| Assay ID | Title | Year | Journal | Article |
|---|
| AID1873007 | Oral bioavailability in Sprague-Dawley rat at 2 mg/kg by LC-MS/MS method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1129403 | Drug metabolism in human hepatocytes assessed as (2S,3S,4S,5R,6S)-6-(2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxyli | 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. |
| 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. |
| AID1422086 | Intrinsic clearance in human hepatocytes assessed per million cells | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. |
| AID1075183 | Antiproliferative activity against p53 -deficient human HCT116 cells after 16 hrs by BrdU proliferation 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. |
| AID1075187 | Clearance in cynomolgus monkey | 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. |
| AID1195706 | Drug metabolism in dog hepatocytes assessed as acyl glucuronide M1 formation at 10 uM after 2 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1195690 | Binding affinity to human MDM2 by by isothermal titration calorimetry | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1195688 | Intrinsic clearance in human hepatocytes measured per million cells | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1075190 | Clearance in rat at 0.5 mg/kg, iv | 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. |
| AID1075182 | Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as induction of p21 mRNA at 50 mg/kg, po by qRT-PCR 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. |
| AID1674912 | Growth inhibition of human p53 +/+ H1299 cells upto 10 uM incubated for 48 hrs | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| Mdm2 inhibitors as a platform for the design of P-glycoprotein inhibitors. |
| AID1195705 | Drug metabolism in rat hepatocytes assessed as acyl glucuronide M1 formation at 10 uM after 2 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1908064 | Inhibition of human MDM2/p53 interaction by HTRF based biochemical assay | | | |
| 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. |
| AID1129401 | Drug metabolism in dog hepatocytes assessed as (2S,3S,4S,5R,6S)-6-(2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic | 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. |
| AID1873010 | Oral bioavailability in Beagle dog at 2 mg/kg by LC-MS/MS method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1075188 | Half life in rat at 0.5 mg/kg, iv | 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. |
| AID1075177 | Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as unbound concentration causing inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treat | 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. |
| AID1195687 | Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 16 hrs by Click-iT EdU HCS assay in presence of 10% human serum | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1195685 | Binding affinity to human GST-thrombin-tagged MDM2 ( 1 to 188 aa) assessed as inhibition of interaction with human p53 preincubated with compound for 20 mins by HTRF assay | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1674909 | Inhibition of P-gp-mediated Rhodamine-123 efflux in human p53 -/- HCT-116 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. |
| AID1392509 | Activation of p53 in human U2OS cells harboring p53-dependent EGFP reporter gene assessed as increase in p53 transcriptional activity at 5 uM after 48 hrs by propidium iodide satining-based automated fluorescent imaging analysis relative to Nutlin-3a | 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. |
| AID1873009 | Oral bioavailability in cynomolgus monkey at 2 mg/kg by LC-MS/MS method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1075194 | Binding affinity to human GST-thrombin-tagged MDM2 assessed as inhibition of interaction with human p53 after 1 hr by HTRF 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. |
| 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. |
| 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. |
| AID1075184 | Antiproliferative activity against human HCT116 cells expressing p53 wild type after 16 hrs by BrdU proliferation 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. |
| AID1075179 | Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth treated after 11 days of tumor xenograft upto 25 days through oral gavage relative to vehicle treated control | 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. |
| AID1873004 | Fraction unbound clearance in Sprague-Dawley rat hepatocytes assessed as per million cells at 0.5 uM incubated for 15 mins by ultracentrifugation method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1195707 | Drug metabolism in cynomolgus monkey hepatocytes assessed as acyl glucuronide M1 formation at 10 uM after 2 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1075181 | Antiproliferative activity against human SJSA1 cells xenografted in po dosed athymic nude mouse assessed as induction of p21 mRNA after 1 to 24 hrs by qRT-PCR 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. |
| AID1075186 | Induction of PXR (unknown origin) | 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. |
| AID1674911 | Growth inhibition of human p53 -/- NCI-HCT-116 cells upto 10 uM incubated for 48 hrs | 2020 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 30, Issue:18
| Mdm2 inhibitors as a platform for the design of P-glycoprotein inhibitors. |
| AID1075189 | Time dependent inhibition of CYP3A4 (unknown origin) | 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. |
| AID1674907 | Inhibition of P-gp-mediated Rhodamine-123 efflux in human MCF7 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. |
| 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. |
| AID1392507 | Induction of apoptosis in human HCT116 p53+ cells at 5 uM by Annexin V-FITC staining-based flow cytometric analysis relative to Nutlin-3a | 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. |
| AID1195708 | Drug metabolism in human hepatocytes assessed as acyl glucuronide M1 formation at 10 uM after 2 hrs by LC/MS analysis | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| 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. |
| AID1873005 | Fraction unbound clearance in CD-1 mouse hepatocytes assessed as per million cells at 0.5 uM incubated for 15 mins by ultracentrifugation method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1873008 | Oral bioavailability in CD-1 mouse at 5 mg/kg by LC-MS/MS method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1129402 | Drug metabolism in monkey hepatocytes assessed as (2S,3S,4S,5R,6S)-6-(2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxyl | 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. |
| AID1422085 | Oral bioavailability in cynomolgus monkey | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. |
| AID1195689 | Binding affinity to human MDM2 by by surface plasmon resonace spectroscopy | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1195686 | Binding affinity to MDM2 in human SJSA1 cells assessed as induction of p21 gene level after 7 hrs by qRT-PCR assay in presence of 10% human serum | 2014 | Journal of medicinal chemistry, Dec-26, Volume: 57, Issue:24
| Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction. |
| AID1129399 | Drug metabolism in mouse hepatocytes assessed as (2S,3S,4S,5R,6S)-6-(2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxyli | 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. |
| AID1422088 | Selectivity ratio of compound effect for human p53 null HCT116 cells to compound effect for human HCT116 cells harboring wild type p53 | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. |
| AID1908065 | Inhibition of MDM4 (unknown origin) | | | |
| AID1422087 | Antitumor activity against human SJSA1 cells xenografted in athymic nude mouse administered once via oral gavage | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. |
| AID1873003 | Metabolic stability in human hepatocytes assessed as intrinsic clearance measured per million cells at 500 nM and measured upto 90 mins by LC-MS/MS analysis | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| AID1422084 | Clearance in cynomolgus monkey | 2018 | European journal of medicinal chemistry, Nov-05, Volume: 159 | The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. |
| AID1075185 | Oral bioavailability in cynomolgus monkey | 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. |
| AID1075191 | Intrinsic clearance in human hepatocytes measured per 10'6 cells | 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. |
| AID1075180 | Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as induction of p21 mRNA at 50 mg/kg, po after 4 hrs by qRT-PCR assay relative to vehicle treated control | 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. |
| AID1075178 | Antiproliferative activity against human SJSA1 cells xenografted in athymic nude mouse assessed as complete inhibition of tumor growth treated at 60 mg/kg, po after 11 days of tumor xenograft upto 25 days relative to vehicle treated control | 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. |
| AID1129400 | Drug metabolism in rat hepatocytes assessed as (2S,3S,4S,5R,6S)-6-(2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetoxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-carboxylic | 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. |
| AID1873006 | Fraction unbound clearance in cynomolgus monkey hepatocytes assessed as per million cells at 0.5 uM incubated for 15 mins by ultracentrifugation method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Small-molecule MDM2 inhibitors in clinical trials for cancer therapy. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |