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 staining | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1564997 | Displacement 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID1192744 | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
| Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents. |
AID706604 | Antiproliferative activity against human SJSA1 cells after 3 days by EdU incorporation assay in presence of 10% human serum | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-based design of novel inhibitors of the MDM2-p53 interaction. |
AID756951 | Cytotoxicity against human PC3 cells after 24 hrs by MTT assay | 2013 | Journal 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. |
AID1908060 | Upregulation of p21 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1285813 | Increase in p53 expression in human IMR32 cells nuclei after 24 hrs by DAPI staining based immunofluorescence microscopy | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID1361651 | Induction 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%) | 2018 | Journal 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. |
AID1565010 | Inhibition 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 analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID453615 | Binding to GST-tagged HDMX expressed in Escherichia coli BL21 (DE3) by fluorescence anisotropy competition method | 2009 | Bioorganic & medicinal chemistry, Dec-01, Volume: 17, Issue:23
| N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53. |
AID1296609 | Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of MDM2 expression after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1296599 | Displacement 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 assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1908071 | Inhibition of GST-tagged MDM4/Biotin-tagged p53 interaction (unknown origin) incubated for 40 mins by TR-FRET assay | | | |
AID503042 | Induction of apoptosis in human MCF7 cells co-transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1633982 | Inhibition 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 control | 2019 | Bioorganic & 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. |
AID1908083 | Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay | | | |
AID756952 | Cytotoxicity against human U937 cells after 24 hrs by MTT assay | 2013 | Journal 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. |
AID267242 | Binding affinity to MDM2 | 2006 | Journal 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. |
AID1361649 | Induction 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%) | 2018 | Journal 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. |
AID707324 | Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay | 2012 | Journal 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. |
AID1908090 | Upregulation of p21 expression in human RKO cells incubated for 24 hrs by Western blot analysis | | | |
AID684828 | Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. |
AID1908082 | Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay | | | |
AID1908089 | Upregulation of p53 expression in human RKO cells incubated for 24 hrs by Western blot analysis | | | |
AID362384 | Binding affinity to human recombinant Mdm2 K98W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| NMR screening for lead compounds using tryptophan-mutated proteins. |
AID1212310 | Drug uptake in C57BL/6 mouse adipose tissue at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID1366813 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID707310 | Induction of apoptosis in human A549 cells expressing wild type p53 after 48 hrs using annexin V-FITC staining by flow cytometry assay | 2012 | Journal 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. |
AID749325 | Cytotoxicity against human A549 cells expressing wild type p53 assessed as growth inhibition after 72 hrs by SRB assay | 2013 | Bioorganic & 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. |
AID1212305 | Drug uptake in C57BL/6 mouse muscle at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID1633968 | Inhibition 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 control | 2019 | Bioorganic & 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. |
AID1057110 | Cytotoxicity against human H1299 cells after 72 hrs by CellTiterGlo luciferase-based assay | 2013 | Bioorganic & 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. |
AID415698 | Inhibition of interaction between human DM2(1-549) and p53 | 2009 | Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
| Beta-peptides with improved affinity for hDM2 and hDMX. |
AID1366815 | Inhibition 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 control | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID1057105 | Induction of p53 translocation in human HCT116 cells assessed as protein nuclear to cytosolic ratio at 3.3 uM after 20 hrs by immunofluorescence analysis | 2013 | Bioorganic & 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. |
AID1212306 | Drug uptake in C57BL/6 mouse retina at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID707312 | Induction of apoptosis in human A549 cells expressing wild type p53 at 10 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay | 2012 | Journal 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. |
AID1212307 | Drug uptake in C57BL/6 mouse brain at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID438431 | Induction of p53 in human HCT116 cells coexpressing pp53TA-luc assessed as inhibition of cell proliferation after 8 hrs by firefly/renilla luciferase reporter assay | 2009 | Journal 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. |
AID1192746 | Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
| Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents. |
AID503029 | Antiproliferative 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 staining | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1361659 | Antitumor 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 implantation | 2018 | Journal 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. |
AID1565009 | Inhibition 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 analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID1296608 | Cell cycle arrest in human HCT116 p53+/+ cells assessed as accumulation at 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. | |
AID1565011 | Inhibition 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 analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID755375 | Antitumor 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 control | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors. |
AID756920 | Induction 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 analysis | 2013 | Journal 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. |
AID1366820 | Inhibition of MDM2/p53 (unknown origin) complex at 10 uM by ELISA | 2017 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
| Proapoptotic modification of substituted isoindolinones as MDM2-p53 inhibitors. |
AID1238646 | Inhibition of mouse MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID1503133 | Antiproliferative activity in p53 (+/+) human HCT116 cells incubated for 72 hrs by MTS assay | | | |
AID1421138 | Inhibition of Cy5-labeled p53 derived TFSDLWKLL peptide binding to C-terminal biotin-labelled human MDM2 (2 to 188 residues) by TR-FRET assay | 2018 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
| In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor. |
AID438437 | Inhibition of human p21 deficient HCT116 cell proliferation after 16 hrs by BrdU assay | 2009 | Journal 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. |
AID756933 | Induction of apoptosis in human MCF7 cells assessed as accumulation at subG1 phase at 3 uM by propidium iodide staining-based FACS analysis | 2013 | Journal 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. |
AID684826 | Antiproliferative activity against human p53-deficient Saos2 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. |
AID756922 | Induction 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 analysis | 2013 | Journal 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. |
AID588015 | Cytotoxicity against human NGP cells after 72 hrs by sulforhodamine B assay | 2011 | Journal 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. |
AID1212299 | Drug uptake in C57BL/6 mouse intestine at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID503027 | Antiproliferative activity against human MCF7 cells assessed as appearance of flattened phenotype at 4 uM after 14 days by coomassie staining | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1908026 | Upregulation of MDM2 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1212303 | Drug uptake in C57BL/6 mouse adrenal gland at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID425674 | Inhibition of GST-tagged MDM2/His6-tagged p53 interaction by surface plasmon resonance study | 2009 | Bioorganic & 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. |
AID755374 | Toxicity 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 control | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors. |
AID1387293 | Antiproliferative activity against p53 -/- human NCI-H1299 cells incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives. |
AID707323 | Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay | 2012 | Journal 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. |
AID748502 | AUClast in mouse at 100 mg/kg, po | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID706601 | Inhibition of human MDM2-p53 interaction after 18 hrs by HTRF assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-based design of novel inhibitors of the MDM2-p53 interaction. |
AID1285802 | Inhibition of Flag-tagged p53/GST-tagged DAPK1 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID707317 | Inhibition of p53-MDMX interaction after 1 hr by fluorescence polarization assay | 2012 | Journal 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. |
AID684829 | Antiproliferative activity against human p53-deficient NCI-H1299 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. |
AID1908049 | Downregulation of MDM4 protein expression in human NCI-H460 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1143672 | Induction 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%) | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1503134 | Antiproliferative activity in p53 (-/-) human HCT116 cells incubated for 72 hrs by MTS assay | | | |
AID749489 | Cytotoxicity against human A549 cells expressing wild type p53 after 72 hrs by SRB assay | 2013 | Bioorganic & 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. |
AID1238648 | Selectivity index, ratio of Ki for dog MDM2 to Ki for human MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID1361636 | Inhibition of MDM2/P53 interaction in human A549 cells assessed as increase in p53 expression after 24 hrs by Western blot analysis | 2018 | Journal 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. |
AID621850 | Growth inhibition of human SJSA1 cells expressing MDM2 by SRB assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
| MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. |
AID1212289 | Drug uptake in C57BL/6 mouse spleen at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1249873 | Stabilization of p53 in human U2OS cells assessed as intracellular p53 level at 2.5 uM after 12 hrs by Western blotting | 2015 | ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8
| Discovery of Novel Isatin-Based p53 Inducers. |
AID1633969 | Inhibition 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 control | 2019 | Bioorganic & 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. |
AID756949 | Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay | 2013 | Journal 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. |
AID1143673 | Induction 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%) | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1285812 | Upregulation of Mdm2 in human MCF7 cells after 24 hrs by Western blot analysis | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID1238645 | Inhibition of dog MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID1300245 | Inhibition 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 assay | 2016 | ACS 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. |
AID1212287 | Drug uptake in C57BL/6 mouse intestine at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1143660 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID756925 | Induction 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 analysis | 2013 | Journal 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. |
AID1143661 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID438436 | Inhibition of human p53 deficient HCT116 cell proliferation after 16 hrs by BrdU assay | 2009 | Journal 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. |
AID1212298 | Drug uptake in C57BL/6 mouse vitreous humor at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1195730 | Binding affinity to MDM2 (unknown origin) | 2015 | Journal 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. |
AID503038 | Induction of p21CIP1 expression in irradiated human BJ cells at 3 uM by Western blot analysis | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1212309 | Drug uptake in C57BL/6 mouse vitreous humor at 10 mg/kg, iv as single dose measured at 24 hrs | 2011 | Drug 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. |
AID503031 | Induction 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 assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID626521 | Antitumor activity against p53 deficient human Saos2 cells after 72 hrs by MTT assay | 2011 | European 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. |
AID1908047 | Effect on MDM4 protein expression in human MCF7 cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID707327 | Induction of apoptosis in human A549 cells expressing wild type p53 at 5 uM after 48 hrs using annexin V-FITC staining by flow cytometry assay | 2012 | Journal 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. |
AID684827 | Antiproliferative activity against human U2OS cells expressing wild type p53 after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. |
AID736742 | Inhibition of human MDM2 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell cycle arrest after 42 hrs | 2013 | Journal 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. |
AID417066 | Binding affinity to MDM2 | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
| Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics. |
AID1565007 | Induction 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 %) | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID684825 | Inhibition of MDM2 binding domain assessed as inhibition of p53 binding to MDM2 after 1 hr by fluorescence polarization assay | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. |
AID707322 | Antiproliferative activity against p53 deficient human NCI-H1299 cells after 72 hrs by MTT assay | 2012 | Journal 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. |
AID1143665 | Induction of apoptosis in human HCT116 cells after 48 hrs by propidium iodide staining-based flow cytometry | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1212286 | Cytotoxicity against doxorubicin-resistant human UKF-NB-3 cells after 96 hrs by MTT assay | 2011 | Drug 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. |
AID588008 | Inhibition 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 analysis | 2011 | Journal 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. |
AID756859 | Inhibition of MDM2-p53 interaction in human SJSA1 cells assessed as MDM2 accumulation after 24 hrs by Western blot analysis | 2013 | Journal 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. |
AID503035 | Induction of CDKN1A gene expression in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA by Western blot analysis | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID243263 | Potency against MDM2 (murine double minute-2 gene) binding to p53; Range =100-300 nM | 2005 | Journal of medicinal chemistry, Jul-14, Volume: 48, Issue:14
| p53 Activation by small molecules: application in oncology. |
AID1908039 | Effect on MDM4 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID503041 | Induction of cell cycle arrest in human MCF7 cells transfected with 53BP1-targeting iRNA-based shRNA at 4 uM after 14 days by BrdU incorporation assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1415891 | Inhibition 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 assay | 2017 | MedChemComm, May-01, Volume: 8, Issue:5
| Scaffold hopping via ANCHOR.QUERY: β-lactams as potent p53-MDM2 antagonists |
AID1296598 | Displacement 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 assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID736744 | Inhibition of human p53 expressed in Saccharomyces cerevisiae CG379 assessed as effect on cell growth at 10 uM after 42 hrs | 2013 | Journal 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. |
AID1908091 | Upregulation of MDM2 expression in human RKO cells incubated for 24 hrs by Western blot analysis | | | |
AID706603 | Activity 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 serum | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Structure-based design of novel inhibitors of the MDM2-p53 interaction. |
AID748500 | Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as cell viability after 5 days by MTT assay | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID738713 | Antiproliferative activity against human SJSA1 cells expressing wild type p53 after 5 days by MTS assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID503030 | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S phase at 4 uM after 48 hrs by BrdU incorporation assay | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID588007 | Inhibition 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 analysis | 2011 | Journal 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. |
AID587350 | Inhibition of human GST-tagged MDMX expressed in Escherichia coli harboring integrated p53-Hmd2 protein assessed as blockade of enzyme-p53 interaction by ELISA assay | 2011 | Bioorganic & 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. |
AID1212291 | Drug uptake in C57BL/6 mouse adipose tissue at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID721248 | Inhibition of human p53/MDM2 interaction | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3
| Lead optimization of novel p53-MDM2 interaction inhibitors possessing dihydroimidazothiazole scaffold. |
AID1300911 | Antiproliferative activity against human MDA-MB-435S cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & 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. |
AID756947 | Cytotoxicity against human C643 cells after 24 hrs by MTT assay | 2013 | Journal 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. |
AID1387291 | Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives. |
AID738979 | Antiproliferative activity against human HeLa cells harboring p53 mutant at 10 uM after 5 days by MTS assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID1296621 | Cell cycle arrest in human HCT116 p53-/- cells assessed as accumulation at 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. | |
AID1143659 | Antiproliferative activity against p53-deficient human HCT116 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1361652 | Induction 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%) | 2018 | Journal 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. |
AID1656007 | Binding affinity to 6xHis-taged MDM2 (unknown origin) expressed in Escherichia coli Gold (DE3) assessed as inhibition constant | 2020 | ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
| HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR. |
AID1192745 | Cytotoxicity against human HEK293 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
| Design and synthesis of new bioisosteres of spirooxindoles (MI-63/219) as anti-breast cancer agents. |
AID1361629 | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID1238644 | Inhibition of human MDM2 by TR-FRET assay | 2015 | Journal 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. |
AID1908059 | Upregulation of MDM2 protein expression in human U2OS cells at 10 uM measured after 24 hrs by Western blot analysis | | | |
AID1387290 | Antiproliferative activity against human SJSA1 cells expressing wild type p53 incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
| Inhibition of p53-Murine Double Minute 2 (MDM2) Interactions with 3,3'-Spirocyclopentene Oxindole Derivatives. |
AID588018 | Cytotoxicity against human Saos2 cells after 72 hrs by sulforhodamine B assay | 2011 | Journal 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. |
AID503040 | Antiproliferative 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 staining | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1296610 | Inhibition of MDM2-p53 interaction in human HCT116 p53+/+ cells assessed as upregulation of p21 expression after 12 hrs by immunoblotting method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID1361645 | Cell 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%) | 2018 | Journal 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. |
AID1195734 | Antitumor activity against human SJSA1 cells xenografted in mouse assessed as tumor growth inhibition at 200 mg/kg, po bid administered for 20 days | 2015 | Journal 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. |
AID1296622 | Cell 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%) | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics. |
AID736738 | Inhibition 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 hrs | 2013 | Journal 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. |
AID1633978 | Inhibition 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 control | 2019 | Bioorganic & 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. |
AID362378 | Binding affinity to human wild type Mdm2 by isothermal titration calorimetry | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| NMR screening for lead compounds using tryptophan-mutated proteins. |
AID1378961 | Inhibition 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 analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | In vitro targeting of colon cancer cells using spiropyrazoline oxindoles. |
AID1300912 | Inhibition 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 assay | 2016 | Bioorganic & 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. |
AID1580651 | Antiproliferative activity against human SJSA1 cells expressing wild-type p53 incubated for 72 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
| Enhancing the Cell Permeability of Stapled Peptides with a Cyclic Cell-Penetrating Peptide. |
AID1392511 | Antiproliferative activity against human HCT116 p53+/+ cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis | 2018 | Bioorganic & 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. |
AID1361630 | Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay | 2018 | Journal 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. |
AID265956 | Antiproliferative activity against human LnCAP cell line with wild type p53 | 2006 | Journal 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. |
AID738725 | Antiproliferative activity against human SW480 cells harboring p53 mutant at 10 uM after 5 days by MTS assay | 2013 | Bioorganic & medicinal chemistry, Apr-15, Volume: 21, Issue:8
| Synthesis and evaluation of an imidazole derivative-fluorescein conjugate. |
AID503043 | Induction of p21 expression in irradiated human BJ cells at 3 uM by Western blot analysis | 2006 | Nature chemical biology, Apr, Volume: 2, Issue:4
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. |
AID1285801 | Inhibition of Flag-tagged p53/GST-tagged Mdmx (unknown origin) expressed in Escherichia coli BL21 after 1 hr by ELISA microplate reader method | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
| Discovery of new low-molecular-weight p53-Mdmx disruptors and their anti-cancer activities. |
AID1057104 | Induction of p53 translocation in human HCT116 cells assessed as protein nuclear to cytosolic ratio at 10 uM after 20 hrs by immunofluorescence analysis | 2013 | Bioorganic & 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. |
AID1361642 | Cell 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%) | 2018 | Journal 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. |
AID736735 | Inhibition 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 assay | 2013 | Journal 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. |
AID1212288 | Drug uptake in C57BL/6 mouse liver at 50 to 200 mg/kg, po as single dose measured at 2 hrs | 2011 | Drug 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. |
AID1143667 | Induction 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 control | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1392512 | Antiproliferative activity against human HCT116 p53-/- cells assessed as growth inhibition after 24 hrs by EdU/Hoechst 33342 staining-based fluorescence analysis | 2018 | Bioorganic & 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. |
AID1143666 | Induction 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 control | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Design, 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. |
AID1300909 | Antiproliferative activity against human p53-null HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & 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. |
AID748503 | Cmax in mouse at 100 mg/kg, po | 2013 | ACS medicinal chemistry letters, May-09, Volume: 4, Issue:5
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. |
AID362382 | Binding affinity to human recombinant Mdm2 T101W mutant expressed in Escherichia coli BL21 (DE3) cells by antagonist induced dissociation assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| NMR screening for lead compounds using tryptophan-mutated proteins. |
AID736736 | Inhibition 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 assay | 2013 | Journal 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. |
AID1564998 | Displacement 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 assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID749323 | Selectivity ratio of IC50 for human p53-null PC3 cells to IC50 for human A549 cells expressing wild type p53 | 2013 | Bioorganic & 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. |
AID1565012 | Inhibition 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 analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2013 | Acta 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] |