nutlin 1: an MDM2 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 10008863 |
| CHEMBL ID | 1818538 |
| SCHEMBL ID | 1155826 |
| MeSH ID | M0461685 |
| Synonym |
|---|
| CHEMBL1818538 , |
| bdbm50433562 |
| SCHEMBL1155826 |
| nutlin 1 |
| 1-[4-[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-1-yl]ethanone |
| rac-1-{4-[4,5-bis-(4-chloro-phenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-1-yl}-ethanone |
| IYDMGGPKSVWQRT-UHFFFAOYSA-N |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cellular tumor antigen p53 | Homo sapiens (human) | IC50 (µMol) | 4.7800 | 0.0006 | 0.8850 | 8.2000 | AID644263 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Ki | 1.2400 | 0.0030 | 1.0736 | 5.8600 | AID614426 |
| E3 ubiquitin-protein ligase Mdm2 | Homo sapiens (human) | IC50 (µMol) | 1.7133 | 0.0006 | 0.3582 | 10.0000 | AID1420852; AID644263; AID746383 |
| E3 ubiquitin-protein ligase Mdm2 | Homo sapiens (human) | Ki | 1.2400 | 0.0009 | 0.1981 | 1.2400 | AID614426 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID644263 | Competitive inhibition of MDM2/P53 interaction after 1 hr by fluorescence polarization assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614426 | Inhibition of p53-MDM2 expressed in Escherichia coli BL-21 (DE3) after 1 hr by fluorescence polarization competitive binding assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID644266 | Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614428 | Antiproliferative activity against human KB cells expressing p53 mutant after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID644265 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614429 | Antiproliferative activity against human A549 cells expressing wild type p53 after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614430 | Antiproliferative activity against human HCT116 cells expressing wild type p53 after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID644268 | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614459 | Cell cycle arrest in human A549 cells expressing wild type p53 assessed as accumulation at G2/M phase at 10 uM after 72 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 7.49%) | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614427 | Antiproliferative activity against p53 deficient human PC3 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| 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. |
| AID644264 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID644267 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4 | Design, synthesis and CoMFA studies of N1-amino acid substituted 2,4,5-triphenyl imidazoline derivatives as p53-MDM2 binding inhibitors. |
| 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 | Inhibitors of the p53/hdm2 protein-protein interaction-path to the clinic. |
| AID614460 | Cell cycle arrest in human A549 cells expressing wild type p53 assessed as accumulation at S phase at 10 uM after 72 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 19.23%) | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| AID614458 | Cell cycle arrest in human A549 cells expressing wild type p53 assessed as accumulation at G0/G1 phase at 10 uM after 72 hrs using propidium iodide staining by flow cytometric analysis (Rvb = 73.28%) | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18 | Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 17 (43.59) | 29.6817 |
| 2010's | 19 (48.72) | 24.3611 |
| 2020's | 3 (7.69) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (15.97) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 7 (17.95%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 32 (82.05%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||