Assay ID | Title | Year | Journal | Article |
AID1483357 | Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 accumulation at 1 uM after 7 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID1182123 | Oral bioavailability in C57 mouse at 50 mg/kg | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID759673 | Cell cycle arrest in human SJSA1 cells assessed as accumulation at G2/M phase after 24 hrs | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1182120 | Cmax in C57 mouse at 50 mg/kg, po | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID1075195 | Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. |
AID759675 | Cell cycle arrest in human SJSA1 cells assessed as accumulation at G1 phase after 24 hrs | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1483352 | Inhibition of p53-MDM2 interaction in human HCT116 cells assessed as p53 activation by measuring increase in MDM2 expression at 1 uM after 7 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID1483334 | Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 activation by measuring increase in MDM2 expression at 1 uM after 7 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID1807821 | Binding affinity to HDM2 (unknown origin) | 2021 | Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
| Discovery of |
AID759670 | Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 25 mg/kg, po after 2 weeks relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1483347 | Cell cycle arrest in wild type p53 expressing human U2OS cells assessed as increase in accumulation at G1 phase at 1 uM after 24 hrs by propidium iodide-based FACS analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID1483335 | Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 activation by measuring increase in p21 expression at 1 uM after 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID759643 | Oral bioavailability in C57 mouse at 50 mg/kg | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1182119 | AUC in C57 mouse at 50 mg/kg, po | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID1483359 | Induction of human N-terminal MDM2 (1 to 125 residues) dimerization expressed in Escherichia coli BL21 (DE3) by 1H NMR spectroscopic method | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID759652 | Cmax in C57 mouse at 50 mg/kg, po | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759653 | AUC in C57 mouse at 50 mg/kg, po | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1483358 | Induction of human N-terminal MDM2 (1 to 118 residues) dimerization expressed in Escherichia coli BL21 (DE3) by 1H NMR spectroscopic method | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID759667 | AUC in nude mouse xenografted with human SJSA1 cells at 25 mg/kg, po | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759666 | AUC in nude mouse xenografted with human SJSA1 cells at 12.5 mg/kg, po | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759661 | Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759647 | Apparent terminal half-life in C57 mouse at 5 mg/kg, iv | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759658 | Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1483348 | Inhibition of p53-MDM2 interaction in human U2OS cells assessed as p53 activation by measuring p21 accumulation at 1 uM after 7 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID1483360 | Induction of human N-terminal MDM2 (18 to 125 residues) dimerization expressed in Escherichia coli BL21 (DE3) by 1H NMR spectroscopic method | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID1182113 | Clearance in human liver microsomes at 1 mM preincubated for 5 mins in presence of NADPH by LC-MS/MS method | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID759672 | Induction of apoptosis in human SJSA1 cells after 48 hrs by annexin V staining assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759660 | Binding affinity to GST-tagged MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by HTRF assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759662 | Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1075196 | Binding affinity to human MDM2 by by Surface Plasmon Resonace (SPR) spectroscopy binding assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
| Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development. |
AID1182117 | Apparent terminal half life in C57 mouse at 5 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID759663 | Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1182116 | Total plasma clearance in C57 mouse at 5 mg/kg, iv | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID1483346 | Cell cycle arrest in wild type p53 expressing human U2OS cells assessed as decrease in accumulation at S phase at 1 uM after 24 hrs by propidium iodide-based FACS analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID759656 | Clearance in human liver microsomes at 1 mM by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1182107 | Inhibition of p53-MDM2 (unknown origin) interaction using 0.02% BSA buffer after 1 hr by HTRF assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID1555896 | Inhibition of MDM2 (unknown origin) | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Development of selective small molecule MDM2 degraders based on nutlin. |
AID1182106 | Inhibition of p53-MDM2 (unknown origin) interaction using 0.2% BSA buffer after 1 hr by HTRF assay | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15
| Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. |
AID1129365 | Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
| Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres. |
AID759649 | Total plasma clearance in C57 mouse at 5 mg/kg, iv | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759674 | Inhibition of MDM2 in human SJSA1 cells assessed as induction of p53 stabilization after 20 hrs by Western blot analysis | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID759671 | Antitumor activity against human SJSA1 cells xenografted in nude mouse assessed as tumor growth inhibition at 12.5 mg/kg, po after 2 weeks relative to control | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1483353 | Inhibition of p53-MDM2 interaction in human HCT116 cells assessed as p53 activation by measuring increase in p21 expression at 1 uM after 24 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. |
AID759659 | Cytotoxicity against human SW480 cells expressing p53 mutant assessed as growth inhibition by MTT assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. |
AID1347172 | Secondary qRT-PCR qHTS assay for selected 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. |
AID1347170 | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected 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. |
AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
AID1347164 | 384 well plate NINDS Rhodamine confirmatory 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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |